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quinazolines

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Description

Quinazolines are a class of nitrogen-containing heterocyclic compounds that are known for their diverse pharmacological activities. They have been extensively investigated for their potential therapeutic applications in various disease areas, including cancer, infectious diseases, and neurological disorders. The presence of the quinazoline scaffold provides a unique structural framework that can be readily modified to fine-tune their biological properties. '

Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID9210
CHEMBL ID301359
CHEBI ID36621
SCHEMBL ID5920
MeSH IDM0018336

Synonyms (48)

Synonym
AC-18352
BIDD:GT0070
chinazolin
CHEBI:36621 ,
bdbm50049572
NCIOPEN2_000549
AC-907/25014195
nsc72372
benzo[a]pyrimidine
wln: t66 bn dnj
nsc-72372
1,3-diazanaphthalene
5,6-benzopyrimidine
phenmiazine
1,3-benzodiazine
253-82-7
quinazoline
inchi=1/c8h6n2/c1-2-4-8-7(3-1)5-9-6-10-8/h1-6
quinazoline, 99%
CU-00000000401-1
quinazolines
CHEMBL301359 ,
quz ,
Q0055
benzo(a)pyrimidine
unii-ub9qur18nl
ub9qur18nl ,
einecs 205-965-3
nsc 72372
A817834
benzopyrimidine
FT-0631892
AKOS015900554
quinazoline [mi]
SCHEMBL5920
mfcd00006712
SY006075
benzo(e)pyrimidine
4.5-benzopyrimidine
DTXSID7075214
J-524172
CS-W002010
GS-3258
J-015972
Q426278
PB47603
EN300-84601
Z1251332997

Research Excerpts

Overview

Quinazolines are a class of nitrogen heterocyclic compounds with biological and pharmacological effects in vivo and in vitro.

ExcerptReferenceRelevance
"Quinazolines are a class of nitrogen heterocyclic compounds with biological and pharmacological effects in vivo and in vitro."( A Novel Quinazoline Derivative Prevents and Treats Arsenic-Induced Liver Injury by Regulating the Expression of RecQ Family Helicase.
Cheng, S; Li, J; Luo, H; Mo, M; Sun, B; Xu, B; Yang, H; Yang, L; Yu, J; Zhang, A, 2023
)
1.63
"Quinazolines are a common class of nitrogen-containing heterocyclic scaffolds, which exhibit a broad spectrum of pharmacological activities."( A Novel Quinazoline-4-one Derivatives as a Promising Cytokine Inhibitors: Synthesis, Molecular Docking, and Structure-activity Relationship.
Borik, RM; Hussein, MA, 2022
)
2.16
"Quinazolines are a big family of heterocyclic compounds with anti-cancer properties."( Synthesis, Characterization of 4-Anilino-6,7-Dimethoxy Quinazoline Derivatives as Potential Anti-Angiogenic Agents.
Balaji, KS; Devegowda, PS; Jayarama, S; Kameshwar, VH; Prasanna, DS; Rangappa, KS; Siddalingaiah, L; Swaroop, TR, 2018
)
1.92

Effects

ExcerptReferenceRelevance
"Quinazolines have been identified as inhibitors of CDK4/D1 and CDK2/E. "( Quinazolines as cyclin dependent kinase inhibitors.
Benfield, PA; Boisclair, M; Boylan, J; Burton, CR; Chang, CH; Chen, H; Cox, S; Grafstrom, RH; Johnson, TL; Liu, J; Muckelbauer, JK; Seitz, SP; Sielecki, TM; Smallwood, A; Trainor, GL, 2001
)
3.2

Actions

Quinazolines increase SMN2 promoter activity and inhibit the ribonucleic acid scavenger enzyme DcpS. They were found to inhibit receptor autophosphorylation and signaling through MAP kinase, but had minimal effects on association of EGFRvIII with Grb2/SOS.

ExcerptReferenceRelevance
"Quinazolines increase SMN2 promoter activity and inhibit the ribonucleic acid scavenger enzyme DcpS."( The DcpS inhibitor RG3039 improves motor function in SMA mice.
Feng, Z; Gibbs, RM; Jacques, V; Ko, CP; Li, DK; Lin, MY; Miao, W; Pellizzoni, L; Plasterer, HL; Rucki, AA; Rusche, JR; Sharma, S; Sumner, CJ; Van Meerbeke, JP; Wee, CD; Xia, B, 2013
)
1.11
"Quinazolines were found to inhibit receptor autophosphorylation and signaling through MAP kinase, but had minimal effects on association of EGFRvIII with Grb2/SOS."( Antagonistic and agonistic effects of quinazoline tyrosine kinase inhibitors on mutant EGF receptor function.
Montgomery, RB, 2002
)
1.04

Toxicity

ExcerptReferenceRelevance
" No side effects or adverse reactions have been observed except a "first-dose" fall in blood pressure, and there is no evidence of development of tolerance to the agent."( Long-term efficacy and safety of prazosin in essential hypertension.
Okun, R, 1975
)
0.25
" Stomatitis was observed in only one case as a side effect of this drug."( [Usefulness and safety of bunazosin hydrochloride in neurogenic bladder after prolonged administration].
Gotoh, S; Hiraga, S; Hosoda, K; Kakehi, R; Kaneoya, F; Kojima, S; Mizuo, T; Satoh, T; Tanizawa, A; Yokokawa, M, 1992
)
0.28
"In four phase II trials of trimetrexate given iv daily for 5 days, we noted marked variability among patients in the development of severe or life-threatening toxic effects."( Trimetrexate: predictors of severe or life-threatening toxic effects.
Eisenhauer, EA; Pater, JL; Walsh, WR; Zee, BC, 1988
)
0.27
" The toxic effects of thymidylate synthase inhibition may be prevented by salvage of exogenous thymidine."( Potentiation of quinazoline antifolate (CB3717) toxicity by dipyridamole in human lung carcinoma, A549, cells.
Curtin, NJ; Harris, AL, 1988
)
0.27
" Monitoring of serum hepatic-enzyme concentrations is recommended for patients receiving NSAIDs from the indole, pyrazolone, and propionic acid classes since these agents have been associated with the greatest incidence of adverse hepatic reactions."( Hepatic toxicity of nonsteroidal anti-inflammatory drugs.
Lewis, JH,
)
0.13
" Maximum repair was observed in both strains of mice at 5 x 10(-5) M batracylin, a concentration that was toxic to rat hepatocytes."( Species variation in the genotoxicity of batracylin.
McQueen, CA; Stevens, GJ, 1994
)
0.29
" However, the toxic effects of piritrexim and trimetrexate suggest that dihydrofolate reductase (DHFR) activity is essential for the parasite, most probably because of the role of this enzyme in the synthesis of thymidine nucleotides via thymidylate synthase."( The toxicity of antifolates in Babesia bovis.
Bagnara, AS; Nott, SE, 1993
)
0.29
" Clinical safety was assessed using spontaneous reporting of adverse events leading to discontinuation of treatment."( Safety profile of 3 months' therapy with alfuzosin in 13,389 patients suffering from benign prostatic hypertrophy.
Blondin, P; Du Boys, B; Grippon, P; Lassale, C; Lukacs, B; MacCarthy, C, 1996
)
0.29
" Nine patients dropped out for adverse events with SR-alfuzosin (4."( Efficacy and safety of sustained-release alfuzosin 5 mg in patients with benign prostatic hyperplasia. ALGEBI Study Group.
Buzelin, JM; Delauche-Cavallier, MC; Geffriaud-Ricouard, C; Roth, S, 1997
)
0.3
"Anagrelide is efficacious and safe in ET, both for platelet and symptom control."( Efficacy, safety and tolerability of anagrelide in the treatment of essential thrombocythaemia.
Bashford, J; Brigden, MC; Bunce, I; Eliadis, P; Kelly, C; Mills, AK; Olsen, T; Rentoul, A; Seeley, G; Taylor, KM; Wright, SJ, 1999
)
0.3
" RTX induces proliferating tissue toxicities that are largely confined to the intestine, with diarrhea being a severe side effect in a small but significant minority of patients."( Balb/c mice as a preclinical model for raltitrexed-induced gastrointestinal toxicity.
Aherne, GW; Benstead, J; Clarke, SJ; Farrugia, DC; Jackman, AL; Pritchard, DM, 2000
)
0.31
" In addition, vasodilatory adverse events appeared to be less frequent with the once daily than the thrice daily formulation (6."( Efficacy and safety of a new prolonged release formulation of alfuzosin 10 mg once daily versus alfuzosin 2.5 mg thrice daily and placebo in patients with symptomatic benign prostatic hyperplasia. ALFORTI Study Group.
Jardin, A; Laval, KU; van Cangh, P; van Kerrebroeck, P, 2000
)
0.31
" Safety was assessed by monitoring blood pressure and spontaneous adverse events."( Safety and efficacy of sustained-release alfuzosin on lower urinary tract symptoms suggestive of benign prostatic hyperplasia in 3,095 Spanish patients evaluated during general practice.
Alfaro, V; Badiella, L; Fernández-Hernando, N; Guil, M; Sánchez-Chapado, M, 2000
)
0.31
"101 adverse events were reported in 82 patients (2."( Safety and efficacy of sustained-release alfuzosin on lower urinary tract symptoms suggestive of benign prostatic hyperplasia in 3,095 Spanish patients evaluated during general practice.
Alfaro, V; Badiella, L; Fernández-Hernando, N; Guil, M; Sánchez-Chapado, M, 2000
)
0.31
" The appearance of adverse medical events (AMEs) was carefully monitored and recorded throughout the trial."( Safety, efficacy and impact on Patients' quality of life of a long-term treatment with the alpha(1)-blocker alfuzosin in symptomatic patients with BPH. The Italian Alfuzosin Co-Operative Group.
, 2000
)
0.31
" Potentiation of cytotoxicity was obtained at concentrations of NU1025 and NU1085 that were not toxic per se; however, NU1085 alone was 3-fold more cytotoxic (LC50 values ranged from 83 to 94 microM) than NU1025 alone (LC50 > 900 microM)."( Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines.
Calvert, AH; Curtin, NJ; Delaney, CA; Durkacz, BW; Hostomsky, Z; Kyle, S; Newell, DR; Wang, LZ; White, AW, 2000
)
0.31
"4%) reporting adverse events potentially related to alpha-blockade (mainly dizziness)."( Long-term safety and efficacy of a once-daily formulation of alfuzosin 10 mg in patients with symptomatic benign prostatic hyperplasia: open-label extension study.
Jardin, A; Laval, KU; van Cangh, P; van Kerrebroec, P, 2002
)
0.31
" This study also demonstrates the satisfactory long-term safety of this formulation, and its safe use even in at-risk populations."( Long-term safety and efficacy of a once-daily formulation of alfuzosin 10 mg in patients with symptomatic benign prostatic hyperplasia: open-label extension study.
Jardin, A; Laval, KU; van Cangh, P; van Kerrebroec, P, 2002
)
0.31
" Three toxic deaths occurred (3%)."( Raltitrexed in the treatment of elderly patients with advanced colorectal cancer: an active and low toxicity regimen.
Aparicio, J; Camps, C; Escudero, P; Feliu, J; García Girón, C; González Barón, M; Mel, JR; Menéndez, D; Rodriguez, MR; Sánchez, JJ, 2002
)
0.31
" The most frequent drug-related adverse events (AEs) were acne-like rash (64%) and diarrhea (47%), which were generally mild (grade 1/2) and reversible on cessation of treatment."( Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types.
Albanell, J; Averbuch, SD; Baselga, J; Bjork, T; Calvert, H; Feyereislova, A; Gianni, L; Harris, A; Kaye, SB; Kieback, DG; Ranson, M; Raymond, E; Rischin, D; Rojo, F; Swaisland, H, 2002
)
0.31
" Emergent vasodilatory adverse events were reported by 4 of 26 subjects."( Pharmacokinetics and safety of a single oral dose of once-daily alfuzosin, 10 mg, in male subjects with mild to severe renal impairment.
Blum, RA; Marbury, TC; Pinquier, JL; Rauch, C, 2002
)
0.31
" Alfuzosin was well tolerated; the number of withdrawals for adverse events was comparable in both treatment groups."( Safety and efficacy of alfuzosin 10 mg once-daily in the treatment of lower urinary tract symptoms and clinical benign prostatic hyperplasia: a pooled analysis of three double-blind, placebo-controlled studies.
Nordling, J; Roehrborn, CG; Van Kerrebroeck, P, 2003
)
0.32
"Since many trials claimed a favorable therapeutic index with raltitrexed, the aim of our preliminary study was to evaluate the anticancer activity and the toxic profile of this drug in the elderly."( Favorable toxicity profile of raltitrexed in elderly patients treated for colorectal cancer: a case series.
Caporale, A; Fabiani, O; Franchi, F; Pastore, C; Rossi, L; Seminara, P,
)
0.13
" Though recent reports suggest some concern about severe complications of treatment with raltitrexed, administration of reduced doses of this drug seems to be a putative therapy for those patients who, because of their age, are highly susceptible to the adverse effects of chemotherapy."( Favorable toxicity profile of raltitrexed in elderly patients treated for colorectal cancer: a case series.
Caporale, A; Fabiani, O; Franchi, F; Pastore, C; Rossi, L; Seminara, P,
)
0.13
" This study confirmed TOM-based hepatotoxicity as a clinical relevant side-effect and a major factor for treatment delays or discontinuation."( Raltitrexed-induced hepatotoxicity: multivariate analysis of predictive factors.
Bonsignori, M; Delprete, S; La Cesa, A; Marcucci, F; Massacesi, C; Rocchi, MB; Santini, D; Tonini, G; Vincenzi, B, 2003
)
0.32
" The most commonly reported adverse events were diarrhea, acne-like skin rash, nausea, vomiting and asthenia."( Fatal pulmonary toxicity in a patient treated with gefitinib for non-small cell lung cancer after previous hemolytic-uremic syndrome due to gemcitabine.
Herchenhorn, D; Rabinowits, G; Rabinowits, M; Torres, W; Weatge, D, 2003
)
0.32
" OSI-7904L was much more toxic than OSI-7904 in the mouse with primary toxicities to the intestines, bone marrow, and thymus."( Pharmacokinetics, safety, and efficacy of a liposome encapsulated thymidylate synthase inhibitor, OSI-7904L [(S)-2-[5-[(1,2-dihydro-3-methyl-1-oxobenzo[f]quinazolin-9-yl)methyl]amino-1-oxo-2-isoindolynl]-glutaric acid] in mice.
Abbott, E; Brown, EN; Colagiovanni, DB; Desjardins, J; Drolet, DW; Emerson, DL, 2004
)
0.32
" The most common cutaneous adverse effect was the development of an acneiform eruption on the face, anterior trunk and back (39%)."( Cutaneous side effects in non-small cell lung cancer patients treated with Iressa (ZD1839), an inhibitor of epidermal growth factor.
Choi, JH; Kim, SW; Koh, JK; Lee, HW; Lee, MW; Moon, KC; Seo, CW; Yang, HJ, 2004
)
0.32
"Side effects and toxic discontinuation rates were higher than in previous studies, probably because this is the first long-term prospective study of the feasibility and toxicity of anagrelide treatment."( Adverse effects and benefits of two years of anagrelide treatment for thrombocythemia in chronic myeloproliferative disorders.
Birgegård, G; Björkholm, M; Kutti, J; Lärfars, G; Löfvenberg, E; Markevärn, B; Mauritzson, N; Merup, M; Palmblad, J; Samuelsson, J; Westin, J, 2004
)
0.32
" In this report, we investigated the efficacy and adverse events during treatment with gefitinib."( Acute lung injury as an adverse event of gefitinib.
Abe, S; Inomata, S; Nagata, M; Saitoh, T; Sato, T; Satoh, M; Shiratori, M; Takahashi, H; Tanaka, H; Yamada, G, 2004
)
0.32
" A history and several investigations were conducted to determine the etiology of this adverse event."( Priapism as a possible acute side effect of radical radiotherapy for prostate cancer.
Hayter, C; Lomaga, MA, 2004
)
0.32
" Sixteen adverse events (AEs) were reported by eight of 41 volunteers after BIBN 4096 BS compared to five AEs reported by four of 14 volunteers after placebo."( Safety, tolerability and pharmacokinetics of BIBN 4096 BS, the first selective small molecule calcitonin gene-related peptide receptor antagonist, following single intravenous administration in healthy volunteers.
Feifel, U; Iovino, M; Wallenstein, G; Wolters, JM; Yong, CL, 2004
)
0.32
" Adverse events (AEs) were generally mild (grade 1 and 2) and reversible."( Evaluation of safety and efficacy of gefitinib ('iressa', zd1839) as monotherapy in a series of Chinese patients with advanced non-small-cell lung cancer: experience from a compassionate-use programme.
Li, LY; Mu, XL; Wang, MZ; Wang, SL; Zhang, XT, 2004
)
0.32
" Three volunteers experienced adverse events (AEs) that were considered possibly related to gefitinib (pruritus and dry skin), and 6 volunteers experienced procedure-related AEs (cannula-site reaction and rhinorrhea); these AEs were mild or moderate."( Relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers.
Bailey, C; Cantarini, MV; Marshall, AL; McFarquhar, T; Smith, RP, 2004
)
0.32
" Most drug-related adverse events were mild."( Gefitinib is active in patients with brain metastases from non-small cell lung cancer and response is related to skin toxicity.
Chen, YM; Chiang, SC; Chiu, CH; Liou, JL; Perng, RP; Tsai, CM, 2005
)
0.33
" Both doses of alfuzosin were well tolerated, with dizziness the most frequent adverse event (placebo, 4%; alfuzosin 10 mg, 6%; 15 mg, 7%; tamsulosin, 2%); the respective incidence rates of sexual function adverse events were 0%, 3%, 1% and 8%."( Efficacy and safety of two doses (10 and 15 mg) of alfuzosin or tamsulosin (0.4 mg) once daily for treating symptomatic benign prostatic hyperplasia.
Nordling, J, 2005
)
0.33
" The incidence of sexual function adverse events was higher with tamsulosin than with placebo."( Efficacy and safety of two doses (10 and 15 mg) of alfuzosin or tamsulosin (0.4 mg) once daily for treating symptomatic benign prostatic hyperplasia.
Nordling, J, 2005
)
0.33
" The most frequently reported drug-related adverse events were diarrhea (42%) and rash (31%)."( Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas.
Blackwell, KL; Burris, HA; Dees, EC; Dowlati, A; Ellis, MJ; Harris, JL; Hurwitz, HI; Jones, SF; Koch, KM; Mangum, S; Marcom, PK; O'Neil, B; Overmoyer, B; Smith, DA; Spector, NL; Stead, A, 2005
)
0.33
" A specific adverse effect common to this class of agent is a papulopustular rash, usually on the face and upper torso, which generally occurs in a dose-dependent manner."( Cutaneous adverse effects with HER1/EGFR-targeted agents: is there a silver lining?
Peréz-Soler, R; Saltz, L, 2005
)
0.33
" We examined the correlations between the plasma levels of several cytokines and the risk of development of adverse events, especially skin toxicity, induced by the administration of gefitinib as first-line monotherapy in non-small cell lung cancer (NSCLC) patients."( Plasma MIP-1beta levels and skin toxicity in Japanese non-small cell lung cancer patients treated with the EGFR-targeted tyrosine kinase inhibitor, gefitinib.
Kasahara, K; Kimura, H; Nishio, K; Sekijima, M; Tamura, T, 2005
)
0.33
" The most frequent erlotinib-related adverse events were rash (68%) and diarrhea (38%)."( Efficacy and safety of erlotinib HCl, an epidermal growth factor receptor (HER1/EGFR) tyrosine kinase inhibitor, in patients with advanced ovarian carcinoma: results from a phase II multicenter study.
Barrett, E; Crozier, M; Edwards, RP; Finkler, N; Garcia, AA; Gordon, AN; Irwin, DH,
)
0.13
" Safety data for 38 recruited patients (18 gefitinib and 20 placebo) showed no unexpected adverse drug reactions (ADRs), with the most common being grade 1/2 gastrointestinal and skin disorders in 12 and 16 patients receiving gefitinib and in five and six patients receiving placebo, respectively."( Gefitinib in the adjuvant setting: safety results from a phase III study in patients with completely resected non-small cell lung cancer.
Fukuoka, M; Ichinose, Y; Jiang, H; Kato, H; Nagai, K; Tada, H; Tsuboi, M; Tsuchiya, R; Wada, H, 2005
)
0.33
" The incidence of adverse events was similar for tamsulosin (25%) and alfuzosin (19."( A comparative study on the safety and efficacy of tamsulosin and alfuzosin in the management of symptomatic benign prostatic hyperplasia: a randomized controlled clinical trial.
Acepcion, V; Lapitan, MC; Mangubat, J,
)
0.13
" In the elderly group, adverse events were generally mild to moderate and grade 3-4 adverse events were observed in 8 (9%) patients."( Safety and efficacy of gefitinib treatment in elderly patients with non-small-cell lung cancer: Okayama Lung Cancer Study Group experience.
Bessho, A; Gemba, K; Harita, S; Hotta, K; Kiura, K; Maeda, T; Ogino, A; Tabata, M; Tanimoto, M; Ueoka, H; Umemura, S; Yonei, T, 2005
)
0.33
"To evaluate the efficacy and adverse effects of alfuzosin for the treatment of lower urinary tract symptoms associated with benign prostatic hyperplasia (BPH)."( Alfuzosin for treatment of lower urinary tract symptoms compatible with benign prostatic hyperplasia: a systematic review of efficacy and adverse effects.
MacDonald, R; Wilt, TJ, 2005
)
0.33
"Skin toxicity, a common drug-related adverse event observed in cancer patients treated with epidermal growth factor receptor (EGFR)-directed therapies is rarely seen with therapies targeting HER2."( Epidermal growth factor receptor dimerization status determines skin toxicity to HER-kinase targeted therapies.
Agus, DB; Jain, A; Laux, I; Singh, S, 2006
)
0.33
"In the current Phase II study, the authors evaluated the association between genomic polymorphic variants in uridine diphosphate glucuronosyl transferase (UGT1A1), methylenetetrahydrofolate reductase (MTHFR), and thymidylate synthase (TS) genes, and the incidence of the adverse effects of irinotecan and raltitrexed in previously heavily treated patients with metastatic colorectal carcinoma."( Uridine diphosphate glucuronosyl transferase 1A1 promoter polymorphism predicts the risk of gastrointestinal toxicity and fatigue induced by irinotecan-based chemotherapy.
Bisonni, R; Leon, A; Lippe, P; Lombardo, M; Marcucci, F; Massacesi, C; Mattioli, R; Pilone, A; Rocchi, MB; Terrazzino, S, 2006
)
0.33
" Nineteen variables related to patient, disease, and treatment characteristics, together with genotypes, were analyzed using a binary logistic regression model with stepwise selection to evaluate their correlation with adverse reactions."( Uridine diphosphate glucuronosyl transferase 1A1 promoter polymorphism predicts the risk of gastrointestinal toxicity and fatigue induced by irinotecan-based chemotherapy.
Bisonni, R; Leon, A; Lippe, P; Lombardo, M; Marcucci, F; Massacesi, C; Mattioli, R; Pilone, A; Rocchi, MB; Terrazzino, S, 2006
)
0.33
" MTHFR C677T polymorphism was not found to be associated with any adverse reaction."( Uridine diphosphate glucuronosyl transferase 1A1 promoter polymorphism predicts the risk of gastrointestinal toxicity and fatigue induced by irinotecan-based chemotherapy.
Bisonni, R; Leon, A; Lippe, P; Lombardo, M; Marcucci, F; Massacesi, C; Mattioli, R; Pilone, A; Rocchi, MB; Terrazzino, S, 2006
)
0.33
" Alfuzosin 10 mg was well tolerated; the most common adverse event related to vasodilatation was dizziness/postural dizziness (3."( Long-term efficacy and safety of alfuzosin 10 mg once daily: a 2-year experience in 'real-life' practice.
Alcaraz, A; Elhilali, M; Emberton, M; Hartung, R; Harving, N; Matzkin, H; Vallancien, G; van Moorselaar, RJ, 2006
)
0.33
"alpha(1)-Blockers were effective and safe for treating young and middle-aged men with symptomatic bladder neck obstruction."( Obstructive primary bladder neck disease: evaluation of the efficacy and safety of alpha1-blockers.
Artibani, W; Calpista, A; Cisternino, A; De Marco, V; Iafrate, M; Prayer Galetti, T; Zeccolini, G, 2006
)
0.33
" However, the relationship between EGFR mutation and adverse events of gefitinib is still unknown."( Relationship between epidermal growth factor receptor gene mutations and the severity of adverse events by gefitinib in patients with advanced non-small cell lung cancer.
Aoe, M; Date, H; Fujiwara, Y; Hotta, K; Kiura, K; Matsuo, K; Tabata, M; Takigawa, N; Tanimoto, M; Tokumo, M; Toyooka, S, 2006
)
0.33
" We retrospectively reviewed the clinical records and compared EGFR mutation status with adverse events during gefitinib treatment."( Relationship between epidermal growth factor receptor gene mutations and the severity of adverse events by gefitinib in patients with advanced non-small cell lung cancer.
Aoe, M; Date, H; Fujiwara, Y; Hotta, K; Kiura, K; Matsuo, K; Tabata, M; Takigawa, N; Tanimoto, M; Tokumo, M; Toyooka, S, 2006
)
0.33
" The principal adverse event was skin rash (89%), diarrhea (39%), and liver injury (39%)."( Relationship between epidermal growth factor receptor gene mutations and the severity of adverse events by gefitinib in patients with advanced non-small cell lung cancer.
Aoe, M; Date, H; Fujiwara, Y; Hotta, K; Kiura, K; Matsuo, K; Tabata, M; Takigawa, N; Tanimoto, M; Tokumo, M; Toyooka, S, 2006
)
0.33
"Our study did not demonstrate the presence of close relationships between EGFR mutation status and adverse events during gefitinib treatment."( Relationship between epidermal growth factor receptor gene mutations and the severity of adverse events by gefitinib in patients with advanced non-small cell lung cancer.
Aoe, M; Date, H; Fujiwara, Y; Hotta, K; Kiura, K; Matsuo, K; Tabata, M; Takigawa, N; Tanimoto, M; Tokumo, M; Toyooka, S, 2006
)
0.33
"We measured serum levels of soluble (s) P-selectin and thromboxane B2 (TxB2) in patients with lung cancer treated with gefitinib, and investigated the effect of low-dose aspirin on some adverse effects of gefitinib."( Aspirin reduces adverse effects of gefitinib.
Kanazawa, S; Kinoshita, Y; Komiyama, Y; Muramatsu, M; Nomura, S; Yamaguchi, K, 2006
)
0.33
" The most common adverse effects are rash, diarrhoea, acne, dry skin, nausea and vomiting."( Gefitinib: an adverse effects profile.
Cersosimo, RJ, 2006
)
0.33
"The most common side effect of anti-EGFR therapy is skin toxicity, which is generally mild to moderate, but may be severe in up to 18% of patients."( Common side effects of anti-EGFR therapy: acneform rash.
Sipples, R, 2006
)
0.33
" IC87114 did not have direct adverse effects or enhance the activity of VP16 on the proliferation and survival of normal haemopoietic progenitors."( A selective inhibitor of the p110delta isoform of PI 3-kinase inhibits AML cell proliferation and survival and increases the cytotoxic effects of VP16.
Billottet, C; Gale, RE; Grandage, VL; Khwaja, A; Quattropani, A; Rommel, C; Vanhaesebroeck, B, 2006
)
0.33
" However, some nondermatologic adverse events can also be common."( Nondermatologic adverse events associated with anti-EGFR therapy.
Sandler, AB, 2006
)
0.33
" The most common adverse events were diarrhea (31."( Efficacy and safety of gefitinib in chemonaive patients with advanced non-small cell lung cancer treated in an Expanded Access Program.
Belani, CP; Govindan, R; Hensing, T; Herbst, R; Kelly, K; Krebs, A; Natale, R; Ochs, J; Reiling, R; Wade, J; Wozniak, A, 2006
)
0.33
" Effects of covariates on erlotinib clearance and correlations with adverse event severity were provided to aid in the detection of a treatment-emergent effect."( Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure-safety relationship in patients with non-small cell lung cancer.
Bruno, R; Eppler, SM; Hamilton, M; Lu, JF; Lum, BL; Rakhit, A; Wolf, J, 2006
)
0.33
" Severe enterocolitis, a hitherto infrequently recognized adverse event, which has been described in association with 5-fluorouracil/leucovorin and oxaliplatin chemotherapy, may also occur with raltitrexed and oxaliplatin."( Severe enteropathy associated with raltitrexed and oxaliplatin chemotherapy: report of two patients experiencing this rare, potentially lethal gastrointestinal adverse event.
Funk, G; Kornek, GV; Oehler, L; Scheithauer, W; Schwarz, C; Urbauer, E; Wenzel, C, 2006
)
0.33
" Our aim was to describe key clinical features of common dermatologic adverse reactions among EGFR inhibitors, focusing mainly on skin toxicity, as well as to discuss the pathology, possible causes, and suggested treatments for these reactions."( Dermatologic side effects associated with the epidermal growth factor receptor inhibitors.
Agero, AL; Benvenuto-Andrade, C; Busam, KJ; Dusza, SW; Halpern, AC; Myskowski, P, 2006
)
0.33
"Factors predicting gefitinib sensitivity and adverse events in non-small cell lung cancer (NSCLC) remain controversial."( The characterization of gefitinib sensitivity and adverse events in patients with non-small cell lung cancer.
Hagiwara, K; Inase, N; Jinn, Y; Kanazawa, M; Koyama, N; Miyake, S; Takabe, K; Usui, Y; Yoshizawa, M; Yoshizawa, Y,
)
0.13
"Correlations among clinicopathological characteristics, gefitinib sensitivity and adverse events were studied in 154 patients with NSCLC, whereas epidermal growth factor receptor (EGFR) mutations were analyzed in 44 patients."( The characterization of gefitinib sensitivity and adverse events in patients with non-small cell lung cancer.
Hagiwara, K; Inase, N; Jinn, Y; Kanazawa, M; Koyama, N; Miyake, S; Takabe, K; Usui, Y; Yoshizawa, M; Yoshizawa, Y,
)
0.13
"Certain clinicopathological characteristics and EGFR mutations can be either predictive of gefitinib sensitivity or adverse events."( The characterization of gefitinib sensitivity and adverse events in patients with non-small cell lung cancer.
Hagiwara, K; Inase, N; Jinn, Y; Kanazawa, M; Koyama, N; Miyake, S; Takabe, K; Usui, Y; Yoshizawa, M; Yoshizawa, Y,
)
0.13
" To our knowledge, the periorbital rash resulting in bilateral lower eyelid ectropion associated with epiphora is a newly recognized side effect of erlotinib that is completely reversible with discontinuation of the drug."( Newly recognized ocular side effects of erlotinib.
Gausas, RE; Methvin, AB,
)
0.13
" Treatment-related adverse events were nausea (58%), asthenia (23%), hyperbilirubinemia (27%), elevated transaminases (30%), and skin rash (30%); neither diarrhea nor cardiomyopathy was observed."( First study of the safety, tolerability, and pharmacokinetics of CP-724,714 in patients with advanced malignant solid HER2-expressing tumors.
Britten, CD; Denis, L; Gelmon, K; Guo, F; Letrent, SP; Minton, SE; Mita, M; Moulder, S; Munster, PN; Slamon, DJ; Tolcher, AW, 2007
)
0.34
" PK data indicated that the bioavailability of oral PQD-A4 was greatly limited at high dose levels, that PQD-A4 was slowly converted to PQD via a sequential three-step process of conversion, and that PQD-A4 was significantly less toxic than the one-step hydrolysis drug, PQD-BE."( Pharmacokinetics, safety, and hydrolysis of oral pyrroloquinazolinediamines administered in single and multiple doses in rats.
Anova, L; Kozar, MP; Li, Q; Lin, AJ; Milhous, WK; Shearer, TW; Si, Y; Skillman, DR; Smith, KS; Xie, LH; Zhang, J, 2007
)
0.34
" At least one of these adverse events would be observed in 40."( [Safety and efficacy of gefitinib for treatment of advanced non-small cell lung cancer].
Han, Y; Li, YM; Liu, XQ; Song, ST; Xu, JM; Yang, WW; Zhang, Y, 2007
)
0.34
" Both therapeutic agents were suspected as a possible cause of this adverse event."( Severe lung and skin toxicity during treatment with gemcitabine and erlotinib for metastatic pancreatic cancer.
Boeck, S; Hausmann, A; Heinemann, V; Reibke, R; Schulz, C, 2007
)
0.34
" The adverse pulmonary effects of erlotinib are less well known."( Pulmonary toxicity associated with erlotinib.
Azzoli, CG; Ginsberg, MS; Kris, MG; Liu, V; Miller, VA; Travis, W; White, DA; Zakowski, MF, 2007
)
0.34
"Skin toxicity is a common adverse effect of erlotinib and other anti-epidermal growth factor receptor (EGFR) agents."( Markers in the epidermal growth factor receptor pathway and skin toxicity during erlotinib treatment.
Nguyen, D; Parr, AL; Steinberg, SM; Tan, AR; Yang, SX, 2008
)
0.35
" No unexpected adverse events were noted."( Phase II study of efficacy and safety of bevacizumab in combination with chemotherapy or erlotinib compared with chemotherapy alone for treatment of recurrent or refractory non small-cell lung cancer.
Belani, CP; Bonomi, PD; Fehrenbacher, L; Hart, L; Herbst, RS; Lin, M; Melnyk, O; O'Neill, VJ; Ramies, D; Sandler, A, 2007
)
0.34
"The target of novel signal transduction inhibitors may be present on normal as well as tumor cells, resulting in mechanistic adverse effects (AE) in addition to antitumor activity."( Validation of treatment induced specific adverse effect as a predictor of treatment benefit: a case study of NCIC CTG BR21.
Ding, K; Pater, J; Seymour, L; Shepherd, FA; Whitehead, M, 2008
)
0.35
" Severe hematological adverse events related to gefitinib treatment were not observed in any of the included trials."( The safety and efficacy of gefitinib versus platinum-based doublets chemotherapy as the first-line treatment for advanced non-small-cell lung cancer patients in East Asia: a meta-analysis.
Chan, KA; Chang, CH; Chen, KY; Kurth, T; Orav, EJ; Yang, PC; Young-Xu, Y, 2008
)
0.35
" Common adverse events were diarrhea, rash, dry skin, asthenia, nausea, anorexia."( Efficacy and safety of erlotinib in patients with locally advanced or metastatic breast cancer.
Cobleigh, MA; Dickler, MN; Klein, PM; Miller, KD; Winer, EP, 2009
)
0.35
" We analyzed cardiac events defined as symptomatic (grade 3 or 4 left ventricular systolic dysfunction according to the National Cancer Institute Common Terminology Criteria for Adverse Events) or asymptomatic (LVEF decreases > or = 20% relative to baseline and below the institution's lower limit of normal; no symptoms)."( Cardiac safety of lapatinib: pooled analysis of 3689 patients enrolled in clinical trials.
Byrne, J; Ewer, MS; Koehler, M; Perez, EA; Preston, AJ; Rappold, E, 2008
)
0.35
" BI 1356 was well tolerated and safe up to and including a dose of 600 mg."( Safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of BI 1356, an inhibitor of dipeptidyl peptidase 4, in healthy male volunteers.
Dugi, KA; Graefe-Mody, EU; Hüttner, S; Ring, A; Withopf, B, 2008
)
0.35
" Adverse events were generally mild (grade 1 and 2) and reversible."( [Evaluation of efficacy and safety of ZD1839 as monotherapy in Chinese patients with advanced non-small cell lung cancer].
Li, JR; Li, LY; Wang, MZ; Wang, SL; Zhang, L; Zhang, XT; Zhong, W, 2008
)
0.35
" Adverse drug reactions were frequently observed in the skin, gastrointestinal tract, and liver, but they were generally mild in severity and reversible."( Bilateral subdural hemorrhage as a possible adverse event of gefitinib in a patient with non-small cell lung cancer.
Ahn, BM; Choi, DR; Choi, JS; Jung, JY; Kim, HJ; Kim, HS; Kim, HY; Kim, JH; Kwon, JH; Lee, KM; Park, S; Shin, YC; Song, HH; Zang, DY, 2009
)
0.35
" Discontinuation due to adverse events occurred in 11 patients (18%)."( Efficacy and safety of erlotinib monotherapy for Japanese patients with advanced non-small cell lung cancer: a phase II study.
Fukuoka, M; Hida, T; Katakami, N; Kawahara, M; Kubota, K; Matsui, K; Nakagawa, K; Nishiwaki, Y; Noda, K; Saijo, N; Takeda, K; Tamura, T; Watanabe, K; Yokoyama, A, 2008
)
0.35
" It is a dose-dependent side effect of certain cytostatic drugs."( [Hand-foot syndrome: A new side effect of erlotinib].
Descourt, R; Misery, L; Roguedas, AM; Rouxel, AM, 2008
)
0.35
" This study provides likely explanations for clinically observed adverse liver effects of CP-724,714."( Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714.
Bi, YA; Campbell, S; Davidson, R; Duignan, DB; Dunn, MC; Feng, B; Kostrubsky, VE; Mireles, R; Smith, AR; Wang, HF; Xu, JJ, 2009
)
0.35
" Papulopustular eruptions are the most frequent adverse effect, their occurrence being associated with increased survival in some studies."( Description and management of cutaneous side effects during erlotinib and cetuximab treatment in lung and colorectal cancer patients: a prospective and descriptive study of 19 patients.
Baptista, A; Barroso, A; de Noronha e Menezes, NM; Lima, R; Moreira, A; Parente, B; Varela, P,
)
0.13
"Common adverse events included grade 1 skin rash (63%), grade 1 to 2 gastrointestinal symptoms including anorexia, nausea, vomiting, and diarrhea occurred in 63% of patients, grade 3 nausea occurred in 45% of patients."( Results of a phase I trial of 12 patients with locally advanced pancreatic carcinoma combining gefitinib, paclitaxel, and 3-dimensional conformal radiation: report of toxicity and evaluation of circulating K-ras as a potential biomarker of response to the
Chen, H; Chen, Y; Eckhardt, SG; Kane, M; Leong, S; Mack, P; McCarter, MD; Olsen, CC; Raben, D; Schefter, TE; Stiegmann, G, 2009
)
0.35
" Skin rash is a well-known side effect related with all EGFR blocking agents."( Staphylococcus aureus bacteremia related with erlotinib skin toxicity in a patient with pancreatic cancer.
Kaley, K; Li, J; Peccerillo, J; Saif, MW, 2009
)
0.35
" Progression-free survival was assessed and adverse reactions were recorded in the medical records."( [Effectiveness and safety of erlotinib in 2 patients with carcinoma of the cervix].
Albornoz López, R; Fernández García, I; Pérez Rodrigo, I; Soto Rojas, M; Torres Degayón, V,
)
0.13
" The adverse reactions to the treatment were slight."( [Effectiveness and safety of erlotinib in 2 patients with carcinoma of the cervix].
Albornoz López, R; Fernández García, I; Pérez Rodrigo, I; Soto Rojas, M; Torres Degayón, V,
)
0.13
"Erlotinib presented some similar results to those obtained from cisplatin doublets in women with refractory cervical cancer, with minor adverse effects."( [Effectiveness and safety of erlotinib in 2 patients with carcinoma of the cervix].
Albornoz López, R; Fernández García, I; Pérez Rodrigo, I; Soto Rojas, M; Torres Degayón, V,
)
0.13
" Adverse events included skin rash, dry skin, diarrhea and elevation of serum glutamate pyruvate transaminase (SGPT), and were usually mild."( [Analysis of the efficacy and safety of gefitinib in the treatment of recurrent advanced non-small cell lung cancer in an expanded access program (EAP)].
Guan, ZZ; Huang, H; Wang, ZQ; Xu, F; Xu, GC; Zhang, L; Zhang, Y; Zhao, HY, 2009
)
0.35
" The patients with controlled disease may achieve a long survival, and the adverse reactions are mild and tolerable."( [Analysis of the efficacy and safety of gefitinib in the treatment of recurrent advanced non-small cell lung cancer in an expanded access program (EAP)].
Guan, ZZ; Huang, H; Wang, ZQ; Xu, F; Xu, GC; Zhang, L; Zhang, Y; Zhao, HY, 2009
)
0.35
"A multicenter observational study looking at safety by adverse events (AEs) incidence, efficacy by changes in International Prostate Symptom Score (I-PSS), quality of life index (QOL), sexual function using Danish Prostate Symptom Score (DAN-PSS sex), and flow rates."( Safety and efficacy of a prolonged-release formulation of alfuzosin 10 mg once daily in patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia.
Chodchoy, V; Kongkanand, A; Lojanapiwat, B; Pumpaisanchai, S; Ratana-Olarn, K; Sae-Tang, P; Taweemonkongsap, T, 2009
)
0.35
"Addition of bevacizumab to various chemotherapy agents or erlotinib in patients with NSCLC and treated brain metastases seems to be safe and is associated with a low incidence of CNS hemorrhage."( Safety of bevacizumab in patients with non-small-cell lung cancer and brain metastases.
Akerley, W; Compton, P; Huang, JE; Kolb, MM; Langer, CJ; Socinski, MA; Wang, L, 2009
)
0.35
" Collectively, our data demonstrate that Obatoclax mediated inhibition of MCL-1 rapidly enhances Lapatinib toxicity in tumor cells via a toxic form of autophagy and via AIF release from the mitochondrion."( Inhibition of MCL-1 enhances lapatinib toxicity and overcomes lapatinib resistance via BAK-dependent autophagy.
Dent, P; Grant, S; Martin, AP; Mitchell, C; Nephew, KP; Rahmani, M, 2009
)
0.35
" No side effect was observed."( [A case of non-small cell lung cancer treated safely by whole brain radiation therapy and erlotinib].
Nagai, A; Shiroma, T; Yamaguchi, M, 2009
)
0.35
" The most frequent adverse event was diarrhoea."( Lapatinib monotherapy in patients with relapsed, advanced, or metastatic breast cancer: efficacy, safety, and biomarker results from Japanese patients phase II studies.
Allen, KE; Aogi, K; Arai, T; Ellis, CE; Fujiwara, Y; Gagnon, RC; Ito, Y; Iwata, H; Katsura, K; Nakamura, S; Rai, Y; Sasaki, Y; Taguchi, T; Takashima, S; Toi, M; Tokuda, Y; Wakamatsu, T; Watanabe, J, 2009
)
0.35
" Their cutaneous toxicity is a specific and frequent side effect that has shown to be correlated to the antitumoral effect."( [Cutaneous side effects of EGF receptor inhibitors].
Aractingi, S; Nassar, D; Soutou, B, 2009
)
0.35
"Q141K substitution, is more prevalent in Asian populations, the putative relationship between gefitinib-induced adverse effects and this functional polymorphism was investigated in Japanese patients."( Impact of functional ABCG2 polymorphisms on the adverse effects of gefitinib in Japanese patients with non-small-cell lung cancer.
Abe, K; Akasaka, K; Imai, Y; Imura, J; Kaburagi, T; Nagao, K; Ohmori, K; Sagara, H; Ueda, Y; Yasuda, S, 2010
)
0.36
"ABCG2 gene polymorphisms were evaluated in 75 patients with non-small-cell lung cancer treated with gefitinib 250 mg/day orally, and results were correlated with treatment-related adverse effects."( Impact of functional ABCG2 polymorphisms on the adverse effects of gefitinib in Japanese patients with non-small-cell lung cancer.
Abe, K; Akasaka, K; Imai, Y; Imura, J; Kaburagi, T; Nagao, K; Ohmori, K; Sagara, H; Ueda, Y; Yasuda, S, 2010
)
0.36
" No significant group difference was observed in frequency of gefitinib-related diarrhea or other adverse effects."( Impact of functional ABCG2 polymorphisms on the adverse effects of gefitinib in Japanese patients with non-small-cell lung cancer.
Abe, K; Akasaka, K; Imai, Y; Imura, J; Kaburagi, T; Nagao, K; Ohmori, K; Sagara, H; Ueda, Y; Yasuda, S, 2010
)
0.36
"421C > A, and susceptibility to gefitinib-induced adverse effects."( Impact of functional ABCG2 polymorphisms on the adverse effects of gefitinib in Japanese patients with non-small-cell lung cancer.
Abe, K; Akasaka, K; Imai, Y; Imura, J; Kaburagi, T; Nagao, K; Ohmori, K; Sagara, H; Ueda, Y; Yasuda, S, 2010
)
0.36
" Adverse events were documented in 46 patients (23."( Anagrelide for the treatment of thrombocythaemia in daily clinical practice: a post-marketing observational survey on efficacy and safety performed in Germany.
Schlag, R; Schmitz, S; Stauch, M, 2010
)
0.36
" Our results show that Erlotinib-HCl delivered in the form of nanoparticles has less toxic effect than the free drug in experimental rats."( Poly(D,L-lactic-co-glycolic acid) nanoencapsulation reduces Erlotinib-induced subacute toxicity in rat.
Franklin, G; Kalaichelvan, VK; Manavalan, R; Marslin, G; Reddy, PN; Sheeba, CJ, 2009
)
0.35
"To observe the efficacy and the adverse effects of erlotinib in the treatment for advanced non-small cell lung cancer (NSCLC) in Chinese patients."( [Efficacy and safety of Erlotinib in the treatment for advanced non-small cell lung cancer in Chinese patients].
Liao, ML; Qin, SK; Sun, Y; Wu, YL; Zhou, CC, 2010
)
0.36
" The major erlotinib treatment-related adverse events (AE) were mild (CTC AE 1/2), only 3 cases had severe adverse effect, 1 case had interstitial lung disease and died of respiratory failure."( [Efficacy and safety of Erlotinib in the treatment for advanced non-small cell lung cancer in Chinese patients].
Liao, ML; Qin, SK; Sun, Y; Wu, YL; Zhou, CC, 2010
)
0.36
"The study presents excellent response rates, time to progression and overall survival of erlotinib treatment for advanced NSCLC in Chinese patients, and its adverse events are tolerable."( [Efficacy and safety of Erlotinib in the treatment for advanced non-small cell lung cancer in Chinese patients].
Liao, ML; Qin, SK; Sun, Y; Wu, YL; Zhou, CC, 2010
)
0.36
" Discontinuation was predominantly due to disease progression, rather than adverse events, in both the whole cohort (82% vs."( Association between poor performance status and risk for toxicity during erlotinib monotherapy in Japanese patients with non-small cell lung cancer: Okayama Lung Cancer Study Group experience.
Hotta, K; Inoue, K; Kishino, D; Kiura, K; Okada, T; Suzuki, E; Tabata, M; Takigawa, N; Tanimoto, M; Ueoka, H; Yoshioka, H, 2010
)
0.36
" Grade 3/4 adverse events (AEs) were reported by 6 patients and treatment-related Grade 3 AEs by 3 patients."( A multicenter phase II study to evaluate the efficacy and safety of gefitinib as first-line treatment for Korean patients with advanced pulmonary adenocarcinoma harboring EGFR mutations.
Heo, DS; Kang, JH; Kim, DW; Kim, HK; Kim, SY; Lee, JS; Lee, MA; Lee, SH; Shin, SW, 2011
)
0.37
"The most common adverse events (AEs) were skin rash (96%) and diarrhea (32%)."( [Efficacy and safety of erlotinib as monotherapy for advanced non-small cell lung cancer].
Li, LY; Wang, MZ; Xu, LY; Zhang, L; Zhang, XT; Zhang, XY; Zhong, W, 2010
)
0.36
"Erlotinib monotherapy is safe and effective for some Chinese NSCLC patients after failure of prior chemotherapy."( [Efficacy and safety of erlotinib as monotherapy for advanced non-small cell lung cancer].
Li, LY; Wang, MZ; Xu, LY; Zhang, L; Zhang, XT; Zhang, XY; Zhong, W, 2010
)
0.36
" Common adverse events included diarrhea, rash, alopecia, and nausea (> 50% of patients in both cohorts)."( Phase II study to evaluate the efficacy and safety of neoadjuvant lapatinib plus paclitaxel in patients with inflammatory breast cancer.
Boussen, H; Cristofanilli, M; DeSilvio, M; Salazar, V; Spector, N; Zaks, T, 2010
)
0.36
" Diarrhea and rash were the most common adverse events (AEs); 23% of patients experienced grade 3-4 drug-related AEs."( Safety and efficacy of erlotinib in first-relapse glioblastoma: a phase II open-label study.
Cloughesy, TF; Gilbert, MR; Klencke, B; Nghiemphu, P; Prados, MD; Reardon, DA; Vredenburgh, JJ; Yung, WK, 2010
)
0.36
" Tolerable dose, need for supportive treatments, and early signals for toxic effect were evaluated in a planned safety analysis of 270 patients."( Integrating bevacizumab, everolimus, and lapatinib into current neoadjuvant chemotherapy regimen for primary breast cancer. Safety results of the GeparQuinto trial.
Blohmer, JU; Costa, SD; Eidtmann, H; Fasching, PA; Fehm, T; Gerber, B; Hanusch, C; Hilfrich, J; Kreienberg, R; Loibl, S; Nekljudova, V; Solbach, C; Strumberg, D; Untch, M; von Minckwitz, G, 2011
)
0.37
" Among the 6580 patients included in the safety analysis, 799 (12%) experienced one or more erlotinib-related adverse events (AEs, other than prespecified AEs defined in the protocol), and only 4% experienced an erlotinib-related serious AE."( Erlotinib in advanced non-small cell lung cancer: efficacy and safety findings of the global phase IV Tarceva Lung Cancer Survival Treatment study.
Allan, S; Baliko, Z; Gridelli, C; Heigener, D; Krzakowski, M; Reck, M; Rischin, D; van Zandwijk, N, 2010
)
0.36
" Seventeen percent of these patients experienced one or more erlotinib-related adverse event (AE) (other than the most frequently occurring AEs prespecified in the protocol) and 2% experienced an erlotinib-related serious AE."( Efficacy and safety of erlotinib in 1242 East/South-East Asian patients with advanced non-small cell lung cancer.
Au, JS; Mok, T; Park, K; Perng, RP; Wu, YL; Zhang, L; Zhou, C, 2010
)
0.36
" Adverse events such as congestive heart failure and life threatening diarrhoea are sometimes observed because of off-target drug effects."( Prevention and management of major side effects of targeted agents in breast cancer.
Awada, A; Azim, HA; Metzger Filho, O; Saini, KS, 2012
)
0.38
" The most common adverse events were rash and diarrhoea."( Safety and efficacy of the combination of erlotinib and sirolimus for the treatment of metastatic renal cell carcinoma after failure of sunitinib or sorafenib.
Breaker, K; Costa, LJ; Crighton, F; Drabkin, H; Flaig, TW; Gustafson, DL; Kim, FJ; Schultz, MK, 2010
)
0.36
"1%) patients reported adverse events; the incidence was similar across all five groups."( Linagliptin (BI 1356), a potent and selective DPP-4 inhibitor, is safe and efficacious in combination with metformin in patients with inadequately controlled Type 2 diabetes.
Dugi, KA; Forst, T; Friedrich, C; Graefe-Mody, U; Herbach, K; Ring, A; Uhlig-Laske, B; Woerle, HJ, 2010
)
0.36
" The main adverse events of rash and diarrhea are typically mild or moderate in severity, and rarely lead to treatment withdrawal."( Reviewing the safety of erlotinib in non-small cell lung cancer.
Heigener, D; Mok, T; Reck, M; Wolf, J; Wu, YL, 2011
)
0.37
" The severe hematological adverse events related to EGFR TKIs treatment were rare."( The safety and efficacy of EGFR TKIs monotherapy versus single-agent chemotherapy using third-generation cytotoxics as the first-line treatment for patients with advanced non-small cell lung cancer and poor performance status.
Chen, B; Liu, S; Wang, D; Wang, Y; Wu, J; Zhao, W, 2011
)
0.37
"Hepatobiliary adverse events (AEs) have been observed in a small proportion of patients with metastatic breast cancer (MBC) treated with lapatinib."( HLA-DQA1*02:01 is a major risk factor for lapatinib-induced hepatotoxicity in women with advanced breast cancer.
Bing, N; Briley, LP; Budde, LR; Cardon, LR; Cox, CJ; King, KS; Mooser, VE; Preston, AJ; Spraggs, CF; Stein, SH; Whittaker, JC, 2011
)
0.37
" Significantly different adverse events have been associated with gefitinib and erlotinib."( Differences in adverse events between 250 mg daily gefitinib and 150 mg daily erlotinib in Japanese patients with non-small cell lung cancer.
Fujita, S; Fukuhara, A; Hatachi, Y; Kim, YH; Masago, K; Mio, T; Mishima, M; Nagai, H; Sakamori, Y; Togashi, Y, 2011
)
0.37
"A retrospective investigation examining the adverse events and tolerances of 250 mg daily gefitinib and 150 mg daily erlotinib in Japanese patients with non-small cell lung cancer (NSCLC) was performed."( Differences in adverse events between 250 mg daily gefitinib and 150 mg daily erlotinib in Japanese patients with non-small cell lung cancer.
Fujita, S; Fukuhara, A; Hatachi, Y; Kim, YH; Masago, K; Mio, T; Mishima, M; Nagai, H; Sakamori, Y; Togashi, Y, 2011
)
0.37
"More adverse events including skin disorders, diarrhea, oral mucositis, asthenic conditions, anorexia, nausea, vomiting, and gastrointestinal bleeding were observed in the erlotinib group."( Differences in adverse events between 250 mg daily gefitinib and 150 mg daily erlotinib in Japanese patients with non-small cell lung cancer.
Fujita, S; Fukuhara, A; Hatachi, Y; Kim, YH; Masago, K; Mio, T; Mishima, M; Nagai, H; Sakamori, Y; Togashi, Y, 2011
)
0.37
" The proportion of patients that experienced at least one adverse event was similar for both groups."( Efficacy and safety of initial combination therapy with linagliptin and pioglitazone in patients with inadequately controlled type 2 diabetes: a randomized, double-blind, placebo-controlled study.
Dugi, KA; Espadero, RM; Gomis, R; Jones, R; Woerle, HJ, 2011
)
0.37
" Although agents such as gefitinib, erlotinib, cetuximab, lapatinib, and panitumumab have less systemic side-effects than traditional cytotoxic chemotherapy, dermatologic adverse events from EGFRIs are significantly more common."( Prophylaxis and treatment of dermatologic adverse events from epidermal growth factor receptor inhibitors.
Anadkat, MJ; Balagula, Y; Lacouture, ME; Wu, PA, 2011
)
0.37
"This review provides a symptom-based treatment approach to the common dermatologic adverse effects seen with the epidermal growth factor receptor antagonists: papulopustular rash, xerosis, pruritus as well as hair, nail, and mucosal changes."( Prophylaxis and treatment of dermatologic adverse events from epidermal growth factor receptor inhibitors.
Anadkat, MJ; Balagula, Y; Lacouture, ME; Wu, PA, 2011
)
0.37
"Although the field continues to evolve, this review presents the most up-to-date information on managing dermatologic adverse effects of EGFRIs."( Prophylaxis and treatment of dermatologic adverse events from epidermal growth factor receptor inhibitors.
Anadkat, MJ; Balagula, Y; Lacouture, ME; Wu, PA, 2011
)
0.37
" Neutropenia and febrile neutropenia were the most commonly reported adverse events."( A Phase I study to assess the safety, pharmacokinetics and efficacy of barasertib (AZD1152), an Aurora B kinase inhibitor, in Japanese patients with advanced acute myeloid leukemia.
Ando, K; Asou, H; Fujisawa, S; Hotta, T; Kihara, R; Miyawaki, S; Sakura, T; Tobinai, K; Tsuboi, K; Uike, N; Watanabe, T; Yamauchi, T; Yokozawa, T, 2011
)
0.37
"Objective of this indirect economic comparison was to estimate and compare management costs of grade 3/4 adverse events (AEs) reported for first-line erlotinib or pemetrexed maintenance therapy in patients with advanced non-small cell lung cancer (NSCLC)."( Comparison of treatment costs of grade 3/4 adverse events associated with erlotinib or pemetrexed maintenance therapy for patients with advanced non-small-cell lung cancer (NSCLC) in Germany, France, Italy, and Spain.
Banz, K; Bischoff, H; Brunner, M; Chouaid, C; de Castro Carpeño, J; de Marinis, F; Grossi, F; Vergnenègre, A; Walzer, S, 2011
)
0.37
" Adverse drug reactions of erlotinib in Japanese, which may be very different from those in Caucasians because of differences in genetic background, have not been fully reported."( Safety of erlotinib treatment in outpatients with previously treated non-small-cell lung cancer in Japan.
Date, H; Mishima, M; Nagai, H; Niimi, M; Sasaki, T; Seo, N; Tanaka, S; Yanagihara, K; Yasuda, H, 2011
)
0.37
" Erlotinib 150 mg/day was administered until progressive disease or discontinuation due to adverse events."( Safety of erlotinib treatment in outpatients with previously treated non-small-cell lung cancer in Japan.
Date, H; Mishima, M; Nagai, H; Niimi, M; Sasaki, T; Seo, N; Tanaka, S; Yanagihara, K; Yasuda, H, 2011
)
0.37
" However, these adverse events were well controllable in outpatients treated with erlotinib."( Safety of erlotinib treatment in outpatients with previously treated non-small-cell lung cancer in Japan.
Date, H; Mishima, M; Nagai, H; Niimi, M; Sasaki, T; Seo, N; Tanaka, S; Yanagihara, K; Yasuda, H, 2011
)
0.37
" Close collaboration with cardiology colleagues for early indicators of serious cardiac adverse events will likely minimize toxicity while optimizing the therapeutic potential of VDAs and ultimately enhancing patient outcomes."( Cardiovascular toxicity profiles of vascular-disrupting agents.
Lenihan, DJ; Subbiah, IM; Tsimberidou, AM, 2011
)
0.37
"6%) out of 232 ET patients experienced 88 cardiovascular adverse events (CV-AEs) during anagrelide treatment (522 pt-y)."( Low impact of cardiovascular adverse events on anagrelide treatment discontinuation in a cohort of 232 patients with essential thrombocythemia.
Cacciola, E; Cacciola, R; Candoni, A; Ciancia, R; Codeluppi, K; Crugnola, M; Grossi, A; Gugliotta, L; Iurlo, A; Liberati, AM; Lunghi, M; Martinelli, V; Mazzucconi, MG; Palmieri, F; Pierri, I; Scalzulli, PR; Specchia, G; Tieghi, A; Tortorella, G; Usala, E; Vannucchi, AM; Vianelli, N, 2011
)
0.37
" Toxicity was evaluated according to the Common Terminology Criteria for Adverse Events (CTCAE)."( [Efficacy and toxicity of erlotinib in non-small cell lung cancer treatment].
Arias-Santos, I; Constenla-Caramés, L; Lago-Rivero, N; Mucientes-Molina, A; Pedrido-Reino, E; Romero-Ventosa, EY,
)
0.13
"Survival analysis findings suggest lower efficacy in our patient population in comparison with data seen in other publications, and adverse events followed the expected pattern."( [Efficacy and toxicity of erlotinib in non-small cell lung cancer treatment].
Arias-Santos, I; Constenla-Caramés, L; Lago-Rivero, N; Mucientes-Molina, A; Pedrido-Reino, E; Romero-Ventosa, EY,
)
0.13
" In all, 19 out of 60 patients discontinued cediranib or placebo during chemotherapy because of adverse events/intercurrent illness (n=9); disease progression (n=1); death (n=3); patient decision (n=1); administrative reasons (n=1); and multiple reasons (n=4)."( Initial toxicity assessment of ICON6: a randomised trial of cediranib plus chemotherapy in platinum-sensitive relapsed ovarian cancer.
Griffin, CL; Hirte, H; Ledermann, JA; Parmar, MK; Qian, W; Raja, FA; Swart, AM, 2011
)
0.37
"Historically, skin toxicity has been assessed in prospective clinical trials using the clinician-reported National Cancer Institute Common Terminology Criteria for Adverse Events (CTCAE)."( Using the Skindex-16 and Common Terminology Criteria for Adverse Events to assess rash symptoms: results of a pooled-analysis (N0993).
Atherton, PJ; Burger, KN; Jatoi, A; Loprinzi, CL; Miller, RC; Neben Wittich, MA; Sloan, JA, 2012
)
0.38
" Statistical procedures, including Pearson correlations, were utilized to determine relationships between adverse event (AE) grades and Skindex-16 scores."( Using the Skindex-16 and Common Terminology Criteria for Adverse Events to assess rash symptoms: results of a pooled-analysis (N0993).
Atherton, PJ; Burger, KN; Jatoi, A; Loprinzi, CL; Miller, RC; Neben Wittich, MA; Sloan, JA, 2012
)
0.38
" Since many immunosuppressive agents have toxic effects on the function of transplanted islets, we investigated whether this was also the case with AEB."( AEB071 (sotrastaurin) does not exhibit toxic effects on human islets in vitro, nor after transplantation into immunodeficient mice.
Davis, J; Edgar, RL; Emamaullee, JA; Kin, T; McCall, M; Merani, S; Pawlick, RL; Shapiro, AM; Toso, C,
)
0.13
"While new anticancer angiogenesis inhibitors present a well-tolerated safety profile, they are not without adverse events."( [Dermatologic side effects induced by new angiogenesis inhibitors].
Chevreau, C; Cottura, E; Garrido-Stowhas, I; Sibaud, V, 2011
)
0.37
" The most common gefitinib-related adverse events were nausea and diarrhea, vomiting, and rash."( Safety and pharmacokinetics of high-dose gefitinib in patients with solid tumors: results of a phase I study.
Agus, DB; Gross, ME; Leichman, L; Lowe, ES; Swaisland, A, 2012
)
0.38
" Drug-related adverse event rates were comparable across treatment groups over 12 weeks (9."( Linagliptin monotherapy provides superior glycaemic control versus placebo or voglibose with comparable safety in Japanese patients with type 2 diabetes: a randomized, placebo and active comparator-controlled, double-blind study.
Araki, E; Dugi, KA; Gong, Y; Hayashi, N; Horie, Y; Inagaki, N; Kawamori, R; Sarashina, A; von Eynatten, M; Watada, H; Woerle, HJ, 2012
)
0.38
"To review the cutaneous adverse events related to EGFR inhibitors."( The management of EGFR inhibitor adverse events: a case series and treatment paradigm.
Chachoua, A; Cohen, DE; de Souza, A; Wnorowski, AM, 2012
)
0.38
"A retrospective chart review of all cases referred for the management of cutaneous adverse events after the initiation of EGFR inhibitor therapy between the years of 2006 and 2009 was performed."( The management of EGFR inhibitor adverse events: a case series and treatment paradigm.
Chachoua, A; Cohen, DE; de Souza, A; Wnorowski, AM, 2012
)
0.38
"Four men and 11 women had cutaneous adverse events while receiving erlotinib (mean dose: 112."( The management of EGFR inhibitor adverse events: a case series and treatment paradigm.
Chachoua, A; Cohen, DE; de Souza, A; Wnorowski, AM, 2012
)
0.38
"The most common cutaneous adverse event in our cohort was papulopustular rash, followed by eczema and xerosis."( The management of EGFR inhibitor adverse events: a case series and treatment paradigm.
Chachoua, A; Cohen, DE; de Souza, A; Wnorowski, AM, 2012
)
0.38
" The overall incidence of adverse events (AEs) or serious AEs with linagliptin was similar to placebo (AEs 55."( Safety and tolerability of linagliptin: a pooled analysis of data from randomized controlled trials in 3572 patients with type 2 diabetes mellitus.
Barnett, AH; Emser, A; Patel, S; Schernthaner, G; Troost, J; von Eynatten, M; Woerle, HJ, 2012
)
0.38
" Rash (98/196 [50%] in the erlotinib group vs 10/213 [5%] in the chemotherapy group for all grades; nine [5%] vs none for grade 3 or 4) and diarrhoea (36 [18%] vs four [2%] for all grades; five [3%] vs none for grade 3 or 4) were the most common treatment-related adverse events with erlotinib, whereas alopecia (none vs 23 [11%] for all grades; none vs one [<1%] for grade 3/4) was the most common treatment-related adverse event with chemotherapy."( Efficacy and safety of erlotinib versus chemotherapy in second-line treatment of patients with advanced, non-small-cell lung cancer with poor prognosis (TITAN): a randomised multicentre, open-label, phase 3 study.
Cicenas, S; Ciuleanu, T; Gonzalez, EE; Grigorescu, AC; Hillenbach, C; Johannsdottir, HK; Klughammer, B; Miliauskas, S; Stelmakh, L, 2012
)
0.38
" Vandetanib was associated with more frequent adverse events."( Efficacy and safety of vandetanib, a dual VEGFR and EGFR inhibitor, in advanced non-small-cell lung cancer: a systematic review and meta-analysis.
Bai, C; He, J; Li, H; Qin, Y; Song, H; Wang, C; Wei, L; Wu, C; Wu, M; Xu, J; Zhang, X; Zhu, T, 2011
)
0.37
" The most common adverse events were diarrhoea (67 %), nausea (67 %), decreased appetite (58 %), lymphopenia (50 %) and pyrexia (50 %)."( First report of the safety, tolerability, and pharmacokinetics of the Src kinase inhibitor saracatinib (AZD0530) in Japanese patients with advanced solid tumours.
Boku, N; Fujisaka, Y; Goto, I; Kurata, T; Machida, N; Onozawa, Y; Shi, X; Shimada, H; Watanabe, J; Yamazaki, K; Yasui, H, 2013
)
0.39
" The most common treatment-related adverse events were rash, diarrhea and pruritus."( Efficacy and safety of maintenance erlotinib in Asian patients with advanced non-small-cell lung cancer: a subanalysis of the phase III, randomized SATURN study.
Kim, JH; Klingelschmitt, G; Ng, C; Park, K; Wu, YL; Zaatar, A, 2012
)
0.38
" Treatment-emergent adverse events were generally mild and included fatigue, nausea, vomiting, and chills."( Safety and pharmacokinetics of ganitumab (AMG 479) combined with sorafenib, panitumumab, erlotinib, or gemcitabine in patients with advanced solid tumors.
Chan, E; Deng, H; Friberg, G; Gilbert, J; Hwang, YC; Mahalingam, D; McCaffery, I; Michael, SA; Mita, AC; Mita, MM; Mulay, M; Puzanov, I; Rosen, LS; Sarantopoulos, J; Shubhakar, P; Zhu, M, 2012
)
0.38
"Ganitumab up to 12 mg/kg was well tolerated, without adverse effects on pharmacokinetics in combination with either sorafenib, panitumumab, erlotinib, or gemcitabine."( Safety and pharmacokinetics of ganitumab (AMG 479) combined with sorafenib, panitumumab, erlotinib, or gemcitabine in patients with advanced solid tumors.
Chan, E; Deng, H; Friberg, G; Gilbert, J; Hwang, YC; Mahalingam, D; McCaffery, I; Michael, SA; Mita, AC; Mita, MM; Mulay, M; Puzanov, I; Rosen, LS; Sarantopoulos, J; Shubhakar, P; Zhu, M, 2012
)
0.38
" Eighty-seven subpopulation patients (18%) had an erlotinib-related AE; other than the protocol-defined frequent adverse events (AEs); 4% had a grade ≥3 erlotinib-related AE, 7% had an erlotinib-related serious AE."( Efficacy and safety of first-line erlotinib in elderly patients with advanced non-small cell lung cancer.
Au, JS; Cheng, CK; Merimsky, O; Reck, M; von Pawel, J, 2012
)
0.38
" According to our findings, lapatinib was safe and well tolerated and has a low incidence of cardiac side effects."( Evaluation of cardiac safety of lapatinib therapy for ErbB2-positive metastatic breast cancer: a single center experience.
Altundag, K; Dogan, E; Ozer, N; Ozisik, Y; Petekkaya, I; Yorgun, H, 2012
)
0.38
" The most frequently observed afatinib-associated adverse events (AEs) were gastrointestinal and skin-related side effects, which were manageable by symptomatic treatment and dose reductions."( A phase II trial to assess efficacy and safety of afatinib in extensively pretreated patients with HER2-negative metastatic breast cancer.
Awada, A; Beckmann, MW; Besse-Hammer, T; Canon, JL; De Grève, J; Dirix, L; Fasching, PA; Fleischer, F; Gottschalk, N; Harbeck, N; Harter, P; Jonat, W; Neven, P; Piccart, M; Possinger, K; Schmidt, M; Schuler, M; Schütte, J; Uttenreuther-Fischer, M; Wind, S, 2012
)
0.38
"Objectives were to assess maximum tolerated dose, dose-limiting toxicity (DLT) and to recommend a safe dose of LAP when administered with 4 cycles of TPF followed by CRT."( EORTC 24051: unexpected side effects in a phase I study of TPF induction chemotherapy followed by chemoradiation with lapatinib, a dual EGFR/ErbB2 inhibitor, in patients with locally advanced resectable larynx and hypopharynx squamous cell carcinoma.
Andry, G; Awada, A; Bogaerts, J; El-Hariry, I; Fortpied, C; Lacombe, D; Lalami, Y; Langendijk, JA; Liberatoscioli, C; Specenier, PM; Vermorken, JB, 2012
)
0.38
" Overall adverse event incidence was similar over 1 year (94."( Long-term efficacy and safety of linagliptin in patients with type 2 diabetes and severe renal impairment: a 1-year, randomized, double-blind, placebo-controlled study.
McGill, JB; Newman, J; Patel, S; Sauce, C; Sloan, L; von Eynatten, M; Woerle, HJ, 2013
)
0.39
"Rash, liver dysfunction, and diarrhea are known as adverse events of erlotinib and gefitinib."( Comparison of adverse events of erlotinib with those of gefitinib in patients with non-small cell lung cancer: a case-control study in a Japanese population.
Hirata, K; Kimura, T; Kira, Y; Kudoh, S; Mitsuoka, S; Nagata, M; Suzumura, T; Tanaka, H; Umekawa, K; Yoshimura, N, 2012
)
0.38
"The frequency of each adverse event was evaluated in a case-control study on Japanese patients who were treated with gefitinib or erlotinib."( Comparison of adverse events of erlotinib with those of gefitinib in patients with non-small cell lung cancer: a case-control study in a Japanese population.
Hirata, K; Kimura, T; Kira, Y; Kudoh, S; Mitsuoka, S; Nagata, M; Suzumura, T; Tanaka, H; Umekawa, K; Yoshimura, N, 2012
)
0.38
" Reduced function of CYP2D6 was not associated with an increased risk of any adverse events in both gefitinib and erlotinib cohorts."( Comparison of adverse events of erlotinib with those of gefitinib in patients with non-small cell lung cancer: a case-control study in a Japanese population.
Hirata, K; Kimura, T; Kira, Y; Kudoh, S; Mitsuoka, S; Nagata, M; Suzumura, T; Tanaka, H; Umekawa, K; Yoshimura, N, 2012
)
0.38
" Long-term treatment with linagliptin was well tolerated; adverse events (AEs) of special interest and serious AEs occurred in small percentages of patients."( Long-term safety of linagliptin monotherapy in Japanese patients with type 2 diabetes.
Araki, E; Dugi, K; Hayashi, N; Horie, Y; Inagaki, N; Kawamori, R; Sarashina, A; Thiemann, S; von Eynatten, M; Watada, H; Woerle, HJ, 2013
)
0.39
" The most frequent adverse events (AEs) were headache (60 %) and palpitations (40 %)."( Cardiovascular safety of anagrelide in healthy subjects: effects of caffeine and food intake on pharmacokinetics and adverse reactions.
Datino, T; Fernández-Avilés, F; Figueiras-Graillet, L; Franklin, R; Gama, JG; Jones, C; Martínez-Sellés, M, 2013
)
0.39
" However, the efficacy of these agents against EGFR wild-type (-wt) NSCLC remains unclear, and the frequency of adverse events (AEs) appears to differ between them at each approved dose."( Comparison of adverse events and efficacy between gefitinib and erlotinib in patients with non-small-cell lung cancer: a retrospective analysis.
Abe, H; Azuma, K; Hattori, S; Hoshino, T; Kage, M; Kawahara, A; Yamada, K; Yamashita, F; Yoshida, T; Zaizen, Y, 2013
)
0.39
" Most frequent adverse events (AEs, any grade) were diarrhea and nausea."( A phase Ib, open-label study to assess the safety of continuous oral treatment with afatinib in combination with two chemotherapy regimens: cisplatin plus paclitaxel and cisplatin plus 5-fluorouracil, in patients with advanced solid tumors.
Ehrnrooth, E; Lahogue, A; Machiels, JP; Pelling, K; Rottey, S; Vermorken, JB; Wind, S, 2013
)
0.39
" α(1) Blockers generally lead to more adverse effects compared with placebo, and those caused by terazosin were more frequent than others."( The efficacy and safety of alpha-1 blockers for benign prostatic hyperplasia: an overview of 15 systematic reviews.
Liu, Y; Mao, C; Qin, X; Yang, K; Yang, Z; Yuan, J, 2013
)
0.39
" The adverse effects caused by α(1) blockers are generally mild and well-tolerated."( The efficacy and safety of alpha-1 blockers for benign prostatic hyperplasia: an overview of 15 systematic reviews.
Liu, Y; Mao, C; Qin, X; Yang, K; Yang, Z; Yuan, J, 2013
)
0.39
" Adverse events were mild or moderate, and none led to discontinuation."( Open-label, dose-titration and continuation study to assess efficacy, safety, and pharmacokinetics of anagrelide in treatment-naïve Japanese patients with essential thrombocythemia.
Abhyankar, B; Hodgson, I; Kanakura, Y; Miyakawa, Y; Okamoto, S; Smith, J; Troy, S, 2013
)
0.39
" Adverse event rates were similar for linagliptin (61."( Efficacy and safety of linagliptin in subjects with type 2 diabetes mellitus and poor glycemic control: pooled analysis of data from three placebo-controlled phase III trials.
Chiavetta, S; Del Prato, S; Emser, A; Gong, Y; Owens, DR; Patel, S; Taskinen, MR; von Eynatten, M; Woerle, HJ,
)
0.13
" Even if linagliptin is safe in patients with renal impairment, the use of metformin (and thus of the linagliptin plus metformin FDC) is still controversial in this population."( Efficacy and safety of Jentadueto® (linagliptin plus metformin).
Scheen, AJ, 2013
)
0.39
"Dermatologic adverse events (AEs) are frequently observed in patients receiving EGF receptor (EGFR; also known as ErbB1) tyrosine kinase inhibitor therapy."( Dermatologic adverse events associated with afatinib: an oral ErbB family blocker.
Chu, CY; Hauschild, A; Lacouture, ME; O'Brien, D; Schadendorf, D; Stammberger, U; Uttenreuther-Fischer, M, 2013
)
0.39
" The adverse effects (AEs) were also considered."( Comparison of the efficacy and safety of single-agent erlotinib and doublet molecular targeted agents based on erlotinib in advanced non-small cell lung cancer (NSCLC): a systematic review and meta-analysis.
Ke, S; Pan, G; Zhao, J, 2013
)
0.39
" Incidents of adverse cardiac drug reactions are more common in patients with preexisting heart disease than the general population."( Drug screening using a library of human induced pluripotent stem cell-derived cardiomyocytes reveals disease-specific patterns of cardiotoxicity.
Bers, DM; Diecke, S; Gong, T; Knowles, JW; Lan, F; Lee, AS; Liang, P; Nguyen, PK; Robbins, RC; Sallam, K; Sanchez-Freire, V; Wang, PJ; Wang, Y; Wu, JC, 2013
)
0.39
" Our data indicate that healthy and diseased individuals exhibit different susceptibilities to cardiotoxic drugs and that use of disease-specific hiPSC-CMs may predict adverse drug responses more accurately than the standard human ether-a-go-go-related gene test or healthy control hiPSC-CM/hESC-CM screening assays."( Drug screening using a library of human induced pluripotent stem cell-derived cardiomyocytes reveals disease-specific patterns of cardiotoxicity.
Bers, DM; Diecke, S; Gong, T; Knowles, JW; Lan, F; Lee, AS; Liang, P; Nguyen, PK; Robbins, RC; Sallam, K; Sanchez-Freire, V; Wang, PJ; Wang, Y; Wu, JC, 2013
)
0.39
" It has a favorable toxicity profile but may induce unexpected adverse effects, such as an infiammatory reaction in the bladder."( Gefitinib in non-small cell lung carcinoma: a case report of an unusual side effect and complete response in advanced disease.
Brangi, M; Cartenì, G; Chiurazzi, B; Laterza, MM; Riccardi, F,
)
0.13
" Despite their selective molecular targeting and demonstrated clinical benefit, TKIs produce a range of serious adverse events, including drug-induced liver injury, that require careful patient management to maintain treatment benefit without harm."( Genetic characterization to improve interpretation and clinical management of hepatotoxicity caused by tyrosine kinase inhibitors.
Hunt, CM; Spraggs, CF; Xu, CF, 2013
)
0.39
" The incidence of drug-related adverse events was similar for linagliptin and placebo (10."( Efficacy and safety of linagliptin in type 2 diabetes subjects at high risk for renal and cardiovascular disease: a pooled analysis of six phase III clinical trials.
Emser, A; Gong, Y; von Eynatten, M; Woerle, HJ, 2013
)
0.39
" Stomatitis and febrile neutropenia were the most common adverse events with barasertib versus LDAC (71% vs 15% and 67% vs 19%, respectively)."( Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia.
Ando, K; Bay, JO; Giagounidis, A; Gröpper, S; Jabbour, EJ; Kantarjian, HM; Martinelli, G; Owen, K; Papayannidis, C; Pike, L; Quintás-Cardama, A; Schmitt, N; Stockman, PK; Wei, A, 2013
)
0.39
"Barasertib produced a significant improvement in the OCRR versus LDAC and had a more toxic but manageable safety profile, consistent with previous studies."( Stage I of a phase 2 study assessing the efficacy, safety, and tolerability of barasertib (AZD1152) versus low-dose cytosine arabinoside in elderly patients with acute myeloid leukemia.
Ando, K; Bay, JO; Giagounidis, A; Gröpper, S; Jabbour, EJ; Kantarjian, HM; Martinelli, G; Owen, K; Papayannidis, C; Pike, L; Quintás-Cardama, A; Schmitt, N; Stockman, PK; Wei, A, 2013
)
0.39
"Although dual HER2 blockade shows promising results in patients with HER2-positive breast cancer it is unclear whether this treatment strategy increases the risk for cardiac adverse events."( Cardiac toxicity in breast cancer patients treated with dual HER2 blockade.
Lind, P; Nearchou, A; Polyzos, NP; Valachis, A, 2013
)
0.39
" Overall adverse event (AE) rates with linagliptin and placebo including background medication were similar (38."( Efficacy and safety of linagliptin added to metformin and sulphonylurea in Chinese patients with type 2 diabetes: a sub-analysis of data from a randomised clinical trial.
Gong, Y; Tong, N; Woerle, HJ; Yan, S; Yang, JK; Zeng, Z; Zhang, X, 2013
)
0.39
" The majority of drug-related adverse events were mild to moderate (grade 1 or 2); the most common adverse events reported were palmar-plantar erythrodysesthesia syndrome (76 %), diarrhea (67 %) and stomatitis (41 %)."( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study.
Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015
)
0.42
"The most frequent adverse events (AEs) for all cohorts were diarrhea (89%), rash (79%), fatigue (73%), alopecia (63%), nausea (63%), and vomiting (40%)."( An open-label safety study of lapatinib plus trastuzumab plus paclitaxel in first-line HER2-positive metastatic breast cancer.
Brewster, AM; Esteva, FJ; Florance, AM; Franco, SX; Hagan, MK; Perez, A; Somer, RA; Stein, S; Turner, S; Williams, W, 2013
)
0.39
" However, frequent repeated dosing is required, and hepatic and cardiac adverse events may occur."( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis.
Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013
)
0.39
" Most adverse events were mild or moderate, and treatment-related adverse events were all ≤3%."( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis.
Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013
)
0.39
" The 3 drugs clinically associated with severe cardiac adverse events (crizotinib, sunitinib, nilotinib) all proved to be cardiotoxic in our in vitro tests while the relatively cardiac-safe drug erlotinib showed only minor changes in cardiac cell health."( Multi-parameter in vitro toxicity testing of crizotinib, sunitinib, erlotinib, and nilotinib in human cardiomyocytes.
Bacus, S; Brown, AM; Doherty, KR; Kramer, JW; Moran, DM; Shell, SA; Talbert, DR; Trusk, PB; Wappel, RL, 2013
)
0.39
" The MTD was defined as the highest dose at which ≤ 1 patient within a cohort of 6 experienced a dose-limiting toxicity (DLT) (clinically significant adverse event [AE] or laboratory abnormality considered related to barasertib)."( Phase I study assessing the safety and tolerability of barasertib (AZD1152) with low-dose cytosine arabinoside in elderly patients with AML.
Garcia-Manero, G; Jabbour, EJ; Kantarjian, HM; Oliver, SD; Owen, K; Ribrag, V; Rousselot, P; Sekeres, MA; Stockman, PK, 2013
)
0.39
" DLTs were reported in 2 patients (both, National Cancer Institute Common Terminology Criteria for Adverse Events grade 3 stomatitis/mucositis; 1200 mg cohort)."( Phase I study assessing the safety and tolerability of barasertib (AZD1152) with low-dose cytosine arabinoside in elderly patients with AML.
Garcia-Manero, G; Jabbour, EJ; Kantarjian, HM; Oliver, SD; Owen, K; Ribrag, V; Rousselot, P; Sekeres, MA; Stockman, PK, 2013
)
0.39
"The dermatologic side effects are the most common adverse effects associated with Epidermal Growth Factor Receptor tyrosine kinase inhibitors."( IL-33/IL-31 axis: a new pathological mechanisms for EGFR tyrosine kinase inhibitors-associated skin toxicity.
Adamo, V; David, A; Franchina, T; Gangemi, S; Kennez, I; Minciullo, PL; Profita, M; Zanghì, M, 2013
)
0.39
" Safety was assessed by recording the adverse events."( [The evaluation of efficacy and safety of treatment with dalfaz SR in patients with prostatic adenoma].
Pushkar', DIu; Rasner, PI,
)
0.13
" Adverse event rates were similar between groups, with most events being mild or moderate, and the incidence of investigator-defined hypoglycaemia was low, with no severe events."( Initial combination of linagliptin and metformin in patients with type 2 diabetes: efficacy and safety in a randomised, double-blind 1-year extension study.
Haak, T; Jones, R; Meinicke, T; von Eynatten, M; Weber, S; Woerle, HJ, 2013
)
0.39
" Serious adverse event was defined as grade 3/4 hematological and non-hematological toxicities."( Concurrent chemoradiation with weekly cisplatin, docetaxel and gefitinib: A study to assess feasibility, toxicity and immediate response.
Azmi, KS; Eswaran, P,
)
0.13
"All patients (three in dose level 1 [5 mg/m(2)], level 2 [10 mg/m(2)] and level 3 [15 mg/m(2)]) did not experience any hematological serious adverse events."( Concurrent chemoradiation with weekly cisplatin, docetaxel and gefitinib: A study to assess feasibility, toxicity and immediate response.
Azmi, KS; Eswaran, P,
)
0.13
"Gefitinib, a selective inhibitor of the epidermal growth factor receptor-tyrosine kinase, it's one of the most frequent drug-related adverse effects (AEs) reported in literature is dermatologic AEs."( A severe dermatologic adverse effect related with gefitinib: case report and review of the literature.
Li, YQ; Sun, H; Xue, D, 2013
)
0.39
" Given the potential for long-term vandetanib therapy in this setting, in addition to treatment for disease-related symptoms, effective management of related adverse events (AEs) is vital to ensure patient compliance and maximize clinical benefit with vandetanib therapy."( Vandetanib in advanced medullary thyroid cancer: review of adverse event management strategies.
Capdevila, J; Filetti, S; Grande, E; Kreissl, MC; Newbold, K; Reinisch, W; Robert, C; Schlumberger, M; Tolstrup, LK; Zamorano, JL, 2013
)
0.39
"Cardiac toxicity an uncommon but serious side-effect of some fluoropyrimides."( Final results of Australasian Gastrointestinal Trials Group ARCTIC study: an audit of raltitrexed for patients with cardiac toxicity induced by fluoropyrimidines.
Ferry, D; Fournier, M; Gebski, V; Gordon, S; Karapetis, CS; Price, TJ; Ransom, D; Simes, RJ; Tebbutt, N; Wilson, K; Yip, D, 2014
)
0.4
" Raltitrexed, alone or in combination with oxaliplatin or irinotecan, provides a safe option in terms of cardiac toxicity for such patients."( Final results of Australasian Gastrointestinal Trials Group ARCTIC study: an audit of raltitrexed for patients with cardiac toxicity induced by fluoropyrimidines.
Ferry, D; Fournier, M; Gebski, V; Gordon, S; Karapetis, CS; Price, TJ; Ransom, D; Simes, RJ; Tebbutt, N; Wilson, K; Yip, D, 2014
)
0.4
" At least one drug related adverse event was observed in 65."( Efficacy and safety of icotinib in Chinese patients with advanced non-small cell lung cancer after failure of chemotherapy.
He, C; Lin, B; Lou, G; Shao, L; Song, Z; Yu, X; Zhang, B; Zhang, Y, 2014
)
0.4
" Patients were evaluated for adverse events (AEs)."( Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors.
Cohen, RB; Engelman, JA; Felip, E; Jänne, PA; Laird, AD; Macé, S; Martinez, P; Rockich, K; Ruiz-Soto, R; Shapiro, GI; Xu, J, 2014
)
0.4
" As a result, we proposed tetrahydroquinazoline-type derivative as a safe and effective antimalarial candidate."( Synthesis of febrifugine derivatives and development of an effective and safe tetrahydroquinazoline-type antimalarial.
Hariguchi, N; Horoiwa, S; Kasahara, R; Kikuchi, H; Matsumoto, M; Oshima, Y, 2014
)
0.4
" Treatment discontinuation due to adverse events was more common in Arm A compared to Arm B (42 vs."( A randomized phase II efficacy and safety study of vandetanib (ZD6474) in combination with bicalutamide versus bicalutamide alone in patients with chemotherapy naïve castration-resistant prostate cancer.
Azad, AA; Beardsley, EK; Chi, KN; Chin, J; Ellard, SL; Hotte, SJ; Klotz, L; Kollmannsberger, C; Mukherjee, SD, 2014
)
0.4
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" Adverse events, effects, and survival condition were observed."( [Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].
Guo, L; Li, M; Liu, Z; Meng, Q; Shi, L; Tang, J; Tao, H; Tong, L; Wu, H; Wu, W; Xu, L; Zhu, Y, 2014
)
0.4
"The most common adverse events were diarrhea (n=5, 100%), skin rash (n=4, 80%), and mucositis/stomatitis (n=4, 80%)."( [Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].
Guo, L; Li, M; Liu, Z; Meng, Q; Shi, L; Tang, J; Tao, H; Tong, L; Wu, H; Wu, W; Xu, L; Zhu, Y, 2014
)
0.4
" The most common adverse events were diarrhea and skin rash."( [Adverse events of afatinib as first-line treatment for five cases of advanced lung adenocarcinoma and review of literature].
Guo, L; Li, M; Liu, Z; Meng, Q; Shi, L; Tang, J; Tao, H; Tong, L; Wu, H; Wu, W; Xu, L; Zhu, Y, 2014
)
0.4
" The most common treatment-emergent adverse events (TEAEs) were diarrhea (74 %), nausea (51 %), fatigue (51 %), rash (51 %), and injection-site reactions (49 %)."( Antitumor activity and safety of combination therapy with the Toll-like receptor 9 agonist IMO-2055, erlotinib, and bevacizumab in advanced or metastatic non-small cell lung cancer patients who have progressed following chemotherapy.
Bexon, AS; Boyd, TE; Conkling, P; de La Bourdonnaye, G; Mita, AC; Nemunaitis, JJ; Richards, DA; Smith, DA; Wages, D, 2014
)
0.4
" Safety was assessed by incidence and severity of adverse events (AEs) with a focus on hypoglycaemia."( Safety and efficacy of the dipeptidyl peptidase-4 inhibitor linagliptin in elderly patients with type 2 diabetes: a comprehensive analysis of data from 1331 individuals aged ≥ 65 years.
Barnett, AH; Hehnke, U; Patel, S; Schernthaner, G; von Eynatten, M; Woerle, HJ, 2014
)
0.4
" These data show that concentration-dependent disruption of the presumed targets for these inhibitors produce adverse outcomes at advanced life stages."( Immediate and long-term consequences of vascular toxicity during zebrafish development.
Bondesson, M; Hans, C; Harris, PS; Hemmer, MJ; Kleinstreuer, N; Knudsen, TB; McCollum, CW; Merchant, FA; Olin, J; Padilla, S; Shah, S; Tal, TL; Wood, CE, 2014
)
0.4
" From a literature review and this observation, arguments have been provided to justify erlotinib as a safe and well-tolered alternative for patients who have to stop gefitinib after a severe hepatotoxicity."( [Treatment with erlotinib after gefitinib induced hepatotoxicity: literature review and case report].
Durand, M; Fonrose, X; Logerot, S; Schir, E,
)
0.13
" The 4-week application of topical E6005 twice daily was safe and well tolerated."( Safety and efficacy of topical E6005, a phosphodiesterase 4 inhibitor, in Japanese adult patients with atopic dermatitis: results of a randomized, vehicle-controlled, multicenter clinical trial.
Akama, H; Furue, M; Hayashi, N; Hojo, S; Kitahara, Y; Nakagawa, H, 2014
)
0.4
" This low transplacental transfer is an important report, as potential side effect toxicity on the fetus is likely correlated to gefitinib blood concentration."( Efficacy and safety of gefitinib during pregnancy: case report and literature review.
Ayoubi, JM; Broutin, S; Couderc, LJ; Friard, S; Gil, S; Goetgheluck, J; Paci, A; Picone, O; Tcherakian, C, 2014
)
0.4
" In a cell-based model, sunitinib reduced CDK5 phosphorylation (pCDK5), calpain-dependent p35/p25 conversion and protected neuronal cells from the toxic effects of gp120."( Neuroprotective effects of the anti-cancer drug sunitinib in models of HIV neurotoxicity suggests potential for the treatment of neurodegenerative disorders.
Crews, LA; Gonzales, T; Kouznetsova, VL; Masliah, E; Overk, CR; Patrick, C; Paulino, A; Price, D; Rockenstein, E; Stocking, E; Tsigelny, IF; Wrasidlo, W, 2014
)
0.4
" The most common adverse events observed during anagrelide treatment were anemia, headache, palpitations, and diarrhea."( Phase III, single-arm study investigating the efficacy, safety, and tolerability of anagrelide as a second-line treatment in high-risk Japanese patients with essential thrombocythemia.
Achenbach, H; Kanakura, Y; Miyakawa, Y; Okamoto, S; Smith, J; Wilde, P, 2014
)
0.4
" Outcomes included pathologic complete response (pCR), overall survival (OS), progression-free survival (PFS), and adverse events."( Effect and safety of dual anti-human epidermal growth factor receptor 2 therapy compared to monotherapy in patients with human epidermal growth factor receptor 2-positive breast cancer: a systematic review.
He, J; Li, YS; Wei, X; Yu, FF; Zhang, TY; Zhang, X; Zhang, XJ, 2014
)
0.4
" Dual anti-HER2 therapy was associated with more frequent adverse events than monotherapy, but no statistical differences were observed in cardiac toxicity."( Effect and safety of dual anti-human epidermal growth factor receptor 2 therapy compared to monotherapy in patients with human epidermal growth factor receptor 2-positive breast cancer: a systematic review.
He, J; Li, YS; Wei, X; Yu, FF; Zhang, TY; Zhang, X; Zhang, XJ, 2014
)
0.4
" Safety data were pooled from a wider group of 10 trials with varying durations to capture the largest possible incidence of adverse events (AEs)."( Efficacy and safety of linagliptin as monotherapy or add-on treatment in Asian patients with suboptimal glycemic control: a pooled analysis.
Choi, DS; Emser, A; Gong, Y; Mohan, V; Patel, S; Siddiqui, K; Woerle, HJ; Zeng, Z, 2015
)
0.42
" As observed with reversible EGFR TKIs, it can induce class-effect adverse events."( Management of the adverse events of afatinib: a consensus of the recommendations of the Spanish expert panel.
Arriola, E; Artal, A; Cobo, M; Esteban, E; García-Campelo, R; García-Muret, MP; Reguart, N; Rodríguez, MC, 2015
)
0.42
" Herein, the authors emphasize the importance of recognizing this side effect in order to avoid from severe complications such as corneal ulcers in uncared patients."( Ocular side effects and trichomegaly of eyelashes induced by erlotinib: a case report and review of the literature.
Celik, T; Kosker, M, 2015
)
0.42
" The overall incidence of adverse drug reactions (ADRs) of any grade was 31."( A single-arm, multicenter, safety-monitoring, phase IV study of icotinib in treating advanced non-small cell lung cancer (NSCLC).
Ding, L; Gu, A; Han, B; He, J; Hu, X; Jia, X; Jiao, SC; Ma, K; Peng, J; Sun, Y; Tan, F; Wang, CL; Wang, J; Wang, Y; Wu, M; Ying, K; You, C; Zhang, L; Zhang, S; Zhang, Y, 2014
)
0.4
" Abnormal clinical observations and adverse effects on clinical pathology, urinalysis, and histology indicated acute renal damage and urothelial damage and bone marrow dysfunction."( Characterization of Batracylin-induced Renal and Bladder Toxicity in Rats.
Altera, KP; Ames, MM; Buhrow, SA; Bunin, DI; Davis, M; Ji, J; Kinders, RJ; Lawrence, SM; Parman, T; Rausch, LL; Reid, JM; Samuelsson, SJ; Walden, C, 2015
)
0.42
" Most of the patients on erlotinib show cutaneous adverse effects."( Erlotinib-induced cutaneous toxicity: findings on 18F-FDG PET/CT imaging.
Bal, C; Gupta, RK; Kumar, K; Kumar, R; Singh, H, 2015
)
0.42
" Overall survival, progression-free survival, and occurrence of adverse drug reactions were secondary endpoints."( Final safety and efficacy of erlotinib in the phase 4 POLARSTAR surveillance study of 10 708 Japanese patients with non-small-cell lung cancer.
Ando, M; Arakawa, H; Ebina, M; Fukuda, Y; Fukuoka, M; Gemma, A; Inoue, Y; Ishii, T; Johkoh, T; Kudoh, S; Kusumoto, M; Kuwano, K; Nakagawa, K; Ohe, Y; Sakai, F; Seki, A; Taniguchi, H; Yamazaki, N, 2014
)
0.4
" The most common drug-related adverse events were diarrhea (88%) and palmar-plantar erythrodysesthesia syndrome (48%)."( Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2-positive breast cancer.
Baselga, J; Cortés, J; Garcia-Saenz, JA; Germa, C; Harb, W; Kiger, C; Kim, SB; Martin, M; Moroose, R; Pluard, T; Saura, C; Wang, K; Xu, B, 2014
)
0.4
" Common adverse events (AEs) were also studied."( Efficacy and safety of angiogenesis inhibitors in advanced non-small cell lung cancer: a systematic review and meta-analysis.
Chen, Y; Hong, S; Luo, S; Tan, M; Wang, S; Zhang, L, 2015
)
0.42
" However, few studies focused on the risk and adverse events (AEs) of combined targeted therapy."( Safety profile of combined therapy inhibiting EFGR and VEGF pathways in patients with advanced non-small-cell lung cancer: A meta-analysis of 15 phase II/III randomized trials.
Huang, J; Ji, LJ; Liu, H; Liu, Y; Ma, W; Qi, X; Xu, M; Zhu, Y, 2015
)
0.42
" EF is a toxic drug and causes hepatotoxicity in humans."( Toxicity of Evodiae fructus on rat liver mitochondria: the role of oxidative stress and mitochondrial permeability transition.
Cai, Q; Li, W; Shi, S; Wang, Q; Wei, J; Wei, R; Zhang, Y; Zhao, W, 2014
)
0.4
" Common treatment-related adverse events were dermatitis acneiform, diarrhea, and paronychia; there were no treatment-related grade 4 or 5 adverse events."( Safety and efficacy of dacomitinib in korean patients with KRAS wild-type advanced non-small-cell lung cancer refractory to chemotherapy and erlotinib or gefitinib: a phase I/II trial.
Ahn, MJ; Campbell, AK; Cho, BC; Gernhardt, D; Giri, N; Heo, DS; Kim, DW; Lee, SY; Letrent, SP; O'Connell, J; Park, K; Taylor, I; Zhang, H, 2014
)
0.4
" We compared the frequencies of severe adverse events (AEs) among EGFR mutation-positive NSCLC patients treated with these three EGFR-TKIs."( Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer.
Nakagawa, K; Okamoto, I; Takeda, M, 2015
)
0.42
" Based on these findings, KST9046 can be further evaluated as a promising safe new hit for the development of broad spectrum anticancer agents with a selectivity for DDR1 kinase."( Discovery of a broad spectrum antiproliferative agent with selectivity for DDR1 kinase: cell line-based assay, kinase panel, molecular docking, and toxicity studies.
Cho, NC; Elkamhawy, A; Pae, AN; Park, JE; Roh, EJ; Sim, T, 2016
)
0.43
" Overall, the safety profile of linagliptin in this patient group was comparable to that of placebo, with comparable incidence of adverse events; linagliptin was weight-neutral in this patient population."( Efficacy and safety of the dipeptidyl peptidase-4 inhibitor linagliptin in black/African American patients with type 2 diabetes: Pooled analysis from eight Phase III trials.
Crowe, S; Kountz, DS; Thrasher, J; von Eynatten, M; Woerle, HJ, 2015
)
0.42
" The most common adverse events (AEs) related to the study treatment were alopecia, diarrhea and decreased hemoglobin."( Safety, pharmacokinetics and efficacy findings in an open-label, single-arm study of weekly paclitaxel plus lapatinib as first-line therapy for Japanese women with HER2-positive metastatic breast cancer.
Aogi, K; Armour, A; Inoue, K; Iwata, H; Kuroi, K; Masuda, N; Nakayama, T; Nishimura, Y; Rai, Y; Sasaki, Y; Shimizu, S, 2015
)
0.42
"Previous reports regarding the cutaneous adverse events of epidermal growth factor receptor inhibitors are mostly limited to small case reports and case series, mainly involving Caucasian patients."( Cutaneous adverse events of epidermal growth factor receptor inhibitors: A retrospective review of 99 cases.
Chanprapaph, K; Pongcharoen, P; Vachiramon, V,
)
0.13
"We describe the trends in the clinical presentation of Asian patients who had cutaneous adverse events induced by epidermal growth factor receptor inhibitors and to explore the relationship between skin adverse events and tumor response."( Cutaneous adverse events of epidermal growth factor receptor inhibitors: A retrospective review of 99 cases.
Chanprapaph, K; Pongcharoen, P; Vachiramon, V,
)
0.13
" Cutaneous adverse events occurred in 43 (57."( Cutaneous adverse events of epidermal growth factor receptor inhibitors: A retrospective review of 99 cases.
Chanprapaph, K; Pongcharoen, P; Vachiramon, V,
)
0.13
"The limitations of study include its retrospective nature, and the initial screening of cutaneous adverse events was done by non-dermatologists."( Cutaneous adverse events of epidermal growth factor receptor inhibitors: A retrospective review of 99 cases.
Chanprapaph, K; Pongcharoen, P; Vachiramon, V,
)
0.13
"Cutaneous adverse events due to epidermal growth factor receptor inhibitors are not uncommon in the Asian population."( Cutaneous adverse events of epidermal growth factor receptor inhibitors: A retrospective review of 99 cases.
Chanprapaph, K; Pongcharoen, P; Vachiramon, V,
)
0.13
" TKIs plus radiotherapy significantly prolong the CNS-TTP and MOS of patients without enhancing overall severe adverse events."( Evaluation on efficacy and safety of tyrosine kinase inhibitors plus radiotherapy in NSCLC patients with brain metastases.
Chen, L; Chen, X; Luo, S; Xie, X, 2015
)
0.42
" The incidence of adverse events was significantly fewer in the icotinib group than in the chemotherapy group (P=0."( [Comparison of the Efficacy and Safety of Icotinib with Standard Second-line 
Chemotherapy in Previously Treated Advanced Non-small Cell Lung Cancer].
Li, Y; Qian, K; Wang, R; Yao, S; Zhang, Y, 2015
)
0.42
"Compared with the standard second-line chemotherapy, icotinib is active in the treatment of advanced NSCLC patients, especially with EGFR unknown in the second line, with an acceptable adverse event profile."( [Comparison of the Efficacy and Safety of Icotinib with Standard Second-line 
Chemotherapy in Previously Treated Advanced Non-small Cell Lung Cancer].
Li, Y; Qian, K; Wang, R; Yao, S; Zhang, Y, 2015
)
0.42
" The objective of this study was to estimate the costs of managing treatment-related grade ≥ 3 adverse events (AEs) that occurred in ≥ 2% of patients and grade 2 AEs that occurred in ≥ 5% of patients taking T-DM1 compared with patients taking CAP + LAP based on the EMILIA trial, from the perspective of Canadian public payers."( Safety Profile and Costs of Related Adverse Events of Trastuzumab Emtansine for the Treatment of HER2-Positive Locally Advanced or Metastatic Breast Cancer Compared to Capecitabine Plus Lapatinib from the Perspective of the Canadian Health-Care System.
Moser, A; Piwko, C; Pollex, E; Prady, C; Yunger, S, 2015
)
0.42
" Toxicity was obtained during four cycles by Common Terminology Criteria for Adverse Events."( Nutritional Status, Body Surface, and Low Lean Body Mass/Body Mass Index Are Related to Dose Reduction and Severe Gastrointestinal Toxicity Induced by Afatinib in Patients With Non-Small Cell Lung Cancer.
Arrieta, O; Baracos, VE; De la Torre-Vallejo, M; López-Macías, D; Macedo-Pérez, EO; Orta, D; Ramírez-Tirado, LA; Sánchez-Lara, K; Turcott, J, 2015
)
0.42
"Alfuzosin has been widely used to treat benign prostatic hyperplasia and prostatitis, and is claimed to be a selective agent for the lower urinary tract with low incidence of adverse side-effects and hypotensive changes."( Efficacy and Safety of Alfuzosin as Medical Expulsive Therapy for Ureteral Stones: A Systematic Review and Meta-Analysis.
Chen, K; Kang, R; Li, J; Liu, C; Wan, SP; Wu, W; Zeng, G, 2015
)
0.42
"Alfuzosin is a safe and effective agent for the expulsive therapy of ureteral stones smaller than 10 mm in size."( Efficacy and Safety of Alfuzosin as Medical Expulsive Therapy for Ureteral Stones: A Systematic Review and Meta-Analysis.
Chen, K; Kang, R; Li, J; Liu, C; Wan, SP; Wu, W; Zeng, G, 2015
)
0.42
" Frequency of anagrelide related adverse events was 65."( [Efficacy and safety of anagrelide in treatment of essential thrombocythemia: multicenter, randomized controlled clinical trial].
Cao, X; Fu, J; Gao, D; Ge, X; Hou, M; Jiang, B; Jin, J; Li, J; Li, K; Qian, W; Su, L; Sun, A; Wang, S; Wang, Z; Xiao, Z; Yang, L; Yang, R; Zhang, W; Zhang, X; Zhao, Y, 2015
)
0.42
" Incidence of adverse events was undifferentiated between anagrelide and hydroxyurea, but anagrelide treatment had tolerable adverse effects and no hematologic toxicity."( [Efficacy and safety of anagrelide in treatment of essential thrombocythemia: multicenter, randomized controlled clinical trial].
Cao, X; Fu, J; Gao, D; Ge, X; Hou, M; Jiang, B; Jin, J; Li, J; Li, K; Qian, W; Su, L; Sun, A; Wang, S; Wang, Z; Xiao, Z; Yang, L; Yang, R; Zhang, W; Zhang, X; Zhao, Y, 2015
)
0.42
" Four subjects receiving E6005 in Study 001 experienced a treatment-emergent adverse event (application site edema, increased alanine aminotransferase or erythema); three of these subjects discontinued the study."( Safety, tolerability and pharmacokinetics of a novel phosphodiesterase inhibitor, E6005 ointment, in healthy volunteers and in patients with atopic dermatitis.
Akama, H; Hojo, S; Nomoto, M; Ohba, F, 2016
)
0.43
" The most frequent treatment-related adverse events were rash (26%, 33/127), diarrhea (12."( The Efficacy and Safety of Icotinib in Patients with Advanced Non-Small Cell Lung Cancer Previously Treated with Chemotherapy: A Single-Arm, Multi-Center, Prospective Study.
Ding, L; Feng, J; Hu, C; Hu, X; Li, Q; Liu, X; Luo, R; Qin, S; Shi, Y; Song, Y; Sun, Y; Tan, F; Wang, D; Wang, J; Wang, Y; Xv, N; Zhang, L; Zhang, S; Zhou, C; Zhou, J, 2015
)
0.42
" Our study showed that long-term gefitinib-induced hepatotoxicity was a common adverse event, especially for the cohort with a duration of longer than 14 months."( Observation of hepatotoxicity during long-term gefitinib administration in patients with non-small-cell lung cancer.
Dong, M; He, X; Li, J; Wang, J; Wang, Y; Wang, Z; Wu, Y, 2016
)
0.43
" The majority of reported adverse events (AE) were grade 1 and 2 in severity with diarrhea being the most commonly observed AE CONCLUSION: In this heavily pretreated patient population, combination of vinorelbine plus lapatinib showed encouraging activity and was characterized by an acceptable safety profile."( Phase II study on the efficacy and safety of Lapatinib administered beyond disease progression and combined with vinorelbine in HER-2/neu- positive advanced breast cancer: results of the CECOG LaVie trial.
Bartsch, R; Brodowicz, T; Knittelfelder, R; Kuhar, CG; Lang, I; Melichar, B; Petruzelka, L; Singer, CF; Thallinger, C; Zielinski, C, 2016
)
0.43
" The common adverse events were skin toxicity (68% of patients), diarrhea (46%), and liver injury (63%)."( Association of pharmacokinetics and pharmacogenomics with safety and efficacy of gefitinib in patients with EGFR mutation positive advanced non-small cell lung cancer.
Fujita, K; Hirose, T; Ishida, H; Kusumoto, S; Murata, Y; Nakashima, M; Ohmori, T; Oki, Y; Okuda, K; Sasaki, Y; Shirai, T; Sugiyama, T; Yamaoka, T, 2016
)
0.43
" Conversion to MPS was associated with a higher incidence of adverse events."( Efficacy and Safety of Elective Conversion From Sotrastaurin (STN) to Tacrolimus (TAC) or Mycophenolate (MPS) in Stable Kidney Transplant Recipients.
Aguiar, W; Campos, E; Cristelli, M; Felipe, C; Ferreira, A; Franco, M; Gerbase de Lima, M; Hannun, P; Medina-Pestana, J; Sandes-Freitas, T; Tedesco-Silva, H, 2016
)
0.43
"The analysis of adverse events plays an important role in the benefit assessment of drugs."( Biometrical issues in the analysis of adverse events within the benefit assessment of drugs.
Beckmann, L; Bender, R; Lange, S, 2016
)
0.43
"Gefitinib (GEF) is a multi-targeted tyrosine kinase inhibitor with anti-cancer properties, yet few cases of cardiotoxicity has been reported as a significant side effect associated with GEF treatment."( Molecular mechanisms of cardiotoxicity of gefitinib in vivo and in vitro rat cardiomyocyte: Role of apoptosis and oxidative stress.
Ahmad, SF; Al-Alallah, IA; Alhaider, AA; Anazi, FE; Ansari, MA; Assiri, MA; Attafi, IM; Belali, OM; Korashy, HM, 2016
)
0.43
" This includes less toxic drugs, more selective towards tumor cells, causing less damage to the patient."( Phosphatidylinositol 3-Kinase/AKT Pathway Inhibition by Doxazosin Promotes Glioblastoma Cells Death, Upregulation of p53 and Triggers Low Neurotoxicity.
Battastini, AM; Coelho, BP; de Quadros, AH; Gaelzer, MM; Gonçalves, CA; Guerra, MC; Guma, FC; Hoppe, JB; Salbego, CG; Setton-Avruj, P; Terra, SR; Usach, V, 2016
)
0.43
" The most common adverse events are skin reaction and diarrhea, both of which are generally mild, noncumulative, and manageable."( Safety of gefitinib in non-small cell lung cancer treatment.
Hsiue, EH; Lee, JH; Lin, CC; Yang, JC, 2016
)
0.43
" Adverse events were assessed using National Cancer Institute Common Terminology Criteria for Adverse Events v4."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" The most common grade 3/4 adverse events were hand-foot skin reaction, hypertension, and thrombocytopenia."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" Our study suggests that the combination of two anti-HER2 agents does not significantly increase the risk for adverse compared with anti-HER2 monotherapy in patients with adequate cardiac function prior to start of therapy."( Applications of cardiotoxicity in breast cancer: a meta-analysis.
Davoodzadeh, H; Ebadi, A; Rahmani, H; Shahriary, A; Sheikhi, MA, 2017
)
0.46
" The elimination half-life was not a significant factor for PFS, but it was significantly correlated with high-grade adverse events."( Pharmacokinetic parameters of gefitinib predict efficacy and toxicity in patients with advanced non-small cell lung cancer harboring EGFR mutations.
Fukuda, M; Ikeda, T; Ikegami, Y; Izumikawa, K; Mizoguchi, K; Motoshima, K; Mukae, H; Nakamura, Y; Nakatomi, K; Ogawara, D; Sano, K; Sato, S; Senju, H; Sugasaki, N; Takemoto, S; Yamaguchi, H, 2016
)
0.43
" On the other hand, long elimination half-life was related to high-grade adverse events in these patients."( Pharmacokinetic parameters of gefitinib predict efficacy and toxicity in patients with advanced non-small cell lung cancer harboring EGFR mutations.
Fukuda, M; Ikeda, T; Ikegami, Y; Izumikawa, K; Mizoguchi, K; Motoshima, K; Mukae, H; Nakamura, Y; Nakatomi, K; Ogawara, D; Sano, K; Sato, S; Senju, H; Sugasaki, N; Takemoto, S; Yamaguchi, H, 2016
)
0.43
" Like other EGFR inhibitors, afatinib can provoke adverse events such as diarrhoea, rash, paronychia or mucositis."( [Toxicity associated with EGRF inhibition: review and key aspects in the management of afatinib].
Taus, Á, 2016
)
0.43
" In the case of drug-related grade ≥3 or selected prolonged grade 2 adverse events (AEs), the dose can be reduced by 10 mg decrements to a minimum of 20 mg."( Effect of dose adjustment on the safety and efficacy of afatinib for EGFR mutation-positive lung adenocarcinoma: post hoc analyses of the randomized LUX-Lung 3 and 6 trials.
Dickgreber, N; Feng, J; Geater, SL; Hirsh, V; Hu, CP; Huang, Y; Lu, S; Märten, A; Massey, D; Mok, T; O'Byrne, K; Okamoto, I; Schuler, M; Sebastian, M; Sequist, LV; Shah, R; Wind, S; Wu, YL; Yamamoto, N; Yang, JC; Zhou, C, 2016
)
0.43
" Diarrhea, mucositis and rash are frequent adverse events induced by afatinib, these can impair quality of life and sometimes afatinib discontinuation is necessary."( The safety of afatinib for the treatment of non-small cell lung cancer.
Arrieta, O; Barron, F; Cardona, AF; de la Torre-Vallejo, M; Luna-Palencia, RL, 2016
)
0.43
" The most common adverse events in vandetanib-treated patients are: diarrhea, rash, folliculitis, nausea, QTc prolongation, hypertension and fatigue."( The safety and efficacy of vandetanib in the treatment of progressive medullary thyroid cancer.
Antonelli, A; Baldini, E; Biricotti, M; Fallahi, P; Ferrari, SM; Materazzi, G; Miccoli, P; Ulisse, S, 2016
)
0.43
"3%) of 26 patients experienced at least one adverse event (AE); rash (61."( A Phase I Study of the Safety and Pharmacokinetics of Higher-Dose Icotinib in Patients With Advanced Non-Small Cell Lung Cancer.
Chen, J; Ding, L; Hu, X; Liu, J; Shentu, J; Tan, F; Wang, Y; Wu, G; Wu, L; Xu, W; Zhou, H; Zhu, M, 2016
)
0.43
" All patients experienced at least one adverse event (AE), and 7 patients (50%) experienced grade ≥3 AEs."( SAFETY AND TOLERABILITY OF VANDETANIB IN JAPANESE PATIENTS WITH MEDULLARY THYROID CANCER: A PHASE I/II OPEN-LABEL STUDY.
Horiuchi, K; Ito, Y; Komoda, M; Okamoto, T; Rito, K; Takahashi, S; Todo, T; Tomomatsu, J; Tsuji, A; Uchino, K, 2017
)
0.46
" The common adverse effects (AEs) included skin rash (31."( Efficacy and safety of icotinib in treating non-small cell lung cancer: a systematic evaluation and meta-analysis based on 15 studies.
Biaoxue, R; Hua, L; Shuanying, Y; Wenlong, G, 2016
)
0.43
"Interstitial lung disease is a well-known pulmonary adverse event that occurs during epidermal growth factor receptor-tyrosine kinase inhibitor (EGFR-TKI) therapy and results in restrictive ventilatory dysfunction."( An autopsy case of bronchiolitis obliterans as a previously unrecognized adverse event of afatinib treatment.
Bandoh, S; Chiba, Y; Ishii, T; Kadowaki, N; Kanaji, N; Kita, N; Sato, A; Tadokoro, A; Ueno, M; Watanabe, N, 2017
)
0.46
" The most common grade 3-4 adverse events were hypertension and hand-foot skin reaction."( Safety and efficacy of fruquintinib in patients with previously treated metastatic colorectal cancer: a phase Ib study and a randomized double-blind phase II study.
Bai, Y; Cao, J; Fan, S; Hua, Y; Li, J; Liu, T; Pan, H; Shen, L; Su, W; Wang, L; Xu, J; Xu, RH; Zhang, D, 2017
)
0.46
" More frequent grade 3 or 4 adverse events, including diarrhoea, rash or erythema, neutropenia and hepatic adverse events, were found in the combination group than in the trastuzumab or lapatinib group."( Efficacy and safety of lapatinib and trastuzumab for HER2-positive breast cancer: a systematic review and meta-analysis of randomised controlled trials.
Gao, L; Gao, X; Li, N; Liu, PJ; Tie, XJ; Xu, ZQ; Zhang, Y, 2017
)
0.46
" The cediranib intermittent schedule (n = 6) was examined because of recurrent grade 2 and non-dose-limiting toxicity grade 3 and 4 adverse events (AEs) on the daily schedule (n = 8)."( Safety and Clinical Activity of the Programmed Death-Ligand 1 Inhibitor Durvalumab in Combination With Poly (ADP-Ribose) Polymerase Inhibitor Olaparib or Vascular Endothelial Growth Factor Receptor 1-3 Inhibitor Cediranib in Women's Cancers: A Dose-Escala
Annunziata, CM; Botesteanu, DA; Cao, L; Cimino-Mathews, A; Figg, WD; Harrell, MI; Ho, TW; Houston, N; Kohn, EC; Lee, JM; Lipkowitz, S; Nguyen, J; Ogurtsova, A; Peer, CJ; Swisher, EM; Taube, JM; Thompson, E; Xu, H; Zimmer, A, 2017
)
0.46
" It is also essential to carefully monitor patients using TKI regarding possible adverse effects, which should be properly managed when occurring."( Medullary thyroid carcinoma - Adverse events during systemic treatment: risk-benefit ratio.
Maciel, LMZ; Magalhães, PKR,
)
0.13
" We aimed to determine whether or not pulse high-dose lapatinib was a safe and tolerable regimen in addition to standard therapy."( Report of safety of pulse dosing of lapatinib with temozolomide and radiation therapy for newly-diagnosed glioblastoma in a pilot phase II study.
Cloughesy, TF; Faiq, N; Green, R; Green, S; Hu, J; Lai, A; Mellinghoff, I; Nghiemphu, PL; Yu, A, 2017
)
0.46
" Dose-limiting toxic effects occurred in two (67%) of three patients who received 500 mg twice a day in the dose-escalation phase (grade 3 acne [n=1] and intolerable grade 2 mucosal inflammation [n=1]); hence, doses of 200 mg and 300 mg twice a day were selected for further assessment in the dose-expansion phase."( Activity and safety of AZD3759 in EGFR-mutant non-small-cell lung cancer with CNS metastases (BLOOM): a phase 1, open-label, dose-escalation and dose-expansion study.
Ahn, JS; Ahn, MJ; Cho, BC; Goldman, JW; Harrop, B; John, T; Kao, S; Kim, DW; Kim, HR; Kim, SW; Kim, TM; Lee, JS; Lin, CC; Natale, R; Overend, P; Rabbie, S; Su, WC; Yang, JC; Yang, Z, 2017
)
0.46
" This review summarizes the current state of knowledge of FIC with special regard to proposed pathogenetic models (coronary vasospasm, endothelium and cardiomyocytes damage, toxic metabolites, dihydropyrimidine dehydrogenase deficiency); risk and predictive factors; efficacy and usefulness in detection of laboratory markers, electrocardiographic changes and cardiac imaging; and specific treatment, including a novel agent, uridine triacetate."( Fluoropyrimidine-induced cardiotoxicity.
Aglietta, M; Bonzano, A; Cagnazzo, C; Depetris, I; Filippi, R; Leone, F; Marino, D, 2018
)
0.48
"Vandetanib, a multi-kinase inhibitor used for the treatment of various cancers, has been reported to induce several adverse cardiac effects."( Electrophysiological mechanisms of vandetanib-induced cardiotoxicity: Comparison of action potentials in rabbit Purkinje fibers and pluripotent stem cell-derived cardiomyocytes.
Byun, B; Chae, JH; Hyun, SA; Kim, KS; Lee, HA, 2018
)
0.48
" Antitumor effectiveness (overall survival [OS], progression-free survival [PFS], objective response rate [ORR] and disease control rate [DCR]) and adverse effects [AEs]) were assessed."( Gefitinib provides similar effectiveness and improved safety than erlotinib for advanced non-small cell lung cancer: A meta-analysis.
Peng, J; Wei, Y; Xu, J; Yu, D; Zhang, W, 2018
)
0.48
" In terms of safety, letermovir was at least similar in comparison with placebo and most agents while both letermovir and acyclovir showed significantly reduced risk for serious adverse events compared with ganciclovir, with RRs of ."( Comparative Efficacy and Safety of Different Antiviral Agents for Cytomegalovirus Prophylaxis in Allogeneic Hematopoietic Cell Transplantation: A Systematic Review and Meta-Analysis.
Gagelmann, N; Kröger, N; Ljungman, P; Styczynski, J, 2018
)
0.48
" A total of 143 adverse events (AEs) were reported, of which 87 were associated with cipatinib treatment and comprised: neutropenia (38%), hypertriglyceridemia (15%), fatigue (15%), nausea (12%), fever (19%), and myocardial ischemia (19%)."( Phase I safety and pharmacokinetic study of cipatinib, an original dual tyrosine kinase inhibitor.
Cai, R; Chen, S; Fan, Y; Han, Y; Li, Q; Luo, Y; Ma, F; Shi, X; Wang, J; Xu, B; Yuan, P; Zhang, P, 2018
)
0.48
" Grade 3 or 4 adverse events were reported for 24 (26."( Efficacy and safety of raltitrexed-based transarterial chemoembolization for colorectal cancer liver metastases.
Cao, H; Ding, W; Li, C; Li, W; Liu, R; Lu, L; Shao, G; Song, J; Wang, J; Xiang, H; Yang, J; Yang, Z, 2018
)
0.48
" TKIs also act systemically causing various adverse events (AEs)."( Pazopanib, Cabozantinib, and Vandetanib in the Treatment of Progressive Medullary Thyroid Cancer with a Special Focus on the Adverse Effects on Hypertension.
Bauer, J; Grimm, D; Grosse, J; Infanger, M; Kopp, S; Krüger, M; Milling, RV; Wehland, M, 2018
)
0.48
" The network meta-analysis is applied to compare the efficacies and adverse events of five targeted agents (erlotinib, gefitinib, vandetanib, dacomitinib, and icotinib) for advanced or metastatic NSCLC."( Efficacy and adverse events of five targeted agents in the treatment of advanced or metastatic non-small-cell lung cancer: A network meta-analysis of nine eligible randomized controlled trials involving 5,059 patients.
Li, XF; Liu, GF; Miao, YY; Yu, SN; Zhang, SH, 2019
)
0.51
" The most common adverse events (AEs) included diarrhea, hypocalcemia, asthenia, QTc prolongation, hypokalemia and keratopathy, all at generally higher incidence with 300 vs 150 mg (Part A)."( Safety and efficacy of two starting doses of vandetanib in advanced medullary thyroid cancer.
Dedecjus, M; Druce, M; Elisei, R; Gagel, RF; Hu, MI; Kapiteijn, E; Krajewska, J; Locati, L; Pacini, F; Popovtzer, A; Weiss, R, 2019
)
0.51
" Although the drug is generally well-tolerated, it can be associated with several unique and potentially serious adverse effects (AEs)."( Optimal Management of Adverse Events From Copanlisib in the Treatment of Patients With Non-Hodgkin Lymphomas.
Cheson, BD; Dreyling, M; Ewer, MS; Farooki, A; Fisher, RI; Goncalves, MD; Lenz, G; O'Brien, S; Yu, A; Zinzani, PL, 2019
)
0.51
" The common adverse events were skin toxicities(50."( [Efficacy and Safety of Gefitinib as First-Line Chemotherapy for Elderly Patients with Advanced Non-Small Cell Lung Cancer(NSCLC)].
Kawai, S; Kitazono, M; Murata, K; Ohashi, K; Takahashi, Y; Takamori, M; Wada, A; Yamamoto, M, 2019
)
0.51
" Despite of their potential in treatment of cancer, drug resistance and adverse toxicity such as peripheral neuropathy are some of the negative criteria of anti-tubulin agents."( 2,4-Disubstituted Quinazoline Derivatives Act as Inducers of Tubulin Polymerization: Synthesis and Cytotoxicity.
Amini, M; Csuk, R; Faramarzi, MA; Fischer, L; Javadi, I; Moghadam, ES; Rashidi, A; Tehrani, MH, 2019
)
0.51
"Data from 53 ET patients who received anagrelide as a first-line therapy were reviewed for patient characteristics, antiplatelet status, cytoreduction status, therapeutic effects, adverse events, thrombohemorrhagic event development, progression to myelofibrosis or acute leukemia, and cause of death."( Efficacy and safety of anagrelide as a first-line drug in cytoreductive treatment-naïve essential thrombocythemia patients in a real-world setting.
Fujita, S; Hashimoto, A; Hashimoto, Y; Hotta, M; Ishii, K; Ito, T; Kondo, T; Konishi, A; Nakanishi, T; Nakaya, A; Nomura, S; Omura, H; Satake, A; Shinzato, I; Tanaka, T; Tanaka, Y; Yoshimura, H, 2019
)
0.51
" Safety assessments included the incidence and severity of adverse events (AEs), local tolerability at the treatment area, vital signs, and laboratory examinations."( Pharmacokinetics and Safety of Icotinib Hydrochloride Cream in Patients with Mild to Moderate Chronic Plaque Psoriasis: A Randomized Double-Blind Vehicle-Controlled Phase 1 Study.
Liu, L; Lou, H; Ruan, Z; Shen, Y; Zheng, M; Zhou, J, 2019
)
0.51
"9%) patients experienced at least one AE, of which application-site adverse drug reactions (ADRs) were reported in 6 (14."( Pharmacokinetics and Safety of Icotinib Hydrochloride Cream in Patients with Mild to Moderate Chronic Plaque Psoriasis: A Randomized Double-Blind Vehicle-Controlled Phase 1 Study.
Liu, L; Lou, H; Ruan, Z; Shen, Y; Zheng, M; Zhou, J, 2019
)
0.51
" The incidence of all adverse events(AEs)was higher in the ANA monotherapy(45."( Clinical Evaluation of the Efficacy and Safety of Anagrelide Used with or without Hydroxycarbamide in Japanese Patients with Essential Thrombocythemia-A Retrospective Single-Center Study of 35 Cases.
Fukuda, Y; Hamano, Y; Iizuka, H; Inano, T; Izumi, H; Nakamura, N; Noguchi, M; Okubo, M; Sakajiri, S; Sawada, T; Sekiguchi, Y; Sugimoto, K; Takizawa, H; Tomita, S; Wakabayashi, M, 2019
)
0.51
" Across p16 status and smoking history subgroups, the most common treatment-related adverse events (AEs) were diarrhea (70-91%), rash/acne (72-84%), stomatitis (34-73%) with afatinib; and included stomatitis (39-100%), fatigue (22-50%), nausea (19-36%) with methotrexate."( Afatinib as second-line treatment in patients with recurrent/metastatic squamous cell carcinoma of the head and neck: Subgroup analyses of treatment adherence, safety and mode of afatinib administration in the LUX-Head and Neck 1 trial.
Clement, PM; Cohen, EEW; Cupissol, D; de Souza Viana, L; Fayette, J; Gauler, T; Geng, Y; Geoffrois, L; Guigay, J; Haddad, R; Keilholz, U; Kornek, G; Licitra, L; Machiels, JP; Melichar, B; Rauch, D; Ribaldo Nicolau, U; Rolland, F; Tahara, M; Vermorken, J; Zanetta-Devauges, S; Zografos, E, 2019
)
0.51
" Letermovir is safe and effective compared with alternative prophylaxis approaches following CBT through day 100."( Letermovir prophylaxis through day 100 post transplant is safe and effective compared with alternative CMV prophylaxis strategies following adult cord blood and haploidentical cord blood transplantation.
Abidi, MZ; Bajrovic, V; Benamu, E; Chase, S; Gakhar, N; Gutman, JA; Haverkos, BM; Kaiser, J; MacDonald, J; Miller, M; Purev, E; Sharma, P; Tobin, J; Weinberg, A, 2020
)
0.56
"During escalation, four dose-limiting toxicities were observed among 24 patients: skin rash (1) and failure to deliver 100% of Xelox because of treatment-associated grade III-IV adverse events (AEs) (3: diarrhoea and vomiting; vomiting; fatigue)."( Dual Erb B Inhibition in Oesophago-gastric Cancer (DEBIOC): A phase I dose escalating safety study and randomised dose expansion of AZD8931 in combination with oxaliplatin and capecitabine chemotherapy in patients with oesophagogastric adenocarcinoma.
Anthoney, DA; Collins, L; Eatock, M; Elhussein, L; Falk, S; Goff, M; Lord, SR; Love, S; Middleton, MR; Moschandreas, J; Thomas, A; Turkington, RC; Virdee, PS, 2020
)
0.56
"Chagas disease, caused by the protozoan Trypanosoma cruzi, has increased in the world due to migration, travelling and climate change; at present, the principal problem is that common trypanocidal agents have resulted in toxic or inconvenient side effects."( Genotoxicity assessment of four novel quinazoline-derived trypanocidal agents in the Drosophila wing somatic mutation and recombination test.
Castañeda-Partida, L; Dueñas-García, IE; Durán-Díaz, Á; García-Salomé, M; Heres-Pulido, ME; Hernández-Luis, F; Hernández-Portilla, LB; Mendoza-Martínez, C; Olvera-Romero, ZY; Piedra-Ibarra, E; Ramírez-Cruz, BG; Santos-Cruz, LF, 2020
)
0.56
" Common treatment-emergent adverse events (TEAEs) (all grade/grade 3/grade 4) were transient hyperglycemia (50."( Long-term safety and efficacy of the PI3K inhibitor copanlisib in patients with relapsed or refractory indolent lymphoma: 2-year follow-up of the CHRONOS-1 study.
Bouabdallah, K; Childs, BH; Demeter, J; Dimou, M; Dreyling, M; Follows, G; Garcia-Vargas, J; Hiemeyer, F; Kim, WS; Kosinova, M; Lenz, G; Leppä, S; Miriyala, A; Mollica, L; Morschhauser, F; Munoz, J; Nagler, A; Özcan, M; Rodrigues, L; Santoro, A; Stevens, DA; Trevarthen, D; Zinzani, PL, 2020
)
0.56
" Anaemia was the most common adverse event in patients receiving ruxolitinib (rates per 100 patient-years of exposure were 8·9 for ruxolitinib and 8·8 for the crossover population), though most anaemia events were mild to moderate in severity (grade 1 or 2 anaemia rates per 100 patient-years of exposure were 8·0 for ruxolitinib and 8·2 for the crossover population)."( Long-term efficacy and safety of ruxolitinib versus best available therapy in polycythaemia vera (RESPONSE): 5-year follow up of a phase 3 study.
Besses, C; Blau, IW; Dong, T; Durrant, S; Francillard, N; Griesshammer, M; Harrison, CN; Hino, M; Kiladjian, JJ; Kirito, K; Masszi, T; Mesa, R; Miller, CB; Moiraghi, B; Pane, F; Passamonti, F; Rosti, V; Rumi, E; Vannucchi, AM; Verstovsek, S; Wroclawska, M; Zachee, P, 2020
)
0.56
"We showed that ruxolitinib is a safe and effective long-term treatment option for patients with polycythaemia vera who are resistant to or intolerant of hydroxyurea."( Long-term efficacy and safety of ruxolitinib versus best available therapy in polycythaemia vera (RESPONSE): 5-year follow up of a phase 3 study.
Besses, C; Blau, IW; Dong, T; Durrant, S; Francillard, N; Griesshammer, M; Harrison, CN; Hino, M; Kiladjian, JJ; Kirito, K; Masszi, T; Mesa, R; Miller, CB; Moiraghi, B; Pane, F; Passamonti, F; Rosti, V; Rumi, E; Vannucchi, AM; Verstovsek, S; Wroclawska, M; Zachee, P, 2020
)
0.56
"Prolonged use of opioids causes analgesic tolerance and adverse effects including constipation and dependence."( Improved efficacy, tolerance, safety, and abuse liability profile of the combination of CR4056 and morphine over morphine alone in rodent models.
Bonazzi, A; Borsi Franchini, M; Caselli, G; Comi, E; Ferrari, F; Lanza, M; Milia, C; Rovati, LC; Sabatini, C; Sala, E, 2020
)
0.56
" Opioid-induced adverse effects were assessed in rodent models of morphine-induced constipation, sedation (open field, sedation rating scale, and rotarod), physical dependence (naloxone-induced withdrawal), and abuse (conditioned place preference-associated reward)."( Improved efficacy, tolerance, safety, and abuse liability profile of the combination of CR4056 and morphine over morphine alone in rodent models.
Bonazzi, A; Borsi Franchini, M; Caselli, G; Comi, E; Ferrari, F; Lanza, M; Milia, C; Rovati, LC; Sabatini, C; Sala, E, 2020
)
0.56
" Twenty-two adverse events were observed in 19 (36."( First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects.
Cao, Y; Gong, LY; Guo, CX; Hua, Y; Huang, J; Kuang, Y; Pei, Q; Wang, MN; Yang, GP, 2020
)
0.56
" Meanwhile, more efforts should be made to develop novel efficient and low toxic derivatives."( Evodiamine: A review of its pharmacology, toxicity, pharmacokinetics and preparation researches.
Li, X; Song, J; Sun, Q; Xie, L, 2020
)
0.56
" In addition, unresolved issues include toxic mechanisms, pharmacokinetics, novel pharmaceutical researches and relationship between residues and intestinal environment, which are still being explored and excavate before achieving integration into clinical practice."( Evodiamine: A review of its pharmacology, toxicity, pharmacokinetics and preparation researches.
Li, X; Song, J; Sun, Q; Xie, L, 2020
)
0.56
" The pooled incidence of partial response (PR), stable disease (SD), TKI-related adverse events (AEs), and pooled median progression-free survival (PFS) were calculated with 95% confidence intervals (CI)."( Comparative efficacy and safety of tyrosine kinase inhibitors for thyroid cancer: a systematic review and meta-analysis.
Chino, T; Ito, KI; Ito, T; Kanai, T; Maeno, K; Oba, T; Ono, M; Shimizu, T; Soma, A, 2020
)
0.56
" However, its safety profile, including adverse events of special interest (AESIs) and treatment-emergent adverse events (TEAEs) by age, sex, and body mass index (BMI), is not well known."( Safety Profile and Adverse Events of Special Interest for Fruquintinib in Chinese Patients with Previously Treated Metastatic Colorectal Cancer: Analysis of the Phase 3 FRESCO Trial.
Bai, Y; Cao, P; Chen, D; Chen, H; Chen, Z; Cheng, Y; Deng, Y; Fan, S; Guo, W; Guo, X; Han, R; Li, J; Li, W; Liu, T; Ma, D; Pan, H; Qin, S; Shen, L; Shu, Y; Sun, S; Wang, H; Wang, N; Wang, S; Wu, C; Xu, J; Xu, N; Xu, R; Yang, L; Yu, Z; Yuan, Y; Zhang, B; Zhong, H; Zhou, J, 2020
)
0.56
" There were no significant differences in adverse events between treatment groups, and no reports of malignant transformation."( Cardiovascular Safety of Anagrelide Hydrochloride versus Hydroxyurea in Essential Thrombocythaemia.
Achenbach, H; Egyed, M; Gercheva, L; Gotic, M; Kvasnicka, HM; Warzocha, K; Wu, J, 2021
)
0.62
"We identified patients with metastatic colorectal cancer who were treated with raltitrexed-based systemic therapy after developing serious adverse events with fluoropyrimidine-based treatment in a large Canadian province from 2004 to 2018."( Real-world Safety and Efficacy of Raltitrexed in Patients With Metastatic Colorectal Cancer.
Batra, A; Cheung, WY; Hannouf, MB; Rigo, R, 2021
)
0.62
" Raltitrexed was well-tolerated with common adverse events that included anemia in 41."( Real-world Safety and Efficacy of Raltitrexed in Patients With Metastatic Colorectal Cancer.
Batra, A; Cheung, WY; Hannouf, MB; Rigo, R, 2021
)
0.62
" The most common all-grade treatment-emergent adverse events (TEAEs) included fatigue (52."( Efficacy and safety of copanlisib in patients with relapsed or refractory marginal zone lymphoma.
Childs, BH; Dreyling, M; Follows, GA; Garcia-Vargas, J; Hiemeyer, F; Mollica, L; Nagler, A; Özcan, M; Panayiotidis, P; Santoro, A; Stevens, D; Trevarthen, D; Zinzani, PL, 2021
)
0.62
" VAN + EV combination is safe and active in refractory solid tumors."( Safety and activity of vandetanib in combination with everolimus in patients with advanced solid tumors: a phase I study.
Amini, B; Bhatt, T; Cascone, T; Conley, AP; Drobnitzky, N; Falchook, GS; Fu, S; Hess, KR; Heymach, JV; Hong, DS; Janku, F; Karp, D; Meric-Bernstam, F; Naing, A; Piha-Paul, SA; Ryan, AJ; Sacks, RL; Sherman, SI; Subbiah, IM; Subbiah, V, 2021
)
0.62
" Seven patients came off treatment before the first restaging scan: six because of clinical progression and one because of an adverse event."( Clinical Activity and Safety of Cediranib and Olaparib Combination in Patients with Metastatic Pancreatic Ductal Adenocarcinoma without BRCA Mutation.
Cardin, DB; Glazer, PM; Grossman, SR; Ivy, SP; Kato, S; Kim, JW; LoRusso, PM; Shyr, Y; Vaishampayan, UN, 2021
)
0.62
" The FRESCO-2 study is being conducted globally to determine how safe and effective fruquintinib is at treating patients with metastatic colorectal cancer that has grown or spread following other forms of treatment, such as chemotherapy."( FRESCO-2: a global Phase III study investigating the efficacy and safety of fruquintinib in metastatic colorectal cancer.
Chien, C; Dasari, A; Eng, C; Kania, M; Schelman, W; Sobrero, A; Tabernero, J; Yang, Z; Yao, J; Yoshino, T, 2021
)
0.62
" The main adverse events (AEs) included reactive cutaneous capillary endothelial proliferation (RCCEP) (81."( Efficacy and safety of regorafenib or fruquintinib plus camrelizumab in patients with microsatellite stable and/or proficient mismatch repair metastatic colorectal cancer: an observational pilot study.
Jiang, FE; Liu, AN; Yu, CY; Zhang, HJ, 2021
)
0.62
"9 % experienced adverse drug reactions, the most frequent of which were renal impairment (2."( Safety and Effectiveness of Letermovir in Allogenic Hematopoietic Stem Cell Transplantation Recipients: Interim Report of Post-marketing Surveillance in Japan.
Hiraishi, I; Maekawa, S; Ueno, R; Watanabe, A, 2021
)
0.62
" Primary safety outcomes included risk of grade ≥ 3 treatment-emergent adverse events (TEAEs); primary efficacy outcomes included objective response rate (ORR)."( A Matching-Adjusted Indirect Comparison of Single-Arm Trials in Patients with Relapsed or Refractory Follicular Lymphoma Who Received at Least Two Prior Systemic Treatments: Tazemetostat was Associated with a Lower Risk for Safety Outcomes Versus the PI3-
Adib, D; Gupta, D; Mamlouk, K; Nellesen, D; Proudman, D; Yang, J, 2022
)
0.72
" The primary outcome was time-to-treatment failure (TTF), and secondary outcomes were overall survival (OS) and adverse events."( Efficacy and Safety Comparison of Regorafenib and Fruquintinib in Metastatic Colorectal Cancer-An Observational Cohort Study in the Real World.
Cao, Y; Chen, M; Li, J; Lu, M; Peng, Z; Qi, C; Shen, L; Wang, X; Wang, Z; Zhang, J; Zhang, Q, 2022
)
0.72
" The incidences of most adverse events were similar between the two groups, while any grade of hand-foot skin reaction and hyperbilirubinemia were more frequently observed in the regorafenib group and ≥grade 3 hypertension was more common in the fruquintinib group."( Efficacy and Safety Comparison of Regorafenib and Fruquintinib in Metastatic Colorectal Cancer-An Observational Cohort Study in the Real World.
Cao, Y; Chen, M; Li, J; Lu, M; Peng, Z; Qi, C; Shen, L; Wang, X; Wang, Z; Zhang, J; Zhang, Q, 2022
)
0.72
" Mechanistically, downregulated expression of the DNA repair protein HMGB1 played a critical role in these toxic reaction processes."( Decreased HMGB1 expression contributed to cutaneous toxicity caused by lapatinib.
Ai, L; He, Q; Jiang, L; Luo, P; Xu, Z; Yan, H; Yang, B; Yang, X; Zeng, Y, 2022
)
0.72
"3% experienced adverse drug reactions (ADRs)."( Safety and efficacy of anagrelide in Japanese post-marketing surveillance, with subgroup analyses on the effect of previous cytoreductive therapies, age, and starting dose.
Akimoto, T; Baba, T; Fernandez, J; Hashimoto, Y; Komatsu, N; Otsuka, M, 2022
)
0.72
" Treatment-emergent adverse events-including headaches, cardiac palpitations and arrhythmias, nausea, vomiting and/or diarrhea-led to ANA discontinuation in 76."( Anagrelide for platelet-directed cytoreduction in polycythemia vera: Insights into utility and safety outcomes from a large multi-center database.
Fleischman, A; Gotlib, J; Heaney, M; Hoffman, R; Kremyanskaya, M; Kuykendall, A; Mascarenhas, J; Mesa, R; O'Connell, C; Podoltsev, N; Rippel, N; Shammo, JM; Tremblay, D; Yacoub, A; Zubizarreta, N, 2022
)
0.72
" Although all patients experienced at least one treatment-emergent adverse event (TEAE), with hyperglycemia being the most common AE, no AE-related deaths were reported."( Safety and antitumor activity of copanlisib in Japanese patients with relapsed/refractory indolent non-Hodgkin lymphoma: a phase Ib/II study.
Childs, BH; Fukuhara, N; Garcia-Vargas, J; Hatake, K; Iriyama, C; Kamezaki, K; Kuroda, J; Kusumoto, S; Makita, S; Maruyama, D; Masuda, S; Minami, H; Nagai, H; Suehiro, Y; Terao, Y; Tobinai, K; Tsujino, T; Tsukamoto, N; Uchida, T; Yanada, M; Yasuda, M, 2023
)
0.91
"The toxic effects of gefitinib were confirmed by the increased liver index, decreased body weight and survival rate, injured liver function and histopathology followed 16 days of oral administration."( Study on the hepatotoxicity and potential mechanism of gefitinib based on CYP450 in mice and AML12 cells.
Bai, M; Li, C; Li, M; Li, Y; Liu, H; Lu, S; Ma, S; Su, P; Yin, X; Zhang, C, 2023
)
0.91

Pharmacokinetics

ExcerptReferenceRelevance
"In order to determine and compare the pharmacodynamic responses to single and multiple dose prazosin therapy in cardiac failure, 14 patients with severe low-output heart failure underwent central and regional hemodynamic measurements after random placement in one of two prazosin dosing schedules."( Development of pharmacodynamic tolerance to prozosin in congestive heart failure.
Blanford, MF; Desch, CE; Leier, CV; Magorien, RD; Triffon, DW; Unverferth, DV, 1979
)
0.26
" After the first dose, pelanserin was absorbed reaching a Cmax value of 39."( Pharmacokinetics and antihypertensive effect of oral pelanserin in renal hypertensive dogs.
Castañeda-Hernández, G; Flores-Murrieta, FJ; Hong, E, 1992
)
0.28
" The steady-state volume of distribution, Vdss, and terminal elimination half-life were significantly greater on Day 5 of TMTX-DDP compared to baseline."( Pharmacokinetic study of trimetrexate in combination with cisplatin.
Comis, RL; Hudes, GR; LaCreta, F; Litwin, S; O'Dwyer, PJ; Tinsley, P; Walczak, J, 1991
)
0.28
" The drug had a mean terminal half-life of 13 hours."( A phase I and pharmacokinetic study of trimetrexate using a 24-hour continuous-injection schedule.
Allegra, CJ; Balis, F; Brooks, J; Curt, GA; Drake, JC; Jenkins, J; Thomas, R; Weiss, RB, 1990
)
0.28
" The pharmacokinetic and pharmacodynamic profiles of pelanserin allow to predict that this drug could have a place in the therapeutics of arterial hypertension."( [Pharmacokinetics and antihypertensive effect of pelanserin in dogs ].
Castañeda Hernández, G; Flores Murrieta, FJ; Hong, E,
)
0.13
"Based on pharmacokinetic data from mice, rats, and rabbits, the prediction of pharmacokinetics of intravenous metazosin in man has been performed."( Interspecies pharmacokinetic scaling of metazosin, a novel alpha-adrenergic antagonist.
Lapka, R; Peterková, M; Rejholec, V; Sechser, T; Smíd, M,
)
0.13
" The apparent terminal elimination half-life ranged from 24."( Pharmacokinetics of halofuginone in cattle.
Kinabo, LD; McKellar, QA,
)
0.13
" After 1 and 5 mg, tmax ranged from 1-2 h; Cmax (4."( Haemodynamic and pharmacokinetic evaluation of alfuzosin in man. A dose ranging study and comparison with prazosin.
Deering, AH; Harron, DW; McMahon, MT; Scott, MG; Shanks, RG, 1989
)
0.28
" TMTX plasma concentrations were measured after the first dose and the data were fit by two- or three-compartment mammillary pharmacokinetic models."( A phase I trial of trimetrexate glucuronate (NSC 352122) given every 3 weeks: clinical pharmacology and pharmacodynamics.
Donehower, RC; Ettinger, DS; Grochow, LB; Noe, DA, 1989
)
0.28
"5-1 ng ml-1, which is sensitive enough for pharmacokinetic studies in man."( High-performance liquid chromatographic determination of alfuzosin in biological fluids with fluorimetric detection and large-volume injection.
Broquaire, M; Colafranceschi, C; Guinebault, P; Thénot, JP, 1986
)
0.27
" TMTX concentrations were measured 1 and 24 hours after each dose, and the data were fit by use of a one-compartment pharmacokinetic model."( Phase I trial of trimetrexate glucuronate on a five-day bolus schedule: clinical pharmacology and pharmacodynamics.
Dole, GB; Donehower, RC; Ettinger, DS; Graham, ML; Grochow, LB; McGuire, WP; Noe, DA; Rowinsky, EK, 1989
)
0.28
" The pharmacokinetic behavior of trimetrexate was characterized by triexponential plasma disappearance, elimination primarily by biotransformation, substantial plasma protein binding, poor CSF penetration, and limited oral bioavailability."( Pharmacokinetics of trimetrexate (NSC 352122) in monkeys.
Balis, FM; Lester, CM; Poplack, DG, 1986
)
0.27
" The half-life of the terminal elimination-phase was 16."( Phase I studies with trimetrexate: clinical pharmacology, analytical methodology, and pharmacokinetics.
Baker, M; Bertino, JR; Cashmore, AR; Delap, R; Dreyer, RN; Ernstoff, M; Grillo-Lopez, A; Lin, JT; Marsh, JC; Whitfield, LR, 1987
)
0.27
" Estimates of pharmacokinetic parameters were similar when determined by either compartmental or noncompartmental methods."( Pharmacokinetics of trimetrexate administered by five-day continuous infusion to patients with advanced cancer.
Bishop, JF; Morris, RG; Olver, IN; Raghavan, D; Reece, PA, 1987
)
0.27
"2 to 215 ml/min/m2) and half-life (2."( Pediatric phase I trial and pharmacokinetic study of trimetrexate.
Balis, FM; Belasco, J; Doherty, KM; Ettinger, LJ; Holcenberg, JS; Luks, E; Patel, R; Reaman, GH; Tan, C; Zimm, S, 1987
)
0.27
" Plasma concentrations and pharmacokinetic parameters were nearly proportional to dose over the 150 to 750 mg dose range studied."( Pharmacokinetics of single and multiple ascending doses of the antiallergic agent tiacrilast in man.
Dunton, A; Keigher, N; Massarella, JW; Pao, J; Silvestri, TM, 1987
)
0.27
" Pharmacokinetic data showed that maximal serum phospholipid and NSC 251635 concentrations were obtained at the end of the liposome infusion."( Intravenous infusion of high doses of liposomes containing NSC 251635, a water-insoluble cytostatic agent. A pilot study with pharmacokinetic data.
Atassi, G; Brassinne, C; Coune, A; Frühling, J; Laduron, C; Ruysschaert, JM; Sculier, JP, 1986
)
0.27
" The optimum use of prazosin in clinical practice depends on an understanding of the pharmacokinetic properties of the drug."( Clinical pharmacokinetics of prazosin--1985.
Elliott, HL; Meredith, PA; Reid, JL; Rubin, PC; Vincent, J,
)
0.13
" These pharmacokinetic studies have shown that, by analogy with experimental systems, cytotoxic plasma levels of CB 3717 are archieved in man."( The clinical pharmacokinetics of the novel antifolate N10-propargyl-5,8-dideazafolic acid (CB 3717).
Alison, DL; Calvert, AH; Harland, SJ; Harrap, KR; Hart, LI; Newell, DR; Sessa, C, 1985
)
0.27
" The method described is suitable for routine clinical and pharmacokinetic studies."( Determination of proquazone and its m-hydroxy metabolite by high-performance liquid chromatography. Clinical application: pharmacokinetics of proquazone in children with juvenile rheumatoid arthritis.
Lempiäinen, M; Mäkelä, AL, 1985
)
0.27
"A pharmacokinetic study of fenquizone (Idrolone), a thiazide-like diuretic, was conducted with single oral doses in 6 healthy volunteers."( Single-dose pharmacokinetics of fenquizone in healthy volunteers.
Donati, C; Gueli Alletti, D; Maggi, GC, 1985
)
0.27
" The pharmacodynamic response was a dose-related fall in the systemic arterial pressure, both supine and standing; dose-response effects were most evident in the upright posture."( The pharmacokinetic, pharmacodynamic and haemodynamic effects of acute and chronic alpha-adrenoceptor blockade in chronic heart failure.
Silke, B; Taylor, SH, 1981
)
0.26
" Time of maximum plasma concentration (2 hr) and half-life in plasma (5."( Pharmacokinetic and pharmacodynamic studies with prazosin in chronic heart failure.
Lakhani, ZM; Silke, B; Taylor, SH,
)
0.13
"Extractive alkylation was carried out on fenquizone, a sulphonamide diuretic, in order to devise a suitable method for its determination in pharmacokinetic and bioavailability studies."( Gas-liquid chromatographic evaluation of fenquizone in biological samples for pharmacokinetic investigations.
Marzo, A; Quadro, G; Treffner, E, 1983
)
0.27
" In normal healthy volunteers, the time of peak concentration occurs between 1 and 3 hours after oral administration, with wide interindividual variations."( Clinical pharmacokinetics of prazosin.
Jaillon, P,
)
0.13
" The method was applied to a pharmacokinetic study of evodiamine in rats after 2 mg/kg intravenous administration."( High-performance liquid chromatographic determination of evodiamine in rat plasma: application to pharmacokinetic studies.
Chen, CF; Chou, CJ; Jeng, KF; Lin, LC; Lin, YH; Tsai, TH, 1995
)
0.29
" There were, however, neither prolongation of apparent elimination half-life (t1/2), nor increase in Cmax, nor area under the plasma concentration-time curve (AUC0-24) after consecutive dosing in both groups."( Pharmacokinetics and pharmacodynamics of the alpha 1-adrenergic antagonist bunazosin retard in hypertensives.
Gotoh, E; Ishii, M; Minamisawa, K; Minamisawa, M; Shionoiri, H; Sugimoto, K; Takasaki, I; Takizawa, T; Ueda, S, 1994
)
0.29
" The elimination of alfuzosin being almost entirely metabolic, the potential pharmacokinetic interaction with cimetidine (H2-receptor antagonist) was investigated in 10 healthy young subjects."( The effect of cimetidine on the pharmacokinetics of single oral doses of alfuzosin.
Bianchetti, G; Desager, JP; Harvengt, C; Rosenzweig, P, 1993
)
0.29
" It was applied to the pharmacokinetic study of rutaecarpine in rat after a 2 mg/kg intravenous administration."( High-performance liquid chromatographic determination of rutaecarpine in rat plasma: application to a pharmacokinetic study.
Chen, CF; Chou, CJ; Hsu, SY; Ko, HC; Li, SY; Tsai, TH, 1994
)
0.29
" In the present study, we have investigated the pharmacokinetic and pharmacodynamic characteristics of ibopamine after ocular application."( Ocular pharmacokinetics and pharmacodynamics in rabbits of ibopamine, a new mydriatic agent.
Galbiati, I; Gazzaniga, A; Gianesello, V; Soldati, L; Virno, M, 1993
)
0.29
" In female acute and chronic diabetic rats, pharmacokinetic parameters were similar to those in the control."( Pharmacokinetics of zenarestat, an aldose reductase inhibitor, in male and female diabetic rats.
Kimura, T; Sawamoto, T; Suzuki, A; Tanaka, Y,
)
0.13
" Pharmacokinetic studies in normotensive volunteers showed that plasma peak concentration (Cmax) of bunazosin retard and bioavailability were approximately 50% and 81%, respectively, of the values of the standard non-retarded formulation."( Pharmacokinetic and pharmacodynamic properties and therapeutic use of bunazosin in hypertension. A review.
Weidinger, G, 1995
)
0.29
"To establish the maximum tolerated dose (MTD), dose-limiting and other major toxicities and the major pharmacokinetic parameters of a 10-day infusion of the nonclassical antifolate Thymitaq."( Initial clinical trial and pharmacokinetics of Thymitaq (AG337) by 10-day continuous infusion in patients with advanced solid tumors.
Clendeninn, NJ; Creaven, PJ; Dixon, M; Johnston, A; Loewen, GM; Meropol, NJ; Pendyala, L; Proefrock, A; Wu, EY, 1998
)
0.3
" The primary end points were area under the plasma raltitrexed concentration-time curve from the start of the infusion to the last determined concentration (AUC(0-tldc)) and AUC to infinity (AUC(0-infinity)); secondary end points were peak concentrations of raltitrexed (Cmax) and elimination half-life (t(1/2gamma))."( Effects of impaired renal function on the pharmacokinetics of raltitrexed (Tomudex ZD1694).
Beale, P; Berry, C; Hanwell, J; Hoskin, P; Judson, I; Maughan, T; Primrose, J; Sutcliffe, F; Walker, M, 1998
)
0.3
" A pharmacokinetic program was used to fit concentration-time (C-T) data and a combined pharmacokinetic-pharmacodynamic model was used to analyze effect-time (E-T) data in individual dogs."( Pharmacokinetic-pharmacodynamic analysis of changrolin in dogs with arrhythmia.
Feng, JL; Gu, YB; Liu, CX; Sun, JL; Wei, GL; Xiao, SH, 1996
)
0.29
"The purpose of the present study was to examine the pharmacodynamic and pharmacokinetic features of the novel mast cell inhibitor 4-(3'-Hydroxyphenyl)-amino-6,7-dimethoxyquinazoline (WHI-P180) in mice."( Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice.
Bechard, B; Chen, CL; Chen, H; Liu, XP; Malaviya, R; Mitcheltree, G; Navara, C; Uckun, FM, 1999
)
0.3
" The plasma concentration-time data was fit to a single compartment pharmacokinetic model by using the WinNonlin program to calculate the pharmacokinetic parameters."( Pharmacokinetics and biologic activity of the novel mast cell inhibitor, 4-(3-hydroxyphenyl)-amino-6,7-dimethoxyquinazoline in mice.
Bechard, B; Chen, CL; Chen, H; Liu, XP; Malaviya, R; Mitcheltree, G; Navara, C; Uckun, FM, 1999
)
0.3
" The practical utility of this new HPLC method was confirmed in a pilot pharmacokinetic study in BALB/c mice as well as in a cellular drug uptake and disposition study in RBL-2H3 mast cells."( Quantitative high-performance liquid chromatographic method for pharmacokinetic studies of the potent mast cell inhibitor 4-(4'-hydroxyphenyl)amino-6,7-dimethoxyquinazoline (WHI-P131).
Chen, CL; Chen, H; Liu, XP; Malaviya, R; Uckun, FM, 1999
)
0.3
" The pharmacokinetic parameters of bunazosin elimination half-life and time to peak level were not statistically significantly affected by renal insufficiency."( Pharmacokinetics and pharmacodynamics of bunazosin in patients with renal insufficiency.
Koike, Y; Mineshita, S; Mizoguchi, H; Nomura, Y, 1999
)
0.3
" administration, the terminal elimination half-life of WHI-P131 was 73."( In vivo toxicity and pharmacokinetic features of the janus kinase 3 inhibitor WHI-P131 [4-(4'hydroxyphenyl)-amino-6,7- dimethoxyquinazoline.
Chen, CL; Ek, O; Liu, XP; Uckun, FM, 1999
)
0.3
" A three-compartment pharmacokinetic model was fitted to the raltitrexed plasma concentration-time data."( The plasma pharmacokinetics and cerebrospinal fluid penetration of the thymidylate synthase inhibitor raltitrexed (Tomudex) in a nonhuman primate model.
Adamson, PC; Balis, FM; Godwin, KS; McCully, C; Widemann, BC, 1999
)
0.3
" The pharmacokinetic profile is consistent with extensive polyglutamation and intracellular retention of ralitrexed."( The plasma pharmacokinetics and cerebrospinal fluid penetration of the thymidylate synthase inhibitor raltitrexed (Tomudex) in a nonhuman primate model.
Adamson, PC; Balis, FM; Godwin, KS; McCully, C; Widemann, BC, 1999
)
0.3
" The pharmacokinetics of the classical antifolate methotrexate have been well-defined and pharmacokinetic data can be exploited to reduce the toxicity and enhance the activity of the drug."( Clinical pharmacokinetics of antitumor antifolates.
Newell, DR, 1999
)
0.3
" Pharmacokinetic parameters of AA were determined in male rats after administering a single 10 mg/kg intravenous dose (i."( Pharmacokinetics and in-situ absorption studies of a new anti-allergic compound 73/602 in rats.
Dwivedi, AK; Gutpa, RC; Paliwa, JK; Singh, S, 2000
)
0.31
" The aims were to optimize the schedule of administration and determine any pharmacokinetic (PK) interactions between the two drugs."( Clinical pharmacokinetic and in vitro combination studies of nolatrexed dihydrochloride (AG337, Thymitaq) and paclitaxel.
Boddy, AV; Calvert, AH; Griffin, MJ; Hughes, AN; Johnston, A; Kerr, B; Lee, C; Liang, B; Newell, DR, 2000
)
0.31
" Chromatograms and pharmacodynamic data from a Phase 1 Clinical Trial of a new antifolate drug, ZD9331 are included to illustrate the utility of the method."( Modified high-performance liquid chromatography assay for the measurement of 2'-deoxyuridine in human plasma and its application to pharmacodynamic studies of antimetabolite drugs.
Jackman, AL; Lynn, S; Mitchell, F, 2000
)
0.31
" The disposition of raltitrexed in patients is best described by a 3-compartment model with a terminal half-life (t1/2gamma) of 260 hours, the latter being subject to significant interpatient variability."( Clinical and preclinical pharmacokinetics of raltitrexed.
Beale, PJ; Clarke, SJ; Rivory, LP, 2000
)
0.31
" Cmax and area under the concentration-time curve (AUC) were dose-proportional from 10 to 100mg."( Pharmacokinetics and tolerability of the orally active selective epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in healthy volunteers.
Dane, A; Jones, H; Laight, A; Morris, C; Stafford, L; Swaisland, H; Yates, R, 2001
)
0.31
" The elimination half-life suggests that once daily oral administration is appropriate."( Pharmacokinetics and tolerability of the orally active selective epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in healthy volunteers.
Dane, A; Jones, H; Laight, A; Morris, C; Stafford, L; Swaisland, H; Yates, R, 2001
)
0.31
" The study also sought to characterize the pharmacokinetic behavior of 1843U89 and to seek preliminary evidence of anticancer activity."( A phase I and pharmacokinetic study of 1843U89, a noncompetitive inhibitor of thymidylate synthase, in patients with advanced solid malignancies.
Burris, H; Goetz, A; Hohneker, JA; Johnson, TR; Lampkin, T; Rowinsky, EK; Sailstad, J; Schwartz, G; Smetzer, L; Von Hoff, DD, 2001
)
0.31
" In various tumor types, such as head and neck squamous carcinoma and gastric and breast adenocarcinoma, a relationship between EGFR and downstream markers (such as phosphorylated MAPK) has been characterized, further supporting the potential of these molecules for pharmacodynamic studies."( Pharmacodynamic studies with the epidermal growth factor receptor tyrosine kinase inhibitor ZD1839.
Albanell, J; Baselga, J; Rojo, F, 2001
)
0.31
" A once-daily formulation of alfuzosin administered through a novel prolonged-release system has been recently developed to improve the convenience of dosing and to provide optimal pharmacokinetic coverage over 24 hours."( Alfuzosin: overview of pharmacokinetics, safety, and efficacy of a clinically uroselective alpha-blocker.
Roehrborn, CG, 2001
)
0.31
" We studied the pharmacodynamic effects of ZD1839 on EGFR in the skin, an EGFR-dependent tissue, in cancer patients participating in ZD1839 phase I clinical trials."( Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition.
Albanell, J; Averbuch, S; Baselga, J; Feyereislova, A; Gee, J; Herbst, R; LoRusso, P; Mascaro, JM; Nicholson, RI; Rischin, D; Rojo, F; Sauleda, S, 2002
)
0.31
" These effects were profound at doses well below the one producing unacceptable toxicity, a finding that strongly supports pharmacodynamic assessments to select optimal doses instead of a maximum-tolerated dose for definitive efficacy and safety trials."( Pharmacodynamic studies of the epidermal growth factor receptor inhibitor ZD1839 in skin from cancer patients: histopathologic and molecular consequences of receptor inhibition.
Albanell, J; Averbuch, S; Baselga, J; Feyereislova, A; Gee, J; Herbst, R; LoRusso, P; Mascaro, JM; Nicholson, RI; Rischin, D; Rojo, F; Sauleda, S, 2002
)
0.31
" infusion on day 1 of a 4-week cycle to allow full pharmacokinetic assessment."( Effects of impaired renal function on the pharmacokinetics and toxicity of i.v. ZD9331, a novel non-polyglutamated thymidylate synthase inhibitor, in adult patients with solid tumors.
Bonneterre, J; Culine, S; de Jonge, MJ; de Vries, EG; Droz, J; Glimelius, B; Smith, R; Van Groeningen, C; Verweij, J; Young, J, 2002
)
0.31
" No pharmacologic interactions were observed between these agents, and no correlations between pharmacokinetic parameters and toxicity were noted."( Phase I and pharmacokinetic study of irinotecan in combination with raltitrexed.
Adams, AL; Brady, D; Engstrom, PF; Gallo, JM; Kilpatrick, D; Lewis, NL; Litwin, S; Meropol, NJ; Scher, R; Szarka, CE; Weiner, LM, 2002
)
0.31
"To establish the safety and tolerability of ZD1839 (Iressa), a selective epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, and to explore its pharmacokinetic and pharmacodynamic effects in patients with selected solid tumor types."( Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types.
Albanell, J; Averbuch, SD; Baselga, J; Bjork, T; Calvert, H; Feyereislova, A; Gianni, L; Harris, A; Kaye, SB; Kieback, DG; Ranson, M; Raymond, E; Rischin, D; Rojo, F; Swaisland, H, 2002
)
0.31
" Pharmacodynamic changes in skin confirmed inhibition of EGFR signaling, which was predicted from the mode of action of ZD1839."( Phase I safety, pharmacokinetic, and pharmacodynamic trial of ZD1839, a selective oral epidermal growth factor receptor tyrosine kinase inhibitor, in patients with five selected solid tumor types.
Albanell, J; Averbuch, SD; Baselga, J; Bjork, T; Calvert, H; Feyereislova, A; Gianni, L; Harris, A; Kaye, SB; Kieback, DG; Ranson, M; Raymond, E; Rischin, D; Rojo, F; Swaisland, H, 2002
)
0.31
" Pharmacokinetic follow-up was done for both drugs (RTX by LC-MS-MS and VRB by HPLC-UV detection)."( The raltitrexed-vinorelbine combination: a phase I pharmacokinetic and pharmacodynamic trial in advanced breast cancer.
Chamorey, E; Ferrero, JM; Largillier, R; Leccia, F; Magné, N; Milano, G; Namer, M, 2002
)
0.31
" It is deliverable on an outpatient basis, shows an acceptable toxicity profile potentially manageable by VRB pharmacokinetic follow-up, and has promising antitumor activity in taxane-anthracycline-refractory patients."( The raltitrexed-vinorelbine combination: a phase I pharmacokinetic and pharmacodynamic trial in advanced breast cancer.
Chamorey, E; Ferrero, JM; Largillier, R; Leccia, F; Magné, N; Milano, G; Namer, M, 2002
)
0.31
"To define the pharmacokinetic and toxicity profile of raltitrexed administered by intraperitoneal route in a normothermic pig model."( Pharmacokinetics studies and toxicity profile of raltitrexed used by intraperitoneal route in normothermia in a pig model.
Dube, P; Emond, C; Leclerc, Y; Nguyen, D; Sherman, I, 2003
)
0.32
" Cmax in plasma were of 28 ng/ml and 54 ng/ml for group 1 and 2, respectively."( Pharmacokinetics studies and toxicity profile of raltitrexed used by intraperitoneal route in normothermia in a pig model.
Dube, P; Emond, C; Leclerc, Y; Nguyen, D; Sherman, I, 2003
)
0.32
" This method was used for a pharmacokinetic study in rat."( HPLC assay in plasma and preliminary pharmacokinetic study of a quinazolinone derivative with spasmolytic effect.
Jira, T; Kastner, P; Klimes, J; Láznícek, M, 2003
)
0.32
" Mean terminal half-life following multiple dosing was 50."( Phase I pharmacokinetic trial of the selective oral epidermal growth factor receptor tyrosine kinase inhibitor gefitinib ('Iressa', ZD1839) in Japanese patients with solid malignant tumors.
Dong, RP; Fukuoka, M; Hirose, M; Kudoh, S; Nakagawa, K; Nakatani, I; Negoro, S; Swaisland, H; Takeda, K; Tamura, T; Yamamoto, N, 2003
)
0.32
" The safety profile, pharmacokinetic parameters and antitumor activity observed in our study are comparable to those observed in patients from the USA and Europe."( Phase I pharmacokinetic trial of the selective oral epidermal growth factor receptor tyrosine kinase inhibitor gefitinib ('Iressa', ZD1839) in Japanese patients with solid malignant tumors.
Dong, RP; Fukuoka, M; Hirose, M; Kudoh, S; Nakagawa, K; Nakatani, I; Negoro, S; Swaisland, H; Takeda, K; Tamura, T; Yamamoto, N, 2003
)
0.32
"Pharmacokinetic and pharmacodynamic studies have an important role in the optimization of targeted agents."( Pharmacokinetics and pharmacodynamics: maximizing the clinical potential of Erlotinib (Tarceva).
Bloedow, D; Hidalgo, M, 2003
)
0.32
" This study evaluated the pharmacodynamic effects of OSI-774 in normal skin tissues collected from patients treated with the agent in a Phase I study."( Pharmacodynamic evaluation of the epidermal growth factor receptor inhibitor OSI-774 in human epidermis of cancer patients.
Bacus, S; Brattain, MG; deGraffenried, L; Hammond, LA; Hidalgo, M; Kreisberg, JI; Malik, SN; Rizzo, J; Rowinsky, EK; Siu, LL, 2003
)
0.32
"OSI-774 exerted pharmacodynamic effects in skin tissues of 30-50% of patients treated with the agent."( Pharmacodynamic evaluation of the epidermal growth factor receptor inhibitor OSI-774 in human epidermis of cancer patients.
Bacus, S; Brattain, MG; deGraffenried, L; Hammond, LA; Hidalgo, M; Kreisberg, JI; Malik, SN; Rizzo, J; Rowinsky, EK; Siu, LL, 2003
)
0.32
" The potential for drug interactions between gefitinib and cytotoxic agents was evaluated through pharmacokinetic assessments."( Pharmacokinetic evaluation of gefitinib when administered with chemotherapy.
Hammond, LA, 2003
)
0.32
" In 8 patients, plasma levels of irinotecan and its metabolites SN-38 and SN-38 glucuronide (SN-38glu) were measured by high-performance liquid chromatography and main pharmacokinetic parameters, including steady-state concentration, area under the time-concentration curve, and clearance, were calculated and normalized to the dose level of 22."( A phase I and pharmacokinetic study of irinotecan given as a 7-day continuous infusion in metastatic colorectal cancer patients pretreated with 5-fluorouracil or raltitrexed.
Allegrini, G; Barbara, C; Cupini, S; Danesi, R; Del Tacca, M; Di Paolo, A; Falcone, A; Masi, G, 2004
)
0.32
" The pharmacokinetic data provided evidence that continuous infusion increased the metabolism of irinotecan to SN-38 with respect to standard 30/90-min administration."( A phase I and pharmacokinetic study of irinotecan given as a 7-day continuous infusion in metastatic colorectal cancer patients pretreated with 5-fluorouracil or raltitrexed.
Allegrini, G; Barbara, C; Cupini, S; Danesi, R; Del Tacca, M; Di Paolo, A; Falcone, A; Masi, G, 2004
)
0.32
" The relationship between individual estimates of the pharmacokinetic parameters and patient covariates was examined and the influence of significant covariates on the population parameter estimates and their variance was investigated using stepwise multiple linear regression."( Population pharmacokinetics of raltitrexed in patients with advanced solid tumours.
Blair, EY; Clarke, SJ; McLachlan, AJ; Rivory, LP, 2004
)
0.32
"three-compartment pharmacokinetic model was used to fit the concentration-time data of raltitrexed."( Population pharmacokinetics of raltitrexed in patients with advanced solid tumours.
Blair, EY; Clarke, SJ; McLachlan, AJ; Rivory, LP, 2004
)
0.32
"A population pharmacokinetic model has been developed for raltitrexed in patients with advanced cancer."( Population pharmacokinetics of raltitrexed in patients with advanced solid tumours.
Blair, EY; Clarke, SJ; McLachlan, AJ; Rivory, LP, 2004
)
0.32
" Specifically, we compare the pharmacokinetic and pharmacodynamic properties of these EGFR inhibitors examined in preclinical and clinical studies."( Pharmacokinetic and pharmacodynamic properties of EGFR inhibitors under clinical investigation.
Grandis, JR; Thomas, SM, 2004
)
0.32
" Pharmacokinetic sampling was also obtained."( Evaluation of biologic end points and pharmacokinetics in patients with metastatic breast cancer after treatment with erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor.
Bacharach, SL; Berman, A; Brahim, JS; Carrasquillo, JA; Chow, C; Ettenberg, SA; Figg, WD; Hewitt, SM; Lepper, ER; Lipkowitz, S; Parr, AL; Sparreboom, A; Steinberg, SM; Swain, SM; Tan, AR; Whatley, M; Yang, X, 2004
)
0.32
" This ZD9331/docetaxel regimen does not appear to be associated with either major pharmacokinetic or toxicologic drug-drug interactions."( A phase I and pharmacokinetic study of the nonpolyglutamatable thymidylate synthase inhibitor ZD9331 plus docetaxel in patients with advanced solid malignancies.
Garrison, M; Jones, CB; McCreery, H; Patnaik, A; Rowinsky, EK; Schwartz, GH; Skinner, M; Takimoto, C; Tolcher, AW, 2004
)
0.32
" The purpose of this study is to assess the effect of heat on the pharmacokinetic profile of Raltitrexed administered intraperitoneally in rats."( A study of the effect of temperature on the pharmacokinetic profile of raltitrexed administered by intraperitoneal route in the rat.
Bendavid, Y; Dubé, P; Leblond, FA, 2005
)
0.33
" In this report, we describe a noninvasive pharmacodynamic model in which topical application of capsaicin is utilized to induce the release of endogenous CGRP and a vasodilatory response which can be measured using laser Doppler imaging."( Investigation of the species selectivity of a nonpeptide CGRP receptor antagonist using a novel pharmacodynamic assay.
Baskin, EP; Corcoran, HA; Hargreaves, RJ; Hershey, JC; Kane, SA; Koblan, KS; Mosser, S; Salvatore, CA; Williams, TM, 2005
)
0.33
" To evaluate the pharmacokinetic interaction of theophylline with rutaecarpine, the effects of rutaecarpine on CYP1A2 activity and theophylline pharmacokinetics were investigated."( Alteration of the pharmacokinetics of theophylline by rutaecarpine, an alkaloid of the medicinal herb Evodia rutaecarpa, in rats.
Chen, RM; Chen, TL; Don, MJ; Tsai, TH; Ueng, YF, 2005
)
0.33
"4-L volume of distribution, an initial half-life (t(1/2alpha)) of 6 minutes, and a terminal half-life (t(1/2beta)) of 45 minutes."( Phase I trial and pharmacokinetic study of raltitrexed in children with recurrent or refractory leukemia: a pediatric oncology group study.
Berg, SL; Bernstein, M; Blaney, SM; Horton, TM; Kamen, B; Kuhn, J; Langevin, AM; Weitman, S, 2005
)
0.33
" Following intravenous dosing (5 mg kg(-1), gefitinib plasma half-life was 3-6h in rats and dogs, although studies using a more sensitive HPLC-MS assay produced longer estimates of half-life (7-14h)."( Pharmacokinetics of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat and dog.
Bardsley, J; Hutchison, M; McKillop, D; Parry, AC; Partridge, EA; Rhead, SA; Swaisland, HC; Woodman, HM, 2004
)
0.32
"In this phase II multicenter trial, the primary objective was assessment of the tumor response rate with gefitinib; secondary objectives included analysis of the pharmacodynamic and biologic profiles in healthy and tumor tissue."( Phase II and tumor pharmacodynamic study of gefitinib in patients with advanced breast cancer.
Albanell, J; Baselga, J; Gascón, P; González, S; Guillém, V; Koehler, MT; Lluch, A; Marimón, I; Rojo, F; Ruiz, A; Sauleda, S; Tabernero, JM, 2005
)
0.33
" Pharmacokinetic samples were obtained on days 1 and 20."( Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas.
Blackwell, KL; Burris, HA; Dees, EC; Dowlati, A; Ellis, MJ; Harris, JL; Hurwitz, HI; Jones, SF; Koch, KM; Mangum, S; Marcom, PK; O'Neil, B; Overmoyer, B; Smith, DA; Spector, NL; Stead, A, 2005
)
0.33
" Pharmacokinetic and safety assessments were conducted throughout the trial."( A phase I study to determine the effect of tamoxifen on the pharmacokinetics of a single 250 mg oral dose of gefitinib (IRESSA) in healthy male volunteers.
Bailey, CJ; Cantarini, MV; Macpherson, MP; Marshall, AL; Robinson, AV, 2005
)
0.33
" The presence of tamoxifen did not have a clinically significant effect on the primary variables AUC and Cmax of gefitinib, nor on the secondary variables AUC(0-t), tmax, t1/2, and lambdaz."( A phase I study to determine the effect of tamoxifen on the pharmacokinetics of a single 250 mg oral dose of gefitinib (IRESSA) in healthy male volunteers.
Bailey, CJ; Cantarini, MV; Macpherson, MP; Marshall, AL; Robinson, AV, 2005
)
0.33
" Pharmacokinetic data were calculated by a non-compartmental model."( Effects of Evodia rutaecarpa and rutaecarpine on the pharmacokinetics of caffeine in rats.
Chang, CH; Lin, LC; Tsai, TH, 2005
)
0.33
" Pharmacokinetic studies were performed during course one (day 1 through 28)."( Phase I and pharmacokinetic study of gefitinib in children with refractory solid tumors: a Children's Oncology Group Study.
Adamson, PC; Bernstein, ML; Blaney, SM; Croop, JM; Dancey, JE; Daw, NC; Furman, WL; Iacono, LC; Krailo, M; Reaman, GH; Speights, RA; Stewart, CF, 2005
)
0.33
" The median apparent clearance and median half-life were 14."( Phase I and pharmacokinetic study of gefitinib in children with refractory solid tumors: a Children's Oncology Group Study.
Adamson, PC; Bernstein, ML; Blaney, SM; Croop, JM; Dancey, JE; Daw, NC; Furman, WL; Iacono, LC; Krailo, M; Reaman, GH; Speights, RA; Stewart, CF, 2005
)
0.33
" Based on these findings, three clinical studies were carried out to investigate pharmacokinetic drug interactions in vivo with gefitinib."( Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol.
Laight, A; Leadbetter, J; McKillop, D; Ranson, M; Smith, RP; Swaisland, HC; Wild, MJ, 2005
)
0.33
" Appropriate pharmacokinetic parameters were determined by noncompartmental methods."( Single-dose clinical pharmacokinetic studies of gefitinib.
Duvauchelle, T; Kerr, DJ; Laight, A; Ranson, M; Smith, RP; Swaisland, HC; Wilder-Smith, CH, 2005
)
0.33
" Absorption was again moderately slow, with gmean Cmax of 159 ng/mL (range 48."( Single-dose clinical pharmacokinetic studies of gefitinib.
Duvauchelle, T; Kerr, DJ; Laight, A; Ranson, M; Smith, RP; Swaisland, HC; Wilder-Smith, CH, 2005
)
0.33
" Gefitinib undergoes rapid plasma clearance and has an extensive volume of distribution, resulting in a pharmacokinetic profile supportive of a once-daily dosage regimen."( Single-dose clinical pharmacokinetic studies of gefitinib.
Duvauchelle, T; Kerr, DJ; Laight, A; Ranson, M; Smith, RP; Swaisland, HC; Wilder-Smith, CH, 2005
)
0.33
"Quantitative structure-pharmacokinetic relationships (QSPkR) have increasingly been used for the prediction of the pharmacokinetic properties of drug leads."( Quantitative structure-pharmacokinetic relationships for drug clearance by using statistical learning methods.
Chen, YZ; Li, ZR; Yap, CW, 2006
)
0.33
"To compare the pharmacokinetic variables of erlotinib in current smokers with nonsmokers after receiving a single oral 150 or 300 mg dose of erlotinib."( Effects of smoking on the pharmacokinetics of erlotinib.
Beard, SE; Cagnoni, PJ; Clark, GM; Hamilton, M; Rusk, J; Witt, K; Wolf, JL, 2006
)
0.33
"This was a single-center, open-label pharmacokinetic study in healthy male subjects."( Effects of smoking on the pharmacokinetics of erlotinib.
Beard, SE; Cagnoni, PJ; Clark, GM; Hamilton, M; Rusk, J; Witt, K; Wolf, JL, 2006
)
0.33
" In an attempt to explain this variability, three pharmacokinetic studies were carried out in healthy volunteers to investigate the relationship between exposure to gefitinib and cytochrome P450 (CYP) 3A phenotype (study 1), CYP3A5 genotype (study 2) and CYP2D6 genotype (study 3)."( Exploring the relationship between expression of cytochrome P450 enzymes and gefitinib pharmacokinetics.
Cantarini, MV; Fuhr, R; Holt, A; Swaisland, HC, 2006
)
0.33
" In study 2, 73 healthy volunteers with previously defined single-dose gefitinib pharmacokinetic profiles were genotyped for CYP3A5."( Exploring the relationship between expression of cytochrome P450 enzymes and gefitinib pharmacokinetics.
Cantarini, MV; Fuhr, R; Holt, A; Swaisland, HC, 2006
)
0.33
" Herein we provide the preclinical and clinical rationale for studies examining the concept of pharmacodynamic separation as a means for overcoming hypothesized antagonism of EGFR TKIs and chemotherapy."( Pharmacodynamic separation of epidermal growth factor receptor tyrosine kinase inhibitors and chemotherapy in non-small-cell lung cancer.
Davies, AM; Gandara, DR; Gumerlock, PH; Ho, C; Lara, PN; Mack, P, 2006
)
0.33
" Strategies to lower volume of distribution and shorten half-life through structure and pKa modulation are discussed."( Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
Ballard, P; Bradbury, RH; Harris, CS; Hennequin, LF; Hickinson, M; Kendrew, J; Kettle, JG; Klinowska, T; Ogilvie, DJ; Pearson, SE; Williams, EJ; Wilson, I, 2006
)
0.33
" For pharmacokinetic analysis plasma sampling was performed during the first and second course and assayed using a validated high-performance liquid chromatographic assay with mass spectrometric detection."( Phase I and pharmacokinetic study of halofuginone, an oral quinazolinone derivative in patients with advanced solid tumours.
de Jonge, MJ; Dumez, H; Lacombe, D; Marréaud, S; Punt, CJ; Snyder, D; van Oosterom, A; Verweij, J; Yamaguchi, T; Yarkoni, S, 2006
)
0.33
" Pharmacokinetic data showed high interpatient variability."( Multicentre phase II pharmacokinetic and pharmacodynamic study of OSI-7904L in previously untreated patients with advanced gastric or gastroesophageal junction adenocarcinoma.
Ajani, J; Albert, D; Anthoney, A; Chick, J; Drolet, DW; Eatock, M; Falk, S; Ferry, D; Glen, H; Valle, JW; Van Cutsem, E, 2006
)
0.33
"The population pharmacokinetic analysis was performed by use of NONMEM based on 4068 concentration samples from 1047 patients receiving erlotinib as a single agent or in combination with chemotherapy."( Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure-safety relationship in patients with non-small cell lung cancer.
Bruno, R; Eppler, SM; Hamilton, M; Lu, JF; Lum, BL; Rakhit, A; Wolf, J, 2006
)
0.33
" The median erlotinib half-life based on this patient population was 36."( Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure-safety relationship in patients with non-small cell lung cancer.
Bruno, R; Eppler, SM; Hamilton, M; Lu, JF; Lum, BL; Rakhit, A; Wolf, J, 2006
)
0.33
"The long half-life of erlotinib supports the current once-daily dosing regimen at 150 mg/d."( Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure-safety relationship in patients with non-small cell lung cancer.
Bruno, R; Eppler, SM; Hamilton, M; Lu, JF; Lum, BL; Rakhit, A; Wolf, J, 2006
)
0.33
"A physiological pharmacokinetic (PBPK) model was used to estimate tumor microcirculation in nude mice with a grafted tumor."( Evaluation of antiangiogenic treatment effects on tumors' microcirculation by Bayesian physiological pharmacokinetic modeling and magnetic resonance imaging.
Balvay, D; Bessoud, B; Bois, FY; Brochot, C; Cuénod, CA; Siauve, N, 2006
)
0.33
"To assess the feasibility of administering erlotinib, an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, in combination with paclitaxel and carboplatin, and to identify pharmacokinetic interactions, evaluate downstream effects of EGFR inhibition on surrogate tissues, and seek preliminary evidence for clinical activity."( Phase I, pharmacokinetic, and biological study of erlotinib in combination with paclitaxel and carboplatin in patients with advanced solid tumors.
Beeram, M; Hamilton, M; Hammond, LA; Hidalgo, M; Kreisberg, JI; Mita, MM; Nadler, P; Patnaik, A; Rowinsky, EK; Schwartz, G; Tolcher, AW; Wolf, J; Wood, D, 2006
)
0.33
" There was no evidence of pharmacokinetic interactions between paclitaxel and erlotinib; however, total carboplatin exposure trended higher in the presence of erlotinib."( Phase I, pharmacokinetic, and biological study of erlotinib in combination with paclitaxel and carboplatin in patients with advanced solid tumors.
Beeram, M; Hamilton, M; Hammond, LA; Hidalgo, M; Kreisberg, JI; Mita, MM; Nadler, P; Patnaik, A; Rowinsky, EK; Schwartz, G; Tolcher, AW; Wolf, J; Wood, D, 2006
)
0.33
"To develop a population pharmacokinetic (popPK) model for CP-724,714, a novel HER2 tyrosine kinase inhibitor is under development for the treatment of advanced HER2 positive cancers."( Population pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors.
Guo, F; Letrent, SP; Sharma, A, 2007
)
0.34
"A 2-compartment first-order absorption pharmacokinetic (PK) model with inter-subject variability (ISV) on the apparent oral elimination clearance (CL/F), apparent central volume of distribution (V1/F), apparent peripheral volume of distribution (V2/F), and first-order oral absorption rate constant (ka), interoccasion variability (IOV) on CL/F, and body weight (WT) as covariate on CL/F was developed."( Population pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors.
Guo, F; Letrent, SP; Sharma, A, 2007
)
0.34
" Future studies will further assess the importance of WT as a pharmacokinetic covariate."( Population pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors.
Guo, F; Letrent, SP; Sharma, A, 2007
)
0.34
"The purpose of the study was to evaluate the effects of erlotinib on epidermal growth factor receptor (EGFR)-related signaling elements in tumor and skin from patients with advanced squamous cell carcinoma of the head and neck (HNSCC) and seek relationships between relevant clinical, biological, and pharmacokinetic parameters."( Assessment of erlotinib pharmacodynamics in tumors and skin of patients with head and neck cancer.
Baillargeon, GM; Calvo, E; Chin, SF; Hidalgo, M; Irish, J; Kreisberg, JI; Malik, SN; Rowinsky, EK; Santabarbara, P; Siu, LL, 2007
)
0.34
" Pharmacokinetic studies were done for calcitriol and gefitinib."( A phase I pharmacokinetic and pharmacodynamic study of intravenous calcitriol in combination with oral gefitinib in patients with advanced solid tumors.
Bernardi, RJ; Black, JD; Brattain, MG; Creaven, PJ; Fakih, MG; French, R; Hutson, A; Johnson, CS; Muindi, JR; Schwartz, J; Trump, DL, 2007
)
0.34
" Erlotinib and OSI-420 plasma pharmacokinetic variables on days 8 and 34 overlapped to suggest that steady state had been reached."( Plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite OSI-420.
Bai, F; Broniscer, A; Fraga, C; Gajjar, A; Krasin, MJ; O'Shaughnessy, M; Panetta, JC; Stewart, CF, 2007
)
0.34
" Pharmacokinetic analysis was performed."( Phase I dose escalation and pharmacokinetic study of AZD2171, an inhibitor of the vascular endothelial growth factor receptor tyrosine kinase, in patients with hormone refractory prostate cancer (HRPC).
Conry, S; Hutcheon, D; Morris, C; Puchalski, T; Roth, B; Ryan, CJ; Small, EJ; Stadler, WM, 2007
)
0.34
"To investigate whether differences in plasma pharmacokinetic profiles of gefitinib between healthy subjects having normal (N; t(1/2)>20h) and altered (A; t(1/2)<20h) pharmacokinetic (PK) profiles might be explained by inter-individual variability in gastric emptying and/or precipitation/dissolution of gefitinib in the proximal small intestine."( Pharmacokinetics of gefitinib in humans: the influence of gastrointestinal factors.
Bergman, E; Cantarini, MV; Dickinson, P; Farmer, MR; Forsell, P; Knutson, L; Lennernäs, H; Persson, EM; Smith, R; Swaisland, H, 2007
)
0.34
"The objectives of this phase I dose-finding study of erlotinib were to investigate the toxicity profile, to confirm the acceptable toxicity of doses up to 150 mg/day, and to assess the pharmacokinetic (PK) profile and antitumor activity in Japanese patients with solid tumors."( Phase I dose-finding and pharmacokinetic study of the oral epidermal growth factor receptor tyrosine kinase inhibitor Ro50-8231 (erlotinib) in Japanese patients with solid tumors.
Fujisaka, Y; Horiike, A; Murakami, H; Shimoyama, T; Tamura, T; Yamada, Y; Yamamoto, N, 2008
)
0.35
"A rational drug discovery process was initiated to design a potent and prostate-selective alpha1(L)-adrenoceptor antagonist with pharmacokinetic properties suitable for once a day administration after oral dosing, for the treatment of benign prostatic hyperplasia."( Impact of physicochemical and structural properties on the pharmacokinetics of a series of alpha1L-adrenoceptor antagonists.
Atkinson, F; Beaumont, K; Betts, A; Fox, D; Gardner, I; Morgan, P; Webster, R, 2007
)
0.34
"PURPOSE Pharmacodynamic tissue studies were conducted on a phase I/II trial of erlotinib and cisplatin in patients with recurrent or metastatic head and neck squamous cell carcinoma (HNSCC)."( Predictive and pharmacodynamic biomarker studies in tumor and skin tissue samples of patients with recurrent or metastatic squamous cell carcinoma of the head and neck treated with erlotinib.
Agulnik, M; Chen, EX; Chen, H; Chen, S; da Cunha Santos, G; Dancey, J; Dos Reis, PP; Hedley, D; Ho, J; Kamel-Reid, S; Marrano, P; Nicklee, T; Pond, GR; Shyr, Y; Siu, LL; Soulieres, D; Squire, JA; Tsao, MS; Winquist, E, 2007
)
0.34
" Further evaluation of PQD-A4 and PQD-BE in single and multiple pharmacokinetic (PK) studies as well as corresponding toxicity studies was conducted with rats."( Pharmacokinetics, safety, and hydrolysis of oral pyrroloquinazolinediamines administered in single and multiple doses in rats.
Anova, L; Kozar, MP; Li, Q; Lin, AJ; Milhous, WK; Shearer, TW; Si, Y; Skillman, DR; Smith, KS; Xie, LH; Zhang, J, 2007
)
0.34
" Part 1 was designed to determine the OTR and part 2 was the pharmacokinetic part of the study."( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors.
Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007
)
0.34
" Here, we show pharmacodynamic changes in VEGFR-2 phosphorylation induced by AZD2171."( Acute pharmacodynamic and antivascular effects of the vascular endothelial growth factor signaling inhibitor AZD2171 in Calu-6 human lung tumor xenografts.
Barry, ST; Copley, C; James, NH; Jürgensmeier, JM; Kendrew, J; Oakley, I; Smith, NR; Wainwright, A; Wedge, SR; Womersley, LM, 2007
)
0.34
" Additional patients were treated at the OTR dose level to further evaluate safety and for pharmacokinetic analyses."( Phase I and pharmacokinetic study of lapatinib in combination with capecitabine in patients with advanced solid malignancies.
Arya, N; Chu, QS; Curtright, J; de Bono, J; Fleming, RA; Ho, PT; Koch, KM; Pandite, L; Rowinsky, EK; Schwartz, G; Smith, DA; Versola, MJ, 2007
)
0.34
"Lapatinib and capecitabine administered on a 3-week schedule were well tolerated, and no pharmacokinetic interaction was observed."( Phase I and pharmacokinetic study of lapatinib in combination with capecitabine in patients with advanced solid malignancies.
Arya, N; Chu, QS; Curtright, J; de Bono, J; Fleming, RA; Ho, PT; Koch, KM; Pandite, L; Rowinsky, EK; Schwartz, G; Smith, DA; Versola, MJ, 2007
)
0.34
" Co-administration of lapatinib increased the area under the plasma concentration-time curve of SN-38, the active metabolite of irinotecan, by an average of 41%; no other pharmacokinetic interactions were observed."( A phase I and pharmacokinetic study of lapatinib in combination with infusional 5-fluorouracil, leucovorin and irinotecan.
Flaherty, KT; Fleming, RA; Kerr, DJ; Koch, KM; Middleton, MR; Midgley, RS; O'Dwyer, PJ; Pratap, SE; Smith, DA; Stevenson, JP; Versola, M; Ward, C, 2007
)
0.34
" Pharmacokinetic parameters were estimated using non-compartmental and compartmental methods."( The plasma and cerebrospinal fluid pharmacokinetics of erlotinib and its active metabolite (OSI-420) after intravenous administration of erlotinib in non-human primates.
Balis, FM; Fox, E; McCully, C; Meany, HJ; Tucker, C, 2008
)
0.35
" We hypothesize that cell cycle arrest induced by erlotinib accounts for these findings in the presence of wild-type EGFR and that pharmacodynamic separation of the 2 drug classes will ameliorate these effects."( Schedule-dependent apoptosis in K-ras mutant non-small-cell lung cancer cell lines treated with docetaxel and erlotinib: rationale for pharmacodynamic separation.
Davies, AM; Gandara, DR; Gumerlock, PH; Holland, W; Lara, PN; Mack, PC; Mahaffey, CM; Pryde, B, 2007
)
0.34
" These results suggest that rutaecarpine might cause changes in the pharmacokinetic parameters of APAP in rats."( The effects of rutaecarpine on the pharmacokinetics of acetaminophen in rats.
Bista, SR; Jahng, Y; Jeong, H; Jeong, TC; Kang, MJ; Kim, DH; Lee, SK, 2007
)
0.34
"Epidermal growth factor receptor (EGFR) inhibitors, such as gefitinib, are examples of targeted anticancer drugs whose drug sensitivity is related to gene mutations that adds a pharmacogenetic (PG) dimension to any pharmacokinetic (PK) and pharmacodynamic (PD) analysis."( Preclinical pharmacokinetic/pharmacodynamic models of gefitinib and the design of equivalent dosing regimens in EGFR wild-type and mutant tumor models.
Gallo, JM; Guo, P; Wang, S; Wang, X; Zhou, Q, 2008
)
0.35
"To assess the pharmacogenomic and pharmacokinetic determinants of skin rash and diarrhea, the two primary dose-limiting toxicities of the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor erlotinib."( Pharmacogenomic and pharmacokinetic determinants of erlotinib toxicity.
Armstrong, DK; Brahmer, JR; Carducci, MA; Chen, P; Das, S; Desai, A; Fackenthal, DL; Fleming, GF; Janisch, L; Jiang, X; Karrison, T; Liu, W; Poonkuzhali, B; Ramirez, J; Ratain, MJ; Rudin, CM; Schuetz, E; Vokes, EE, 2008
)
0.35
"A novel diplotype of two polymorphic loci in the ABCG2 promoter involving -15622C/T and 1143C/T was identified, with alleles conferring lower ABCG2 levels associated with higher erlotinib pharmacokinetic parameters, including area under the curve (P = ."( Pharmacogenomic and pharmacokinetic determinants of erlotinib toxicity.
Armstrong, DK; Brahmer, JR; Carducci, MA; Chen, P; Das, S; Desai, A; Fackenthal, DL; Fleming, GF; Janisch, L; Jiang, X; Karrison, T; Liu, W; Poonkuzhali, B; Ramirez, J; Ratain, MJ; Rudin, CM; Schuetz, E; Vokes, EE, 2008
)
0.35
"Although exploratory in nature, this combined pharmacogenomic and pharmacokinetic model helps to define and differentiate the primary determinants of skin and gastrointestinal toxicity of erlotinib."( Pharmacogenomic and pharmacokinetic determinants of erlotinib toxicity.
Armstrong, DK; Brahmer, JR; Carducci, MA; Chen, P; Das, S; Desai, A; Fackenthal, DL; Fleming, GF; Janisch, L; Jiang, X; Karrison, T; Liu, W; Poonkuzhali, B; Ramirez, J; Ratain, MJ; Rudin, CM; Schuetz, E; Vokes, EE, 2008
)
0.35
" Paclitaxel clearance decreased during cycle 2, but no other significant pharmacokinetic interactions were observed."( Phase I and pharmacokinetic study of daily oral AZD2171, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with carboplatin and paclitaxel in patients with advanced non-small-cell lung cancer: the National Cancer Institut
Arnold, A; Chen, E; Ellis, PM; Gauthier, I; Goss, G; Laurie, SA; Powers, J; Puchalski, TA; Robertson, J; Seymour, L; Shepherd, FA; Tu, D; Walsh, W, 2008
)
0.35
" The aim of this clinical trial was to evaluate the tolerance and single-dose pharmacokinetic profile of DOP in healthy human volunteers."( Phase I clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: tolerance and pharmacokinetics study of escalating single oral doses.
Algorta, J; Alvarez-González, A; Maraschiello, C; Maruhn, D; Mucke, HA; Pena, MA; Windisch, M, 2008
)
0.35
" No pharmacokinetic interaction was observed."( Phase I and pharmacokinetic study of lapatinib and docetaxel in patients with advanced cancer.
Arya, N; Burris, HA; Fleming, RA; Gadgeel, S; Jones, SF; Koch, KM; Loftiss, J; LoRusso, PM; Pandite, L; Weber, BL, 2008
)
0.35
" Additional patients were enrolled at the OTR dose level to further evaluate safety and for pharmacokinetic analyses."( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer.
Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008
)
0.35
"Thirty-nine patients were enrolled in the study: 12 in the dose-escalation group, 7 in the OTR safety group, and 20 in the pharmacokinetic group."( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer.
Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008
)
0.35
"Clinically relevant doses of lapatinib in combination with letrozole were well tolerated and did not result in a pharmacokinetic interaction, and clinical antitumor activity was observed."( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer.
Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008
)
0.35
"We have constructed a new ocular pharmacokinetic pharmacodynamic (PK/PD) model for anti-glaucoma drugs to describe ocular hypotensive effects on intraocular pressure (IOP) after instillation of a combination of an alpha(1)-adrenergic antagonist, bunazosin, and a beta-adrenergic antagonist, timolol, into rabbits."( Ocular pharmacokinetic/pharmacodynamic modeling for multiple anti-glaucoma drugs.
Higuchi, S; Kawazu, K; Kitahara, T; Nakamura, J; Nakashima, M; Nishida, K; Sakanaka, K; Sasaki, H; Tomonari, M, 2008
)
0.35
"We conducted a phase I and pharmacokinetic study of the epidermal growth factor receptor (EGFR) inhibitor erlotinib as a single agent and in combination with temozolomide in children with refractory solid tumors."( Pediatric phase I and pharmacokinetic study of erlotinib followed by the combination of erlotinib and temozolomide: a Children's Oncology Group Phase I Consortium Study.
Adamson, PC; Blaney, SM; Dancey, JE; Gilbertson, RJ; Hamilton, M; Ingle, AM; Jakacki, RI; Krailo, MD; Tersak, J; Voss, SD, 2008
)
0.35
" Pharmacokinetic studies and ERBB-receptor expression and signaling studies were performed."( Pediatric phase I and pharmacokinetic study of erlotinib followed by the combination of erlotinib and temozolomide: a Children's Oncology Group Phase I Consortium Study.
Adamson, PC; Blaney, SM; Dancey, JE; Gilbertson, RJ; Hamilton, M; Ingle, AM; Jakacki, RI; Krailo, MD; Tersak, J; Voss, SD, 2008
)
0.35
"This randomized, double-blind, parallel, placebo-controlled, single rising-dose study investigated the safety, tolerability, pharmacokinetic, and pharmacodynamic profiles of BI 1356 (once-daily, given orally) in healthy men."( Safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of BI 1356, an inhibitor of dipeptidyl peptidase 4, in healthy male volunteers.
Dugi, KA; Graefe-Mody, EU; Hüttner, S; Ring, A; Withopf, B, 2008
)
0.35
"To evaluate the safety and describe the pharmacokinetic profile of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, in combination with cisplatin (CDDP) in adults with advanced solid tumors."( Phase I, pharmacokinetic and biological correlative study of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, and cisplatin in patients with solid tumors.
Berlin, JD; Chick, J; Drolet, DW; Horan, J; Papadopoulos, KP; Quaratino-Baker, C; Ricart, AD; Rothenberg, ML; Rowinsky, EK; Syed, S; Tolcher, AW; Vermeulen, W, 2008
)
0.35
" Pharmacokinetic samples, baseline plasma homocysteine, and genotype polymorphisms were evaluated."( Phase I, pharmacokinetic and biological correlative study of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, and cisplatin in patients with solid tumors.
Berlin, JD; Chick, J; Drolet, DW; Horan, J; Papadopoulos, KP; Quaratino-Baker, C; Ricart, AD; Rothenberg, ML; Rowinsky, EK; Syed, S; Tolcher, AW; Vermeulen, W, 2008
)
0.35
" No major pharmacokinetic interactions between CDDP and OSI-7904L were observed."( Phase I, pharmacokinetic and biological correlative study of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, and cisplatin in patients with solid tumors.
Berlin, JD; Chick, J; Drolet, DW; Horan, J; Papadopoulos, KP; Quaratino-Baker, C; Ricart, AD; Rothenberg, ML; Rowinsky, EK; Syed, S; Tolcher, AW; Vermeulen, W, 2008
)
0.35
" Pharmacokinetic interaction between the agents was not apparent."( Phase I, pharmacokinetic and biological correlative study of OSI-7904L, a novel liposomal thymidylate synthase inhibitor, and cisplatin in patients with solid tumors.
Berlin, JD; Chick, J; Drolet, DW; Horan, J; Papadopoulos, KP; Quaratino-Baker, C; Ricart, AD; Rothenberg, ML; Rowinsky, EK; Syed, S; Tolcher, AW; Vermeulen, W, 2008
)
0.35
" The pharmacokinetic profile of lapatinib in Japanese patients was comparable to that of western subjects."( Phase I dose-escalation and pharmacokinetic trial of lapatinib (GW572016), a selective oral dual inhibitor of ErbB-1 and -2 tyrosine kinases, in Japanese patients with solid tumors.
Fukuoka, M; Kanezaki, M; Kawada, K; Kurata, T; Minami, H; Minamide, Y; Mukai, H; Mukaiyama, A; Nakagawa, K; Nogami, T; Sasaki, Y; Uejima, H, 2009
)
0.35
" Pharmacokinetic studies were obtained after first dose and on day 8 of therapy."( Phase I and pharmacokinetic studies of erlotinib administered concurrently with radiotherapy for children, adolescents, and young adults with high-grade glioma.
Baker, SJ; Broniscer, A; Ellison, DW; Endersby, R; Gajjar, A; Kocak, M; Laningham, FH; Merchant, TE; Morris, EB; Schaiquevich, P; Stewart, CF, 2009
)
0.35
" The pharmacokinetic variables of erlotinib and OSI-420 in children were similar to those described in adults."( Phase I and pharmacokinetic studies of erlotinib administered concurrently with radiotherapy for children, adolescents, and young adults with high-grade glioma.
Baker, SJ; Broniscer, A; Ellison, DW; Endersby, R; Gajjar, A; Kocak, M; Laningham, FH; Merchant, TE; Morris, EB; Schaiquevich, P; Stewart, CF, 2009
)
0.35
"Although the MTD of erlotinib in children with newly diagnosed high-grade glioma was 120 mg/m(2) per day, pharmacokinetic studies showed wide interpatient variability in drug exposure."( Phase I and pharmacokinetic studies of erlotinib administered concurrently with radiotherapy for children, adolescents, and young adults with high-grade glioma.
Baker, SJ; Broniscer, A; Ellison, DW; Endersby, R; Gajjar, A; Kocak, M; Laningham, FH; Merchant, TE; Morris, EB; Schaiquevich, P; Stewart, CF, 2009
)
0.35
" Because the formulations and manufacturers differed, the differences in tolerability, as well as platelet counts, might have been related to differences in pharmacokinetic properties between the 2 formulations."( Pharmacokinetics, bioequivalence, tolerability, and effects on platelet counts of two formulations of anagrelide in healthy volunteers and patients with thrombocythemia associated with chronic myeloproliferation.
Gisslinger, H; Krumpl, G; Linkesch, W; Petrides, PE; Schüller, A; Steurer, M; Widmann, R, 2009
)
0.35
"The present series of investigations (1) determined the pharmacokinetic profile of anagrelide and its metabolites; (2) compared the pharmacokinetic profiles of the test and reference formulations of anagrelide; (3) investigated the in vitro release of anagrelide as a marker of intragastric anagrelide release of the test and reference formulations; and (4) compared the platelet-reducing effects of the test and reference formulations in patients with thrombocythemia in 2 longitudinal studies over 4 weeks."( Pharmacokinetics, bioequivalence, tolerability, and effects on platelet counts of two formulations of anagrelide in healthy volunteers and patients with thrombocythemia associated with chronic myeloproliferation.
Gisslinger, H; Krumpl, G; Linkesch, W; Petrides, PE; Schüller, A; Steurer, M; Widmann, R, 2009
)
0.35
" In a pilot, prospective, singledose study in healthy volunteers, the pharmacokinetic properties (C(max), T(max), and AUC(0-infinity)) of a test formulation of anagrelide were assessed using high-performance liquid chromatography analysis of plasma samples."( Pharmacokinetics, bioequivalence, tolerability, and effects on platelet counts of two formulations of anagrelide in healthy volunteers and patients with thrombocythemia associated with chronic myeloproliferation.
Gisslinger, H; Krumpl, G; Linkesch, W; Petrides, PE; Schüller, A; Steurer, M; Widmann, R, 2009
)
0.35
"The pilot pharmacokinetic study of the test formulation in 16 volunteers (10 women, 6 men; mean [SD] age, 20."( Pharmacokinetics, bioequivalence, tolerability, and effects on platelet counts of two formulations of anagrelide in healthy volunteers and patients with thrombocythemia associated with chronic myeloproliferation.
Gisslinger, H; Krumpl, G; Linkesch, W; Petrides, PE; Schüller, A; Steurer, M; Widmann, R, 2009
)
0.35
"The pharmacokinetic properties, adverse event rates, and in vitro dissolution profile differed between the test and reference anagrelide formulations in these healthy volunteers."( Pharmacokinetics, bioequivalence, tolerability, and effects on platelet counts of two formulations of anagrelide in healthy volunteers and patients with thrombocythemia associated with chronic myeloproliferation.
Gisslinger, H; Krumpl, G; Linkesch, W; Petrides, PE; Schüller, A; Steurer, M; Widmann, R, 2009
)
0.35
" Pharmacokinetic analysis confirmed cediranib as suitable for once-daily oral dosing."( Phase I, dose escalation and pharmacokinetic study of cediranib (RECENTIN), a highly potent and selective VEGFR signaling inhibitor, in Japanese patients with advanced solid tumors.
Boku, N; Fujiwara, Y; Murakami, H; Nokihara, H; Puchalski, TA; Shin, E; Takahashi, T; Tamura, T; Yamada, K; Yamada, Y; Yamamoto, N; Yamazaki, K, 2009
)
0.35
"To investigate the safety, tolerability, pharmacokinetic and pharmacodynamic properties of multiple oral doses of the dipeptidyl peptidase-4 (DPP-4) inhibitor linagliptin (BI 1356) in patients with type 2 diabetes mellitus."( Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients.
Dugi, KA; Graefe-Mody, EU; Heise, T; Hüttner, S; Ring, A; Trommeshauser, D, 2009
)
0.35
" Accumulation half-life was short (8."( Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients.
Dugi, KA; Graefe-Mody, EU; Heise, T; Hüttner, S; Ring, A; Trommeshauser, D, 2009
)
0.35
" Pharmacodynamic separation by intermittent delivery of epidermal growth factor receptor tyrosine kinase inhibitors with chemotherapy may increase efficacy by overcoming hypothesized antagonism."( Intermittent erlotinib in combination with pemetrexed: phase I schedules designed to achieve pharmacodynamic separation.
Beckett, L; Davies, AM; Gandara, DR; Ho, C; Lara, PN; Lau, D; Perkins, N; Scudder, SA, 2009
)
0.35
"The goals of this investigation were to illustrate the use of pharmacokinetic (PK)/pharmacodynamic (PD) modeling strategies in drug development based on a multiple-dose study of gefitinib in a preclinical tumor model."( Demonstration of the equivalent pharmacokinetic/pharmacodynamic dosing strategy in a multiple-dose study of gefitinib.
Gallo, JM; Wang, S; Zhou, Q, 2009
)
0.35
" Linagliptin improves glycaemic control in type 2 diabetic patients by increasing the half-life of the incretin hormone glucagon-like peptide-1 (GLP-1)."( Evaluation of the potential for steady-state pharmacokinetic and pharmacodynamic interactions between the DPP-4 inhibitor linagliptin and metformin in healthy subjects.
Dugi, KA; Graefe-Mody, EU; Padula, S; Ring, A; Withopf, B, 2009
)
0.35
" Pharmacokinetic studies were conducted to assess the effect of pancreatic enzyme deficiency and intestinal malabsorption secondary to cystic fibrosis on the bioavailability of orally administered erlotinib, a lipophilic drug."( Pharmacokinetics of erlotinib for the treatment of high-grade glioma in a pediatric patient with cystic fibrosis: case report and review of the literature.
Broniscer, A; Christiansen, SR; Panetta, JC; Stewart, CF, 2009
)
0.35
"The aim of the present human pharmacology clinical trial was to assess the oral bioavailability, pharmacokinetic profile and tolerability of desoxypeganine, administered in a multiple-dose regimen to healthy volunteers."( Randomized, crossover, single-blind, placebo-controlled, human pharmacology clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: multiple-dose pharmacokinetics.
Algorta, J; Alvarez, A; Maraschiello, C; Maruhn, D; Mucke, HA; Pena, MA; Windisch, M, 2009
)
0.35
" Main pharmacokinetic parameters after single and multiple doses were estimated."( Randomized, crossover, single-blind, placebo-controlled, human pharmacology clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: multiple-dose pharmacokinetics.
Algorta, J; Alvarez, A; Maraschiello, C; Maruhn, D; Mucke, HA; Pena, MA; Windisch, M, 2009
)
0.35
" Cmax and AUC are approximately double with the dose of 100 mg comparing with the dose of 50 mg."( Randomized, crossover, single-blind, placebo-controlled, human pharmacology clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: multiple-dose pharmacokinetics.
Algorta, J; Alvarez, A; Maraschiello, C; Maruhn, D; Mucke, HA; Pena, MA; Windisch, M, 2009
)
0.35
"The present clinical trial describes the pharmacokinetic profile of two doses of desoxypeganine, administered orally in multiple dose to healthy volunteers."( Randomized, crossover, single-blind, placebo-controlled, human pharmacology clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: multiple-dose pharmacokinetics.
Algorta, J; Alvarez, A; Maraschiello, C; Maruhn, D; Mucke, HA; Pena, MA; Windisch, M, 2009
)
0.35
" Post marketing study commitments have been made upon (accelerated) approval such as additional pharmacokinetic studies in patients with renal- or hepatic impairment, in children, additional interactions studies and studies on the relative or absolute bioavailability."( Clinical pharmacokinetics of tyrosine kinase inhibitors.
Gelderblom, H; Guchelaar, HJ; van Erp, NP, 2009
)
0.35
" Clinical assessments of safety and antitumor activity were recorded and blood was sampled for pharmacokinetic assessments."( A phase I and pharmacokinetic study of oral lapatinib administered once or twice daily in patients with solid malignancies.
Arya, N; Burris, HA; Fleming, RA; Jones, SF; Koch, KM; Pandite, L; Smith, DA; Spector, N; Taylor, CW; Versola, MJ; Wilding, G, 2009
)
0.35
" Four patients with locally advanced esophageal adenocarcinoma were treated with gefitinib (250 mg/day) for 14 days and pharmacokinetic (PK) studies were conducted to monitor plasma drug concentrations."( A novel pharmacodynamic approach to assess and predict tumor response to the epidermal growth factor receptor inhibitor gefitinib in patients with esophageal cancer.
Abdallah, N; Altiok, S; Berman, D; Forastiere, A; Gibson, MK; Jagannath, S; Mezzadra, H; Rudek, MA; Tsottles, N, 2010
)
0.36
" To determine possible drug-drug interaction with this combination, a subset of 24 (12 erlotinib, 12 placebo) patients were enrolled onto an intensive pharmacokinetic (IPK) substudy group at a single site."( Pharmacokinetic study of the phase III, randomized, double-blind, multicenter trial (TRIBUTE) of paclitaxel and carboplatin combined with erlotinib or placebo in patients with advanced Non-small Cell Lung Cancer (NSCLC).
Blumenschein, GR; Herbst, RS; Kim, ES; Lu, C; Lum, BL; Malik, M; Oh, YW; Papadimitrakopoulou, VA; Tran, HT; Zinner, RG, 2011
)
0.37
"Complete blood sampling for pharmacokinetic analysis was obtained in 21 of 24 patients."( Pharmacokinetic study of the phase III, randomized, double-blind, multicenter trial (TRIBUTE) of paclitaxel and carboplatin combined with erlotinib or placebo in patients with advanced Non-small Cell Lung Cancer (NSCLC).
Blumenschein, GR; Herbst, RS; Kim, ES; Lu, C; Lum, BL; Malik, M; Oh, YW; Papadimitrakopoulou, VA; Tran, HT; Zinner, RG, 2011
)
0.37
" The authors determined whether a pharmacokinetic interaction occurs between sotrastaurin and everolimus, both of which are substrates and inhibitors of CYP3A4."( Sotrastaurin and everolimus pharmacokinetics after single-dose coadministration.
Antunes, MC; Bartlett, M; Kovarik, JM; Marbach, P; Rordorf, C; van Marle, S; Winter, S, 2010
)
0.36
" Clinical and pharmacokinetic data were collected to Day 5 after each treatment."( Sotrastaurin and everolimus pharmacokinetics after single-dose coadministration.
Antunes, MC; Bartlett, M; Kovarik, JM; Marbach, P; Rordorf, C; van Marle, S; Winter, S, 2010
)
0.36
" Although unbound linagliptin is cleared efficiently (CL/F 220 L/h), the concentration-dependent binding is responsible for the long terminal half-life (approximatelly 120 hours) of linagliptin and its nonlinear pharmacokinetics."( Impact of target-mediated drug disposition on Linagliptin pharmacokinetics and DPP-4 inhibition in type 2 diabetic patients.
Duval, V; Graefe-Mody, U; Jaehde, U; Retlich, S; Staab, A, 2010
)
0.36
"The aims of this study were to further define the safety of sorafenib and erlotinib, given at their full approved monotherapy doses, and to correlate pharmacokinetic and pharmacodynamic markers with clinical outcome."( Phase I combination of sorafenib and erlotinib therapy in solid tumors: safety, pharmacokinetic, and pharmacodynamic evaluation from an expansion cohort.
Bandarchi-Chamkhaleh, B; Chen, EX; Do, T; Duran, I; Le Tourneau, C; MacLean, M; Mak, TW; Metser, U; Nayyar, R; Pham, NA; Quintela-Fandino, M; Siu, LL; Tsao, M; Tusche, MW; Wang, L; Wright, JJ, 2010
)
0.36
"To establish a SPE-HPLC method for the determination and pharmacokinetic study of evodiamine and rutacarpine in rat plasma."( [Determination of evodiamine and rutaecarpine of compound Wuzhuyu cataplasm in plasma by SPE-HPLC: application to its pharmacokinetics].
Kang, C; Li, M; Liu, S; Tong, H; Wang, Y; Yin, W; Zhou, Z, 2009
)
0.35
"After transdermal administration to rats, the pharmacokinetic behavior of evodiamine and rutaecarpine belongs to the one-compartment model."( [Determination of evodiamine and rutaecarpine of compound Wuzhuyu cataplasm in plasma by SPE-HPLC: application to its pharmacokinetics].
Kang, C; Li, M; Liu, S; Tong, H; Wang, Y; Yin, W; Zhou, Z, 2009
)
0.35
" It is proved to be suitable for pharmacokinetic study of evodiamine and rutaecarpine."( [Determination of evodiamine and rutaecarpine of compound Wuzhuyu cataplasm in plasma by SPE-HPLC: application to its pharmacokinetics].
Kang, C; Li, M; Liu, S; Tong, H; Wang, Y; Yin, W; Zhou, Z, 2009
)
0.35
" How sotrastaurin and tacrolimus could be partnered in an immunosuppressive regimen will need to be established in the context of controlled clinical trials in organ transplant patients, taking into account the pharmacokinetic interaction on tacrolimus and the potentially enhanced immunosuppressive activity of this drug combination."( Sotrastaurin and tacrolimus coadministration: effects on pharmacokinetics and biomarker responses.
Grenet, O; Kovarik, JM; Seiberling, M; Sfikas, N; Slade, A; Stitah, S; Straube, F; Vitaliti, A; Winter, S, 2010
)
0.36
" Pharmacokinetics were studied with LC-MS/MS, standard, and population pharmacokinetic methods."( Phase I and pharmacokinetic study of erlotinib (OSI-774) in combination with docetaxel in squamous cell carcinoma of the head and neck (SSCHN).
Agrawal, A; Aimiumu, J; Chan, KK; Chen, P; Cheng, H; Dancey, J; Grever, MR; Kraut, EH; Lang, J; Rhoades, C; Young, DC; Zhang, Y, 2011
)
0.37
" In 24 patients, the mean Cmax and AUC erlotinib values increased with dose and following cumulative dosing (days 7 and 8 vs."( Phase I and pharmacokinetic study of erlotinib (OSI-774) in combination with docetaxel in squamous cell carcinoma of the head and neck (SSCHN).
Agrawal, A; Aimiumu, J; Chan, KK; Chen, P; Cheng, H; Dancey, J; Grever, MR; Kraut, EH; Lang, J; Rhoades, C; Young, DC; Zhang, Y, 2011
)
0.37
" The elimination half-life of sotrastaurin averages 6 hours."( Overview of sotrastaurin clinical pharmacokinetics.
Kovarik, JM; Slade, A, 2010
)
0.36
" Pharmacokinetic parameters were determined using noncompartmental methods."( Pharmacokinetics of vandetanib in subjects with renal or hepatic impairment.
Langmuir, P; Martin, P; Molz, KH; Oliver, S; Read, J; Smith, R; Weil, A, 2010
)
0.36
" Serial plasma samples for pharmacokinetic analyses were obtained after the first dose."( A pediatric phase I trial and pharmacokinetic study of ispinesib: a Children's Oncology Group phase I consortium study.
Adamson, PC; Blaney, SM; Conlan, MG; Dubowy, RL; Ingle, AM; Souid, AK; Sun, J, 2010
)
0.36
" The median (range) terminal elimination half-life was 16 (8-44) hr and the plasma drug clearance was 5 (1-14) L/hr/m(2) ."( A pediatric phase I trial and pharmacokinetic study of ispinesib: a Children's Oncology Group phase I consortium study.
Adamson, PC; Blaney, SM; Conlan, MG; Dubowy, RL; Ingle, AM; Souid, AK; Sun, J, 2010
)
0.36
" The half-life was ∼40 hours."( Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors.
Baselga, J; Casado, E; Cervantes, A; Chirivella, I; Elvin, P; Hamberg, P; Hoekman, K; Hurwitz, HI; Iacona, R; Jodrell, DI; Martinelli, E; Swaisland, A; Tabernero, J, 2010
)
0.36
" This study aimed to investigate any potential pharmacokinetic interaction between linagliptin and pioglitazone, a CYP 2C8 substrate."( Evaluation of the pharmacokinetic interaction between the dipeptidyl peptidase-4 inhibitor linagliptin and pioglitazone in healthy volunteers.
Dugi, KA; Graefe-Mody, EU; Jungnik, A; Ring, A; Woerle, HJ, 2010
)
0.36
"Linagliptinand pioglitazone have no clinically relevant pharmacokinetic interaction and may be co-administered without dose adjustment."( Evaluation of the pharmacokinetic interaction between the dipeptidyl peptidase-4 inhibitor linagliptin and pioglitazone in healthy volunteers.
Dugi, KA; Graefe-Mody, EU; Jungnik, A; Ring, A; Woerle, HJ, 2010
)
0.36
" Noncompartmental analysis and population pharmacokinetic modelling were performed."( Pharmacokinetics and pharmacodynamics of single rising intravenous doses (0.5 mg-10 mg) and determination of absolute bioavailability of the dipeptidyl peptidase-4 inhibitor linagliptin (BI 1356) in healthy male subjects.
Dugi, KA; Duval, V; Graefe-Mody, U; Hüttner, S; Jaehde, U; Jungnik, A; Retlich, S; Ring, A; Staab, A, 2010
)
0.36
" The terminal elimination half-life was comparable across dose groups (126-139 hours)."( Pharmacokinetics and pharmacodynamics of single rising intravenous doses (0.5 mg-10 mg) and determination of absolute bioavailability of the dipeptidyl peptidase-4 inhibitor linagliptin (BI 1356) in healthy male subjects.
Dugi, KA; Duval, V; Graefe-Mody, U; Hüttner, S; Jaehde, U; Jungnik, A; Retlich, S; Ring, A; Staab, A, 2010
)
0.36
"The nonlinear pharmacokinetic characteristics and the pharmacokinetic/pharmacodynamic relationship of linagliptin were independent of the mode of administration (intravenous or oral)."( Pharmacokinetics and pharmacodynamics of single rising intravenous doses (0.5 mg-10 mg) and determination of absolute bioavailability of the dipeptidyl peptidase-4 inhibitor linagliptin (BI 1356) in healthy male subjects.
Dugi, KA; Duval, V; Graefe-Mody, U; Hüttner, S; Jaehde, U; Jungnik, A; Retlich, S; Ring, A; Staab, A, 2010
)
0.36
" However, this was not seen as clinically relevant due to the absence of a reliable dose-response relationship and the known large pharmacokinetic interindividual variability of glyburide."( Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects.
Graefe-Mody, U; Iovino, M; Ring, A; Rose, P; Woerle, HJ; Zander, K, 2011
)
0.37
" This study evaluated the effect of food on the pharmacokinetics of cediranib and compared the administration of continual cediranib via two dosing strategies using this as a platform to investigate pharmacodynamic imaging biomarkers."( A two-part phase II study of cediranib in patients with advanced solid tumours: the effect of food on single-dose pharmacokinetics and an evaluation of safety, efficacy and imaging pharmacodynamics.
Cheung, S; Evans, J; Fielding, A; Harris, A; Jackson, A; Jayson, GC; Kelly, C; Middleton, M; Mitchell, CL; O'Connor, JP; Parker, GJ; Roberts, C; Rudman, S; Spicer, J; Tessier, J; Watson, Y; Young, H, 2011
)
0.37
" Exploratory pharmacodynamic assessments were performed using DCE-MRI and CT enhancing fraction (EnF)."( A two-part phase II study of cediranib in patients with advanced solid tumours: the effect of food on single-dose pharmacokinetics and an evaluation of safety, efficacy and imaging pharmacodynamics.
Cheung, S; Evans, J; Fielding, A; Harris, A; Jackson, A; Jayson, GC; Kelly, C; Middleton, M; Mitchell, CL; O'Connor, JP; Parker, GJ; Roberts, C; Rudman, S; Spicer, J; Tessier, J; Watson, Y; Young, H, 2011
)
0.37
" In a pharmacokinetic study, 13 de novo liver transplant recipients received 100 mg sotrastaurin once between days 1-3 and once between days 5-8 post-transplant."( Sotrastaurin single-dose pharmacokinetics in de novo liver transplant recipients.
Cillo, U; Gatlik, E; Kovarik, JM; Meiser, K; Neuhaus, P; Slade, A; Stitah, S; Weber, M, 2011
)
0.37
" Tacrolimus exposure was significantly increased by sotrastaurin in the initial weeks posttransplant by a pharmacokinetic interaction."( Pharmacokinetics of sotrastaurin combined with tacrolimus or mycophenolic acid in de novo kidney transplant recipients.
Arns, W; Budde, K; Dantal, J; Grinyo, JM; Kovarik, JM; Proot, P; Rostaing, L; Steiger, JU, 2011
)
0.37
" There were no clinically significant changes in steady-state pharmacokinetic parameters of digoxin when it was co-administered with linagliptin."( Evaluation of the pharmacokinetic interaction after multiple oral doses of linagliptin and digoxin in healthy volunteers.
Brand, T; Friedrich, C; Graefe-Mody, EU; Ring, A; Sennewald, R; Woerle, HJ, 2011
)
0.37
" Pharmacokinetic parameters were determined using non-compartmental methods."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
0.37
" In Study 2, the geometric mean gefitinib steady-state AUC during the 24-h dosing interval was slightly, but not significantly, higher in patients with moderate hepatic impairment; there were, however, no significant differences between groups in gefitinib and metabolite pharmacokinetic parameters."( The effect of different etiologies of hepatic impairment on the pharmacokinetics of gefitinib.
Cantarini, M; Carmichael, J; Harris, AL; Holt, A; Horak, J; Macpherson, M; Swaisland, A; Swaisland, H; Twelves, C; Verrill, M; White, J, 2011
)
0.37
" For pharmacokinetic analysis, 7 time point samples were collected on D1 of cycle 1 for lapatinib and vinorelbine assays."( Pharmacokinetic evaluation of the vinorelbine-lapatinib combination in the treatment of breast cancer patients.
Berille, J; Bonneterre, J; Brain, E; Dieras, V; Isambert, N; Lokiec, F; Rezai, K; Roche, H; Urien, S, 2011
)
0.37
" The population pharmacokinetic parameters were CL = 27."( Pharmacokinetic evaluation of the vinorelbine-lapatinib combination in the treatment of breast cancer patients.
Berille, J; Bonneterre, J; Brain, E; Dieras, V; Isambert, N; Lokiec, F; Rezai, K; Roche, H; Urien, S, 2011
)
0.37
"The pharmacokinetic modeling of vinorelbine and lapatinib was consistent with the results previously reported."( Pharmacokinetic evaluation of the vinorelbine-lapatinib combination in the treatment of breast cancer patients.
Berille, J; Bonneterre, J; Brain, E; Dieras, V; Isambert, N; Lokiec, F; Rezai, K; Roche, H; Urien, S, 2011
)
0.37
"The geometric mean ratios (GMRs) (90% confidence interval (CI)) of AUC0-∞ and Cmax for (linagliptin + warfarin)/warfarin were 98."( Effect of linagliptin on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers.
Brand, T; Graefe-Mody, EU; Iovino, M; Ring, A; Stangier, J; Withopf, B; Woerle, HJ, 2011
)
0.37
" The safety, efficacy and pharmacokinetic (PK) profile of barasertib were investigated in Japanese patients with advanced acute myeloid leukemia."( A Phase I study to assess the safety, pharmacokinetics and efficacy of barasertib (AZD1152), an Aurora B kinase inhibitor, in Japanese patients with advanced acute myeloid leukemia.
Ando, K; Asou, H; Fujisawa, S; Hotta, T; Kihara, R; Miyawaki, S; Sakura, T; Tobinai, K; Tsuboi, K; Uike, N; Watanabe, T; Yamauchi, T; Yokozawa, T, 2011
)
0.37
" The pharmacokinetics of vandetanib in Chinese, Western, and Japanese patients were compared through a combined population pharmacokinetic model."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
" Population pharmacokinetic analysis suggests that vandetanib pharmacokinetics appear to be comparable in Chinese, Western, and Japanese patients."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
"The pharmacokinetic properties of vandetanib in these Chinese patients were characterized by low plasma clearance of approximately 8 L/h, a long half-life of approximately 8 to 10 days, and an accumulation of approximately 8-fold to 15-fold on multiple dosing."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
" The effect of several covariates and single nucleotide polymorphisms (SNP) in ABCB1, ABCG2, and CYP3A5 on pharmacokinetic parameters was evaluated."( Population analysis of erlotinib in adults and children reveals pharmacokinetic characteristics as the main factor explaining tolerance particularities in children.
Chatelut, E; Civade, E; Delord, JP; Geoerger, B; Hennebelle, I; Le Deley, MC; Thomas, F; Vassal, G; White-Koning, M, 2011
)
0.37
"The nonlinear population approach applied to pharmacokinetic data combined with a pharmacokinetic-pharmacodynamic analysis revealed that the higher recommended dose in children (125 mg/m(2)/day) compared with adults (90 mg/m(2)/day) is mainly due to pharmacokinetic rather than pharmacodynamic particularities."( Population analysis of erlotinib in adults and children reveals pharmacokinetic characteristics as the main factor explaining tolerance particularities in children.
Chatelut, E; Civade, E; Delord, JP; Geoerger, B; Hennebelle, I; Le Deley, MC; Thomas, F; Vassal, G; White-Koning, M, 2011
)
0.37
" The accumulation half-life of linagliptin ranged from 14-15 h in subjects with normal renal function to 18 h in severe renal impairment."( Effect of renal impairment on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor linagliptin(*).
Friedrich, C; Graefe-Mody, U; Halabi, A; Heise, T; Port, A; Retlich, S; Ring, A; Woerle, HJ, 2011
)
0.37
" The pharmacokinetic parameters measured were maximum steady-state plasma concentration during a dosage interval (C(max,ss)), time to reach maximum plasma concentration following administration at steady state (t(max,ss)) and area under the plasma concentration-time curve during a dosage interval (τ) at steady state (AUC(τ,ss))."( Effect of multiple oral doses of linagliptin on the steady-state pharmacokinetics of a combination oral contraceptive in healthy female adults: an open-label, two-period, fixed-sequence, multiple-dose study.
Friedrich, C; Giessmann, T; Graefe-Mody, U; Iovino, M; Port, A; Ring, A; Woerle, HJ, 2011
)
0.37
" For analysis of pharmacokinetic properties, linagliptin concentrations were determined from plasma and urinary samples obtained throughout the treatment phase, with more intensive samplings on days 1 and 28."( Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor linagliptin: a 4-week multicenter, randomized, double-blind, placebo-controlled phase IIa study in Japanese type 2 diabetes patients.
Dugi, KA; Graefe-Mody, EU; Hayashi, N; Horie, Y; Kanada, S; Sarashina, A; Taniguchi, A; Watada, H; Woerle, HJ, 2011
)
0.37
" The terminal half-life was long (223-260 hours) but did not reflect the accumulation half-life (10."( Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor linagliptin: a 4-week multicenter, randomized, double-blind, placebo-controlled phase IIa study in Japanese type 2 diabetes patients.
Dugi, KA; Graefe-Mody, EU; Hayashi, N; Horie, Y; Kanada, S; Sarashina, A; Taniguchi, A; Watada, H; Woerle, HJ, 2011
)
0.37
"Linagliptin demonstrated a nonlinear pharmacokinetic profile in these Japanese patients with T2DM consistent with the findings of previous studies in healthy Japanese and white patients."( Pharmacokinetic, pharmacodynamic, and tolerability profiles of the dipeptidyl peptidase-4 inhibitor linagliptin: a 4-week multicenter, randomized, double-blind, placebo-controlled phase IIa study in Japanese type 2 diabetes patients.
Dugi, KA; Graefe-Mody, EU; Hayashi, N; Horie, Y; Kanada, S; Sarashina, A; Taniguchi, A; Watada, H; Woerle, HJ, 2011
)
0.37
" Herein, we report on the structure-activity relationship and the detailed physicochemical and in vivo pharmacokinetic properties of sotrastaurin (AEB071, 1), a novel maleimide-based PKC inhibitor currently in phase II clinical trials."( Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Albert, R; Beerli, C; Cooke, NG; Cottens, S; Evenou, JP; Faller, B; Jean, C; Sedrani, R; von Matt, P; Wagner, J; Weckbecker, G; Wiegand, H; Zenke, G, 2011
)
0.37
" On the basis of preclinical models, we hypothesized pharmacodynamic separation, achieved by intermittent delivery of epidermal growth factor receptor tyrosine kinase inhibitors intercalated with chemotherapy, as a reasonable strategy to deliver combination therapy."( Intercalated erlotinib-docetaxel dosing schedules designed to achieve pharmacodynamic separation: results of a phase I/II trial.
Beckett, LA; Davies, AM; Gandara, DR; Hesketh, PJ; Lara, PN; Lau, D; Li, T; Mack, PC; Perkins, N; Sangha, R, 2011
)
0.37
" The MTD for arm B was chosen for phase II evaluation given the feasibility of administration, number of responses (one complete response and three partial responses), and achievement of pharmacodynamic separation."( Intercalated erlotinib-docetaxel dosing schedules designed to achieve pharmacodynamic separation: results of a phase I/II trial.
Beckett, LA; Davies, AM; Gandara, DR; Hesketh, PJ; Lara, PN; Lau, D; Li, T; Mack, PC; Perkins, N; Sangha, R, 2011
)
0.37
"To compare the pharmacokinetic (PK) parameters of a single dose of erlotinib in cancer patients with moderate hepatic impairment (MHI) to those of cancer patients with adequate hepatic function (AHF)."( An open-label study to describe pharmacokinetic parameters of erlotinib in patients with advanced solid tumors with adequate and moderately impaired hepatic function.
Belani, C; Boinpally, R; Evans, J; Franke, A; Gail Eckhardt, S; Haluska, P; Leong, S; O'Bryant, CL; Ramalingam, S; Ramanathan, RK; Rosen, L; Venugopal, B; Witt, K, 2012
)
0.38
" Pharmacokinetic data demonstrated no consistent increase in exposure to gefitinib with increasing dose across cohorts."( Safety and pharmacokinetics of high-dose gefitinib in patients with solid tumors: results of a phase I study.
Agus, DB; Gross, ME; Leichman, L; Lowe, ES; Swaisland, A, 2012
)
0.38
" The novel compound linagliptin has important different pharmacokinetic (PK) properties, when compared with previously commercialized DPP-4 inhibitors, which may offer some advantages in clinical practice."( Linagliptin for the treatment of type 2 diabetes (pharmacokinetic evaluation).
Scheen, AJ, 2011
)
0.37
"5, 3 and 4h) after administration, the concentrations of Rut and Evo in rat whole blood were determined by HPLC, and main pharmacokinetic parameters were calculated."( Pharmacokinetic comparisons of rutaecarpine and evodiamine after oral administration of Wu-Chu-Yu extracts with different purities to rats.
Chen, F; Ding, J; He, L; Li, Y; Peng, J; Xu, S; Zhang, J, 2012
)
0.38
" Drug pharmacokinetics demonstrated a half-life of approximately 33 h, and dose-proportionality with accumulation by a factor of 3 after repeated administrations."( Phase I study of the safety, tolerability and pharmacokinetics of PHA-848125AC, a dual tropomyosin receptor kinase A and cyclin-dependent kinase inhibitor, in patients with advanced solid malignancies.
Blaydorn, L; Borad, MJ; Ciomei, M; Fiorentini, F; Hidalgo, M; Isaacs, JD; Jameson, G; Jimeno, A; Laheru, D; Pacciarini, MA; Ramanathan, RK; Scaburri, A; Tibes, R; Von Hoff, DD; Weiss, GJ, 2012
)
0.38
" The geometric mean terminal half-life of afatinib was 33."( Afatinib pharmacokinetics and metabolism after oral administration to healthy male volunteers.
Ebner, T; Gansser, D; Marzin, K; Narjes, H; Shahidi, M; Stopfer, P; Uttereuther-Fischer, M, 2012
)
0.38
" Blood samples were collected for pharmacokinetic analysis for up to 28 days after the dose (Studies A and B) and 42 days after the dose (Study C)."( Pharmacokinetics of vandetanib: three phase I studies in healthy subjects.
Clarke, D; Giles, P; Hutchison, M; Kennedy, SJ; Martin, P; Oliver, S; Partridge, E, 2012
)
0.38
" Pharmacokinetic parameters were consistent across all studies (Studies A and C, vandetanib 800 mg: geometric mean CL/F, 13."( Pharmacokinetics of vandetanib: three phase I studies in healthy subjects.
Clarke, D; Giles, P; Hutchison, M; Kennedy, SJ; Martin, P; Oliver, S; Partridge, E, 2012
)
0.38
" Furthermore, the newly developed method is successfully used for the determination of evodiamine and rutecarpine in rabbit plasma for pharmacokinetic study."( Simultaneous determination of evodiamine and rutecarpine in rabbit plasma by LC-ESI-MS and its application to pharmacokinetics.
Cai, J; Li, W; Lin, C; Lin, G; Ma, J; Pan, J; Pan, X; Wang, X, 2011
)
0.37
" Through structure-based design, we discovered a new class of highly potent aminopyrimidine-based B-Raf inhibitors with improved solubility and pharmacokinetic profiles."( Potent and selective aminopyrimidine-based B-Raf inhibitors with favorable physicochemical and pharmacokinetic properties.
Aliagas, I; Alicke, B; Boggs, JW; Buckmelter, AJ; Choo, EF; Dinkel, V; Gloor, SL; Gould, SE; Gradl, SN; Grina, J; Gunzner-Toste, J; Hansen, JD; Hastings, G; Hatzivassiliou, G; Laird, ER; Lee, W; Mathieu, S; Moreno, D; Pulk, R; Ran, Y; Ren, L; Rudolph, J; Voegtli, WC; Wen, Z; Wenglowsky, S; Zhao, G, 2012
)
0.38
"The method described in this report has high sensitivity and selectivity, and was suitable for pharmacokinetic studies of evodiamine and rutaecarpine."( [Studies on pharmacokinetics of evodiamine and rutaecarpine in rats plasma after oral administration extracts of euodiae fructus].
Bao, T; Dong, Y; Li, Y; Weng, X; Yang, Q; Zhang, Y; Zhu, X, 2011
)
0.37
"A simple and sensitive high-performance liquid chromatographic method was developed for the simultaneous determination and pharmacokinetic analysis of seven alkaloids dehydroevodiamine (DHED), 10-hydroxyrutaecarpine (HDR), evodiamine (EDM), rutaecarpine (RCP), 1-methyl-2-n-nonyl-4(1H)quinolone (MNQ), evocarpine (ECP), and dihydroevocarpine (DHE), and two flavonoids isorhamnetin-7-O-rutinoside (RIM) and diosmetin-7-O-β-d-glucopyranoside (GRD) in rat plasma after oral administration of Wuzhuyu decoction."( Simultaneous determination and pharmacokinetic analysis of seven alkaloids and two flavonoids from rat plasma by HPLC-DAD after oral administration of Wuzhuyu decoction.
Hu, CQ; Li, F; Yang, XW, 2012
)
0.38
" Linagliptin has a long terminal half-life (>100 hours); however, its accumulation half-life is much shorter (approximately 10 hours), accounting for the rapid attainment of steady state."( Clinical pharmacokinetics and pharmacodynamics of linagliptin.
Friedrich, C; Graefe-Mody, U; Retlich, S, 2012
)
0.38
"In a single-dose pharmacokinetic study, 12 healthy Chinese volunteers received an oral dose of 600 mg of icotinib."( Effect of the CYP2C19 genotype on the pharmacokinetics of icotinib in healthy male volunteers.
Hu, P; Jiang, J; Liu, DY; Ruan, CJ, 2012
)
0.38
" The pharmacokinetic (PK), metabolic and excretion profiles of barasertib and barasertib-hQPA were characterized in this open-label Phase I study."( Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia.
D'Souza, R; Davies, M; Dennis, M; Oliver, S; Pike, L; Stockman, P, 2012
)
0.38
"Heterogeneity in brain tumors can result in variable drug distribution and possibly drug response; however, there are no readily accessible means to obtain regional pharmacokinetic (PK)/pharmacodynamic (PD) information in preclinical tumor models that typically rely on average drug concentration measurements."( Analytical approach to characterize the intratumoral pharmacokinetics and pharmacodynamics of gefitinib in a glioblastoma model.
Gallo, JM; Lv, H; Sharma, J, 2012
)
0.38
" Three days prior to pharmacokinetic assessment, patients divided their normal daily anagrelide into a structured twice-daily dosing (BID) schedule."( Pharmacokinetics and tolerability of anagrelide hydrochloride in young (18 - 50 years) and elderly (≥ 65 years) patients with essential thrombocythemia.
Alvarez-Larrán, A; Besses, C; Coll, R; Freitag, C; Martin, P; Purkayastha, J; Troy, S; Zeller, W, 2012
)
0.38
"We used mathematical modeling and available clinical trial data to predict how different pharmacokinetic parameters (fast versus slow metabolism) and dosing schedules (low dose versus high dose; missed doses with and without make-up doses) might affect the evolution of T790M-mediated resistance in mixed populations of tumor cells."( Effects of pharmacokinetic processes and varied dosing schedules on the dynamics of acquired resistance to erlotinib in EGFR-mutant lung cancer.
Chmielecki, J; Foo, J; Michor, F; Pao, W, 2012
)
0.38
" During the escalation phase, pazopanib and lapatinib doses were escalated in serial patient cohorts, and a limited blood sampling scheme was applied for pharmacokinetic evaluation."( Phase I and pharmacokinetic study of pazopanib and lapatinib combination therapy in patients with advanced solid tumors.
Arumugham, T; de Jonge, MJ; Hamberg, P; Hodge, J; Hurwitz, HI; Pandite, LN; Savage, S; Suttle, AB; Verweij, J, 2013
)
0.39
" The correlations between these pharmacokinetic variables and the objective responses, including progression-free survival(PFS)and overall survival(OS), were retrospectively analyzed."( The pharmacokinetics and long-term therapeutic effects of gefitinib in patients with lung adenocarcinoma harboring the epidermal growth factor receptor(EGFR)mutation.
Hirano, S; Hojo, M; Iikura, M; Ishii, S; Izumi, S; Kobayashi, N; Kudo, K; Naka, G; Sano, K; Sugiyama, H; Takeda, Y, 2012
)
0.38
"The Cmax of gefitinib in patients with a partial response(PR)was significantly lower than that of patients with stable disease(SD)(median Cmax: 278 vs 588 ng/mL, p<0."( The pharmacokinetics and long-term therapeutic effects of gefitinib in patients with lung adenocarcinoma harboring the epidermal growth factor receptor(EGFR)mutation.
Hirano, S; Hojo, M; Iikura, M; Ishii, S; Izumi, S; Kobayashi, N; Kudo, K; Naka, G; Sano, K; Sugiyama, H; Takeda, Y, 2012
)
0.38
"To investigate the pharmacokinetic and safety profile of linagliptin after single and multiple doses in healthy Chinese volunteers."( Pharmacokinetics of single and multiple oral doses of 5 mg linagliptin in healthy Chinese volunteers.
Friedrich, C; Patel, S; Ring, A; Shi, X; Woerle, HJ; Zeng, P, 2012
)
0.38
"Linagliptin demonstrated a favorable safety profile in healthy Chinese volunteers, with a pharmacokinetic profile that was similar to that observed previously in subjects of Japanese, Caucasian, or African American origin."( Pharmacokinetics of single and multiple oral doses of 5 mg linagliptin in healthy Chinese volunteers.
Friedrich, C; Patel, S; Ring, A; Shi, X; Woerle, HJ; Zeng, P, 2012
)
0.38
" The quantitation method was successfully applied for simultaneous estimation of IC87114, RFM and RFN in a pharmacokinetic drug-drug interaction study in Wistar rats."( Simultaneous quantitation of IC87114, roflumilast and its active metabolite roflumilast N-oxide in plasma by LC-MS/MS: application for a pharmacokinetic study.
Mukkanti, K; Thappali, SR; Vakkalanka, SK; Varanasi, KV; Veeraraghavan, S, 2012
)
0.38
" Using this data, we subsequently developed a physiologically based pharmacokinetic (PBPK) model of lapatinib in mice that accurately predicted the tissue concentrations after doses of 30, 60 and 90 mg/kg."( Physiologically based pharmacokinetic model of lapatinib developed in mice and scaled to humans.
Gustafson, DL; Hudachek, SF, 2013
)
0.39
" Erlotinib and sorafenib have significant pharmacokinetic interactions that may negatively impact the efficacy of the combination regimen."( NABTT 0502: a phase II and pharmacokinetic study of erlotinib and sorafenib for patients with progressive or recurrent glioblastoma multiforme.
Ahluwalia, MS; Grossman, SA; Hilderbrand, SL; Mikkelsen, T; Nabors, LB; Peereboom, DM; Phuphanich, S; Rosenfeld, MR; Supko, JG; Ye, X, 2013
)
0.39
" Linagliptin geometric mean AUC was 194 nmol l(-1) h (geometric coefficient of variation, 26%), with a Cmax of 16."( Pharmacokinetic and pharmacodynamic evaluation of linagliptin in African American patients with type 2 diabetes mellitus.
Friedrich, C; Glund, S; Graefe-Mody, U; Kissling, CJ; Lionetti, D; Patel, S; Retlich, S; Righetti, J; Woerle, HJ, 2013
)
0.39
" No pharmacokinetic interaction between S-1 and gefitinib was detected."( Phase I and pharmacokinetic study of gefitinib and S-1 combination therapy for advanced adenocarcinoma of the lung.
Azuma, K; Daga, H; Hayashi, H; Kiyota, H; Miyazaki, M; Murakami, H; Naito, T; Nakagawa, K; Okada, H; Okamoto, I; Takeda, K; Takeda, M; Tanaka, K; Terashima, M; Yamamoto, N, 2013
)
0.39
" Linagliptin is the most recently launched gliptin, with a unique pharmacokinetic (PK) profile characterized by negligible renal excretion and is now also available as a fixed-dose combination (FDC) with metformin."( Linagliptin plus metformin: a pharmacokinetic and pharmacodynamic evaluation.
Scheen, AJ, 2013
)
0.39
"An extensive literature search was performed to analyze the potential PK and pharmacodynamic interactions between linagliptin and metformin."( Linagliptin plus metformin: a pharmacokinetic and pharmacodynamic evaluation.
Scheen, AJ, 2013
)
0.39
" This cohort of Japanese patients exhibited higher pharmacokinetic exposures of anagrelide and its active metabolite than those previously documented in non-Japanese patients."( Open-label, dose-titration and continuation study to assess efficacy, safety, and pharmacokinetics of anagrelide in treatment-naïve Japanese patients with essential thrombocythemia.
Abhyankar, B; Hodgson, I; Kanakura, Y; Miyakawa, Y; Okamoto, S; Smith, J; Troy, S, 2013
)
0.39
" Using a LC-MS/MS assay validated in cell medium, cellular pharmacokinetic studies revealed that in cells overexpressing the P-gp intracellular concentrations of vandetanib were decreased compared to parental cell line."( Influence of the multidrug transporter P-glycoprotein on the intracellular pharmacokinetics of vandetanib.
Bidart, JM; Broutin, S; Deroussent, A; Farinotti, R; Gil, S; Jovelet, C; Paci, A, 2013
)
0.39
"Erlotinib shows large inter-patient pharmacokinetic variability, but the impact of early drug exposure and genetic variations on the clinical outcomes of erlotinib remains fully investigated."( Population pharmacokinetics/pharmacodynamics of erlotinib and pharmacogenomic analysis of plasma and cerebrospinal fluid drug concentrations in Japanese patients with non-small cell lung cancer.
Fukudo, M; Ikemi, Y; Inui, K; Katsura, T; Kim, YH; Masago, K; Mio, T; Mishima, M; Terada, T; Teramukai, S; Togashi, Y, 2013
)
0.39
" Population pharmacokinetic analysis was performed with the nonlinear mixed-effects modelling program NONMEM."( Population pharmacokinetics/pharmacodynamics of erlotinib and pharmacogenomic analysis of plasma and cerebrospinal fluid drug concentrations in Japanese patients with non-small cell lung cancer.
Fukudo, M; Ikemi, Y; Inui, K; Katsura, T; Kim, YH; Masago, K; Mio, T; Mishima, M; Terada, T; Teramukai, S; Togashi, Y, 2013
)
0.39
" We studied the combination of bexarotene and gefitinib in the third-line treatment of advanced non-small-cell lung cancer to examine pharmacokinetic interactions and establish the maximum tolerated dose."( Phase I and pharmacokinetic study of bexarotene in combination with gefitinib in the third-line treatment of non-small-cell lung cancer: brief report.
Chhatwani, L; Jacobs, CD; Lopez-Anaya, A; Padda, SK; Wakelee, HA; Zhou, L, 2013
)
0.39
"Like many solid tumors, glioblastomas are characterized by intratumoral biologic heterogeneity that may contribute to a variable distribution of drugs and their associated pharmacodynamic responses, such that the standard pharmacokinetic approaches based on analysis of whole-tumor homogenates may be inaccurate."( Intratumoral modeling of gefitinib pharmacokinetics and pharmacodynamics in an orthotopic mouse model of glioblastoma.
Gallo, JM; Lv, H; Sharma, J, 2013
)
0.39
"The pharmacokinetic profile of afatinib supports a once-daily dosage regimen."( Pharmacokinetics of afatinib, a selective irreversible ErbB family blocker, in patients with advanced solid tumours.
Erhardt, J; Goeldner, RG; Schmid, M; Stopfer, P; Wind, S, 2013
)
0.39
"A pharmacokinetic bioequivalence study was conducted in Asian subjects, to compare a fixed dose combination capsule single oral dose of alpha adrenoceptor blocker-Alfuzosin hydrochloride 10mg extended release and muscarinic antagonists-Solifenacin succinate 5mg against individually administered Xatral XL 10mg tablets (Alfuzosin) of Sanofi Synthelabo Limited, United Kingdom (UK) and Vesicare 5mg tablets (Solifenacin) of Astellas Pharma Limited, UK under fed conditions."( Combining benefits of an adrenergic and a muscarinic blocker in a single formulation - a pharmacokinetic evaluation.
Arora, R; Arora, V; Dey, S; Kandhwal, K; Khuroo, AH; Madan, S; Monif, T; Nazarudheen, S; Reyar, S, 2013
)
0.39
" Between RTX and RTX with RA groups, half-life (t1/2), AUC(0-t) and CL showed no statistically significant differences; RA co-administration did not affect the pharmacokinetics of raltitrexed."( [Pharmacokinetics behavior of raltitrexed in rats after single injected with astragali radix].
Song, JW; Xing, R; Zhou, K, 2013
)
0.39
" In vivo pharmacokinetic and pharmacodynamic evaluation was performed in both normal nude mice and a BM model established by intra-carotid artery (ICA) injection of PC-9 cells."( Pharmacokinetic and pharmacodynamic study of Gefitinib in a mouse model of non-small-cell lung carcinoma with brain metastasis.
Chen, Y; Wang, M; Zhao, J; Zhong, W, 2013
)
0.39
" QTcF intervals (QT interval corrected by the Fridericia formula) were evaluated based on electrocardiogram recordings time-matched with pharmacokinetic blood samples after single (Day 1) and continuous (Day 14; steady state) administration."( Phase II, open-label trial to assess QTcF effects, pharmacokinetics and antitumor activity of afatinib in patients with relapsed or refractory solid tumors.
Alam, S; Bent, L; de Bono, J; Kristeleit, H; Middleton, G; Molife, LR; Propper, D; Rudman, SM; Spicer, J; Stopfer, P; Tan, DS; Uttenreuther-Fischer, M; Wallenstein, G, 2013
)
0.39
" The maximum plasma concentration for afatinib was seen at median tmax 3 h after both single dose and at steady state."( Phase II, open-label trial to assess QTcF effects, pharmacokinetics and antitumor activity of afatinib in patients with relapsed or refractory solid tumors.
Alam, S; Bent, L; de Bono, J; Kristeleit, H; Middleton, G; Molife, LR; Propper, D; Rudman, SM; Spicer, J; Stopfer, P; Tan, DS; Uttenreuther-Fischer, M; Wallenstein, G, 2013
)
0.39
" We conducted a phase I and pharmacokinetic study with the erlotinib and celecoxib combination in patients with advanced premalignant lesions."( Chemoprevention of head and neck cancer with celecoxib and erlotinib: results of a phase ib and pharmacokinetic study.
Beitler, JJ; Chen, AY; Chen, Z; Chen, ZG; Grandis, JR; Grist, W; Hurwitz, SJ; Khuri, FR; Kono, SA; Lewis, M; Moore, CE; Moreno-Williams, R; Müller, S; Nannapaneni, S; Owonikoko, TK; Ramalingam, S; Saba, NF; Shin, DM; Shin, HJ; Sica, G; Yang, CS; Zhao, Y, 2014
)
0.4
" In this paper, the pharmacokinetic characteristics (absorption, distribution, metabolism and excretion) and drug-drug interactions of the approved TKIs are reviewed."( [Clinical pharmacokinetics of small molecule tyrosine kinase inhibitors].
Ding, JF; Zhong, DF, 2013
)
0.39
" Finally, the method was successfully used in a pharmacokinetic study that measured IC87114 in mouse plasma, BAL fluid and lung tissue after administration of a single 1mg/kg intratracheal dose of IC87114."( Development and validation of a highly sensitive LC-MS/MS method for quantification of IC87114 in mice plasma, bronchoalveolar lavage and lung samples: Application to pharmacokinetic study.
Bhandary, B; Chae, HJ; Kim, SR; Lee, YC; Marahatta, A, 2014
)
0.4
"In total, 25 patients were included, of whom 12 were evaluable for the pharmacokinetic analysis."( Effects of low-fat and high-fat meals on steady-state pharmacokinetics of lapatinib in patients with advanced solid tumours.
Arya, N; Botbyl, J; Cartee, L; Chu, QS; Devriese, LA; Koch, KM; Ma, WW; Matthys, GM; Mergui-Roelvink, M; Orford, KW; Robidoux, A; Schellens, JH; Stephenson, JJ, 2014
)
0.4
" The method was successfully applied to pharmacokinetic study of CUDC-101 after intravenous administration of single dosage 5 mg/kg in rats."( Determination of CUDC-101 in rat plasma by liquid chromatography mass spectrometry and its application to a pharmacokinetic study.
Ma, J; Wang, X; Wen, C; Xiang, Z; Zhang, Q, 2014
)
0.4
" Several explanations have been suggested, including pharmacokinetic and pharmacogenomic variability."( Correlation between erlotinib pharmacokinetics, cutaneous toxicity and clinical outcomes in patients with advanced non-small cell lung cancer (NSCLC).
Andreoli, R; Ardizzoni, A; Azzoni, C; Bartolotti, M; Bortesi, B; De Palma, G; Gelsomino, F; Goldoni, M; Mozzoni, P; Mutti, A; Silini, EM; Tiseo, M, 2014
)
0.4
"These findings suggest that the pharmacokinetics and metabolism of erlotinib are related to skin toxicity and may support further studies where erlotinib dosing is tailored according to pharmacokinetic parameters."( Correlation between erlotinib pharmacokinetics, cutaneous toxicity and clinical outcomes in patients with advanced non-small cell lung cancer (NSCLC).
Andreoli, R; Ardizzoni, A; Azzoni, C; Bartolotti, M; Bortesi, B; De Palma, G; Gelsomino, F; Goldoni, M; Mozzoni, P; Mutti, A; Silini, EM; Tiseo, M, 2014
)
0.4
" Correlative studies confirmed panobinostat's pharmacodynamic effect in blood, FPB, and tumor samples."( A phase I, pharmacokinetic, and pharmacodynamic study of panobinostat, an HDAC inhibitor, combined with erlotinib in patients with advanced aerodigestive tract tumors.
Akar, A; Altiok, S; Bepler, G; Chiappori, A; Gray, JE; Haura, E; Kish, JA; Kreahling, J; Lush, R; Neuger, A; Pinder-Schenck, M; Schell, MJ; Tanvetyanon, T; Tetteh, L; Williams, CC; Zhao, X, 2014
)
0.4
" This validated method was then successfully applied to a pharmacokinetic study involving twelve healthy Chinese volunteers."( LC-ESI-MS/MS determination of simotinib, a novel epidermal growth factor receptor tyrosine kinase inhibitor: application to a pharmacokinetic study.
Cheng, Z; He, L; Li, S; Liu, X; Ran, L; Xie, F; Yu, P, 2014
)
0.4
" Additional evaluations included pharmacokinetics, pharmacodynamic effects on PI3K and EGFR/mitogen-activated protein kinase signaling pathways in tumor and skin samples, and tumor response."( Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors.
Cohen, RB; Engelman, JA; Felip, E; Jänne, PA; Laird, AD; Macé, S; Martinez, P; Rockich, K; Ruiz-Soto, R; Shapiro, GI; Xu, J, 2014
)
0.4
" No major pharmacokinetic interaction between SAR245409 and erlotinib was noted."( Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors.
Cohen, RB; Engelman, JA; Felip, E; Jänne, PA; Laird, AD; Macé, S; Martinez, P; Rockich, K; Ruiz-Soto, R; Shapiro, GI; Xu, J, 2014
)
0.4
"MTDs of SAR245409 and erlotinib were below the single-agent doses of either agent, despite the lack of major pharmacokinetic interaction."( Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors.
Cohen, RB; Engelman, JA; Felip, E; Jänne, PA; Laird, AD; Macé, S; Martinez, P; Rockich, K; Ruiz-Soto, R; Shapiro, GI; Xu, J, 2014
)
0.4
" This Perspective discusses the use of (18)F-fluorodeoxyglucose-positron emission tomography (FDG-PET) for pharmacodynamic evaluation in a very early phase of treatment to predict clinical outcomes in patients with advanced non-small-cell lung cancer."( Early pharmacodynamic assessment using ¹⁸F-fluorodeoxyglucose positron-emission tomography on molecular targeted therapy and cytotoxic chemotherapy for clinical outcome prediction.
Ando, M; Asami, K; Atagi, S; Ishii, M; Kanazu, M; Kawaguchi, T; Kubo, A; Kusunoki, Y; Maruyama, K; Matsuda, Y; Minomo, S; Ogawa, Y; Takada, M; Uehira, K, 2014
)
0.4
"This population pharmacokinetic model was developed to characterize the pharmacokinetics of the oral irreversible ErbB family blocker afatinib in patients with solid tumors and to investigate the impact of selected intrinsic and extrinsic factors."( Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Fleury, A; Freiwald, M; Schmid, U; Staab, A; Stopfer, P; Wind, S, 2014
)
0.4
"The pharmacokinetic profile of afatinib was best described by a two-compartment disposition model with first-order absorption and linear elimination."( Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Fleury, A; Freiwald, M; Schmid, U; Staab, A; Stopfer, P; Wind, S, 2014
)
0.4
"This population pharmacokinetic model adequately described the pharmacokinetics of afatinib in different cancer patient populations and therefore can be used for simulations exploring covariate effects and possible dose adaptations."( Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Fleury, A; Freiwald, M; Schmid, U; Staab, A; Stopfer, P; Wind, S, 2014
)
0.4
"This review considers the pharmacokinetic profile, adverse effects and drug interactions of DPP-4 inhibitors."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" However, DPP-4 inhibitors have certain differences in their pharmacokinetic properties that may be associated with different clinical effects and adverse event profiles."( The pharmacokinetic considerations and adverse effects of DPP-4 inhibitors [corrected].
Athyros, VG; Elisaf, MS; Filippatos, TD, 2014
)
0.4
" This method is sufficient for pharmacokinetic studies of vandetanib in small animals and may be applied to human pharmacokinetic studies."( Validation of a high-performance liquid chromatographic ultraviolet detection method for the quantification of vandetanib in rat plasma and its application to pharmacokinetic studies.
Bu, Q; Cao, Z; Cui, D; Lin, H; Xu, Y; Zhao, Y,
)
0.13
" It shows moderate oral bioavailability of 42-53 % and Tmax < 4 h in mouse, rat, dog and monkey, with exposure-dose linearity proved in rats and dogs."( Preclinical pharmacokinetics and disposition of a novel selective VEGFR inhibitor fruquintinib (HMPL-013) and the prediction of its human pharmacokinetics.
Gu, Y; Guo, L; Li, K; Ren, H; Sai, Y; Su, W; Wang, J; Zhang, L; Zhang, W, 2014
)
0.4
"71 L/h, elimination half-life to 21."( Erlotinib: another candidate for the therapeutic drug monitoring of targeted therapy of cancer? A pharmacokinetic and pharmacodynamic systematic review of literature.
Buclin, T; Decosterd, LA; Gairard-Dory, AC; Gourieux, B; Guidi, M; Petit-Jean, E; Quoix, E; Ubeaud-Séquier, G; Widmer, N, 2015
)
0.42
" This study examined whether oral administration of MS-275 to the rats with lapatinib led to any pharmacokinetic interactions."( Pharmacokinetic interaction of entinostat and lapatinib following single and co-oral administration in rats.
Chen, M; Hu, L; Yang, X; Zhang, Q, 2014
)
0.4
" Pharmacokinetic parameters after afatinib 50 mg were investigated in subjects with mild (n = 8) or moderate (n = 8) hepatic impairment (Child-Pugh A and B) and healthy controls (n = 16) matched for age, weight and gender."( Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment.
Buschke, S; Fuchs, H; Gansser, D; Goeldner, RG; Halabi, A; Koenen, R; Petersen-Sylla, M; Schnell, D; Stopfer, P; Uttenreuther-Fischer, M; Wind, S, 2014
)
0.4
"Afatinib pharmacokinetic profiles and plasma protein binding were similar in subjects with impaired liver function and healthy controls."( Pharmacokinetics of afatinib in subjects with mild or moderate hepatic impairment.
Buschke, S; Fuchs, H; Gansser, D; Goeldner, RG; Halabi, A; Koenen, R; Petersen-Sylla, M; Schnell, D; Stopfer, P; Uttenreuther-Fischer, M; Wind, S, 2014
)
0.4
"This phase I study assessed the pharmacokinetic (PK), tolerability, safety and preliminary clinical activity of tamoxifen (T) and lapatinib (L) in patients with metastatic breast cancer (MBC)."( A phase I pharmacokinetics study of lapatinib and tamoxifen in metastatic breast cancer (EORTC 10053 Lapatam study).
Awada, A; Bogaerts, J; Brain, E; Cardoso, F; Fumoleau, P; Hayward, L; Koch, KM; Lokiec, F; Marréaud, S; Rezai, K; Werutsky, G, 2014
)
0.4
" Vandetanib + digoxin increased digoxin area under the concentration-time curve from zero to the last quantifiable concentration (AUC0-last) and Cmax by 23 and 29 %, respectively, versus digoxin alone, with only a 9 % decrease in CLR."( Pharmacokinetic evaluations of the co-administrations of vandetanib and metformin, digoxin, midazolam, omeprazole or ranitidine.
Johansson, S; Leese, PT; Li, Y; Lisbon, E; Martin, P; Mathews, D; Oliver, S; Read, J; Steinberg, M, 2014
)
0.4
" We correlated baseline biomarker signatures and pharmacodynamic (PD) biomarkers with PFS and OS."( Serum protein profiling reveals baseline and pharmacodynamic biomarker signatures associated with clinical outcome in mCRC patients treated with chemotherapy ± cediranib.
Barry, ST; Hoff, PM; Jürgensmeier, JM; Morgan, SR; Pommier, AJ; Robertson, JD; Shaw, R; Spencer, SK, 2014
)
0.4
"Sixteen of 19 patients were evaluable, with serial pharmacokinetic studies in ten patients."( Phase I dose escalation and pharmacokinetic study of oral gefitinib and irinotecan in children with refractory solid tumors.
Brennan, RC; Furman, W; Mao, S; McGregor, LM; Santana, V; Stewart, CF; Turner, DC; Wu, J, 2014
)
0.4
" Pharmacokinetic analysis confirms that co-administration of gefitinib increases irinotecan bioavailability leading to an increased SN-38 lactone systemic exposure."( Phase I dose escalation and pharmacokinetic study of oral gefitinib and irinotecan in children with refractory solid tumors.
Brennan, RC; Furman, W; Mao, S; McGregor, LM; Santana, V; Stewart, CF; Turner, DC; Wu, J, 2014
)
0.4
"To develop a population pharmacokinetic (PK) model for HM781-36 (poziotinib) and its metabolites in cancer patients."( Population pharmacokinetics of HM781-36 (poziotinib), pan-human EGF receptor (HER) inhibitor, and its two metabolites in patients with advanced solid malignancies.
Bae, KS; Jung, JA; Lim, HS; Noh, YH; Song, TH, 2015
)
0.42
" Nonlinear mixed effect modeling was employed to develop the population pharmacokinetic model."( Population pharmacokinetics of HM781-36 (poziotinib), pan-human EGF receptor (HER) inhibitor, and its two metabolites in patients with advanced solid malignancies.
Bae, KS; Jung, JA; Lim, HS; Noh, YH; Song, TH, 2015
)
0.42
" Pharmacokinetic parameters, including maximum plasma concentration (C(max)), area under the plasma concentration-time curve to the last sampling time (AUC(t)), AUC from time zero to infinity (AUC(∞)), and time to reach C(max) (t(max)), were measured, and all treatment-emergent adverse events and their relationships with the study medications were recorded throughout the study."( Pharmacokinetic properties of two erlotinib 150 mg formulations with a genetic effect evaluation in healthy Korean subjects.
Cho, SJ; Choi, HG; Im, YJ; Jeon, JY; Kim, MG; Kim, Y; Seo, YH; Song, EK, 2015
)
0.42
" Both formulations had very similar C(max), AUC, terminal half-life (t ½) and t(max) values."( Pharmacokinetic properties of two erlotinib 150 mg formulations with a genetic effect evaluation in healthy Korean subjects.
Cho, SJ; Choi, HG; Im, YJ; Jeon, JY; Kim, MG; Kim, Y; Seo, YH; Song, EK, 2015
)
0.42
"This study suggests that the test and reference formulations of 150 mg erlotinib have similar pharmacokinetic characteristics."( Pharmacokinetic properties of two erlotinib 150 mg formulations with a genetic effect evaluation in healthy Korean subjects.
Cho, SJ; Choi, HG; Im, YJ; Jeon, JY; Kim, MG; Kim, Y; Seo, YH; Song, EK, 2015
)
0.42
"The aim of this study was to evaluate the effect of coadministration of acid-reducing agents on the pharmacokinetic exposure of orally administered epidermal growth factor receptor inhibitor erlotinib, a drug that displays pH-dependent solubility."( Effect of gastric pH on erlotinib pharmacokinetics in healthy individuals: omeprazole and ranitidine.
Abt, M; Ducray, PS; Giraudon, M; Hamilton, M; Kletzl, H; Lum, BL, 2015
)
0.42
" This study was carried out to identify the contribution percentage of CYP450 to icotinib and use the results to develop a physiologically based pharmacokinetic (PBPK) model, which can help to predict drug-drug interaction (DDI)."( Relative contributions of the major human CYP450 to the metabolism of icotinib and its implication in prediction of drug-drug interaction between icotinib and CYP3A4 inhibitors/inducers using physiologically based pharmacokinetic modeling.
Chen, J; Hu, P; Jiang, J; Liu, D; Zhao, Q; Zheng, X, 2015
)
0.42
" This study examines pharmacokinetic interactions in simultaneous oral administration of SAHA and lapatinib to rats."( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats.
Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015
)
0.42
"Statistically significant pharmacokinetic differences appeared for lapatinib levels between the lapatinib and the coadministration group."( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats.
Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015
)
0.42
"The resulting data indicate that, when administered together, lapatinib does not influence the pharmacokinetic profile of SAHA in rats, while, in contrast, SAHA influences the pharmacokinetic profile of lapatinib."( Pharmacokinetic interaction study combining lapatinib with vorinostat in rats.
Geng, P; Lin, F; Wang, S; Wu, C; Zhang, Q; Zhang, X; Zhou, Y; Zou, H, 2015
)
0.42
" The systemic exposure to maximum plasma concentration and area under the plasma concentration curve (AUC) for lapatinib, as well as the AUC of paclitaxel, were increased when combined."( Safety, pharmacokinetics and efficacy findings in an open-label, single-arm study of weekly paclitaxel plus lapatinib as first-line therapy for Japanese women with HER2-positive metastatic breast cancer.
Aogi, K; Armour, A; Inoue, K; Iwata, H; Kuroi, K; Masuda, N; Nakayama, T; Nishimura, Y; Rai, Y; Sasaki, Y; Shimizu, S, 2015
)
0.42
"We conducted a cross-over pharmacokinetic study to compare the fed bioequivalence in the two conditions."( Comparison of the pharmacokinetics of erlotinib administered in complete fasting and 2 h after a meal in patients with lung cancer.
Fujiwara, Y; Goto, Y; Hamada, A; Horinouchi, H; Kanda, S; Katsuya, Y; Nokihara, H; Ohe, Y; Osawa, S; Sunami, K; Takashima, Y; Tamura, T; Utsumi, H; Yamamoto, N, 2015
)
0.42
" This phase I dose-finding study was designed to assess the tolerability and drug-drug interactions in this combination using full pharmacokinetic (PK) samplings."( Phase I dose-finding and pharmacokinetic study of docetaxel and gefitinib in patients with advanced or metastatic non-small-cell lung cancer: evaluation of drug-drug interaction.
Ando-Makihara, R; Hayashi, Y; Makino, Y; Motonaga, M; Ohe, Y; Takano, M; Yamamoto, N, 2015
)
0.42
" We describe here the profile of the novel compound BI 885578, a potent and selective ATP-competitive IGF1R/INSR tyrosine kinase inhibitor distinguished by rapid intestinal absorption and a short in vivo half-life as a result of rapid metabolic clearance."( BI 885578, a Novel IGF1R/INSR Tyrosine Kinase Inhibitor with Pharmacokinetic Properties That Dissociate Antitumor Efficacy and Perturbation of Glucose Homeostasis.
Adolf, GR; Apgar, J; Garin-Chesa, P; Haaksma, E; Hofmann, MH; Kessler, D; Kraut, N; Quant, J; Sanderson, MP; Savchenko, A; Schaaf, O; Treu, M; Tye, H; Zahn, SK; Zoephel, A, 2015
)
0.42
" A comprehensive whole-body physiologically based pharmacokinetic (PBPK) model of gefitinib in mice was developed, which adequately captured gefitinib concentration-time profiles in plasma and various tissues."( A Whole-Body Physiologically Based Pharmacokinetic Model of Gefitinib in Mice and Scale-Up to Humans.
An, G; Bi, Y; Deng, J; Murry, DJ, 2016
)
0.43
" This simple and reproducible high-throughput method was successfully applied to the pharmacokinetic study of gefitinib and its major metabolites in mouse."( Simultaneous determination of gefitinib and its major metabolites in mouse plasma by HPLC-MS/MS and its application to a pharmacokinetics study.
Han, SY; He, XR; Jiang, ST; Li, PP; Xu, GB; Zhao, C; Zheng, N, 2016
)
0.43
" However, the AUC and Cmax were highest and the trough value on day 8 was the second highest in one patient who died of drug-induced ILD."( Association of pharmacokinetics and pharmacogenomics with safety and efficacy of gefitinib in patients with EGFR mutation positive advanced non-small cell lung cancer.
Fujita, K; Hirose, T; Ishida, H; Kusumoto, S; Murata, Y; Nakashima, M; Ohmori, T; Oki, Y; Okuda, K; Sasaki, Y; Shirai, T; Sugiyama, T; Yamaoka, T, 2016
)
0.43
"To compare the pharmacokinetic parameters of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex and free evodiamine suspension in rats, and investigate the pharmacokinetic characteristics of evodiamine inclusion complex."( [A preliminary study of pharmacokinetics of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex].
Feng, J; Lei, TT; Liu, HM; Zhang, JQ; Zhang, X, 2016
)
0.43
" The pharmacokinetic parameters of evodiamine inclusion complex and free evodiamine in rats were as follows: Cmax, 252."( [A preliminary study of pharmacokinetics of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex].
Feng, J; Lei, TT; Liu, HM; Zhang, JQ; Zhang, X, 2016
)
0.43
" Pharmacokinetic parameters were measured after a single dose and in multiple dosing."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" PK analysis showed good and rapid absorption followed by slow terminal elimination with a mean half-life of approximately 42 h which was consistent across all dose groups."( A Phase I study of safety and pharmacokinetics of fruquintinib, a novel selective inhibitor of vascular endothelial growth factor receptor-1, -2, and -3 tyrosine kinases in Chinese patients with advanced solid tumors.
Cao, J; Chen, Z; Fan, S; Li, J; Li, K; Peng, W; Su, W; Zhang, J, 2016
)
0.43
" Plasma concentrations of gefitinib were also measured 10 h after the first administration in 21 of these patients to calculate the elimination half-life of gefitinib."( Pharmacokinetic parameters of gefitinib predict efficacy and toxicity in patients with advanced non-small cell lung cancer harboring EGFR mutations.
Fukuda, M; Ikeda, T; Ikegami, Y; Izumikawa, K; Mizoguchi, K; Motoshima, K; Mukae, H; Nakamura, Y; Nakatomi, K; Ogawara, D; Sano, K; Sato, S; Senju, H; Sugasaki, N; Takemoto, S; Yamaguchi, H, 2016
)
0.43
"709, and the median elimination half-life was 15."( Pharmacokinetic parameters of gefitinib predict efficacy and toxicity in patients with advanced non-small cell lung cancer harboring EGFR mutations.
Fukuda, M; Ikeda, T; Ikegami, Y; Izumikawa, K; Mizoguchi, K; Motoshima, K; Mukae, H; Nakamura, Y; Nakatomi, K; Ogawara, D; Sano, K; Sato, S; Senju, H; Sugasaki, N; Takemoto, S; Yamaguchi, H, 2016
)
0.43
" On the other hand, long elimination half-life was related to high-grade adverse events in these patients."( Pharmacokinetic parameters of gefitinib predict efficacy and toxicity in patients with advanced non-small cell lung cancer harboring EGFR mutations.
Fukuda, M; Ikeda, T; Ikegami, Y; Izumikawa, K; Mizoguchi, K; Motoshima, K; Mukae, H; Nakamura, Y; Nakatomi, K; Ogawara, D; Sano, K; Sato, S; Senju, H; Sugasaki, N; Takemoto, S; Yamaguchi, H, 2016
)
0.43
" In this review, we have comprehensively summarized the pharmacokinetic characteristics of gefitinib: absorption, distribution, metabolism and excretion (ADME)."( Pharmacokinetics of Gefitinib: Roles of Drug Metabolizing Enzymes and Transporters.
Han, SY; Li, PP; Zhao, C, 2017
)
0.46
" Studies in healthy volunteers and patients with advanced solid tumours have shown that once-daily afatinib has time-independent pharmacokinetic characteristics."( Clinical Pharmacokinetics and Pharmacodynamics of Afatinib.
Ebner, T; Freiwald, M; Schnell, D; Stopfer, P; Wind, S, 2017
)
0.46
" Favorable antitumor activity and pharmacokinetic profile were observed in patients with heavily pretreated, advanced NSCLC."( A Phase I Study of the Safety and Pharmacokinetics of Higher-Dose Icotinib in Patients With Advanced Non-Small Cell Lung Cancer.
Chen, J; Ding, L; Hu, X; Liu, J; Shentu, J; Tan, F; Wang, Y; Wu, G; Wu, L; Xu, W; Zhou, H; Zhu, M, 2016
)
0.43
" Our objective was to simulate DDIs between the antineoplastics erlotinib and gefitinib with key antiretroviral drugs and to predict dose adjustments using a physiologically based pharmacokinetic (PBPK) model."( Use of a physiologically based pharmacokinetic model to simulate drug-drug interactions between antineoplastic and antiretroviral drugs.
Back, D; Clotet, B; Miranda, C; Moltó, J; Owen, A; Rajoli, R; Siccardi, M; Valle, M, 2017
)
0.46
"In vitro data describing chemical properties and pharmacokinetic processes of each drug and their effect on cytochrome P450 isoforms were obtained from the literature."( Use of a physiologically based pharmacokinetic model to simulate drug-drug interactions between antineoplastic and antiretroviral drugs.
Back, D; Clotet, B; Miranda, C; Moltó, J; Owen, A; Rajoli, R; Siccardi, M; Valle, M, 2017
)
0.46
"A population pharmacokinetic (PK) model was developed for cediranib to simulate cediranib exposure for different doses, including comedication with strong uridine glucuronosyl transferase/P-glycoprotein inducers such as rifampicin, in cancer patients."( Population pharmacokinetic and exposure simulation analysis for cediranib (AZD2171) in pooled Phase I/II studies in patients with cancer.
Al-Huniti, N; Henningsson, A; Li, J; Masson, E; Tang, W, 2017
)
0.46
" Since green tea polyphenols (GTP) are known to be inhibitors of receptor tyrosine kinases, GTE could likely potentiate the anticancer effect of TKIs, but with a possibility of pharmacokinetic (PK) interaction with co-administered TKIs."( UPLC-ESI-MS/MS study of the effect of green tea extract on the oral bioavailability of erlotinib and lapatinib in rats: Potential risk of pharmacokinetic interaction.
Abahussain, AO; Alzoman, NZ; Maher, HM; Shehata, SM, 2017
)
0.46
" The simple and sensitive LC-MS/MS method was successfully applied to the pharmacokinetic and brain distribution studies following an oral administration of AZD3759 to rats."( Determination of AZD3759 in rat plasma and brain tissue by LC-MS/MS and its application in pharmacokinetic and brain distribution studies.
Deng, Z; Mu, Y; Sun, P; Xiong, S; Xue, M; Zhou, R, 2017
)
0.46
" Copanlisib was rapidly distributed throughout the body with a volume distribution of 1870 L and an elimination half-life of 52."( Pharmacokinetics of intravenous pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor [
Genvresse, I; Gerisch, M; Granvil, C; Lang, D; Reif, S; Reschke, S; Rohde, G; Schwarz, T; van der Mey, D, 2017
)
0.46
"Phase 1, open-label, parallel-group pharmacokinetic and safety comparison of multiple once-daily oral letermovir in female subjects with hepatic impairment and healthy matched controls."( Pharmacokinetics and safety of the anti-human cytomegalovirus drug letermovir in subjects with hepatic impairment.
Erb-Zohar, K; Kobalava, ZD; Kropeit, D; McCormick, D; Moiseev, VS; Rübsamen-Schaeff, H; Stobernack, HP; Zimmermann, H, 2017
)
0.46
" This method was successfully applied to a pharmacokinetic study of volitinib and gefitinib after the administration of an intravenous or oral dose, indicating that the developed assay can be used to simultaneously determine the concentrations of volitinib and gefitinib in rat plasma."( Simultaneous quantification of volitinib and gefitinib in rat plasma by HPLC-MS/MS for application to a pharmacokinetic study in rats.
Chung, SJ; Kim, MS; Lee, JH; Maeng, HJ; Noh, CK, 2017
)
0.46
" The effects of HYT on pharmacokinetics of the two drugs were estimated by non-compartmental analysis and pharmacokinetic modeling."( Alterations in Pharmacokinetics of Gemcitabine and Erlotinib by Concurrent Administration of Hyangsayukgunja-Tang, a Gastroprotective Herbal Medicine.
Bulitta, JB; Jeong, SW; Joo, SH; Kim, S; Kim, TH; Kwon, DR; Lee, DY; Ma, E; Park, GY; Shin, BS; Shin, S; Weon, KY; Yoo, SD, 2017
)
0.46
" To date, systematic studies on the pharmacokinetic drug-drug interaction of icotinib were limited."( Metabolic Pathway of Icotinib In Vitro: The Differential Roles of CYP3A4, CYP3A5, and CYP1A2 on Potential Pharmacokinetic Drug-Drug Interaction.
Li, Z; Lu, C; Ma, L; Wang, J; Zhang, K; Zhang, T; Zhang, Y; Zhu, M; Zhuang, X, 2018
)
0.48
"To evaluate the potential pharmacokinetic interactions of the anticancer agent gefitinib (Iressa®) and the oriental medications Guipi Decoction (, GPD, Guibi-tang in Korean) and Bawu Decoction (, BWD, Palmul-tang in Korean)."( Alterations of Gefitinib Pharmacokinetics by Co-administration of Herbal Medications in Rats.
Jeong, SW; Joo, SH; Kim, MG; Kim, TH; Ma, E; Shin, BS; Shin, S; Weon, KY; Yoo, SD; Youn, YS, 2018
)
0.48
"Diabetes mellitus (DM) is a complex metabolic disorder which affects the function of numerous tissues and alters the pharmacokinetic parameters of many drugs."( A pharmacokinetic study on lapatinib in type 2 diabetic rats.
Grabowski, T; Grześkowiak, E; Karbownik, A; Klupczynska, A; Kokot, ZJ; Moch, M; Plewa, S; Sobańska, K; Szałek, E; Wolc, A, 2018
)
0.48
" In both trials, blood samples were collected for the assessment of the pharmacokinetic profiles of the antifungals, and safety was assessed."( Pharmacokinetics and Tolerability of Letermovir Coadministered With Azole Antifungals (Posaconazole or Voriconazole) in Healthy Subjects.
Butterton, JR; Cho, CR; de Haes, JIU; Drexel, M; Hulskotte, EGJ; Hussaini, A; Iwamoto, M; Jordan, HR; Kantesaria, BS; Liu, F; Macha, S; Marshall, WL; McCrea, JB; Menzel, K; Tsai, C; van Schanke, A, 2018
)
0.48
" Levels of pharmacodynamic plasma markers were not consistently changed after XL647 and no conclusions could be drawn with this limited data set."( A safety, tolerability, and pharmacokinetic analysis of two phase I studies of multitargeted small molecule tyrosine kinase inhibitor XL647 with an intermittent and continuous dosing schedule in patients with advanced solid malignancies.
Adjei, A; Das, M; Frymoyer, A; Lensing, JL; Miles, D; Molina, J; Padda, SK; Sikic, BI; Wakelee, HA, 2018
)
0.48
" However, the metabolic profiling and in vivo pharmacokinetic characteristics of DVAS still remain unknown."( In vivo and in vitro metabolism and pharmacokinetics of cholinesterase inhibitor deoxyvasicine from aerial parts of Peganum harmala Linn in rats via UPLC-ESI-QTOF-MS and UPLC-ESI-MS/MS.
Cao, N; Cheng, X; Deng, G; Ding, W; Guan, H; Liu, W; Ma, C; Rong, X; Wang, C; Wang, Y; Wu, C; Zhang, Y, 2019
)
0.51
"The aim of this present study was to investigate the metabolism and pharmacokinetic properties of DVAS in rats by using ultra-performance liquid chromatography combined with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-QTOF-MS) and ultra-performance liquid chromatography-tandem mass spectrometry (UPLC-ESI-MS/MS) method."( In vivo and in vitro metabolism and pharmacokinetics of cholinesterase inhibitor deoxyvasicine from aerial parts of Peganum harmala Linn in rats via UPLC-ESI-QTOF-MS and UPLC-ESI-MS/MS.
Cao, N; Cheng, X; Deng, G; Ding, W; Guan, H; Liu, W; Ma, C; Rong, X; Wang, C; Wang, Y; Wu, C; Zhang, Y, 2019
)
0.51
" For pharmacokinetic studies, 32 Sprague-Dawley rats were randomly divided into four groups, namely, intravenous dosage group (2 mg/kg DVAS) and three oral dosage groups (5, 15, and 45 mg/kg DVAS)."( In vivo and in vitro metabolism and pharmacokinetics of cholinesterase inhibitor deoxyvasicine from aerial parts of Peganum harmala Linn in rats via UPLC-ESI-QTOF-MS and UPLC-ESI-MS/MS.
Cao, N; Cheng, X; Deng, G; Ding, W; Guan, H; Liu, W; Ma, C; Rong, X; Wang, C; Wang, Y; Wu, C; Zhang, Y, 2019
)
0.51
" The goodness-of-fit plots and visual predictive checks suggested that the proposed pharmacokinetic model agreed well with the observations."( Hepatic Artery and Peripheral Vein Pharmacokinetics of Raltitrexed in Swine After the Administration of a Hepatic Arterial Infusion.
Li, X; Zhang, X; Zheng, N; Zhu, L, 2019
)
0.51
"The pharmacokinetic model could be helpful in quantitatively describing the detailed processes of raltitrexed activity administered by HAI and determining an appropriate dosing regimen for preclinical and clinical studies."( Hepatic Artery and Peripheral Vein Pharmacokinetics of Raltitrexed in Swine After the Administration of a Hepatic Arterial Infusion.
Li, X; Zhang, X; Zheng, N; Zhu, L, 2019
)
0.51
" The objective of the study was to investigate the tolerability and effect of high-fat food on the pharmacokinetic profile of a fruquintinib capsule in healthy Chinese subjects."( Effects of a High-fat Meal on the Pharmacokinetics of the VEGFR Inhibitor Fruquintinib: A Randomized Phase I Study in Healthy Subjects.
Chen, Q; Fan, S; Jia, J; Li, K; Li, T; Liu, Y; Qian, H; Sai, Y; Su, W; Wang, W; Yu, C, 2019
)
0.51
" Blood samples for pharmacokinetic analysis were collected at the designated time points."( Effects of a High-fat Meal on the Pharmacokinetics of the VEGFR Inhibitor Fruquintinib: A Randomized Phase I Study in Healthy Subjects.
Chen, Q; Fan, S; Jia, J; Li, K; Li, T; Liu, Y; Qian, H; Sai, Y; Su, W; Wang, W; Yu, C, 2019
)
0.51
" The analytical method had been validated and applied to a pharmacokinetic study of fruquintinib in rat."( Validated UPLC-MS/MS method for quantification of fruquintinib in rat plasma and its application to pharmacokinetic study.
Guo, J; Luo, SB; Mei, YB; Qiu, XJ; Xie, SL; Ye, LY; Zhang, Q, 2019
)
0.51
" The purpose of the present study was to explain the nonlinear pharmacokinetic profiles using a physiologically based pharmacokinetic (PBPK) model with saturable binding of linagliptin to soluble and membrane-bound DPP-4 in blood and organs including kidneys."( Physiologically Based Pharmacokinetic Model of the DPP-4 Inhibitor Linagliptin to Describe its Nonlinear Pharmacokinetics in Humans.
Chiba, K; Kato, Y; Sarashina, A; Tatami, S, 2020
)
0.56
"5 h, with a mean elimination half-life between 13."( First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects.
Cao, Y; Gong, LY; Guo, CX; Hua, Y; Huang, J; Kuang, Y; Pei, Q; Wang, MN; Yang, GP, 2020
)
0.56
" In pharmacokinetics assay, 23g showed a significant improvement of pharmacokinetic profile for oral administration."( Design, synthesis and biological evaluation of novel HDAC inhibitors with improved pharmacokinetic profile in breast cancer.
He, Z; Huang, J; Jiang, J; Li, C; Wang, J; Yao, D; Zhang, J, 2020
)
0.56
" Two-stage population pharmacokinetic (PK) modeling of letermovir was conducted to support dose rationale and evaluate the impact of intrinsic/extrinsic factors."( Population pharmacokinetics of letermovir following oral and intravenous administration in healthy participants and allogeneic hematopoietic cell transplantation recipients.
Cho, CR; Davis, C; de Alwis, D; Dykstra, K; Fancourt, C; Iwamoto, M; Macha, S; Prohn, M; Sabato, P; Viberg, A; Zhang, D, 2021
)
0.62
"This research demonstrates that a drug-drug interaction between poziotinib and dacomitinib possibly exists when readministered with poziotinib; thus, clinicians should pay attention to the resulting changes in pharmacokinetic parameters and accordingly, adjust the dose of poziotinib in clinical settings."( Effects of dacomitinib on the pharmacokinetics of poziotinib
Chen, F; Dai, D; Ji, W; Meng, D; Shen, J; Wang, B; Wang, C; Wang, S; Zhou, Q; Zhou, Y, 2021
)
0.62
" Such changes in Ctrough,ss warrant further investigation and highlight the ability of pharmacokinetic modelling to investigate populations that may be difficult to recruit for traditional clinical studies."( The Pharmacokinetics of Gefitinib in a Chinese Cancer Population Group: A Virtual Clinical Trials Population Study.
Singh Badhan, RK; Yu, H, 2021
)
0.62
"The aim of this study was to identify factors affecting blood concentrations of voriconazole following letermovir coadministration using population pharmacokinetic (PPK) analysis in allogeneic hematopoietic stem cell transplant (allo-HSCT) recipients."( Effects of Letermovir and/or Methylprednisolone Coadministration on Voriconazole Pharmacokinetics in Hematopoietic Stem Cell Transplantation: A Population Pharmacokinetic Study.
Akashi, K; Egashira, N; Fukumoto, J; Hirota, T; Ieiri, I; Matsukane, R; Miyamoto, T; Mori, Y; Muraki, S; Suetsugu, K, 2021
)
0.62
" The presence of steady-state letermovir reduced digoxin area under the plasma concentration-time curve from administration until last quantifiable measurement by 12% and maximum plasma concentration by 22% compared with digoxin alone; digoxin half-life and elimination rate remained similar in both conditions."( The Effect of Oral Letermovir Administration on the Pharmacokinetics of a Single Oral Dose of P-Glycoprotein Substrate Digoxin in Healthy Volunteers.
Erb-Zohar, K; Kropeit, D; McCormick, D; Rübsamen-Schaeff, H; Scheuenpflug, J; Stobernack, HP; Theis, JGW; Zimmermann, H, 2022
)
0.72
" Following administration of oral single and multiple doses, letermovir was absorbed with a median time to maximum plasma concentration of 2 to 4 hours, and concentrations declined in a biphasic manner with a terminal half-life of ≈10 to 13 hours."( Pharmacokinetics, Safety, and Tolerability of Letermovir Following Single- and Multiple-Dose Administration in Healthy Japanese Subjects.
Asari, K; Fancourt, C; Furihata, K; Ishii, M; Iwamoto, M; McCrea, JB; Stoch, SA; Wakana, A; Yoon, E; Yoshitsugu, H, 2022
)
0.72
" Safety was monitored throughout the study, and plasma copanlisib levels were measured for pharmacokinetic analysis."( A phase I pharmacokinetic study of copanlisib in Chinese patients with relapsed indolent non-Hodgkin lymphoma.
Childs, BH; Cisternas, G; Du, T; Garcia-Vargas, J; Huang, F; Liu, W; Mehra, A; Niu, Y; Ping, L; Reschke, S; Song, Y; Sun, Y; Wang, X; Xie, Y; Zhu, J, 2022
)
0.72
"Data describing the magnitude of the pharmacokinetic interaction between letermovir and tacrolimus in allogeneic hematopoietic cell transplantation (allo-HCT) recipients are limited, and varying outcomes have been reported."( Evaluation of the Pharmacokinetic Interaction Between Letermovir and Tacrolimus in Allogeneic Hematopoietic Cell Transplantation Recipients.
Cumpston, A; Dillaman, M; Marciano, KA; Ross, KG; Seago, K; Veltri, L, 2022
)
0.72
" The proposed LC-MS/MS method was applied to pharmacokinetic studies of lapatinib, with or without TPF-T, in rabbit and rat plasma."( Dose-sparing effect of lapatinib co-administered with a high-fat enteral nutrition emulsion: preclinical pharmacokinetic study.
Ding, H; Fang, L; Kong, S; Song, Y; Tong, Y; Xu, G; Yang, D; Zhu, J, 2023
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
" In 25 patients only prazosin was used and in 20 patients prazosin was combined with a thiazide diuretic."( Prazosin alone and combined with a thiazide diuretic in the treatment of hypertension.
Bhoola, R; Seedat, MA; Seedat, YK, 1977
)
0.26
"The use of prazosin, a new antihypertensive agent, in combination with other conventional antihypertensive agents, in a hospital outpatient clinic setting, was studied in a mixed group of 104 hypertensive patients."( Studies with prazosin--a new effective hypotensive agent. I. Open clinical study of prazosin in combination with other antihypertensive agents.
Hua, AS; Kincaid-Smith, P; Macdonald, IM; Myers, JB, 1976
)
0.26
" Thus, TMTX can be given with 5-FU (400 mg/m2) on a daily x 5-day bolus schedule at the 12 mg/m2 per day dose level, which was the recommended dose of TMTX as a single agent for phase II studies using the 5-day bolus schedule."( Phase I clinical and pharmacologic trial of trimetrexate in combination with 5-fluorouracil.
Catalano, R; Comis, RL; DeLap, RJ; Grillo-Lopez, AJ; Hudes, GR; LaCreta, F, 1989
)
0.28
"The presence of low concentrations of the lipophilic dihydrofolate reductase inhibitors metoprine or trimetrexate, which cause little inhibition in the growth of cultured hepatoma cells in combination with weakly inhibiting concentrations of 5,10-dideazatetrahydrofolate, exhibit greater activity than would be predicted by the activity of the individual components."( Antifolate drug interactions: enhancement of growth inhibition due to the antipurine 5,10-dideazatetrahydrofolic acid by the lipophilic dihydrofolate reductase inhibitors metoprine and trimetrexate.
Boschelli, D; Galivan, J; Kerwar, SS; Nimec, Z; Oronsky, AL; Rhee, M, 1988
)
0.27
"3 microM dThd was sufficient to completely protect sensitive cells from 5-fluoro-2'-deoxyuridine, and 5,8-dideazaisofolic acid at concentrations that produced over 80% lethality in unprotected cells and the same concentration of dThd in combination with 100 microM hypoxanthine fully protected sensitive cells from greater than 99% methotrexate-induced cell lethality."( Highly selective drug combinations for human colon cancer cells resistant in vitro to 5-fluoro-2'-deoxyuridine.
Bertino, JR; Handschumacher, RE; Sobrero, AF, 1985
)
0.27
" Since IAHQ has only modest activity against L1210 leukemia in mice, it was tested in combination with methotrexate (MTX), probenecid, or verapamil in an effort to enhance efficacy."( Effects of 5,8-dideazaisopteroylglutamate (IAHQ) on L1210 leukemia in mice when given alone and in combination with methotrexate, probenecid, or verapamil.
Gale, GR; Hynes, JB; Smith, AB, 1986
)
0.27
" Neither prazosin nor nadolol in combination with thiazide had significant additional adverse effects on total body potassium."( A comparison of prazosin versus nadolol in combination with a diuretic.
Kraut, J; Okun, R, 1984
)
0.27
"The potential of raltitrexed (Tomudex) in combination with 5-fluorouracil (5-FU) as treatment for advanced colorectal cancer has been investigated in two phase I clinical trials."( Raltitrexed (Tomudex) in combination with 5-fluorouracil for the treatment of patients with advanced colorectal cancer: preliminary results from phase I clinical trials.
González Barón, M; Harstrick, A; Schwartz, GK, 1999
)
0.3
" Preclinical studies have shown additive to synergistic effects when ZD1839 is combined with radiation or chemotherapy in colon, head and neck, and non-small cell lung cancers."( ZD1839, a selective epidermal growth factor receptor tyrosine kinase inhibitor, alone and in combination with radiation and chemotherapy as a new therapeutic strategy in non-small cell lung cancer.
Bunn, PA; Chan, D; Helfrich, BA; Johnson, G; Raben, D, 2002
)
0.31
" In this study, we evaluated the ability of CU201 to produce additive or synergistic growth inhibition in combination with various antitumor agents used in lung cancer therapy."( Bradykinin antagonist dimer, CU201, inhibits the growth of human lung cancer cell lines in vitro and in vivo and produces synergistic growth inhibition in combination with other antitumor agents.
Bunn, PA; Chan, DC; Chan, KK; Covey, JM; Feng, WY; Gera, L; Helfrich, B; Stewart, JM; Zhao, TL, 2002
)
0.31
"To determine the maximum tolerated dose (MTD) of raltitrexed when given with irinotecan and to evaluate the pharmacokinetics of these two agents when given in combination."( Phase I and pharmacokinetic study of irinotecan in combination with raltitrexed.
Adams, AL; Brady, D; Engstrom, PF; Gallo, JM; Kilpatrick, D; Lewis, NL; Litwin, S; Meropol, NJ; Scher, R; Szarka, CE; Weiner, LM, 2002
)
0.31
" The use of irinotecan together with raltitrexed is also being investigated, as is its combination with oxaliplatin."( Irinotecan in metastatic colorectal cancer: dose intensification and combination with new agents, including biological response modifiers.
Ducreux, M; Köhne, CH; Schwartz, GK; Vanhoefer, U, 2003
)
0.32
"Clinical trials of gefitinib (Iressa, ZD1839) in combination with cytotoxic agents have been carried out or are ongoing in several varieties of tumor."( The effect of gefitinib (Iressa, ZD1839) in combination with oxaliplatin is schedule-dependent in colon cancer cell lines.
Azzariti, A; Colucci, G; Paradiso, A; Xu, JM, 2003
)
0.32
" We report results from two open-label, multicentre, phase I and phase II trials, investigating the pharmacokinetics, tolerability and efficacy of ZD9331, when used in combination with topotecan in patients with relapsed or refractory tumours."( ZD9331 in combination with topotecan: phase I and II experience.
Benson, A; Poplin, E; Vergote, I, 2003
)
0.32
"ZD9331, in combination with topotecan, showed manageable toxicity and some evidence of activity in patients with ovarian cancer."( ZD9331 in combination with topotecan: phase I and II experience.
Benson, A; Poplin, E; Vergote, I, 2003
)
0.32
" Based on the expectation that this drug combined with immunotherapy would be highly effective, we recently conducted an experiment in tumor-bearing mice."( [Significance of gefitinib combined with immunotherapy in tumor-bearing mice].
Maruyama, S; Sukegawa, Y; Yagita, A, 2003
)
0.32
" In preclinical studies, gefitinib has shown additive and even supra-additive antitumor effects when combined with different cytotoxic agents."( Pharmacokinetic evaluation of gefitinib when administered with chemotherapy.
Hammond, LA, 2003
)
0.32
"To determine the maximum tolerated dose and dose-limiting toxicities (DLTs) of ZD9331 in combination with cisplatin in patients with refractory solid tumors and to describe any preliminary antitumor activity associated with this regimen."( Phase I trial of the antifolate ZD9331 in combination with cisplatin in patients with refractory solid malignancies.
Algazy, K; Bilenker, JH; Flaherty, KT; Garcia-Vargas, JE; Giantonio, BJ; Haller, DG; Koehler, M; McLaughlin, K; O'Dwyer, PJ; Stevenson, JP, 2004
)
0.32
"ZD9331 in combination with cisplatin was well tolerated at a dose of 130/50 mg/m(2) after establishing the principal DLTs of neutropenia and thrombocytopenia."( Phase I trial of the antifolate ZD9331 in combination with cisplatin in patients with refractory solid malignancies.
Algazy, K; Bilenker, JH; Flaherty, KT; Garcia-Vargas, JE; Giantonio, BJ; Haller, DG; Koehler, M; McLaughlin, K; O'Dwyer, PJ; Stevenson, JP, 2004
)
0.32
"Raltitrexed may up-regulate DPD activity in tumor cells, resulting in antagonism when combined with 5-FU."( Up-regulation in dihydropyrimidine dehydrogenase activity by raltitrexed causes antagonism in combination with 5-fluorouracil.
Araki, Y; Fukumori, H; Nozoe, Y; Ogata, Y; Sasatomi, T; Shirouzu, K,
)
0.13
" Gefitinib has demonstrated encouraging efficacy in advanced NSCLC in phase II trials in pretreated patients, and a phase I trial of gefitinib in combination with gemcitabine and cisplatin showed favorable tolerability."( Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1.
Averbuch, SD; Fandi, A; Gatzemeier, U; Giaccone, G; Grous, J; Herbst, RS; Johnson, DH; Manegold, C; Miller, V; Natale, RB; Ochs, JS; Pluzanska, A; Rennie, P; Rosell, R; Scagliotti, G; Schiller, JH; Von Pawel, J; Wolf, MK, 2004
)
0.32
"Gefitinib in combination with gemcitabine and cisplatin in chemotherapy-naive patients with advanced NSCLC did not have improved efficacy over gemcitabine and cisplatin alone."( Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1.
Averbuch, SD; Fandi, A; Gatzemeier, U; Giaccone, G; Grous, J; Herbst, RS; Johnson, DH; Manegold, C; Miller, V; Natale, RB; Ochs, JS; Pluzanska, A; Rennie, P; Rosell, R; Scagliotti, G; Schiller, JH; Von Pawel, J; Wolf, MK, 2004
)
0.32
"Preclinical studies indicate that gefitinib (Iressa, ZD1839; AstraZeneca, Wilmington, DE), an orally active epidermal growth factor receptor tyrosine kinase inhibitor, may enhance antitumor efficacy of cytotoxics, and combination with paclitaxel and carboplatin had acceptable tolerability in a phase I trial."( Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 2.
Averbuch, SD; Fandi, A; Giaccone, G; Grous, J; Herbst, RS; Johnson, DH; Krebs, AD; Manegold, C; Miller, V; Natale, RB; Ochs, JS; Oliff, I; Reeves, JA; Rosell, R; Scagliotti, G; Schiller, JH; Wolf, MK, 2004
)
0.32
" Expected dose-related diarrhea and skin toxicity were observed in gefitinib-treated patients, with no new significant/unexpected safety findings from combination with chemotherapy."( Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 2.
Averbuch, SD; Fandi, A; Giaccone, G; Grous, J; Herbst, RS; Johnson, DH; Krebs, AD; Manegold, C; Miller, V; Natale, RB; Ochs, JS; Oliff, I; Reeves, JA; Rosell, R; Scagliotti, G; Schiller, JH; Wolf, MK, 2004
)
0.32
"Although in vivo efficacy studies in two HER-2/neu overexpressing breast xenograft models showed that the combination of trastuzumab and gefitinib was effective, analyses of various cellular parameters failed to reveal beneficial effects and argue that this drug combination may not be favorable."( Treatment of HER-2/neu overexpressing breast cancer xenograft models with trastuzumab (Herceptin) and gefitinib (ZD1839): drug combination effects on tumor growth, HER-2/neu and epidermal growth factor receptor expression, and viable hypoxic cell fraction
Bally, MB; Chia, S; Denyssevych, T; Dragowska, WH; Gelmon, K; Masin, D; Wallis, AE; Warburton, C; Yan, H, 2004
)
0.32
" The different drug combination schedules were tested in various concentrations by using equiactive concentrations of the two drugs."( The schedule-dependent enhanced cytotoxic activity of 7-ethyl-10-hydroxy-camptothecin (SN-38) in combination with Gefitinib (Iressa, ZD1839).
Azzariti, A; Paradiso, A; Porcelli, L; Xu, JM, 2004
)
0.32
" ZD6126 caused marked vessel destruction through loss of endothelial cells and thrombosis, substantially increasing the level of necrosis seen when combined with radiation therapy."( Antitumor activity of ZD6126, a novel vascular-targeting agent, is enhanced when combined with ZD1839, an epidermal growth factor receptor tyrosine kinase inhibitor, and potentiates the effects of radiation in a human non-small cell lung cancer xenograft
Bianco, AR; Bianco, C; Bianco, R; Bunn, P; Ciardiello, F; Cionini, L; D'Armiento, FP; Damiano, V; Melisi, D; Mignogna, C; Raben, D; Tortora, G, 2004
)
0.32
"In this study we have used a standardised ATP-based tumour chemosensitivity assay (ATP-TCA) to measure the activity of gefitinib alone or in combination with different cytotoxic drugs (cisplatin, gemcitabine, oxaliplatin and treosulfan) against a variety of solid tumours (n = 86), including breast, colorectal, oesophageal and ovarian cancer, carcinoma of unknown primary site, cutaneous and uveal melanoma, non-small cell lung cancer (NSCLC) and sarcoma."( The in vitro effect of gefitinib ('Iressa') alone and in combination with cytotoxic chemotherapy on human solid tumours.
Cree, IA; Di Nicolantonio, F; Glaysher, S; Johnson, P; Knight, LA; Mercer, S; Sharma, S; Whitehouse, P, 2004
)
0.32
" Interestingly, gefitinib had both positive and negative effects when used in combination with different cytotoxics."( The in vitro effect of gefitinib ('Iressa') alone and in combination with cytotoxic chemotherapy on human solid tumours.
Cree, IA; Di Nicolantonio, F; Glaysher, S; Johnson, P; Knight, LA; Mercer, S; Sharma, S; Whitehouse, P, 2004
)
0.32
"To establish the recommended dose (RD) of the thymidylate-synthase inhibitor ZD9331 administered with irinotecan (CPT-11) in patients with pretreated metastatic colorectal cancer, and to assess toxicity profile, pharmacokinetics (PK), and anti-tumor activity in a phase I/II open, multicenter, intrapatient chemotherapy dose escalating trial."( A phase I-II, dose-escalating trial of ZD9331 in combination with irinotecan (CPT11) in previously pretreated metastatic colorectal cancer patients.
André, T; de Gramont, A; Gamelin, E; Garcia, ML; Kalla, S; Lenaers, G; Louvet, C; Méry-Mignard, D; Saavedra, A, 2004
)
0.32
"ZD9331 90 mg/m2 combined with CPT-11 180 mg/m2 may be a viable option for treatment of metastatic colorectal cancer, with possible escalation to 120 mg/m2 of ZD9331 according to safety evaluation."( A phase I-II, dose-escalating trial of ZD9331 in combination with irinotecan (CPT11) in previously pretreated metastatic colorectal cancer patients.
André, T; de Gramont, A; Gamelin, E; Garcia, ML; Kalla, S; Lenaers, G; Louvet, C; Méry-Mignard, D; Saavedra, A, 2004
)
0.32
"5-Fluorouracil (5-FU) and capecitabine alone and in combination with irinotecan/oxaliplatin are clinically active in the treatment of colorectal and other solid tumors."( Synergistic antitumor activity of capecitabine in combination with irinotecan.
Cao, S; Durrani, FA; Rustum, YM, 2005
)
0.33
" We investigated the activity of ZD6474 in combination with SC-236, a selective COX-2 inhibitor, to determine the antitumor activity of the simultaneous blockade of EGFR, COX-2, and VEGF functions."( Antitumor activity of ZD6474, a vascular endothelial growth factor-2 and epidermal growth factor receptor small molecule tyrosine kinase inhibitor, in combination with SC-236, a cyclooxygenase-2 inhibitor.
Bianco, R; Bianco, RA; Ciardiello, F; De Vita, F; Fontanini, G; Martinelli, E; Morgillo, F; Romano, M; Tortora, G; Troiani, T; Tuccillo, C, 2005
)
0.33
"To investigate the inhibitory effect of gefitinib combined with cytotoxic agent cisplatin (CDDP) on hepatocellular carcinoma (HCC)."( Antitumor effect of Gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, combined with cytotoxic agent on murine hepatocellular carcinoma.
Li, X; Li, Y; Lu, QY; Yuan, SJ; Zhao, QC; Zhu, BD, 2005
)
0.33
"2 mg/kg BW; d1-5, or d6-10), Gefitinib (d1-5, or d6-10, or d1-10), and Gefitinib combined with CDDP groups."( Antitumor effect of Gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, combined with cytotoxic agent on murine hepatocellular carcinoma.
Li, X; Li, Y; Lu, QY; Yuan, SJ; Zhao, QC; Zhu, BD, 2005
)
0.33
" The highest inhibitory effect (IR: 56%) on HCC growth was observed in Gefitinib (d1-10) combined with CDDP (d1-5) group."( Antitumor effect of Gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, combined with cytotoxic agent on murine hepatocellular carcinoma.
Li, X; Li, Y; Lu, QY; Yuan, SJ; Zhao, QC; Zhu, BD, 2005
)
0.33
"The aim of this study was to determine the effect of ZD1839 on growth and apoptosis in SCC-15 (a human head and neck cancer cell line) lone, or in combination with cisplatin."( The effect of ZD1839 (Iressa), an epidermal growth factor receptor tyrosine kinase inhibitor, in combination with cisplatin, on apoptosis in SCC-15 cells.
Al-Hazzaa, A; Birchall, MA; Bowen, ID; Randerson, P, 2005
)
0.33
" This open-label pilot trial investigated the safety, pharmacokinetics, and efficacy of 2 doses of gefitinib (250 and 500 mg per day) combined with docetaxel (75 mg/m2) in patients with locally advanced or metastatic NSCLC as first- and second-line chemotherapy."( A pilot trial of gefitinib in combination with docetaxel in patients with locally advanced or metastatic non-small-cell lung cancer.
Buchholz, E; Fandi, A; Gatzemeier, U; Manegold, C; Smith, RP, 2005
)
0.33
"One of the emerging problems concerning the use of antiangiogenic drugs, when used in combination with certain chemotherapy regimens, is enhanced rates and severity of adverse clotting events."( In vitro procoagulant activity induced in endothelial cells by chemotherapy and antiangiogenic drug combinations: modulation by lower-dose chemotherapy.
du Manoir, J; Francia, G; Hicklin, DJ; Kerbel, RS; Ma, L; Rak, J; Viloria-Petit, A, 2005
)
0.33
" In this study, we investigated the anticancer activity of BGC9331 either alone or combined with 5-fluorouracil (5-FU), MTA (multi-target antifolate), oxali-platin and SN-38, the active metabolite of the topoisomerase I inhibitor CPT-11."( Increased anticancer activity of the thymidylate synthase inhibitor BGC9331 combined with the topoisomerase I inhibitor SN-38 in human colorectal and breast cancer cells: induction of apoptosis and ROCK cleavage through caspase-3-dependent and -independen
André, T; Coudray, AM; De Gramont, A; Faivre, S; Gespach, C; Kornprobst, M; Larsen, AK; Louvet, C; Raymond, E; Tournigand, C, 2005
)
0.33
" Erlotinib was combined with chemotherapy to determine if it could improve the outcome of patients with NSCLC."( TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer.
Fehrenbacher, L; Herbst, RS; Hermann, R; Johnson, BE; Johnson, DH; Klein, P; Kris, MG; Li, X; Miller, VA; Prager, D; Ramies, D; Sandler, A; Tran, HT, 2005
)
0.33
"TRIBUTE randomly assigned patients with good performance status and previously untreated advanced (stage IIIB/IV) NSCLC to erlotinib 150 mg/d or placebo combined with up to six cycles of carboplatin and paclitaxel, followed by maintenance monotherapy with erlotinib."( TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer.
Fehrenbacher, L; Herbst, RS; Hermann, R; Johnson, BE; Johnson, DH; Klein, P; Kris, MG; Li, X; Miller, VA; Prager, D; Ramies, D; Sandler, A; Tran, HT, 2005
)
0.33
"The recommended dose of epirubicin for phase II studies is 30 mg/m2 in combination with gefitinib at the daily dose of 250 mg."( Gefitinib (ZD1839) combined with weekly epirubicin in patients with metastatic breast cancer: a phase I study with biological correlate.
Amici, S; Gasparini, G; Gattuso, D; Gion, M; Longo, R; Sarmiento, R; Zancan, M, 2005
)
0.33
"Preclinical studies have suggested antitumor activity of an epidermal growth factor (EGF)-receptor targeted therapy with selective tyrosine kinase inhibitors alone or in combination with conventional cytostatic drugs."( Preclinical evaluation of ZD1839 alone or in combination with oxaliplatin in a panel of human tumor cell lines -- implications for clinical use.
Arnold, D; Mueller, T; Pfeiffer, C; Pickan, V; Simon, H; Voigt, W, 2005
)
0.33
"In the present study, the activity of ZD1839 alone or in combination with oxaliplatin (Eloxatin) was evaluated in 12 human cancer cell lines including colon, testicular, anaplastic thyroid and epidermoid carcinoma cells."( Preclinical evaluation of ZD1839 alone or in combination with oxaliplatin in a panel of human tumor cell lines -- implications for clinical use.
Arnold, D; Mueller, T; Pfeiffer, C; Pickan, V; Simon, H; Voigt, W, 2005
)
0.33
"Up to now, there have been no established predictive markers for response to epidermal growth factor receptor (EGFR/HER1/erbB1) inhibitors alone and in combination with chemotherapy in colorectal cancer."( Epidermal growth factor receptor activity determines response of colorectal cancer cells to gefitinib alone and in combination with chemotherapy.
Galligan, L; Johnston, P; Karaiskou-McCaul, A; Kelly, D; Longley, D; Van Cutsem, E; Van Schaeybroeck, S, 2005
)
0.33
" In contrast to oxaliplatin, 5-FU treatment increased EGFR phosphorylation in all cell lines and this correlated with synergistic decreases in cell viability when 5-FU was combined with gefitinib."( Epidermal growth factor receptor activity determines response of colorectal cancer cells to gefitinib alone and in combination with chemotherapy.
Galligan, L; Johnston, P; Karaiskou-McCaul, A; Kelly, D; Longley, D; Van Cutsem, E; Van Schaeybroeck, S, 2005
)
0.33
"In our phase II trial, CB in combination with R showed a moderate activity with safe administration on an outpatient basis."( Carboplatin in combination with raltitrexed in recurrent and metastatic head and neck squamous cell carcinoma: A multicentre phase II study of the Gruppo Oncologico Dell'Italia Meridionale (G.O.I.M.).
Borsellino, N; Colucci, G; Di Bisceglie, M; Galetta, D; Gebbia, V; Giotta, F; Manzione, L; Rosati, G,
)
0.13
" Erlotinib in combination with capecitabine was not associated with significantly increased toxicity compared with single-agent therapy."( Antitumor activity of erlotinib in combination with capecitabine in human tumor xenograft models.
Ouchi, KF; Sekiguchi, F; Tanaka, Y; Yanagisawa, M, 2006
)
0.33
" The findings of this study support clinical evaluation of erlotinib, both as a single agent and in combination with capecitabine, for the treatment of CRC and breast cancer."( Antitumor activity of erlotinib in combination with capecitabine in human tumor xenograft models.
Ouchi, KF; Sekiguchi, F; Tanaka, Y; Yanagisawa, M, 2006
)
0.33
" Therefore, drug therapy targeted to VEGF receptors and EGFRs, when combined with radiotherapy (RT), may improve tumor control and provide wider applicability."( ZD6474, an inhibitor of VEGFR and EGFR tyrosine kinase activity in combination with radiotherapy.
Bianco, C; Ciardiello, F; Dimery, I; Frederick, B; Gustafson, D; Raben, D, 2006
)
0.33
" Patients with stable or progressive malignant primary glioma received erlotinib alone or combined with temozolomide in this dose-escalation study."( Phase 1 study of erlotinib HCl alone and combined with temozolomide in patients with stable or recurrent malignant glioma.
Burton, E; Butowski, N; Chang, S; Fedoroff, A; Kapadia, A; Kelley, SK; Lamborn, KR; Malec, M; Page, MS; Prados, MD; Rabbitt, J; Xie, D, 2006
)
0.33
" We evaluated the antitumor activity of ZD1839 in combination with HSP90 antagonist, 17-AAG in malignant human glioma cell lines."( Cooperative inhibitory effect of ZD1839 (Iressa) in combination with 17-AAG on glioma cell growth.
Arnold, B; Pollack, IF; Premkumar, DR, 2006
)
0.33
" In this pilot Phase I trial, the authors evaluated the tolerability, efficacy, and pharmacokinetics of gefitinib combined with estramustine and docetaxel in patients with HRPC."( Results from a pilot Phase I trial of gefitinib combined with docetaxel and estramustine in patients with hormone-refractory prostate cancer.
Das-Gupta, A; Small, E; Soulie, P; Trump, D; Wilding, G, 2006
)
0.33
"The results of the current study demonstrated that gefitinib combined with estramustine and docetaxel had acceptable and predictable tolerability."( Results from a pilot Phase I trial of gefitinib combined with docetaxel and estramustine in patients with hormone-refractory prostate cancer.
Das-Gupta, A; Small, E; Soulie, P; Trump, D; Wilding, G, 2006
)
0.33
"We have evaluated the activity and safety of gefitinib, a small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, in combination with docetaxel as first-line treatment of women with metastatic breast cancer (MBC)."( Phase II study of gefitinib in combination with docetaxel as first-line therapy in metastatic breast cancer.
Bianco, AR; Caputo, F; Catalano, G; Ciardiello, F; Colantuoni, G; De Laurentiis, M; De Placido, S; De Vita, F; Diadema, MR; Gridelli, C; Orditura, M; Palmieri, G; Tortora, G; Troiani, T, 2006
)
0.33
"Intravenous (iv) vinorelbine and interperitoneal (ip) cisplatin were administered intermittently (q4d x 3) in combination with sorafenib administered orally (po) once daily for 9 days starting on the same day as the standard agent."( Sorafenib is efficacious and tolerated in combination with cytotoxic or cytostatic agents in preclinical models of human non-small cell lung carcinoma.
Brink, C; Carter, CA; Chen, C; Gilbert, KS; Maxuitenko, YY; Vincent, P; Waud, WR; Zhang, X, 2007
)
0.34
" Primary end points included evaluation of toxicity and determination of the OBD of celecoxib when combined with erlotinib."( A phase I trial to determine the optimal biological dose of celecoxib when combined with erlotinib in advanced non-small cell lung cancer.
Dubinett, SM; Elashoff, RM; Figlin, RA; Krysan, K; Milne, GL; Morrow, JD; Newman, RA; Reckamp, KL; Tucker, C, 2006
)
0.33
"This study defines the OBD of celecoxib when combined with a fixed dose of EGFR TKI."( A phase I trial to determine the optimal biological dose of celecoxib when combined with erlotinib in advanced non-small cell lung cancer.
Dubinett, SM; Elashoff, RM; Figlin, RA; Krysan, K; Milne, GL; Morrow, JD; Newman, RA; Reckamp, KL; Tucker, C, 2006
)
0.33
" ZD6474 in combination with oxaliplatin has synergistic antiproliferative properties in human colorectal cancer cell lines in vitro when oxaliplatin is administered before ZD6474."( Sequence-dependent inhibition of human colon cancer cell growth and of prosurvival pathways by oxaliplatin in combination with ZD6474 (Zactima), an inhibitor of VEGFR and EGFR tyrosine kinases.
Ciardiello, F; Eckhardt, SG; Lockerbie, O; Morrow, M; Troiani, T, 2006
)
0.33
" We have shown that the RTK inhibitor GW282974A (an analogue of GW2016; lapatinib) is effective in chemosensitisation of drug resistant EGFR over-expressing cells giving rise to a synergistic effect when used in combination with either cisplatin or paclitaxel in chemosensitivity assays."( Receptor tyrosine kinase (RTK) inhibition is effective in chemosensitising EGFR-expressing drug resistant human ovarian cancer cell lines when used in combination with cytotoxic agents.
Ajose-Adeogun, A; Coley, HM; Modjtahedi, H; Shotton, CF; Thomas, H, 2006
)
0.33
"To assess the feasibility of administering erlotinib, an inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, in combination with paclitaxel and carboplatin, and to identify pharmacokinetic interactions, evaluate downstream effects of EGFR inhibition on surrogate tissues, and seek preliminary evidence for clinical activity."( Phase I, pharmacokinetic, and biological study of erlotinib in combination with paclitaxel and carboplatin in patients with advanced solid tumors.
Beeram, M; Hamilton, M; Hammond, LA; Hidalgo, M; Kreisberg, JI; Mita, MM; Nadler, P; Patnaik, A; Rowinsky, EK; Schwartz, G; Tolcher, AW; Wolf, J; Wood, D, 2006
)
0.33
"A dose level of erlotinib 125 mg combined with paclitaxel 225 mg/m(2) and carboplatin AUC 6 mg."( Phase I, pharmacokinetic, and biological study of erlotinib in combination with paclitaxel and carboplatin in patients with advanced solid tumors.
Beeram, M; Hamilton, M; Hammond, LA; Hidalgo, M; Kreisberg, JI; Mita, MM; Nadler, P; Patnaik, A; Rowinsky, EK; Schwartz, G; Tolcher, AW; Wolf, J; Wood, D, 2006
)
0.33
" This phase I/II dose-finding study evaluated gefitinib in combination with a 5-fluorouracil (5-FU)/folinic acid (FA)/irinotecan (FOLFIRI-AIO) regimen in patients with metastatic colorectal cancer."( Gefitinib in combination with 5-fluorouracil (5-FU)/folinic acid and irinotecan in patients with 5-FU/oxaliplatin- refractory colorectal cancer: a phase I/II study of the Arbeitsgemeinschaft für Internistische Onkologie (AIO).
Arnold, D; Hochhaus, A; Hofheinz, RD; Kubicka, S; Wollert, J, 2006
)
0.33
"To assess the optimal regimen and its mechanism of ZD1839 in combination with SN38, the active metabolite of irinotecan (CPT-11), in the colon cancer cell lines HT-29 and LoVo."( [Experimental study of effect of epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in combination with irinotecan].
Azzariti, A; Han, Y; Li, YM; Li, ZQ; Paradiso, A; Wang, Y; Xu, JM; Yang, WW; Yuan, SJ; Zhao, CH, 2006
)
0.33
" This trial assessed the maximum tolerated dose (MTD), safety, preliminary efficacy, and pharmacokinetics of erlotinib combined with FOLFOX."( Phase 1b dose escalation study of erlotinib in combination with infusional 5-Fluorouracil, leucovorin, and oxaliplatin in patients with advanced solid tumors.
Bolling, C; Brennscheidt, U; Cassidy, J; Díaz-Rubio, E; Fettner, S; Feyereislova, A; Hanauske, AR; Jones, RJ; Rakhit, A; Sastre, J, 2007
)
0.34
" calcitriol can be administered safely in combination with gefitinib."( A phase I pharmacokinetic and pharmacodynamic study of intravenous calcitriol in combination with oral gefitinib in patients with advanced solid tumors.
Bernardi, RJ; Black, JD; Brattain, MG; Creaven, PJ; Fakih, MG; French, R; Hutson, A; Johnson, CS; Muindi, JR; Schwartz, J; Trump, DL, 2007
)
0.34
" Vandetanib has demonstrated enhanced efficacy in combination with radiation therapy (RT) in human tumor models."( Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
Frederick, B; Gustafson, DL; Merz, AL; Raben, D, 2008
)
0.35
" This phase III, randomized, double-blind, placebo-controlled, multicenter trial evaluated the efficacy and safety of erlotinib in combination with cisplatin and gemcitabine as first-line treatment for advanced non-small-cell lung cancer (NSCLC)."( Phase III study of erlotinib in combination with cisplatin and gemcitabine in advanced non-small-cell lung cancer: the Tarceva Lung Cancer Investigation Trial.
De Rosa, F; Gatzemeier, U; Janaskova, T; Karnicka-Mlodkowski, H; Kaukel, E; Manikhas, GM; Milanowski, J; Pesek, M; Pluzanska, A; Ramlau, R; Roubec, J; Serwatowski, P; Strausz, J; Szczesna, A; Vansteenkiste, J; Von Pawel, J, 2007
)
0.34
"Patients received erlotinib (150 mg/d) or placebo, combined with up to six 21-day cycles of chemotherapy (gemcitabine 1,250 mg/m2 on days 1 and 8 and cisplatin 80 mg/m2 on day 1)."( Phase III study of erlotinib in combination with cisplatin and gemcitabine in advanced non-small-cell lung cancer: the Tarceva Lung Cancer Investigation Trial.
De Rosa, F; Gatzemeier, U; Janaskova, T; Karnicka-Mlodkowski, H; Kaukel, E; Manikhas, GM; Milanowski, J; Pesek, M; Pluzanska, A; Ramlau, R; Roubec, J; Serwatowski, P; Strausz, J; Szczesna, A; Vansteenkiste, J; Von Pawel, J, 2007
)
0.34
" Potential drug-drug interactions and the relationship between pharmacokinetics and toxicity were also assessed."( Phase I trial of sorafenib in combination with gefitinib in patients with refractory or recurrent non-small cell lung cancer.
Adjei, AA; Croghan, G; Hanson, LJ; Jett, JR; Lathia, C; Mandrekar, SJ; Marks, R; Molina, JR; Reid, JR; Simantov, R; Xia, C, 2007
)
0.34
"Sorafenib combined with gefitinib is well tolerated, with promising efficacy in patients with advanced non-small cell lung cancer."( Phase I trial of sorafenib in combination with gefitinib in patients with refractory or recurrent non-small cell lung cancer.
Adjei, AA; Croghan, G; Hanson, LJ; Jett, JR; Lathia, C; Mandrekar, SJ; Marks, R; Molina, JR; Reid, JR; Simantov, R; Xia, C, 2007
)
0.34
" This phase I study evaluated the safety, tolerability and pharmacokinetics (PK) of OSI-7904L administered in combination with oxaliplatin every 21 days in patients with advanced colorectal carcinoma."( A phase I and pharmacokinetic study of OSI-7904L, a liposomal thymidylate synthase inhibitor in combination with oxaliplatin in patients with advanced colorectal cancer.
Chick, J; Clamp, AR; Debois, M; Govaerts, AS; Jayson, GC; Lacombe, D; Marreaud, S; Schöffski, P; Twelves, C; Valle, JW; Wilson, RH, 2008
)
0.35
"Gefitinib, an orally active inhibitor of epidermal growth factor receptor (EGFR) tyrosine kinase, combined with chemotherapy, has shown efficacy as second-line treatment for advanced colorectal cancer (CRC)."( First clinical experience of orally active epidermal growth factor receptor inhibitor combined with simplified FOLFOX6 as first-line treatment for metastatic colorectal cancer.
Boselli, S; de Braud, F; Lorizzo, K; Magni, E; Martignetti, A; Massacesi, C; Santoro, L; Zampino, MG; Zaniboni, A; Zorzino, L, 2007
)
0.34
"Patients with metastatic EGFR-positive CRC received gefitinib at a dose of 250 mg/day combined with simplified FOLFOX6."( First clinical experience of orally active epidermal growth factor receptor inhibitor combined with simplified FOLFOX6 as first-line treatment for metastatic colorectal cancer.
Boselli, S; de Braud, F; Lorizzo, K; Magni, E; Martignetti, A; Massacesi, C; Santoro, L; Zampino, MG; Zaniboni, A; Zorzino, L, 2007
)
0.34
" In vitro, gefitinib, an orally administered tyrosine kinase inhibitor, has shown a significant increase in antitumor activity when combined with chemotherapy."( An open-label, noncomparative phase II trial to evaluate the efficacy and safety of docetaxel in combination with gefitinib in patients with hormone-refractory metastatic prostate cancer.
Borner, M; Knuth, A; Morant, R; Pedrazzini, A; Rochlitz, C; Roggero, E; Salzberg, M; Schönenberger, A; Thalmann, G, 2007
)
0.34
"In this phase II study, the safety and efficacy of gefitinib in combination with docetaxel, a chemotherapeutic agent commonly used for prostate cancer, was investigated in patients with hormone-refractory prostate cancer (HRPC)."( An open-label, noncomparative phase II trial to evaluate the efficacy and safety of docetaxel in combination with gefitinib in patients with hormone-refractory metastatic prostate cancer.
Borner, M; Knuth, A; Morant, R; Pedrazzini, A; Rochlitz, C; Roggero, E; Salzberg, M; Schönenberger, A; Thalmann, G, 2007
)
0.34
" Our results do not support the efficacy of gefitinib in combination with endocrine treatment for hormone-refractory prostate cancer."( Gefitinib combined with endocrine manipulation in patients with hormone-refractory prostate cancer: quality of life and surrogate markers of activity.
Curigliano, G; De Braud, F; De Cobelli, O; De Pas, T; Matei, V; Noberasco, C; Nolè, F; Renne, G; Rocco, B; Scardino, E; Spitaleri, G; Teresa Sandri, M; Verweij, F; Zorzino, L, 2007
)
0.34
"This phase I study was designed to determine the optimally tolerated regimen (OTR), safety, and clinical activity of lapatinib in combination with FOLFOX4 [oxaliplatin/leucovorin/5-fluorouracil (5-FU)] in patients with solid tumors."( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors.
Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007
)
0.34
" No dose-limiting toxicities were observed and the OTR was established at 1,500 mg/d lapatinib in combination with the standard FOLFOX4 regimen."( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors.
Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007
)
0.34
"Lapatinib can be safely administered in combination with the standard FOLFOX4 regimen."( Phase I pharmacokinetic study of the safety and tolerability of lapatinib (GW572016) in combination with oxaliplatin/fluorouracil/leucovorin (FOLFOX4) in patients with solid tumors.
Beijnen, JH; Boot, H; Keessen, M; Koch, KM; Pandite, L; Richel, DJ; Schellens, JH; Siegel-Lakhai, WS; Smith, DA; Versola, M; Vervenne, WL, 2007
)
0.34
"This study determined the optimally tolerated regimen (OTR) of oral lapatinib administered in combination with infusional 5-fluorouracil (5-FU), leucovorin and irinotecan (FOLFIRI) and assessed the safety, tolerability and pharmacokinetics of the combination."( A phase I and pharmacokinetic study of lapatinib in combination with infusional 5-fluorouracil, leucovorin and irinotecan.
Flaherty, KT; Fleming, RA; Kerr, DJ; Koch, KM; Middleton, MR; Midgley, RS; O'Dwyer, PJ; Pratap, SE; Smith, DA; Stevenson, JP; Versola, M; Ward, C, 2007
)
0.34
"Bevacizumab (Bev) has clinical activity in advanced renal cell carcinoma (RCC), and, when combined with erlotinib (Erl), has shown encouraging objective response rate (ORR) and progression-free survival (PFS)."( Randomized phase II study of erlotinib combined with bevacizumab compared with bevacizumab alone in metastatic renal cell cancer.
Bukowski, RM; Drabkin, HA; Dutcher, J; Figlin, RA; Flaherty, K; Kabbinavar, FF; McDermott, D; Ryba, S; Scappaticci, FA; Srinivas, S; Vaishampayan, U; Xia, Q, 2007
)
0.34
"One hundred four patients received intravenous Bev (10 mg/kg) every 2 weeks in combination with oral Erl (150 mg) or placebo daily."( Randomized phase II study of erlotinib combined with bevacizumab compared with bevacizumab alone in metastatic renal cell cancer.
Bukowski, RM; Drabkin, HA; Dutcher, J; Figlin, RA; Flaherty, K; Kabbinavar, FF; McDermott, D; Ryba, S; Scappaticci, FA; Srinivas, S; Vaishampayan, U; Xia, Q, 2007
)
0.34
" The MTD for erlotinib in combination with twice weekly gemcitabine-based chemoradiation was 100 mg/day."( A phase I study of erlotinib in combination with gemcitabine and radiation in locally advanced, non-operable pancreatic adenocarcinoma.
Capanu, M; Duffy, A; Kelsen, DP; Kortmansky, J; Minsky, B; O'Reilly, EM; Puleio, S; Saltz, L; Schwartz, GK, 2008
)
0.35
"In combination with fixed dose gemcitabine at 40 mg/m(2) twice weekly and radiation at 180 cGy/day, the MTD of erlotinib was found to be 100 mg/day."( A phase I study of erlotinib in combination with gemcitabine and radiation in locally advanced, non-operable pancreatic adenocarcinoma.
Capanu, M; Duffy, A; Kelsen, DP; Kortmansky, J; Minsky, B; O'Reilly, EM; Puleio, S; Saltz, L; Schwartz, GK, 2008
)
0.35
" This study also demonstrates the importance of timing of gefitinib administration when this agent is combined with irradiation."( Treatment schedule is of importance when gefitinib is combined with irradiation of glioma and endothelial cells in vitro.
Andersson, U; Behnam-Motlagh, P; Johansson, D; Johansson, M; Malmer, B, 2007
)
0.34
"This in vivo study was designed to determine the optimal doses and schedules of vandetanib, a dual epidermal growth factor receptor (EGFR)-vascular endothelial growth factor receptor tyrosine kinase inhibitor, in combination with irinotecan in a murine xenograft model of human colon cancer."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
"The greatest antitumor efficacy was observed in the groups receiving the highest dose of vandetanib given continuously (concurrent schedule), alone or in combination with irinotecan."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
"These data suggest that higher, sustained concentrations of vandetanib (versus intermittent), alone and in combination with irinotecan, result in optimal antitumor efficacy in this model and may have implications for the design of future clinical studies with this drug."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
" This study was to assess the effects of ZD1839 in combination with oxaliplatin on lung adenocarcinoma cell line A549, and to provide pre-clinical evidence for optimizing the schedule of oxaliplatin combined with ZD1839."( [Cytotoxic effect of epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in combination with oxaliplatin on lung cancer cell line A549].
Ge, FJ; Luo, WD; Wang, Y; Xu, JM; Yuan, SJ; Zhao, CH, 2007
)
0.34
" The effects of oxaliplatin combined with ZD1839 on the proliferation of A549 cells in nude mice were also evaluated."( [Cytotoxic effect of epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in combination with oxaliplatin on lung cancer cell line A549].
Ge, FJ; Luo, WD; Wang, Y; Xu, JM; Yuan, SJ; Zhao, CH, 2007
)
0.34
" We carried out the in vitro study using selective COX-2 inhibitor celecoxib combined with EGFR-tyrosine kinase inhibitor (EGFR-TKI) ZD1839 on NSCLC cell lines to investigate the anti proliferation effect and the cell molecular mechanism."( Selective COX-2 inhibitor celecoxib combined with EGFR-TKI ZD1839 on non-small cell lung cancer cell lines: in vitro toxicity and mechanism study.
Chen, L; He, Y; Huang, H; Liao, H; Wei, W, 2008
)
0.35
"Lapatinib [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, GW572016, Tykerb] is a tyrosine kinase inhibitor approved for use in combination with capecitabine to treat advanced or metastatic breast cancers overexpressing HER2 (ErbB2)."( The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions.
Castellino, S; Harmon, KA; Humphreys, JE; John-Williams, LS; Koch, KM; O'Mara, MJ; Olson, KL; Polli, JW; Serabjit-Singh, CJ, 2008
)
0.35
" The effect of ZD6474, a potent inhibitor of VEGF-receptor-2, was evaluated in combination with either radiotherapy or temozolomide."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
" ZD6474 30 mg/kg was given alone or in combination with radiotherapy 12 Gy x 1 or with temozolomide 100 mg/kg for 3 days."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
"ZD6474 in combination with radiotherapy significantly decreased tumour area by 66% compared with controls whereas the combination with temozolomide decreased tumour area by 74%."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
"ZD6474 in combination with two standard modalities in the treatment of malignant glioma, radiotherapy and chemotherapy, markedly decreased the growth of an intracerebral experimental glioma."( Effects of the VEGFR inhibitor ZD6474 in combination with radiotherapy and temozolomide in an orthotopic glioma model.
Bergenheim, AT; Bergström, P; Henriksson, R; Johansson, M; Sandström, M, 2008
)
0.35
"This study aimed to define the maximum tolerated dose of weekly docetaxel combined with daily erlotinib, an oral epidermal growth factor receptor tyrosine kinase inhibitor."( A phase I and pharmacokinetic trial of erlotinib in combination with weekly docetaxel in patients with taxane-naive malignancies.
Al Omari, AS; Chiorean, EG; Fife, KL; Foster, AE; Jones, DR; Murry, DJ; Porter, JM; Strother, RM; Sweeney, CJ; Yoder, CA; Yu, M, 2008
)
0.35
"Although no maximum tolerated dose was reached in cycle 1 with 35 mg/m(2) docetaxel, repetitive dosing proved intolerable in a substantial number of patients; thus, the recommended phase II dose of weekly docetaxel is 30 mg/m(2) when combined with 150 mg of daily erlotinib."( A phase I and pharmacokinetic trial of erlotinib in combination with weekly docetaxel in patients with taxane-naive malignancies.
Al Omari, AS; Chiorean, EG; Fife, KL; Foster, AE; Jones, DR; Murry, DJ; Porter, JM; Strother, RM; Sweeney, CJ; Yoder, CA; Yu, M, 2008
)
0.35
" This study evaluated escalating doses of AZD2171 in combination with standard chemotherapy in patients with advanced non-small-cell lung cancer."( Phase I and pharmacokinetic study of daily oral AZD2171, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with carboplatin and paclitaxel in patients with advanced non-small-cell lung cancer: the National Cancer Institut
Arnold, A; Chen, E; Ellis, PM; Gauthier, I; Goss, G; Laurie, SA; Powers, J; Puchalski, TA; Robertson, J; Seymour, L; Shepherd, FA; Tu, D; Walsh, W, 2008
)
0.35
"AZD2171 can be combined with standard doses of carboplatin/paclitaxel with encouraging antitumor activity."( Phase I and pharmacokinetic study of daily oral AZD2171, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with carboplatin and paclitaxel in patients with advanced non-small-cell lung cancer: the National Cancer Institut
Arnold, A; Chen, E; Ellis, PM; Gauthier, I; Goss, G; Laurie, SA; Powers, J; Puchalski, TA; Robertson, J; Seymour, L; Shepherd, FA; Tu, D; Walsh, W, 2008
)
0.35
"EGFR blockade combined with conventional chemotherapy results in anti-human STS activity in vitro and in vivo, suggesting the possibility that combining these synergistic treatments will improve anti-STS therapy."( Epidermal growth factor receptor blockade in combination with conventional chemotherapy inhibits soft tissue sarcoma cell growth in vitro and in vivo.
Dicker, A; Heymach, J; Korchin, B; Lazar, A; Lev, D; Pollock, RE; Ren, W; Wei, C; Zhu, QS, 2008
)
0.35
"Cohorts of three patients with ErbB2-positive advanced breast cancer were treated with escalating doses of lapatinib (750 to 1,500 mg) administered once daily (continuous) in combination with trastuzumab (4 mg/kg loading dose then 2 mg/kg weekly) to determine the OTR."( Phase I dose escalation and pharmacokinetic study of lapatinib in combination with trastuzumab in patients with advanced ErbB2-positive breast cancer.
Arya, N; Burris, HA; Fleming, RA; Ho, PT; Jones, SF; Koch, KM; Lebowitz, PF; Loftiss, J; Overmoyer, B; Pandite, L; Paul, E; Peacock, NW; Pegram, MD; Silverman, P; Storniolo, AM, 2008
)
0.35
"Gefitinib at a dose of 250 mg daily in combination with weekly 5-fluorouracil at 2,000 mg/m(2) or gefitinib at a dose of 500 mg daily with 5-fluorouracil at 1,600 mg/m(2) plus oxaliplatin has an acceptable safety profile."( Gefitinib in combination with oxaliplatin and 5-fluorouracil in irinotecan-refractory patients with colorectal cancer: a phase I study of the Arbeits gemeinschaft Internistische Onkologie (AIO).
Bokemeyer, C; Hartmann, JT; Höhler, T; Holtmann, M; Kröning, H; Pintoffl, JP, 2008
)
0.35
" In conclusion, honokiol, either alone or in combination with other therapeutics, could serve as a new, promising approach for breast cancer treatment."( Anti-tumor effect of honokiol alone and in combination with other anti-cancer agents in breast cancer.
Elstner, E; Emde, A; Eucker, J; Kühnl, A; Liu, H; Planas-Silva, MD; Possinger, K; Rosche, M; Schulz, CO; Zang, C, 2008
)
0.35
"The main objectives of this phase I and pharmacokinetic, open-label study were to determine the optimally tolerated regimen (OTR), safety, pharmacokinetics, and clinical activity of lapatinib in combination with letrozole in patients with advanced solid malignancies."( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer.
Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008
)
0.35
"Clinically relevant doses of lapatinib in combination with letrozole were well tolerated and did not result in a pharmacokinetic interaction, and clinical antitumor activity was observed."( A phase I and pharmacokinetic study of lapatinib in combination with letrozole in patients with advanced cancer.
Arya, N; Chu, QS; Cianfrocca, ME; Fleming, RA; Gale, M; Goldstein, LJ; Koch, KM; Loftiss, J; Murray, N; Pandite, L; Paul, E; Rowinsky, EK, 2008
)
0.35
"To determine the maximum tolerated dose (MTD), spectrum of toxicities, clinical activity, and pharmacokinetics of carboplatin given in combination with lapatinib in women with a first recurrence of platinum sensitive epithelial ovarian carcinoma."( A phase I study of lapatinib in combination with carboplatin in women with platinum sensitive recurrent ovarian carcinoma.
Alvarez, RD; Barnes, MN; Estes, JM; Kimball, KJ; Kirby, TO; Koch, KM; Matei, DE; Numnum, TM; Zamboni, WC, 2008
)
0.35
" Cohorts of 3-6 patients were to receive up to 6 cycles of intravenous carboplatin AUC of 6 every 21 days in combination with escalating dosages of oral lapatinib (starting at a dose of 750 mg daily)."( A phase I study of lapatinib in combination with carboplatin in women with platinum sensitive recurrent ovarian carcinoma.
Alvarez, RD; Barnes, MN; Estes, JM; Kimball, KJ; Kirby, TO; Koch, KM; Matei, DE; Numnum, TM; Zamboni, WC, 2008
)
0.35
" The EGFR was inhibited after PDT in A-431 cells only when TPPS2a was located on the plasma membrane, but both treatment regimes resulted in synergistic inhibition of cell growth when combined with Tyrphostin."( Photodynamic targeting of EGFR does not predict the treatment outcome in combination with the EGFR tyrosine kinase inhibitor Tyrphostin AG1478.
Berg, K; Kaalhus, O; Weyergang, A, 2008
)
0.35
"Two large, randomized, placebo-controlled trials (IRESSA NSCLC Trial Assessing Combination Therapy; INTACT 1 and 2) in non-small-cell lung cancer (NSCLC) failed to show survival benefit for gefitinib (IRESSA) in combination with first-line platinum-based chemotherapy."( Epidermal growth factor receptor expression analysis in chemotherapy-naive patients with advanced non-small-cell lung cancer treated with gefitinib or placebo in combination with platinum-based chemotherapy.
Fandi, A; Giaccone, G; Herbst, RS; Iacona, RB; Janas, M; Johnson, DH; Ochs, JS, 2009
)
0.35
"In a modified Fibonacci design, the study aimed to study three cohorts of at least three patients receiving escalating doses of erlotinib (50/100/150 mg) combined with cisplatin (40 mg/m(2), weekly, 5 cycles) and radiotherapy (external beam 4,500 cGy in 25 fractions, followed by 4 fractions/600 cGy/weekly of brachytherapy) in squamous cell cervical carcinoma patients, stage IIB to IIIB."( Phase I trial of erlotinib combined with cisplatin and radiotherapy for patients with locally advanced cervical squamous cell cancer.
Camisão, C; do Carmo, CC; Erlich, F; Ferreira, CG; Fontão, K; Herchenhorn, D; Lima, R; Martins, RG; Moralez, GM; Nogueira-Rodrigues, A; Small, IA; Viegas, C, 2008
)
0.35
" Food and Drug Administration approved lapatinib (Tykerb tablets; GlaxoSmithKline, Philadelphia), an oral, small molecule, dual tyrosine kinase inhibitor of ErbB-2 and ErbB-1, for use in combination with capecitabine for the treatment of patients with human epidermal growth factor receptor (HER)-2-overexpressing metastatic breast cancer who had received prior therapy including an anthracycline, a taxane, and trastuzumab."( FDA drug approval summary: lapatinib in combination with capecitabine for previously treated metastatic breast cancer that overexpresses HER-2.
Cohen, MH; Ibrahim, A; Johnson, J; Justice, R; Ko, CW; Pazdur, R; Ryan, Q; Sridhara, R, 2008
)
0.35
"Women with measurable MBC pretreated with anthracycline- and taxane-based chemotherapy received oral gefitinib (250 mg/day) continuously combined with intravenous gemcitabine 1000 mg/m2 and vinorelbine 25 mg/m2 on day 1, every 2 weeks."( Gefitinib in combination with gemcitabine and vinorelbine in patients with metastatic breast cancer pre-treated with taxane and anthracycline chemotherapy: a phase I/II trial.
Amarantidis, K; Georgoulias, V; Gioulbasanis, I; Ignatiadis, M; Kakolyris, S; Kalbakis, K; Kalykaki, A; Mavroudis, D; Saridaki, Z; Vamvakas, L,
)
0.13
"Cediranib at 30 mg daily can be combined with standard doses of cisplatin/gemcitabine with encouraging anti-tumour activity, and is the recommended phase III dose."( A phase I and pharmacokinetic study of daily oral cediranib, an inhibitor of vascular endothelial growth factor tyrosine kinases, in combination with cisplatin and gemcitabine in patients with advanced non-small cell lung cancer: a study of the National C
Chen, E; Feld, R; Gauthier, I; Goss, G; Laurie, S; Leighl, N; Powers, J; Seymour, L; Shepherd, FA, 2009
)
0.35
" Purposes of this study were to determine the recommended phase II dose of cediranib in combination with standard doses of modified FOLFOX-6 (mFOLFOX-6), and the tolerability, safety, pharmacokinetics, and antitumor activity of this combination in patients with untreated metastatic colorectal cancer."( Phase I study of cediranib in combination with oxaliplatin and infusional 5-Fluorouracil in patients with advanced colorectal cancer.
Chen, E; Gauthier, I; Jonker, D; MacLean, M; Powers, J; Seymour, L; Wells, J, 2009
)
0.35
" The recommended phase II dose is cediranib at 30 mg daily continuously in combination with standard doses of mFOLFOX-6."( Phase I study of cediranib in combination with oxaliplatin and infusional 5-Fluorouracil in patients with advanced colorectal cancer.
Chen, E; Gauthier, I; Jonker, D; MacLean, M; Powers, J; Seymour, L; Wells, J, 2009
)
0.35
" Moreover, in combination with 5-fluorouracil modulated by folinic acid (5FU-FA) or with Raltitrexed (RTX), both commonly used in the treatment of this disease, it showed a clear schedule-dependent synergistic antiproliferative interaction as demonstrated by calculating combination indexes."( Modulation of thymidilate synthase and p53 expression by HDAC inhibitor vorinostat resulted in synergistic antitumor effect in combination with 5FU or raltitrexed.
Avallone, A; Bruzzese, F; Budillon, A; Delrio, P; Di Gennaro, E; Leone, A; Pepe, S; Subbarayan, PR, 2009
)
0.35
") calcitriol administered in combination with a fixed oral dose of dexamethasone and gefitinib in patients with refractory solid tumors."( A phase I and pharmacokinetics study of intravenous calcitriol in combination with oral dexamethasone and gefitinib in patients with advanced solid tumors.
Christy, R; Engler, KL; Fakih, MG; Johnson, CS; Muindi, JR; Trump, DL, 2009
)
0.35
" In this study, we evaluate whether MP470, a novel receptor tyrosine kinase inhibitor alone or in combination with Erlotinib has inhibitory effect on prostate cancer in vitro and in vivo."( MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer.
Bearss, D; Cooke, LS; Croce, KD; Mahadevan, D; Qi, W; Riley, C; Saldanha, JW; Stejskal, A, 2009
)
0.35
" Additive effects on both cytotoxicity and induction of apoptosis were observed when LNCaP were treated with MP470 in combination with Erlotinib."( MP470, a novel receptor tyrosine kinase inhibitor, in combination with Erlotinib inhibits the HER family/PI3K/Akt pathway and tumor growth in prostate cancer.
Bearss, D; Cooke, LS; Croce, KD; Mahadevan, D; Qi, W; Riley, C; Saldanha, JW; Stejskal, A, 2009
)
0.35
" Lung cancer combined with pregnancy is a very rare situation, so we report this case with some references."( [A case of lung cancer combined with pregnancy; dramatically deteriorating condition after caesarian section].
Fujita, S; Harada, Y; Hata, A; Imai, Y; Ishihara, K; Katakami, N; Nishimura, T; Seo, R; Takeshim, Y; Tomii, K, 2009
)
0.35
" The tolerability and efficacy of IPI-504 combined with either trastuzumab or lapatinib were also investigated in HER2(+) tumor xenograft models."( Antitumor efficacy of IPI-504, a selective heat shock protein 90 inhibitor against human epidermal growth factor receptor 2-positive human xenograft models as a single agent and in combination with trastuzumab or lapatinib.
Chang, Y; Chesebrough, J; Coats, S; Coffman, KT; Fazenbaker, CA; Gooya, J; Jackson, D; Jallal, B; Leow, CC; Weng, D, 2009
)
0.35
" The aim of this study was to evaluate the effect of an EGFR tyrosine kinase inhibitor (AG1478) alone and in combination with cisplatin on vulvar cancer cells (A431 and SW962)."( Effect of epidermal growth factor receptor inhibitor alone and in combination with cisplatin on growth of vulvar cancer cells.
Jo, H; Kim, SH; Song, YC; Song, YS, 2009
)
0.35
"Activity and toxiciy of gefitinib in combination with topotecan and cyclophosphamide (CPA) were evaluated in a case-series of relapsed neuroblastoma (NB) patients."( Gefitinib in combination with oral topotecan and cyclophosphamide in relapsed neuroblastoma: pharmacological rationale and clinical response.
Castellano, A; Cialfi, S; De Ioris, MA; De Laurentis, C; De Pasquale, MD; Dominici, C; Donfrancesco, A; Ilari, I; Jenkner, A; McDowell, HP, 2010
)
0.36
" Antitumor activity of gefitinib as single agent and in combination with either topotecan or CPA was assessed in a panel of NB cell lines."( Gefitinib in combination with oral topotecan and cyclophosphamide in relapsed neuroblastoma: pharmacological rationale and clinical response.
Castellano, A; Cialfi, S; De Ioris, MA; De Laurentis, C; De Pasquale, MD; Dominici, C; Donfrancesco, A; Ilari, I; Jenkner, A; McDowell, HP, 2010
)
0.36
"We aimed to investigate and compare the effects of erlotinib and gefitinib on UDP-glucuronosyltransferase (UGT) activities and to quantitatively evaluate their drug-drug interaction (DDI) potential due to UGT inhibition."( Comparison of the drug-drug interactions potential of erlotinib and gefitinib via inhibition of UDP-glucuronosyltransferases.
House, L; Liu, Y; Ramírez, J; Ratain, MJ, 2010
)
0.36
" In this study, we investigated the effects of evo alone and in combination with rosiglitazone (rosi) on in vitro adipocyte differentiation and in vivo obesity related to diabetes."( Inhibitory effect of evodiamine alone and in combination with rosiglitazone on in vitro adipocyte differentiation and in vivo obesity related to diabetes.
Bak, EJ; Cha, JH; Kim, JM; Park, HG; Yoo, YJ, 2010
)
0.36
"The presence of evo or evo combined with rosi during adipogenic induction has been shown to inhibit adipocyte differentiation to a significant degree, particularly at the commitment and early induction stages."( Inhibitory effect of evodiamine alone and in combination with rosiglitazone on in vitro adipocyte differentiation and in vivo obesity related to diabetes.
Bak, EJ; Cha, JH; Kim, JM; Park, HG; Yoo, YJ, 2010
)
0.36
" The chromatographic fingerprints combined with PCA, HCA and LDA could distinguish the seeds of the different species of Peganum investigated."( HPLC fingerprints combined with principal component analysis, hierarchical cluster analysis and linear discriminant analysis for the classification and differentiation of Peganum sp. indigenous to China.
Bligh, SW; Cheng, XM; Wang, CH; Wang, ZT; Yang, T; Zhao, T,
)
0.13
" Drug combination of TMZ plus BG and PHA-848125 produced additive or synergistic effects on cell growth, depending on the cell line."( The cyclin-dependent kinase inhibitor PHA-848125 suppresses the in vitro growth of human melanomas sensitive or resistant to temozolomide, and shows synergistic effects in combination with this triazene compound.
Alvino, E; Bonmassar, E; Brasca, MG; Caporali, S; Castiglia, D; Ciomei, M; Covaciu, C; D'Atri, S; Garbin, A; Levati, L; Starace, G, 2010
)
0.36
" Cediranib pharmacokinetic parameters were not substantially different when given alone or in combination with gefitinib."( Phase I evaluation of cediranib, a selective VEGFR signalling inhibitor, in combination with gefitinib in patients with advanced tumours.
Giaccone, G; Hoekman, K; Jürgensmeier, JM; Meijerink, MR; Puchalski, TA; Punt, CJ; Robertson, J; Saunders, O; van Cruijsen, H; van Herpen, CM; Voest, EE; Witteveen, PO, 2010
)
0.36
"To assess the pharmacokinetics and evaluate potential drug-drug interactions between erlotinib, paclitaxel and carboplatin."( Pharmacokinetic study of the phase III, randomized, double-blind, multicenter trial (TRIBUTE) of paclitaxel and carboplatin combined with erlotinib or placebo in patients with advanced Non-small Cell Lung Cancer (NSCLC).
Blumenschein, GR; Herbst, RS; Kim, ES; Lu, C; Lum, BL; Malik, M; Oh, YW; Papadimitrakopoulou, VA; Tran, HT; Zinner, RG, 2011
)
0.37
"1,079 previously untreated patients with advanced NSCLC were enrolled and randomized in a phase III trial (TRIBUTE) to receive either erlotinib or placebo in combination with paclitaxel 200 mg/m2 IV over 3 h and carboplatin at a calculated dose to achieve an AUC 6 mg∙min/mL."( Pharmacokinetic study of the phase III, randomized, double-blind, multicenter trial (TRIBUTE) of paclitaxel and carboplatin combined with erlotinib or placebo in patients with advanced Non-small Cell Lung Cancer (NSCLC).
Blumenschein, GR; Herbst, RS; Kim, ES; Lu, C; Lum, BL; Malik, M; Oh, YW; Papadimitrakopoulou, VA; Tran, HT; Zinner, RG, 2011
)
0.37
"This phase II investigated efficacy and tolerability of gefitinib in combination with paclitaxel (P) and carboplatin (C) for second-line treatment of patients (pts) with ovarian, tubal or peritoneal adenocarcinoma."( Phase II study of gefitinib in combination with paclitaxel (P) and carboplatin (C) as second-line therapy for ovarian, tubal or peritoneal adenocarcinoma (1839IL/0074).
Bougnoux, P; Carrasco, AT; Fumoleau, P; Joly, F; Kerbrat, P; Lhommé, C; Pautier, P; Petit, T; Ringeisen, F; Rixe, O, 2010
)
0.36
"Gefitinib, administered in combination with paclitaxel and carboplatin, provides a good clinical response but associated with an increased risk of hematologic disorders."( Phase II study of gefitinib in combination with paclitaxel (P) and carboplatin (C) as second-line therapy for ovarian, tubal or peritoneal adenocarcinoma (1839IL/0074).
Bougnoux, P; Carrasco, AT; Fumoleau, P; Joly, F; Kerbrat, P; Lhommé, C; Pautier, P; Petit, T; Ringeisen, F; Rixe, O, 2010
)
0.36
" EGF104900 compared the activity of lapatinib alone or in combination with trastuzumab in patients with ErbB2-positive, trastuzumab-refractory metastatic breast cancer (MBC)."( Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer.
Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Casey, M; Ellis, C; Koehler, M; O'Shaughnessy, J; Rugo, H; Sledge, G; Storniolo, AM; Vukelja, S, 2010
)
0.36
"Patients with ErbB2-positive MBC who experienced progression on prior trastuzumab-containing regimens were randomly assigned to receive either lapatinib alone or in combination with trastuzumab."( Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer.
Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Casey, M; Ellis, C; Koehler, M; O'Shaughnessy, J; Rugo, H; Sledge, G; Storniolo, AM; Vukelja, S, 2010
)
0.36
"Despite disease progression on prior trastuzumab-based therapy, lapatinib in combination with trastuzumab significantly improved PFS and CBR versus lapatinib alone, thus offering a chemotherapy-free option with an acceptable safety profile to patients with ErbB2-positive MBC."( Randomized study of Lapatinib alone or in combination with trastuzumab in women with ErbB2-positive, trastuzumab-refractory metastatic breast cancer.
Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Casey, M; Ellis, C; Koehler, M; O'Shaughnessy, J; Rugo, H; Sledge, G; Storniolo, AM; Vukelja, S, 2010
)
0.36
" These results suggest that: i) lapatinib has antitumor effects in vitro and in vivo; ii) lapatinib may be more effective in combination with cisplatin or paclitaxel; and iii) lapatinib might provide useful clinical benefits to HNSCC patients."( Antitumor effects of lapatinib (GW572016), a dual inhibitor of EGFR and HER-2, in combination with cisplatin or paclitaxel on head and neck squamous cell carcinoma.
Fujita, K; Ishiguro, Y; Kimura, M; Kondo, N; Matsuda, H; Sakakibara, A; Takahashi, H; Toth, G; Tsukuda, M, 2010
)
0.36
"This phase II randomized trial evaluated the efficacy and tolerability of anastrozole combined with gefitinib or anastrozole with placebo in women with hormone receptor-positive metastatic breast cancer (MBC)."( Phase II, randomized trial to compare anastrozole combined with gefitinib or placebo in postmenopausal women with hormone receptor-positive metastatic breast cancer.
Anderson, E; Arena, FP; Bacus, S; Cora, EM; Cristofanilli, M; Curcio, E; Kroener, JF; Magill, PJ; Mangalik, A; Rabinowitz, I; Royce, M; Valero, V; Watkins, C, 2010
)
0.36
"This small randomized study showed that anastrozole in combination with gefitinib is associated with a marked advantage in PFS compared with anastrozole plus placebo, and that the combination was tolerated in postmenopausal women with hormone receptor-positive MBC."( Phase II, randomized trial to compare anastrozole combined with gefitinib or placebo in postmenopausal women with hormone receptor-positive metastatic breast cancer.
Anderson, E; Arena, FP; Bacus, S; Cora, EM; Cristofanilli, M; Curcio, E; Kroener, JF; Magill, PJ; Mangalik, A; Rabinowitz, I; Royce, M; Valero, V; Watkins, C, 2010
)
0.36
"This phase I/II study was conducted to assess the maximal tolerated dose (MTD) and the dose-limiting toxicities (DLTs) of gefitinib in combination with capecitabine in patients with advanced colorectal cancer (aCRC)."( Gefitinib in combination with capecitabine as second-line therapy in patients with advanced colorectal cancer (aCRC): a phase I/II study of the Arbeitsgemeinschaft Internistische Onkologie (AIO).
Frieling, T; Graeven, U; Hegewisch-Becker, S; Lehnert, L; Reinacher-Schick, A; Schmiegel, W; Trarbach, T; Vanhoefer, U, 2010
)
0.36
"After failure of a 1st-line therapy, patients with aCRC received escalating doses of gefitinib once daily in combination with capecitabine twice daily: dose level (DL) 1: gefitinib 250 mg and capecitabine 1,000 mg/m(2), DL 2: gefitinib 250 mg and capecitabine 1,250 mg/m(2), DL 3: gefitinib 500 mg and capecitabine 850 mg/m(2)."( Gefitinib in combination with capecitabine as second-line therapy in patients with advanced colorectal cancer (aCRC): a phase I/II study of the Arbeitsgemeinschaft Internistische Onkologie (AIO).
Frieling, T; Graeven, U; Hegewisch-Becker, S; Lehnert, L; Reinacher-Schick, A; Schmiegel, W; Trarbach, T; Vanhoefer, U, 2010
)
0.36
" In cellular models of wild-type or mutant EGFR (L858R and T790M mutations), SNX-2112 alone and in combination with erlotinib inhibited EGF activation of pAKT(473) and pSTAT3(705)."( Targeting of multiple signaling pathways by the Hsp90 inhibitor SNX-2112 in EGFR resistance models as a single agent or in combination with erlotinib.
Barabasz, A; Fadden, P; Foley, B; Hall, S; Huang, K; Rice, JW; Scott, A; Steed, P; Veal, JM, 2009
)
0.35
"To investigate the killing effect of ZD6474 combined with adriamycin (ADM) on MCF-7 human breast cancer cells."( [Inhibitory effect of ZD6474 combined with adriamycin on MCF-7 human breast cancer cells in vitro].
He, BF; Luo, RC; Miao, JX; Ruan, J; Shen, J; Zhao, P; Zheng, H, 2010
)
0.36
"To investigate the feasibility and efficacy of concurrent chemoradiation in combination with erlotinib for locally advanced esophageal carcinoma."( Phase II study of concurrent chemoradiation in combination with erlotinib for locally advanced esophageal carcinoma.
Deng, X; Hu, W; Li, G; Wang, J; Wu, S; Xie, C; Zhang, P; Zhang, X, 2010
)
0.36
"Application of concurrent chemoradiotherapy in combination with erlotinib for locally advanced esophageal carcinoma yielded satisfactory 2-year overall survival and local-regional control."( Phase II study of concurrent chemoradiation in combination with erlotinib for locally advanced esophageal carcinoma.
Deng, X; Hu, W; Li, G; Wang, J; Wu, S; Xie, C; Zhang, P; Zhang, X, 2010
)
0.36
"Our data suggest that lapatinib combined with fractionated radiotherapy may be useful against EGFR+ and HER2+ breast cancers and that inhibition of downstream signaling to ERK1/2 and AKT correlates with sensitization in EGFR+ and HER2+ cells, respectively."( Lapatinib in combination with radiation diminishes tumor regrowth in HER2+ and basal-like/EGFR+ breast tumor xenografts.
Camp, JT; Kimple, RJ; Livasy, CA; Peters, E; Sambade, MJ; Sartor, CI; Shields, JM, 2010
)
0.36
"Oral cediranib 20, 30, and/or 45 mg/day was given in combination with standard mFOLFOX6; docetaxel; irinotecan; irinotecan and cetuximab; or pemetrexed."( Cediranib in combination with various anticancer regimens: results of a phase I multi-cohort study.
Gadgeel, S; Guthrie, T; Liu, Q; Lorusso, P; Puchalski, T; Shields, AF; Vaishampayan, U; Xu, J, 2011
)
0.37
"Gefitinib (250 mg daily) in combination with RT and CDDP in patients with Stage III NSCLC is feasible, but CDDP likely enhances toxicity."( Gefitinib in combination with irradiation with or without cisplatin in patients with inoperable stage III non-small cell lung cancer: a phase I trial.
Aebersold, DM; Bernier, J; Bucher, SE; Ciernik, IF; Glanzmann, C; Lippuner, T; Lombrieser, N; Lütolf, UM; Ries, G; Rothschild, S; Zouhair, A, 2011
)
0.37
"This Phase I study investigated the safety, tolerability, and pharmacokinetics of vandetanib when administered with either gemcitabine plus cisplatin (GC) or vinorelbine plus cisplatin (VC) in patients with previously untreated locally advanced or metastatic non-small cell lung cancer."( A phase I study of Vandetanib in combination with vinorelbine/cisplatin or gemcitabine/cisplatin as first-line treatment for advanced non-small cell lung cancer.
Blackhall, FH; Kennedy, SJ; Milenkova, T; Nicolson, M; O'brien, M; Schmid, P; Taylor, P; Thatcher, N, 2010
)
0.36
"In this study, in patients with previously untreated advanced non-small cell lung cancer, vandetanib 100 mg/d in combination with either VC or GC was not tolerated."( A phase I study of Vandetanib in combination with vinorelbine/cisplatin or gemcitabine/cisplatin as first-line treatment for advanced non-small cell lung cancer.
Blackhall, FH; Kennedy, SJ; Milenkova, T; Nicolson, M; O'brien, M; Schmid, P; Taylor, P; Thatcher, N, 2010
)
0.36
"Patients with type 2 diabetes mellitus (T2DM) are generally treated with many pharmacological compounds and are exposed to a high risk of drug-drug interactions."( Dipeptidylpeptidase-4 inhibitors (gliptins): focus on drug-drug interactions.
Scheen, AJ, 2010
)
0.36
" The in vitro migration of H1299 cells, which expressed high levels of both VEGF ligands and receptors, was inhibited by treatment with sorafenib, and this effect was significantly increased by the combination with anti-EGFR drugs."( Synergistic antitumor activity of sorafenib in combination with epidermal growth factor receptor inhibitors in colorectal and lung cancer cells.
Berrino, L; Capasso, A; Ciardiello, F; De Vita, F; Eckhardt, SG; Martinelli, E; Morelli, MP; Morgillo, F; Orditura, M; Rodolico, G; Santoro, M; Troiani, T; Tuccillo, C; Vecchione, L; Vitagliano, D, 2010
)
0.36
"To investigate whether EGFR inhibitor AG1478 combined with celecoxib could enhance the inhibitive effects on the growth of gastric cancer cells."( [Effects of EGFR inhibitor AG1478 in combination with celecoxib on the growth of gastric cancer cells].
Li, RK; Liao, J; Qiang, O; Wang, CH, 2010
)
0.36
"AG1478 combined with celecoxib results in enhanced inhibitive effect on the growth of SGC-7901, which may partly due to the suppression of ERK phospholation."( [Effects of EGFR inhibitor AG1478 in combination with celecoxib on the growth of gastric cancer cells].
Li, RK; Liao, J; Qiang, O; Wang, CH, 2010
)
0.36
"To evaluate the efficacy,clinical benefits and toxicities of gemcitabine combined with erlotinib for advanced pancreatic cancer."( [Efficacy of gemcitabine combined with erlotinib in patients with advanced pancreatic cancer].
Bai, CM; Cheng, YJ; Zhang, ZJ, 2010
)
0.36
"Gemcitabine combined with erlotinib is an effective regimen for pancreatic cancer with good clinical tolerance."( [Efficacy of gemcitabine combined with erlotinib in patients with advanced pancreatic cancer].
Bai, CM; Cheng, YJ; Zhang, ZJ, 2010
)
0.36
"Apricoxib, a novel once-daily selective cyclooxygenase-2 inhibitor, was investigated in combination with erlotinib for recurrent stage IIIB/IV nonsmall cell lung cancer to determine the maximum tolerated dose, dose-limiting toxicity, and recommended phase II dose (RP2D) based on changes in urinary prostaglandin E₂ metabolite (PGE-M)."( Biomarker-based phase I dose-escalation, pharmacokinetic, and pharmacodynamic study of oral apricoxib in combination with erlotinib in advanced nonsmall cell lung cancer.
Chen, LC; Gitlitz, B; Jezior, D; Milne, G; Patel, R; Reckamp, K; Syto, M; Zaknoen, S, 2011
)
0.37
"Patients received escalating doses of apricoxib (100, 200, and 400 mg/day) in combination with erlotinib 150 mg/day until disease progression or unacceptable toxicity."( Biomarker-based phase I dose-escalation, pharmacokinetic, and pharmacodynamic study of oral apricoxib in combination with erlotinib in advanced nonsmall cell lung cancer.
Chen, LC; Gitlitz, B; Jezior, D; Milne, G; Patel, R; Reckamp, K; Syto, M; Zaknoen, S, 2011
)
0.37
"VEGF, mTOR, and EGFR inhibitors have demonstrated anti-tumor and anti-angiogenic effects alone and in combination with each other."( A phase I study of bevacizumab (B) in combination with everolimus (E) and erlotinib (E) in advanced cancer (BEE).
Bendell, JC; Blobe, GC; Broadwater, G; Bullock, KE; Gockerman, JP; Howard, LA; Hurwitz, HI; Lager, JJ; Meadows, KL; Morse, MA; O'Neill, MM; Petros, WP; Truax, R; Uronis, HE; Younis, I; Zafar, SY, 2011
)
0.37
"Lapatinib, an orally active tyrosine kinase inhibitor of epidermal growth factor receptor ErbB1 (EGFR) and ErbB2 (HER2), has activity as monotherapy and in combination with chemotherapy in HER2-overexpressing metastatic breast cancer (MBC)."( A single-arm phase II trial of first-line paclitaxel in combination with lapatinib in HER2-overexpressing metastatic breast cancer.
Abbey, R; DeSilvio, M; Dobrovolskaya, N; Jagiello-Gruszfeld, A; Manikhas, A; Pienkowski, T; Ridderheim, M; Tjulandin, S, 2010
)
0.36
"This phase II single-arm trial assessed the safety and efficacy of first-line lapatinib in combination with paclitaxel in previously untreated patients with HER2-overexpressing MBC."( A single-arm phase II trial of first-line paclitaxel in combination with lapatinib in HER2-overexpressing metastatic breast cancer.
Abbey, R; DeSilvio, M; Dobrovolskaya, N; Jagiello-Gruszfeld, A; Manikhas, A; Pienkowski, T; Ridderheim, M; Tjulandin, S, 2010
)
0.36
"The purpose of this study was to determine the ability of radiation therapy (RT) combined with the tyrosine kinase inhibitors (TKI) vandetanib (antiepidermal growth factor receptor [EGFR] plus antivascular endothelial growth factor receptor [anti-VEGFR]) and cediranib (anti-VEGFR) to inhibit glioblastoma multiforme (GBM) growth."( Epidermal growth factor receptor expression modulates antitumor efficacy of vandetanib or cediranib combined with radiotherapy in human glioblastoma xenografts.
Daroczi, B; Dicker, AP; Lawrence, YR; Liu, Y; Wachsberger, PR; Xu, X, 2012
)
0.38
" In U87MG EGFR-null cells, TKI combined with radiation was no better than radiation therapy alone."( Epidermal growth factor receptor expression modulates antitumor efficacy of vandetanib or cediranib combined with radiotherapy in human glioblastoma xenografts.
Daroczi, B; Dicker, AP; Lawrence, YR; Liu, Y; Wachsberger, PR; Xu, X, 2012
)
0.38
" Hence EGFR status plays a major role in determining a tumor's in vivo response to radiation combined with TKI, supporting a "personalized" approach to GBM management."( Epidermal growth factor receptor expression modulates antitumor efficacy of vandetanib or cediranib combined with radiotherapy in human glioblastoma xenografts.
Daroczi, B; Dicker, AP; Lawrence, YR; Liu, Y; Wachsberger, PR; Xu, X, 2012
)
0.38
"4 μg/mL and did not differ when combined with standard-exposure versus reduced-exposure tacrolimus (P=0."( Pharmacokinetics of sotrastaurin combined with tacrolimus or mycophenolic acid in de novo kidney transplant recipients.
Arns, W; Budde, K; Dantal, J; Grinyo, JM; Kovarik, JM; Proot, P; Rostaing, L; Steiger, JU, 2011
)
0.37
"Sotrastaurin pharmacokinetics were similar when combined with reduced-exposure or standard-exposure tacrolimus or with MPA."( Pharmacokinetics of sotrastaurin combined with tacrolimus or mycophenolic acid in de novo kidney transplant recipients.
Arns, W; Budde, K; Dantal, J; Grinyo, JM; Kovarik, JM; Proot, P; Rostaing, L; Steiger, JU, 2011
)
0.37
"This phase I/II study of saracatinib in combination with gemcitabine in patients with advanced pancreatic cancer was conducted by the NCIC Clinical Trials Group."( A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer.
Chen, E; Gauthier, I; Gill, S; Goel, R; Hedley, D; Jonker, D; McIntosh, L; Moore, MJ; Renouf, DJ; Seymour, L; Southwood, B; Walde, D; Walsh, W, 2012
)
0.38
" In phase I saracatinib was escalated in combination with gemcitabine (1000 mg/m(2)) to determine the recommended phase II dose (RP2D)."( A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer.
Chen, E; Gauthier, I; Gill, S; Goel, R; Hedley, D; Jonker, D; McIntosh, L; Moore, MJ; Renouf, DJ; Seymour, L; Southwood, B; Walde, D; Walsh, W, 2012
)
0.38
" Saracatinib 175 mg PO daily was chosen as the RP2D in combination with gemcitabine."( A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer.
Chen, E; Gauthier, I; Gill, S; Goel, R; Hedley, D; Jonker, D; McIntosh, L; Moore, MJ; Renouf, DJ; Seymour, L; Southwood, B; Walde, D; Walsh, W, 2012
)
0.38
"Saracatinib 175 mg daily in combination with gemcitabine is well tolerated but the combination did not improve efficacy over what would be expected from gemcitabine alone."( A phase I/II study of the Src inhibitor saracatinib (AZD0530) in combination with gemcitabine in advanced pancreatic cancer.
Chen, E; Gauthier, I; Gill, S; Goel, R; Hedley, D; Jonker, D; McIntosh, L; Moore, MJ; Renouf, DJ; Seymour, L; Southwood, B; Walde, D; Walsh, W, 2012
)
0.38
" The aim of this multicenter, randomized phase II study was to evaluate clinical activity and safety of sorafenib in combination with erlotinib or gemcitabine in unselected untreated elderly patients with non-small-cell lung cancer (NSCLC)."( Sorafenib in combination with erlotinib or with gemcitabine in elderly patients with advanced non-small-cell lung cancer: a randomized phase II study.
Cerea, G; Chella, A; Ciardiello, F; de Marinis, F; Di Maio, M; Fasano, M; Favaretto, A; Gridelli, C; Maione, P; Mattioli, R; Morgillo, F; Pasello, G; Ricciardi, S; Rossi, A; Tortora, G, 2011
)
0.37
" Therefore, HM781-36B may be useful for the treatment of HER2 amplified gastric cancer alone or in combination with chemotherapeutic agents."( Antitumor activity of HM781-36B, an irreversible Pan-HER inhibitor, alone or in combination with cytotoxic chemotherapeutic agents in gastric cancer.
Bang, YJ; Han, SW; Hur, HS; Im, SA; Kim, HP; Kim, MS; Kim, TY; Lee, GS; Nam, HJ; Oh, DY; Song, SH; Yoon, YK, 2011
)
0.37
"Thus, we showed that L858R receptor mutation in combination with expression of its negative regulator, Mig6, alters signaling outcomes and results in variable drug sensitivity."( Epidermal growth factor receptor mutation in combination with expression of MIG6 alters gefitinib sensitivity.
Nagashima, T; Naka, T; Nakakuki, T; Naruo, Y; Okada-Hatakeyama, M; Saeki, Y; Tanaka, H; Tsai, SF; Ushikoshi-Nakayama, R, 2011
)
0.37
"Vandetanib at doses of 100 mg and 300 mg daily in combination with capecitabine and oxaliplatin was well tolerated."( A phase I trial of vandetanib combined with capecitabine, oxaliplatin and bevacizumab for the first-line treatment of metastatic colorectal cancer.
Cabebe, EC; Fisher, GA; Sikic, BI, 2012
)
0.38
"To confirm the efficacy and toxicity of Erlotinib in combination with Gemcitabine and Capecitabine when used as a first-line therapy in metastatic/recurrent pancreatic cancer (PC)."( A phase II trial of erlotinib in combination with gemcitabine and capecitabine in previously untreated metastatic/recurrent pancreatic cancer: combined analysis with translational research.
Bang, YJ; Kang, HJ; Kim, BS; Kim, JS; Lee, KH; Lee, KW; Oh, DY; Park, YS; Ryoo, HM; Sohn, CH; Song, HS; Zang, DY, 2012
)
0.38
"Exposure to vandetanib, as assessed by AUC(504) in healthy subjects, was reduced by around 40% when a single dose was given in combination with the potent CYP3A4 inducer rifampicin."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
0.37
" Intravenous administration of S(4)TdR, in combination with UVA delivered directly to the bladder, resulted in an antitumour effect in three of five animals treated."( Thiothymidine combined with UVA as a potential novel therapy for bladder cancer.
Boddy, AV; Heer, R; Karran, P; Newell, DR; O'Toole, K; Pridgeon, SW; Robinson, M; Taylor, GA; Xu, YZ, 2011
)
0.37
"This Phase I study investigated the safety, tolerability and pharmacokinetics of cediranib (20 or 30 mg) in combination with mFOLFOX6 in Japanese patients with previously untreated metastatic CRC."( Phase I results from a two-part Phase I/II study of cediranib in combination with mFOLFOX6 in Japanese patients with metastatic colorectal cancer.
Boku, N; Mishima, H; Okamoto, W; Satoh, T; Shi, X; Shimamura, T; Yamaguchi, K; Yamazaki, K, 2012
)
0.38
"Cediranib (20 or 30 mg) in combination with mFOLFOX6 was considered tolerable according to the protocol-defined criteria, providing justification for the Phase II part of this study."( Phase I results from a two-part Phase I/II study of cediranib in combination with mFOLFOX6 in Japanese patients with metastatic colorectal cancer.
Boku, N; Mishima, H; Okamoto, W; Satoh, T; Shi, X; Shimamura, T; Yamaguchi, K; Yamazaki, K, 2012
)
0.38
" Thus, the targeted approach against HER1/EGFR likely requires a synergistic drug combination strategy to ultimately become successful in this disease."( Drug combinations enhancing the antineoplastic effects of erlotinib in high-grade glioma.
Halatsch, ME; Karpel-Massler, G; Wirtz, CR, 2011
)
0.37
"We have investigated in vitro effects of anticancer therapy with the histone deacetylase inhibitor (HDACi) 4-phenylbutyrate (4-PB) combined with receptor tyrosine kinase inhibitors (RTKi) gefitinib or vandetanib on the survival of glioblastoma (U343MGa) and medulloblastoma (D324Med) cells."( Enhanced effects by 4-phenylbutyrate in combination with RTK inhibitors on proliferation in brain tumor cell models.
Baryawno, N; Ekström, TJ; Johnsen, JI; Larsson, C; Marino, AM; Sofiadis, A; Vukojević, V, 2011
)
0.37
"Patients with advanced or metastatic cancer were treated with escalating doses of LY2334737 monotherapy or in combination with continuous daily administration of 100 mg erlotinib."( Phase I study of Oral gemcitabine prodrug (LY2334737) alone and in combination with erlotinib in patients with advanced solid tumors.
Beijnen, JH; Benhadji, KA; Callies, S; Garcia-Ribas, I; Jansen, RS; Koolen, SL; Kronemeijer, RH; Langenberg, MH; Nol, A; Schellens, JH; Slapak, CA; Voest, EE; Witteveen, PO, 2011
)
0.37
"Chemotherapy in combination with small-molecule epidermal growth factor receptor inhibitors has yielded inconsistent results."( Phase I study of continuous and intermittent schedules of lapatinib in combination with vinorelbine in solid tumors.
Chew, HK; Christensen, S; Davies, AM; Gandour-Edwards, R; Gitlitz, B; Linden, H; Mack, PC; Solis, LJ; Somlo, G; Yang, X, 2012
)
0.38
"This phase 1b study assessed the maximum tolerated dose (MTD), safety, and pharmacokinetics of motesanib (a small-molecule antagonist of VEGF receptors 1, 2, and 3; platelet-derived growth factor receptor; and Kit) administered once daily (QD) or twice daily (BID) in combination with erlotinib and gemcitabine in patients with solid tumors."( Safety and pharmacokinetics of motesanib in combination with gemcitabine and erlotinib for the treatment of solid tumors: a phase 1b study.
Adewoye, AH; Desai, J; Johnson, J; Kotasek, D; McCoy, S; Price, T; Siu, LL; Sun, YN; Tebbutt, N; Welch, S, 2011
)
0.37
"Patients received weekly intravenous gemcitabine (1000 mg/m2) and erlotinib (100 mg QD) alone (control cohort) or in combination with motesanib (50 mg QD, 75 mg BID, 125 mg QD, or 100 mg QD; cohorts 1-4); or erlotinib (150 mg QD) in combination with motesanib (100 or 125 mg QD; cohorts 5 and 6)."( Safety and pharmacokinetics of motesanib in combination with gemcitabine and erlotinib for the treatment of solid tumors: a phase 1b study.
Adewoye, AH; Desai, J; Johnson, J; Kotasek, D; McCoy, S; Price, T; Siu, LL; Sun, YN; Tebbutt, N; Welch, S, 2011
)
0.37
" The MTD of motesanib in combination with gemcitabine and erlotinib was 100 mg QD."( Safety and pharmacokinetics of motesanib in combination with gemcitabine and erlotinib for the treatment of solid tumors: a phase 1b study.
Adewoye, AH; Desai, J; Johnson, J; Kotasek, D; McCoy, S; Price, T; Siu, LL; Sun, YN; Tebbutt, N; Welch, S, 2011
)
0.37
" Motesanib 125 mg QD was tolerable only in combination with erlotinib alone."( Safety and pharmacokinetics of motesanib in combination with gemcitabine and erlotinib for the treatment of solid tumors: a phase 1b study.
Adewoye, AH; Desai, J; Johnson, J; Kotasek, D; McCoy, S; Price, T; Siu, LL; Sun, YN; Tebbutt, N; Welch, S, 2011
)
0.37
"In this phase II, double-blind, placebo-controlled study, 172 patients with metastatic CRC were randomised to receive once-daily cediranib (20 or 30 mg) or placebo, each combined with modified FOLFOX6 (mFOLFOX6)."( Cediranib in combination with mFOLFOX6 in Japanese patients with metastatic colorectal cancer: results from the randomised phase II part of a phase I/II study.
Amagai, K; Baba, H; Bando, H; Denda, T; Fukase, K; Hazama, S; Kato, T; Mishima, H; Muro, K; Shi, X; Skamoto, J; Yamaguchi, K, 2012
)
0.38
"The primary objective of this Phase I study was to assess the safety and tolerability of the vascular endothelial growth factor signalling inhibitor cediranib in combination with cisplatin plus an oral fluoropyrimidine, in Japanese patients with previously untreated advanced gastric cancer."( Phase I study of cediranib in combination with cisplatin plus fluoropyrimidine (S-1 or capecitabine) in Japanese patients with previously untreated advanced gastric cancer.
Boku, N; Brown, KH; Hayashi, H; Muro, K; Nakajima, TE; Satoh, T; Shi, X; Shimada, Y; Takahari, D; Taku, K; Yamada, Y, 2012
)
0.38
"Patients received continuous, once-daily oral doses of cediranib 20 mg in combination with either cisplatin (60 mg/m(2) iv day 1) plus S-1 (40-60 mg bid, days 1-21) every 5 weeks for a maximum of eight cycles [Arm A]; or cisplatin (80 mg/m(2) iv, day 1) plus capecitabine (1,000 mg/m(2) bid, days 1-14) every 3 weeks for a maximum of six cycles [Arm B]."( Phase I study of cediranib in combination with cisplatin plus fluoropyrimidine (S-1 or capecitabine) in Japanese patients with previously untreated advanced gastric cancer.
Boku, N; Brown, KH; Hayashi, H; Muro, K; Nakajima, TE; Satoh, T; Shi, X; Shimada, Y; Takahari, D; Taku, K; Yamada, Y, 2012
)
0.38
"Cediranib 20 mg/day in combination with cisplatin and S-1 or capecitabine was tolerable, with no new toxicities identified, and showed preliminary evidence of antitumour activity."( Phase I study of cediranib in combination with cisplatin plus fluoropyrimidine (S-1 or capecitabine) in Japanese patients with previously untreated advanced gastric cancer.
Boku, N; Brown, KH; Hayashi, H; Muro, K; Nakajima, TE; Satoh, T; Shi, X; Shimada, Y; Takahari, D; Taku, K; Yamada, Y, 2012
)
0.38
" Optimal effects are obtained when these compounds are used in combination with chemotherapy, as shown in preclinical models and more recently in clinical trials."( Docetaxel combined with targeted therapies in metastatic breast cancer.
Cortes, J; Roché, H, 2012
)
0.38
" In this study, we evaluated the cytotoxic effects of (ZEGFR:1907)2 in combination with external radiation and the possible inhibitory effects in the EGFR signalling pathways in the colon cancer cell lines HT-29 and HCT116."( The effect of a dimeric Affibody molecule (ZEGFR:1907)2 targeting EGFR in combination with radiation in colon cancer cell lines.
Glimelius, B; Häggblad Sahlberg, S; Lennartsson, J; Nygren, P; Spiegelberg, D; Stenerlöw, B, 2012
)
0.38
" The conventional schedule of capecitabine limits full dosing in combination with other agents due to toxicity."( Phase II trial of a novel capecitabine dosing schedule in combination with lapatinib for the treatment of patients with HER2-positive metastatic breast cancer.
Chen, C; D'Andrea, G; Drullinsky, P; Feigin, K; Gajria, D; Gonzalez, J; Hudis, CA; Lake, D; Norton, L; Patil, S; Theodoulou, M; Traina, TA, 2012
)
0.38
" The primary objective of this open-label phase I trial was to determine the maximum tolerated dose (MTD) and recommended dose (RD) of vandetanib in combination with gemcitabine in patients with unresectable, locally advanced or metastatic pancreatic adenocarcinoma (PAC)."( Phase I dose-finding study of vandetanib in combination with gemcitabine in locally advanced unresectable or metastatic pancreatic adenocarcinoma.
Cerny, T; De Dosso, S; Koeberle, D; Renggli, V; Saletti, P; Sessa, C, 2011
)
0.37
"Vandetanib 100 mg/day is the RD in combination with gemcitabine in the treatment of patients with advanced PAC."( Phase I dose-finding study of vandetanib in combination with gemcitabine in locally advanced unresectable or metastatic pancreatic adenocarcinoma.
Cerny, T; De Dosso, S; Koeberle, D; Renggli, V; Saletti, P; Sessa, C, 2011
)
0.37
" This Phase I study investigated cediranib, an oral inhibitor of vascular endothelial growth factor signalling in combination with saracatinib, an oral Src inhibitor."( Phase I open-label study of cediranib, an oral inhibitor of VEGF signalling, in combination with the oral Src inhibitor saracatinib in patients with advanced solid tumours.
Brown, KH; Drevs, J; Eberhardt, WE; Gauler, TC; Le Scouiller, S; Marotti, M; Schneider, V; Schultheis, B; Strumberg, D; Trarbach, T, 2012
)
0.38
"All cediranib doses were tolerated; however, in patients with advanced solid tumours, for combination with saracatinib 175 mg/day, cediranib 20 or 30 mg/day was more sustainable than 45 mg/day."( Phase I open-label study of cediranib, an oral inhibitor of VEGF signalling, in combination with the oral Src inhibitor saracatinib in patients with advanced solid tumours.
Brown, KH; Drevs, J; Eberhardt, WE; Gauler, TC; Le Scouiller, S; Marotti, M; Schneider, V; Schultheis, B; Strumberg, D; Trarbach, T, 2012
)
0.38
" Patients were randomly assigned to receive erlotinib (150 mg orally once a day) in combination with either placebo, R1507 9 mg/kg weekly, or R1507 16 mg/kg intravenously once every 3 weeks."( Randomized phase II study of erlotinib in combination with placebo or R1507, a monoclonal antibody to insulin-like growth factor-1 receptor, for advanced-stage non-small-cell lung cancer.
Brownstein, CM; Chen, D; Crino, L; Eberhardt, WE; Engelman, JA; Habben, K; Jänne, PA; Liu, L; Novello, S; Ramalingam, SS; Reck, M; Schneider, CP; Spigel, DR; Steins, MB, 2011
)
0.37
"This study investigated the curative effect of cryoablation combined with molecular target therapy for advanced non-small cell lung cancer (NSCLC)."( Cryoablation combined with molecular target therapy improves the curative effect in patients with advanced non-small cell lung cancer.
Fang, W; Gu, XY; Jiang, Z, 2011
)
0.37
"To review the clinical effectiveness and cost-effectiveness evidence base for lapatinib (LAP) in combination with an aromatase inhibitor (AI) and trastuzumab (TRA) in combination with an AI for the first-line treatment of patients who have hormone receptor-positive (HR+)/human epidermal growth factor 2-positive (HER2+) mBC."( Lapatinib and trastuzumab in combination with an aromatase inhibitor for the first-line treatment of metastatic hormone receptor-positive breast cancer which over-expresses human epidermal growth factor 2 (HER2): a systematic review and economic analysis.
Armstrong, A; Bagust, A; Blundell, M; Boland, A; Davis, H; Dickson, R; Dundar, Y; Fleeman, N; Moonan, M; Oyee, J; Thorp, N, 2011
)
0.37
"Three trials were included in the systematic review [the patient populations of the efficacy and safety of lapatinib combined with letrozole (EGF30008) trial, the efficacy and safety of trastuzumab combined with anastrozole (TAnDEM) trial and the efficacy and safety of letrozole combined with trastuzumab (eLEcTRA) trial]."( Lapatinib and trastuzumab in combination with an aromatase inhibitor for the first-line treatment of metastatic hormone receptor-positive breast cancer which over-expresses human epidermal growth factor 2 (HER2): a systematic review and economic analysis.
Armstrong, A; Bagust, A; Blundell, M; Boland, A; Davis, H; Dickson, R; Dundar, Y; Fleeman, N; Moonan, M; Oyee, J; Thorp, N, 2011
)
0.37
"Cynomolgus monkey recipients of life-supporting kidney allografts were treated orally with STN alone or in combination with cyclosporine A (CsA)."( Sotrastaurin (AEB071) alone and in combination with cyclosporine A prolongs survival times of non-human primate recipients of life-supporting kidney allografts.
Audet, M; Beerli, C; Bigaud, M; Blancher, A; Heusser, C; Morris, RE; Wagner, J; Wieczorek, G, 2012
)
0.38
"STN prolonged survival times of non-human primate kidney allograft recipients both as monotherapy and most effectively in combination with CsA."( Sotrastaurin (AEB071) alone and in combination with cyclosporine A prolongs survival times of non-human primate recipients of life-supporting kidney allografts.
Audet, M; Beerli, C; Bigaud, M; Blancher, A; Heusser, C; Morris, RE; Wagner, J; Wieczorek, G, 2012
)
0.38
" Unless long-term outcome data show different results, lapatinib should not be used outside of clinical trials as single anti-HER2-treatment in combination with neoadjuvant chemotherapy."( Lapatinib versus trastuzumab in combination with neoadjuvant anthracycline-taxane-based chemotherapy (GeparQuinto, GBG 44): a randomised phase 3 trial.
Bischoff, J; Blohmer, JU; Eidtmann, H; Fasching, PA; Gerber, B; Hanusch, C; Hilfrich, J; Huober, J; Jackisch, C; Kaufmann, M; Kreienberg, R; Kühn, T; Loibl, S; Nekljudova, V; Rezai, M; Strumberg, D; Tesch, H; Untch, M; von Minckwitz, G, 2012
)
0.38
" There are currently insufficient safety data in human subjects, particularly when ascorbic acid is combined with chemotherapy."( Phase I evaluation of intravenous ascorbic acid in combination with gemcitabine and erlotinib in patients with metastatic pancreatic cancer.
Bazzan, AJ; Deshmukh, S; Levine, M; Littman, S; Mitchell, E; Monti, DA; Newberg, AB; Pillai, MV; Yeo, CJ; Zabrecky, G, 2012
)
0.38
" This, combined with the observed response to treatment, suggests the need for a phase II study of longer duration."( Phase I evaluation of intravenous ascorbic acid in combination with gemcitabine and erlotinib in patients with metastatic pancreatic cancer.
Bazzan, AJ; Deshmukh, S; Levine, M; Littman, S; Mitchell, E; Monti, DA; Newberg, AB; Pillai, MV; Yeo, CJ; Zabrecky, G, 2012
)
0.38
" It is likely that clinical testing of these agents will be in combination with standard therapies to harness the apoptotic potential of both the agents."( The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models.
Alferez, D; Davies, BR; Heaton, SP; Heier, A; Holt, SV; Logié, A; Odedra, R; Smith, PD; Wilkinson, RW, 2012
)
0.38
"The aim of this study was to identify agents, which would be likely to offer clinical benefit when combined with selumetinib."( The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models.
Alferez, D; Davies, BR; Heaton, SP; Heier, A; Holt, SV; Logié, A; Odedra, R; Smith, PD; Wilkinson, RW, 2012
)
0.38
" In several models we observed that continuous exposure to selumetinib in combination with docetaxel results in tumour regression."( The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models.
Alferez, D; Davies, BR; Heaton, SP; Heier, A; Holt, SV; Logié, A; Odedra, R; Smith, PD; Wilkinson, RW, 2012
)
0.38
"The data presented suggests that MEK inhibition in combination with several standard chemotherapeutics or an Aurora B kinase inhibitor is a promising clinical strategy."( The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models.
Alferez, D; Davies, BR; Heaton, SP; Heier, A; Holt, SV; Logié, A; Odedra, R; Smith, PD; Wilkinson, RW, 2012
)
0.38
"This phase 1b dose-escalation study assessed safety, tolerability, and pharmacokinetics of ganitumab, a fully human monoclonal antibody against the insulin-like growth factor 1 (IGF1) receptor, combined with targeted agents or cytotoxic chemotherapy in patients with advanced solid tumors."( Safety and pharmacokinetics of ganitumab (AMG 479) combined with sorafenib, panitumumab, erlotinib, or gemcitabine in patients with advanced solid tumors.
Chan, E; Deng, H; Friberg, G; Gilbert, J; Hwang, YC; Mahalingam, D; McCaffery, I; Michael, SA; Mita, AC; Mita, MM; Mulay, M; Puzanov, I; Rosen, LS; Sarantopoulos, J; Shubhakar, P; Zhu, M, 2012
)
0.38
" every 2 weeks) combined with either sorafenib 400 mg twice daily, panitumumab 6 mg/kg every 2 weeks, erlotinib 150 mg once daily, or gemcitabine 1,000 mg/m(2) on days 1, 8, and 15 of each 4-week cycle."( Safety and pharmacokinetics of ganitumab (AMG 479) combined with sorafenib, panitumumab, erlotinib, or gemcitabine in patients with advanced solid tumors.
Chan, E; Deng, H; Friberg, G; Gilbert, J; Hwang, YC; Mahalingam, D; McCaffery, I; Michael, SA; Mita, AC; Mita, MM; Mulay, M; Puzanov, I; Rosen, LS; Sarantopoulos, J; Shubhakar, P; Zhu, M, 2012
)
0.38
"Ganitumab up to 12 mg/kg appeared well tolerated combined with sorafenib, panitumumab, erlotinib, or gemcitabine."( Safety and pharmacokinetics of ganitumab (AMG 479) combined with sorafenib, panitumumab, erlotinib, or gemcitabine in patients with advanced solid tumors.
Chan, E; Deng, H; Friberg, G; Gilbert, J; Hwang, YC; Mahalingam, D; McCaffery, I; Michael, SA; Mita, AC; Mita, MM; Mulay, M; Puzanov, I; Rosen, LS; Sarantopoulos, J; Shubhakar, P; Zhu, M, 2012
)
0.38
"Ganitumab up to 12 mg/kg was well tolerated, without adverse effects on pharmacokinetics in combination with either sorafenib, panitumumab, erlotinib, or gemcitabine."( Safety and pharmacokinetics of ganitumab (AMG 479) combined with sorafenib, panitumumab, erlotinib, or gemcitabine in patients with advanced solid tumors.
Chan, E; Deng, H; Friberg, G; Gilbert, J; Hwang, YC; Mahalingam, D; McCaffery, I; Michael, SA; Mita, AC; Mita, MM; Mulay, M; Puzanov, I; Rosen, LS; Sarantopoulos, J; Shubhakar, P; Zhu, M, 2012
)
0.38
"The aim of this study was to determine the safety and efficacy of metronomic chemotherapy combined with targeted drugs in patients with metastatic breast cancer (MBC)."( Metronomic chemotherapy combined with bevacizumab and erlotinib in patients with metastatic HER2-negative breast cancer: clinical and biological activity.
Bagnardi, V; Bertolini, F; Calleri, A; Cancello, G; Colleoni, M; Dellapasqua, S; Goldhirsch, A; Intra, M; Luini, A; Montagna, E; Pastrello, D; Perri, G; Rampinelli, C; Veronesi, P; Viale, G, 2012
)
0.38
"The object of this study was to evaluate the safety and efficacy of metronomic chemotherapy in combination with bevacizumab and erlotinib in patients with HER2-negative (HER2(-)) metastatic breast cancer (MBC) and poor hormone receptor expression."( Metronomic chemotherapy combined with bevacizumab and erlotinib in patients with metastatic HER2-negative breast cancer: clinical and biological activity.
Bagnardi, V; Bertolini, F; Calleri, A; Cancello, G; Colleoni, M; Dellapasqua, S; Goldhirsch, A; Intra, M; Luini, A; Montagna, E; Pastrello, D; Perri, G; Rampinelli, C; Veronesi, P; Viale, G, 2012
)
0.38
"Treatment with metronomic chemotherapy in combination with bevacizumab and erlotinib was effective in HER2(-), estrogen receptor (ER)- and progesterone receptor (PR)-poor advanced breast cancer."( Metronomic chemotherapy combined with bevacizumab and erlotinib in patients with metastatic HER2-negative breast cancer: clinical and biological activity.
Bagnardi, V; Bertolini, F; Calleri, A; Cancello, G; Colleoni, M; Dellapasqua, S; Goldhirsch, A; Intra, M; Luini, A; Montagna, E; Pastrello, D; Perri, G; Rampinelli, C; Veronesi, P; Viale, G, 2012
)
0.38
"As a prelude to combination studies aimed at resistance reversal, this dose-escalation/dose-expansion study investigated the selective Src kinase inhibitor saracatinib (AZD0530) in combination with carboplatin and/or paclitaxel."( Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours.
Aamdal, S; Barrett, S; Barriuso, J; Boven, E; Burke, W; de Vries, EG; Emeribe, U; Freyer, G; Hartog, V; Jones, R; Kaye, S; Kristensen, GB; Kuenen, B; Nyakas, M; Pietersma, D; Pujade-Lauraine, E; Ruijter, R; Sandhu, S; Stuart, M; Tan, DS, 2012
)
0.38
"Patients with advanced solid tumours received saracatinib once-daily oral tablets in combination with either carboplatin AUC 5 every 3 weeks (q3w), paclitaxel 175 mg m(-2) q3w, paclitaxel 80 mg m(-2) every 1 week (q1w), or carboplatin AUC 5 plus paclitaxel 175 mg m(-2) q3w."( Phase I study of saracatinib (AZD0530) in combination with paclitaxel and/or carboplatin in patients with solid tumours.
Aamdal, S; Barrett, S; Barriuso, J; Boven, E; Burke, W; de Vries, EG; Emeribe, U; Freyer, G; Hartog, V; Jones, R; Kaye, S; Kristensen, GB; Kuenen, B; Nyakas, M; Pietersma, D; Pujade-Lauraine, E; Ruijter, R; Sandhu, S; Stuart, M; Tan, DS, 2012
)
0.38
"From September 2008 to October 2011, a total of 31 patients of NSCLC with multiple brain metastases (≥3) received selected incranial, bronchial and corresponding target arterial infusion chemotherapy combined with EGFR-TKIs."( [Selected arterial infusion chemotherapy combined with target drugs for non-small cell lung cancer with multiple brain metastase].
Guo, Z; Li, J, 2012
)
0.38
"Patients with HER2-positive MBC whose disease progressed during prior trastuzumab-based therapies were randomly assigned to receive lapatinib monotherapy or lapatinib in combination with trastuzumab."( Overall survival benefit with lapatinib in combination with trastuzumab for patients with human epidermal growth factor receptor 2-positive metastatic breast cancer: final results from the EGF104900 Study.
Aktan, G; Baselga, J; Bischoff, J; Blackwell, KL; Burstein, HJ; Ellis, C; Florance, A; O'Shaughnessy, J; Rugo, HS; Sledge, G; Storniolo, AM; Vukelja, S, 2012
)
0.38
" This phase II study was designed to evaluate the efficacy and safety of erlotinib and enzastaurin in NSCLC, a combination with promise to overcome EGFR resistance based on preclinical models."( A phase II study of enzastaurin in combination with erlotinib in patients with previously treated advanced non-small cell lung cancer.
Bernstein, ED; Clément-Duchêne, C; Dudek, AZ; Jahan, T; Krupitskaya, Y; Latz, JE; Natale, RB; Osarogiagbon, R; Sanborn, RE; Shi, P; Wakelee, HA, 2012
)
0.38
" This study will investigate onartuzumab (MetMAb) in combination with erlotinib compared with erlotinib alone, as second- or third-line treatment, in patients with advanced non-small-cell lung cancer (NSCLC) who are Met-positive by immunohistochemistry."( Treatment Rationale Study Design for the MetLung Trial: A Randomized, Double-Blind Phase III Study of Onartuzumab (MetMAb) in Combination With Erlotinib Versus Erlotinib Alone in Patients Who Have Received Standard Chemotherapy for Stage IIIB or IV Met-Po
Edelman, MJ; Mok, T; O'Byrne, K; Paz-Ares, L; Rittweger, K; Spigel, DR; Thurm, H; Yu, W, 2012
)
0.38
" We used a panel of stably and transiently transfected cell lines to elucidate the carrier-mediated transport processes that are involved in linagliptin disposition in vivo and to assess the potential for drug-drug interactions (DDIs)."( Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods.
Ebner, T; Ishiguro, N; Kishimoto, W; Schaefer, O; Shimizu, H, 2013
)
0.39
"To determine the maximum tolerated dose (MTD) of OSI-930 that can be combined with erlotinib, and establish recommended phase 2 doses when both agents are administered daily in patients with advanced solid tumours."( A phase 1 study of OSI-930 in combination with erlotinib in patients with advanced solid tumours.
Brock, K; Evans, TR; Gedrich, R; Hopkins, CA; Macpherson, IR; Poondru, S; Simon, GR; Stephens, A; Stewart, K, 2013
)
0.39
" We evaluated the antitumor effect of a c-Src/Abl kinase inhibitor, saracatinib (AZD0530), alone or combined with chemotherapeutic agents in gastric cancer cell lines and a NCI-N87 xenograft model."( Antitumor activity of saracatinib (AZD0530), a c-Src/Abl kinase inhibitor, alone or in combination with chemotherapeutic agents in gastric cancer.
Bang, YJ; Elvin, P; Han, SW; Im, SA; Kim, HP; Kim, TY; Min, A; Nam, HJ; Oh, DY; Song, SH; Yoon, YK, 2013
)
0.39
"A phase I study to assess the maximum tolerated dose (MTD) of a short course of afatinib in combination with docetaxel for the treatment of solid tumors."( Phase I study of pulsatile 3-day administration of afatinib (BIBW 2992) in combination with docetaxel in advanced solid tumors.
Awada, AH; Besse-Hammer, T; Dumez, H; Fleischer, F; Hendlisz, A; Piccart, M; Schöffski, P; Stopfer, P; Uttenreuther-Fischer, M; Wolter, P, 2013
)
0.39
" Afatinib doses were escalated to 160 mg/day in combination with 75 mg/m(2) docetaxel."( Phase I study of pulsatile 3-day administration of afatinib (BIBW 2992) in combination with docetaxel in advanced solid tumors.
Awada, AH; Besse-Hammer, T; Dumez, H; Fleischer, F; Hendlisz, A; Piccart, M; Schöffski, P; Stopfer, P; Uttenreuther-Fischer, M; Wolter, P, 2013
)
0.39
" The current study evaluated the tolerability and efficacy of stereotactic body radiation therapy (SBRT) in combined with gefitinib as a second-line or third-line treatment in patients with advanced NSCLC."( Gefitinib combined with stereotactic radiosurgery in previously treated patients with advanced non-small cell lung cancer.
Hou, B; Jiang, WR; Kong, QT; Li, B; Li, J; Liu, ZB; Shen, TZ; Wang, Y; Wang, Z; Wu, XH; Zhu, XX, 2014
)
0.4
"The SBRT combined with gefitinib is a promising treatment strategy for advanced (stage IIIb or IV) NSCLC after the failure of previously chemotherapy."( Gefitinib combined with stereotactic radiosurgery in previously treated patients with advanced non-small cell lung cancer.
Hou, B; Jiang, WR; Kong, QT; Li, B; Li, J; Liu, ZB; Shen, TZ; Wang, Y; Wang, Z; Wu, XH; Zhu, XX, 2014
)
0.4
"The aim of this phase I trial was to define the maximum tolerated dose (MTD), the dose-limiting toxicity (DLT) and the recommended dose of erlotinib combined with capecitabine and gemcitabine in the treatment of advanced pancreatic cancer (APC)."( Phase I trial of gemcitabine combined with capecitabine and erlotinib in advanced pancreatic cancer: a clinical and pharmacological study.
Bennouna, J; Chamorey, E; Douillard, JY; Etienne-Grimaldi, MC; Follana, P; Francois, E; Mari, V; Michel, C; Milano, G; Renée, N; Senellart, H, 2012
)
0.38
" Lapatinib combined with CRT was well-tolerated."( Randomised Phase II study of oral lapatinib combined with chemoradiotherapy in patients with advanced squamous cell carcinoma of the head and neck: rationale for future randomised trials in human papilloma virus-negative disease.
Berrier, A; Biswas-Baldwin, N; Compton, N; de Mendoza, FH; El-Hariry, I; Fayette, J; Franklin, N; Harrington, K; Housset, M; Kumar, R; Lau, M; Legenne, P; Mehanna, H; Remenar, E; Robinson, M, 2013
)
0.39
"Lapatinib combined with CRT is well-tolerated with numeric increases in CRR at 6 months post-CRT and median PFS in p16-negative disease."( Randomised Phase II study of oral lapatinib combined with chemoradiotherapy in patients with advanced squamous cell carcinoma of the head and neck: rationale for future randomised trials in human papilloma virus-negative disease.
Berrier, A; Biswas-Baldwin, N; Compton, N; de Mendoza, FH; El-Hariry, I; Fayette, J; Franklin, N; Harrington, K; Housset, M; Kumar, R; Lau, M; Legenne, P; Mehanna, H; Remenar, E; Robinson, M, 2013
)
0.39
" Among the anti-EGFR agents tested, the strongest biological effect was observed when afatinib was combined with T790M-specific-siRNAs."( Effect of siRNAs targeting the EGFR T790M mutation in a non-small cell lung cancer cell line resistant to EGFR tyrosine kinase inhibitors and combination with various agents.
Chen, G; De Grève, J; Kronenberger, P; Teugels, E; Umelo, IA, 2013
)
0.39
"In this phase Ib, dose-escalation study, the oral irreversible ErbB family blocker afatinib (BIBW 2992) was combined with cisplatin (Cadila Healthcare Ltd, Ahmedabad, India) 50 or 75 mg/m(2)/paclitaxel (Bristol-Myers Squibb Pharmaceuticals Ltd, New York, USA) (Taxol)175 mg/m(2) (regimen A) or cisplatin 75-100 mg/m(2)/5-fluorouracil 750-1000 mg/m(2) (regimen B) in patients with advanced solid tumors."( A phase Ib, open-label study to assess the safety of continuous oral treatment with afatinib in combination with two chemotherapy regimens: cisplatin plus paclitaxel and cisplatin plus 5-fluorouracil, in patients with advanced solid tumors.
Ehrnrooth, E; Lahogue, A; Machiels, JP; Pelling, K; Rottey, S; Vermorken, JB; Wind, S, 2013
)
0.39
"5 or 3 mg/kg/day) was evaluated alone and in combination with either gefitinib, imatinib, ZD6126, saracatinib, selumetinib, bevacizumab, 5-fluorouracil (5-FU), docetaxel, oxaliplatin, gemcitabine, pemetrexed, irinotecan or cisplatin in human tumour xenograft models."( Anti-tumour and anti-vascular effects of cediranib (AZD2171) alone and in combination with other anti-tumour therapies.
Jürgensmeier, JM; Kendrew, J; Logié, A; Odedra, R; Ogilvie, DJ; Pearsall, S; Taylor, PJ; Wedge, SR, 2013
)
0.39
" A combination of cediranib with gefitinib also induced tumour regressions, and cediranib combined with either gemcitabine or irinotecan was found to inhibit tumour growth profoundly (by 99 and 98 %, respectively)."( Anti-tumour and anti-vascular effects of cediranib (AZD2171) alone and in combination with other anti-tumour therapies.
Jürgensmeier, JM; Kendrew, J; Logié, A; Odedra, R; Ogilvie, DJ; Pearsall, S; Taylor, PJ; Wedge, SR, 2013
)
0.39
" In xenograft models, while gefitinib induced marked regression via apoptosis of tumors without the BIM polymorphism, its combination with vorinostat was needed to induce marked regression of tumors with the BIM polymorphism in the same manner."( EGFR-TKI resistance due to BIM polymorphism can be circumvented in combination with HDAC inhibition.
Ebi, H; Hasegawa, Y; Ishikawa, D; Nakagawa, T; Nanjo, S; Sano, T; Sato, M; Sekido, Y; Takeuchi, S; Yamada, T; Yano, S, 2013
)
0.39
" Rutaecarpine has been used in combination with other drugs in the treatment of disorders and found to produce herb-drug interactions."( Rutaecarpine effects on expression of hepatic phase-1, phase-2 metabolism and transporter genes as a basis of herb-drug interactions.
Jin, T; Liu, J; Lu, YF; Wu, Q; Zhang, D; Zhu, QN, 2013
)
0.39
"The results from a phase III trial conducted outside of Japan demonstrated a significant improvement in time to progression (TTP) when lapatinib was combined with capecitabine compared with capecitabine alone in patients with HER2-positive advanced or metastatic breast cancer."( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study.
Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015
)
0.42
"Lapatinib in combination with capecitabine was well tolerated in the 51 patients enrolled in this study."( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study.
Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015
)
0.42
"Lapatinib in combination with capecitabine in Japanese HER2-positive breast cancer patients was well tolerated."( Efficacy, safety, pharmacokinetics and biomarker findings in patients with HER2-positive advanced or metastatic breast cancer treated with lapatinib in combination with capecitabine: results from 51 Japanese patients treated in a clinical study.
Ellis, CE; Fujii, H; Gagnon, RC; Iwata, H; Katsura, K; Masuda, N; Mukai, H; Nakamura, S; Nishimura, Y, 2015
)
0.42
" Metformin is a widely used antidiabetic drug and also displays significant growth-inhibitory and proapoptotic effects in several cancer models, alone or in combination with chemotherapeutic drugs."( Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines.
Ciardiello, F; D'Aiuto, E; De Palma, R; De Vita, F; Della Corte, CM; Martinelli, E; Morgillo, F; Orditura, M; Sasso, FC; Troiani, T; Vitagliano, D, 2013
)
0.39
" However, further studies are required to investigate better the effect of metformin action on the RAS/RAF/MAPK pathway and the best context in which to use metformin in combination with molecular targeted agents."( Synergistic effects of metformin treatment in combination with gefitinib, a selective EGFR tyrosine kinase inhibitor, in LKB1 wild-type NSCLC cell lines.
Ciardiello, F; D'Aiuto, E; De Palma, R; De Vita, F; Della Corte, CM; Martinelli, E; Morgillo, F; Orditura, M; Sasso, FC; Troiani, T; Vitagliano, D, 2013
)
0.39
"Tyrosine kinase inhibitors (TKIs) have revolutionized the treatment of lung adenocarcinoma, and a theoretical basis exists for utilising whole brain radiotherapy (WBRT) combined with erlotinib for the treatment for brain metastases in patients with lung adenocarcinoma."( The theoretical foundation and research progress for WBRT combined with erlotinib for the treatment of multiple brain metastases in patients with lung adenocarcinoma.
Wang, J; Wang, P; Yuan, Z; Zhao, L; Zhuang, H, 2013
)
0.39
" Here we report the first phase 2 study of erlotinib in combination with adjuvant chemoradiation and chemotherapy for resected PDAC."( Phase 2 study of erlotinib combined with adjuvant chemoradiation and chemotherapy in patients with resectable pancreatic cancer.
Blackford, AL; Cameron, JL; Choti, MA; De Jesus-Acosta, A; Donehower, RC; Edil, BH; Ellsworth, S; Fan, KY; Hacker-Prietz, A; Herman, JM; Hidalgo, M; Hruban, RH; Laheru, DA; Le, DT; Pawlik, TM; Schulick, RD; Wild, AT; Wolfgang, CL; Wood, LD; Zheng, L, 2013
)
0.39
"Erlotinib can be safely administered with adjuvant IMRT-based CRT and chemotherapy."( Phase 2 study of erlotinib combined with adjuvant chemoradiation and chemotherapy in patients with resectable pancreatic cancer.
Blackford, AL; Cameron, JL; Choti, MA; De Jesus-Acosta, A; Donehower, RC; Edil, BH; Ellsworth, S; Fan, KY; Hacker-Prietz, A; Herman, JM; Hidalgo, M; Hruban, RH; Laheru, DA; Le, DT; Pawlik, TM; Schulick, RD; Wild, AT; Wolfgang, CL; Wood, LD; Zheng, L, 2013
)
0.39
" In conclusion, p38 MAPK phosphorylation may be a prognostic marker for high-grade glioma patients, and vandetanib combined with a p38 MAPK inhibitor may be useful combination chemotherapy for glioma patients."( Vandetanib combined with a p38 MAPK inhibitor synergistically reduces glioblastoma cell survival.
Alafuzoff, I; Bergqvist, M; Blomquist, E; Edqvist, PH; Ekman, S; Gullbo, J; Jaiswal, A; Johansson, F; Lennartsson, J; Navani, S; Pontén, F; Popova, S; Sooman, L; Tsakonas, G, 2013
)
0.39
" Taken together, these data indicate that CH5164840 has potent antitumor activity and is highly effective in combination with erlotinib against NSCLC tumors with EGFR overexpression and mutations."( Enhanced antitumor activity of erlotinib in combination with the Hsp90 inhibitor CH5164840 against non-small-cell lung cancer.
Aoki, Y; Fujii, T; Ishii, N; Kondoh, O; Mio, T; Ono, N; Sakata, K; Suda, A; Tsukaguchi, T; Tsukuda, T; Yamazaki, T, 2013
)
0.39
"This phase IB, open-label, dose-escalation study evaluated the safety, tolerability, and optimally tolerated regimen (OTR) of lapatinib in combination with docetaxel and trastuzumab in patients with previously untreated stage IV metastatic breast cancer (MBC) tumors overexpressing human epidermal growth factor receptor 2 (HER2)."( Optimally tolerated dose of lapatinib in combination with docetaxel plus trastuzumab in first-line treatment of HER2-positive metastatic breast cancer.
Burris, HA; Crown, J; DeSilvio, M; Diéras, V; Espie, M; Kennedy, MJ; Koch, KM; Kothari, D; Lau, MR; Marty, M; Tresca, P, 2013
)
0.39
"A randomized, phase III, placebo-controlled, partially blinded clinical trial (REGAL [Recent in in Glioblastoma Alone and With Lomustine]) was conducted to determine the efficacy of cediranib, an oral pan-vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor, either as monotherapy or in combination with lomustine versus lomustine in patients with recurrent glioblastoma."( Phase III randomized trial comparing the efficacy of cediranib as monotherapy, and in combination with lomustine, versus lomustine alone in patients with recurrent glioblastoma.
Ashby, LS; Batchelor, TT; Campone, M; Cher, L; Degroot, J; Gattamaneni, R; Jain, RK; Jürgensmeier, JM; Liu, Q; Mason, W; Mikkelsen, T; Mulholland, P; Nabors, LB; Neyns, B; Payer, F; Phuphanich, S; Rosenthal, M; Sorensen, AG; van den Bent, M; Wick, A; Xu, J, 2013
)
0.39
"This study did not meet its primary end point of PFS prolongation with cediranib either as monotherapy or in combination with lomustine versus lomustine in patients with recurrent glioblastoma, although cediranib showed evidence of clinical activity on some secondary end points including time to deterioration in neurologic status and corticosteroid-sparing effects."( Phase III randomized trial comparing the efficacy of cediranib as monotherapy, and in combination with lomustine, versus lomustine alone in patients with recurrent glioblastoma.
Ashby, LS; Batchelor, TT; Campone, M; Cher, L; Degroot, J; Gattamaneni, R; Jain, RK; Jürgensmeier, JM; Liu, Q; Mason, W; Mikkelsen, T; Mulholland, P; Nabors, LB; Neyns, B; Payer, F; Phuphanich, S; Rosenthal, M; Sorensen, AG; van den Bent, M; Wick, A; Xu, J, 2013
)
0.39
"The aim of this explorative phase II study was to evaluate the activity and safety of lapatinib in combination with intravenous vinorelbine in women with HER2 positive metastatic or recurrent breast cancer."( Phase II study of lapatinib in combination with vinorelbine in patients with HER2 positive recurrent or metastatic breast cancer: a multicentric Turkish Oncology Group (TOG) trial.
Basaran, G; Benekli, M; Cetin, B; Eralp, Y; Isikdogan, A; Karaca, H; Kucukoner, M; Onur, H; Ozkan, M; Saip, P; Sen, F; Un, O, 2013
)
0.39
" The TASK study evaluated the efficacy and safety of the epidermal growth factor receptor tyrosine kinase inhibitor erlotinib in combination with the anti-angiogenic agent bevacizumab as first-line therapy in unselected, advanced non-squamous NSCLC patients."( A phase II study of erlotinib in combination with bevacizumab versus chemotherapy plus bevacizumab in the first-line treatment of advanced non-squamous non-small cell lung cancer.
Amoroso, D; Chao, TY; Chung, CY; Ciuleanu, T; Groen, HJ; Heo, DS; Klingelschmitt, G; Klughammer, B; Middleton, G; Milanowski, J; Szczesna, A; Thatcher, N; Tsai, CM; Tsao, CJ; Zeaiter, A, 2013
)
0.39
" These results combined with the worse outcomes observed in MET-negative patients treated with onartuzumab highlight the importance of diagnostic testing in drug development."( Randomized phase II trial of Onartuzumab in combination with erlotinib in patients with advanced non-small-cell lung cancer.
Barlesi, F; Blumenschein, GR; Daniel, DB; Ervin, TJ; Godbert, B; Goldschmidt, JH; Govindan, R; Krzakowski, MJ; Orlov, SV; Patel, PH; Patel, T; Peterson, AC; Phan, SC; Ramlau, RA; Robinet, G; Spigel, DR; Wertheim, MS; Yauch, RL; Yu, W; Zha, J, 2013
)
0.39
" In addition, we aimed to explore differences in drug-drug interactions across multiple GBM-derived cell cultures and predict such differences by use of transcriptional biomarkers."( Comparative drug pair screening across multiple glioblastoma cell lines reveals novel drug-drug interactions.
Baskaran, S; Forsberg Nilsson, K; Gerlee, P; Häggblad, M; Hansson, C; Karlsson-Lindahl, L; Kling, T; Lundgren, B; Martens, U; Monsefi, N; Nelander, S; Olsson, M; Schmidt, L; Uhrbom, L; Westermark, B, 2013
)
0.39
"We performed a screen in which we quantified drug-drug interactions for 465 drug pairs in each of the 5 GBM cell lines U87MG, U343MG, U373MG, A172, and T98G."( Comparative drug pair screening across multiple glioblastoma cell lines reveals novel drug-drug interactions.
Baskaran, S; Forsberg Nilsson, K; Gerlee, P; Häggblad, M; Hansson, C; Karlsson-Lindahl, L; Kling, T; Lundgren, B; Martens, U; Monsefi, N; Nelander, S; Olsson, M; Schmidt, L; Uhrbom, L; Westermark, B, 2013
)
0.39
"Clinical data of 45 patients with advanced NSCLC who received local radiotherapy combined with EGFR-TKI after solitary progression were reviewed and analyzed."( [Local treatment combined with EGFR-TKIs for advanced non-small cell lung cancer with solitary progression during EGFR-TKI treatment].
Chen, S; Hao, X; Li, J; Lin, L; Shi, Y; Wang, B; Zhang, X, 2013
)
0.39
"Local therapies combined with EGFR-TKIs can prolong the PFS of patients with NSCLC who exhibited solitary progression during EGFR-TKI treatment."( [Local treatment combined with EGFR-TKIs for advanced non-small cell lung cancer with solitary progression during EGFR-TKI treatment].
Chen, S; Hao, X; Li, J; Lin, L; Shi, Y; Wang, B; Zhang, X, 2013
)
0.39
"The purpose of the current study was to assess a novel anti-cancer drug, MPT0B014, which is not a substrate for the P-glycoprotein (P-gp) transporter, alone and in combination with erlotinib, against human non-small cell lung cancer (NSCLC)."( In vitro and in vivo anti-tumour effects of MPT0B014, a novel derivative aroylquinoline, and in combination with erlotinib in human non-small-cell lung cancer cells.
Liou, JP; Pai, HC; Pan, SL; Teng, CM; Tsai, AC; Wang, CY; Wang, JC, 2014
)
0.4
" B014 in combination with erlotinib caused significant tumour inhibition in vitro and in vivo."( In vitro and in vivo anti-tumour effects of MPT0B014, a novel derivative aroylquinoline, and in combination with erlotinib in human non-small-cell lung cancer cells.
Liou, JP; Pai, HC; Pan, SL; Teng, CM; Tsai, AC; Wang, CY; Wang, JC, 2014
)
0.4
" Combined with the EGF receptor inhibitor, erlotinib, MPT0B014 exerted significant growth inhibition of A549 cells both in vitro and in vivo."( In vitro and in vivo anti-tumour effects of MPT0B014, a novel derivative aroylquinoline, and in combination with erlotinib in human non-small-cell lung cancer cells.
Liou, JP; Pai, HC; Pan, SL; Teng, CM; Tsai, AC; Wang, CY; Wang, JC, 2014
)
0.4
"Japanese patients with advanced/metastatic NSCLC received tivantinib in combination with erlotinib to evaluate safety and pharmacokinetics."( CYP2C19 genotype-based phase I studies of a c-Met inhibitor tivantinib in combination with erlotinib, in advanced/metastatic non-small cell lung cancer.
Akinaga, S; Fujisaka, Y; Hayashi, H; Hirashima, T; Miyoshi, K; Murakami, H; Nakagawa, K; Satouchi, M; Takahashi, T; Takeda, K; Yamamoto, N, 2013
)
0.39
"Tivantinib, when combined with erlotinib, was well tolerated up to 360 mg BID for EMs and 240 mg BID for PMs, respectively."( CYP2C19 genotype-based phase I studies of a c-Met inhibitor tivantinib in combination with erlotinib, in advanced/metastatic non-small cell lung cancer.
Akinaga, S; Fujisaka, Y; Hayashi, H; Hirashima, T; Miyoshi, K; Murakami, H; Nakagawa, K; Satouchi, M; Takahashi, T; Takeda, K; Yamamoto, N, 2013
)
0.39
"Two doses of tivantinib in combination with erlotinib were recommended based on CYP2C19 genotype: 360 mg BID for EMs and 240 mg BID for PMs."( CYP2C19 genotype-based phase I studies of a c-Met inhibitor tivantinib in combination with erlotinib, in advanced/metastatic non-small cell lung cancer.
Akinaga, S; Fujisaka, Y; Hayashi, H; Hirashima, T; Miyoshi, K; Murakami, H; Nakagawa, K; Satouchi, M; Takahashi, T; Takeda, K; Yamamoto, N, 2013
)
0.39
" A potential pharmacokinetic drug-drug interaction was also investigated."( Phase I dose-escalation study of oral vinflunine in combination with erlotinib in pre-treated and unselected EGFR patients with locally advanced or metastatic non-small-cell lung cancer.
Bennouna, J; Dansin, E; Favrel, S; Hiret, S; Kowalski, D; Krzakowski, M; Penel, N; Tourani, JM, 2014
)
0.4
" As afatinib is not a relevant modulator or substrate of cytochrome P450 enzymes, the drug-drug interaction potential is considered to be low."( Pharmacokinetic drug interactions of afatinib with rifampicin and ritonavir.
Bertulis, J; Brand, T; Gansser, D; Giessmann, T; Hocke, J; Jungnik, A; Marzin, K; Stopfer, P; Wind, S, 2014
)
0.4
" This combination was highly active with a treatment response lasting for 9 months supporting the hypothesis that EGFR monoclonal antibodies in combination with chemotherapy may play a role in reversing EGFR-TKI resistance in EGFR mutation-positive NSCLC."( Overcoming resistance to first generation EGFR TKIs with cetuximab in combination with chemotherapy in an EGFR mutated advanced stage NSCLC patient.
Fiegl, M; Hilbe, W; Manzl, C; Pircher, A; Pirker, R; Popper, H, 2014
)
0.4
"Panobinostat, a histone deacetylase (HDAC) inhibitor, enhances antiproliferative activity in non-small cell lung cancer (NSCLC) cell lines when combined with erlotinib."( A phase I, pharmacokinetic, and pharmacodynamic study of panobinostat, an HDAC inhibitor, combined with erlotinib in patients with advanced aerodigestive tract tumors.
Akar, A; Altiok, S; Bepler, G; Chiappori, A; Gray, JE; Haura, E; Kish, JA; Kreahling, J; Lush, R; Neuger, A; Pinder-Schenck, M; Schell, MJ; Tanvetyanon, T; Tetteh, L; Williams, CC; Zhao, X, 2014
)
0.4
" In a PIK3CA-mutant HER2+ xenograft, PI3K inhibition with BKM120 in combination with lapatinib and trastuzumab was required to achieve tumor regression."( Direct inhibition of PI3K in combination with dual HER2 inhibitors is required for optimal antitumor activity in HER2+ breast cancer cells.
Arteaga, CL; Chanthaphaychith, S; Dahlman, K; Rexer, BN, 2014
)
0.4
" Secondary objectives included evaluation of safety, toxicity and pharmacokinetics of LY2584702 in combination with erlotinib or everolimus."( A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.
Benhadji, KA; Brail, LH; Bumgardner, W; Cohen, EE; Hollebecque, A; Houédé, N; Italiano, A; Massard, C; Miller, J; Soria, JC; Westwood, P, 2014
)
0.4
"Patients with advanced solid tumours were treated with a total daily dose of 50-200mg of LY2584702 in combination with erlotinib 150 mg once daily (Arm A) or everolimus 10mg once daily (Arm B)."( A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.
Benhadji, KA; Brail, LH; Bumgardner, W; Cohen, EE; Hollebecque, A; Houédé, N; Italiano, A; Massard, C; Miller, J; Soria, JC; Westwood, P, 2014
)
0.4
" Exposure of erlotinib increased when administered in combination with LY2584702."( A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.
Benhadji, KA; Brail, LH; Bumgardner, W; Cohen, EE; Hollebecque, A; Houédé, N; Italiano, A; Massard, C; Miller, J; Soria, JC; Westwood, P, 2014
)
0.4
"LY2584702 was not well tolerated when administered with erlotinib, therefore this combination is not feasible."( A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.
Benhadji, KA; Brail, LH; Bumgardner, W; Cohen, EE; Hollebecque, A; Houédé, N; Italiano, A; Massard, C; Miller, J; Soria, JC; Westwood, P, 2014
)
0.4
"A phase 1 study of pazopanib alone or in combination with lapatinib was conducted to assess the safety, tolerability, and pharmacokinetics of these oral tyrosine kinase inhibitors in Japanese patients with solid tumors."( Phase 1 study of pazopanib alone or combined with lapatinib in Japanese patients with solid tumors.
Ando, Y; Araki, K; Inada-Inoue, M; Ishida, H; Kawada, K; Mitsuma, A; Mizuno, K; Nagamatsu, K; Nagashima, F; Sasaki, Y; Sawaki, M; Sunakawa, Y; Takekura, A; Yamashita, K; Yokoyama, T, 2014
)
0.4
"The primary objectives of this phase I study were to evaluate the safety and maximum tolerated dose (MTD) of SAR245409, a pan-class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin inhibitor, combined with erlotinib in patients with advanced solid tumors."( Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors.
Cohen, RB; Engelman, JA; Felip, E; Jänne, PA; Laird, AD; Macé, S; Martinez, P; Rockich, K; Ruiz-Soto, R; Shapiro, GI; Xu, J, 2014
)
0.4
" SAR245409 30, 50, 70, or 90 mg once daily (QD) or 20 or 30 mg twice daily (BID) was administered, in combination with erlotinib 100 mg QD, in 28-day cycles."( Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors.
Cohen, RB; Engelman, JA; Felip, E; Jänne, PA; Laird, AD; Macé, S; Martinez, P; Rockich, K; Ruiz-Soto, R; Shapiro, GI; Xu, J, 2014
)
0.4
"The MTDs of SAR245409, in combination with erlotinib 100 mg QD, were 70 mg QD and 20 mg BID."( Phase I safety and pharmacokinetic study of the PI3K/mTOR inhibitor SAR245409 (XL765) in combination with erlotinib in patients with advanced solid tumors.
Cohen, RB; Engelman, JA; Felip, E; Jänne, PA; Laird, AD; Macé, S; Martinez, P; Rockich, K; Ruiz-Soto, R; Shapiro, GI; Xu, J, 2014
)
0.4
" A stronger inhibitory effect was observed when CUS was combined with gefitinib."( PANC-1 pancreatic cancer cell growth inhibited by cucurmosin alone and in combination with an epidermal growth factor receptor-targeted drug.
Chen, M; Huang, H; Wang, C; Xie, J; Yang, A; Yin, Q; Zhang, B, 2014
)
0.4
" The drug-drug interactions (DDIs) between simotinib and other drugs in combination and the underlying mechanism of its gastrointestinal toxicity remain unclear."( Drug interaction studies reveal that simotinib upregulates intestinal absorption by increasing the paracellular permeability of intestinal epithelial cells.
Cheng, Z; Li, P; Liu, Z; Zhu, Q, 2014
)
0.4
"The effects of the dipeptidyl peptidase-4 (DPP-4) inhibitor, linagliptin, alone and in combination with voglibose or exendin-4, on glycaemic control and body weight were assessed in an animal model of type 2 diabetes."( Effect of linagliptin, alone and in combination with voglibose or exendin-4, on glucose control in male ZDF rats.
Cheetham, SC; Headland, KR; Jones, RB; Klein, T; Mark, M; Vickers, SP, 2014
)
0.4
" Results of a previous phase 1 trial of the EGFR inhibitor erlotinib combined with cisplatin-based CRT (E + CRT) recommended a phase 2 erlotinib dose of 150 mg/day."( Phase 2 trial of erlotinib combined with cisplatin and radiotherapy in patients with locally advanced cervical cancer.
Alves, FV; Carmo, CC; Erlich, F; Ferreira, CG; Grazziotin, R; Mamede, M; Moralez, G; Nogueira-Rodrigues, A; Small, IA; Triginelli, SA; Viegas, C, 2014
)
0.4
" Patients received erlotinib at a dose of 150 mg/day 1 week before and in combination with cisplatin (40 mg/m(2) administered weekly for 5 cycles) and radiotherapy (4500 centigrays in 25 fractions), followed by brachytherapy (4 fractions at a dose of 600 centigrays weekly)."( Phase 2 trial of erlotinib combined with cisplatin and radiotherapy in patients with locally advanced cervical cancer.
Alves, FV; Carmo, CC; Erlich, F; Ferreira, CG; Grazziotin, R; Mamede, M; Moralez, G; Nogueira-Rodrigues, A; Small, IA; Triginelli, SA; Viegas, C, 2014
)
0.4
" Finally, this study demonstrated that MPT0B271 in combination with erlotinib significantly inhibits the growth of the human non-small cell lung cancer A549 cells as compared with erlotinib treatment alone, both in vitro and in vivo."( Orally active microtubule-targeting agent, MPT0B271, for the treatment of human non-small cell lung cancer, alone and in combination with erlotinib.
Chang, JY; Hsiao, CJ; Liou, JP; Pai, HC; Pan, SL; Teng, CM; Tsai, AC; Wang, CY; Wang, JC, 2014
)
0.4
" This randomized phase 2 trial evaluated apricoxib, a novel COX-2 inhibitor, in combination with erlotinib in biomarker-selected patients."( A randomized, placebo-controlled, multicenter, biomarker-selected, phase 2 study of apricoxib in combination with erlotinib in patients with advanced non-small-cell lung cancer.
Bernstein, E; Burrows, F; Gitlitz, BJ; Milne, G; Otterson, GA; Santos, ES; Syto, M; Zaknoen, S, 2014
)
0.4
"We assessed the maximum tolerated regimen (MTR) and dose-limiting toxicities of pazopanib and lapatinib in combination with weekly paclitaxel, and the effect of pazopanib and lapatinib on paclitaxel pharmacokinetics."( Phase I study of weekly paclitaxel in combination with pazopanib and lapatinib in advanced solid malignancies.
Bendell, J; Burris, HA; Dowlati, A; Infante, JR; Jones, SF; Kane, MP; Levinson, KT; Stein, MN; Suttle, AB; Tan, AR, 2014
)
0.4
"Pazopanib 400 mg per day and lapatinib 1000 mg per day can be combined with paclitaxel 80 mg m(-2) in 28-day cycles."( Phase I study of weekly paclitaxel in combination with pazopanib and lapatinib in advanced solid malignancies.
Bendell, J; Burris, HA; Dowlati, A; Infante, JR; Jones, SF; Kane, MP; Levinson, KT; Stein, MN; Suttle, AB; Tan, AR, 2014
)
0.4
" We investigated whether E7820 in combination with erlotinib, an EGFR-TKI, could overcome EGFR-TKI-resistance in the NSCLC cell lines A549 (KRAS; G12S), H1975 (EGFR; L858R/T790M), and H1650 (PTEN; loss, EGFR; exon 19 deletion), which are resistant to erlotinib."( Enhanced anti-angiogenic effect of E7820 in combination with erlotinib in epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer xenograft models.
Asada, M; Funahashi, Y; Ito, K; Semba, T; Uenaka, T; Wakabayashi, T, 2014
)
0.4
" This two-part Japanese study (NCT01003158) assessed the safety/tolerability of AZD8931 monotherapy in patients with advanced solid tumors and in combination with paclitaxel in female patients with advanced breast cancer."( Inhibition of EGFR, HER2 and HER3 signaling with AZD8931 alone and in combination with paclitaxel: phase i study in Japanese patients with advanced solid malignancies and advanced breast cancer.
Fujisaka, Y; Hayashi, H; Hayashi, N; Kawakami, H; Kurata, T; Nakagawa, K; Okamoto, W; Shin, E; Tsurutani, J, 2014
)
0.4
" No dose-limiting toxicities were observed for AZD8931 alone or combined with paclitaxel."( Inhibition of EGFR, HER2 and HER3 signaling with AZD8931 alone and in combination with paclitaxel: phase i study in Japanese patients with advanced solid malignancies and advanced breast cancer.
Fujisaka, Y; Hayashi, H; Hayashi, N; Kawakami, H; Kurata, T; Nakagawa, K; Okamoto, W; Shin, E; Tsurutani, J, 2014
)
0.4
"Although maximum tolerated dose was not confirmed for AZD8931, based on overall incidence of rash and diarrhea AEs in the 80 mg group, doses up to 60 mg bid as monotherapy and 40 mg bid combined with paclitaxel are the feasible AZD8931 doses in Japanese patients."( Inhibition of EGFR, HER2 and HER3 signaling with AZD8931 alone and in combination with paclitaxel: phase i study in Japanese patients with advanced solid malignancies and advanced breast cancer.
Fujisaka, Y; Hayashi, H; Hayashi, N; Kawakami, H; Kurata, T; Nakagawa, K; Okamoto, W; Shin, E; Tsurutani, J, 2014
)
0.4
" Erlotinib combined with pemetrexed/cisplatin may be effective in the treatment of LM in EGFR mutation patients after gefitinib failure."( Erlotinib in combination with pemetrexed/cisplatin for leptomeningeal metastases and cerebrospinal fluid drug concentrations in lung adenocarcinoma patients after gefitinib faliure.
Deng, Q; He, J; Liu, X; Xu, X; Yang, H; Yang, X; Zhang, Y; Zhao, M, 2015
)
0.42
" Image-based profiling and analysis led to the rapid discovery of a drug combination effective against TNBC in vitro and in vivo, and has the potential to lead to the development of new therapeutic options in other hard-to-treat cancers."( Computational analysis of image-based drug profiling predicts synergistic drug combinations: applications in triple-negative breast cancer.
Beck, D; Brandl, MB; Kavallaris, M; Li, F; Pasquier, E; Wong, ST; Zhang, S; Zhao, H, 2014
)
0.4
"In a 3 + 3 dose-escalation design, patients were given intravenous pemetrexed (500 mg/m(2)) on day 1 of a 21-day cycle (maximum 6 cycles), combined with continuous daily oral afatinib (schedule A [SA]; starting dose 30 mg, escalation to 50 mg) or pulsed-dose daily oral afatinib (schedule B [SB]; starting dose 50 mg, escalation to 70 mg) on days 1-6 of each 21-day cycle."( A phase I, dose-escalation trial of continuous- and pulsed-dose afatinib combined with pemetrexed in patients with advanced solid tumors.
Chand, VK; Chu, QS; Hirte, HW; Hotte, SJ; Sangha, R; Schnell, D; Sergenson, G, 2014
)
0.4
"Continuous- or pulsed-dose afatinib combined with pemetrexed exhibited a manageable safety profile."( A phase I, dose-escalation trial of continuous- and pulsed-dose afatinib combined with pemetrexed in patients with advanced solid tumors.
Chand, VK; Chu, QS; Hirte, HW; Hotte, SJ; Sangha, R; Schnell, D; Sergenson, G, 2014
)
0.4
"High EGFR gene copy number or activating EGFR mutations may identify patient subgroups who receive increased clinical benefit from vandetanib in combination with docetaxel in second-line NSCLC."( EGFR biomarkers predict benefit from vandetanib in combination with docetaxel in a randomized phase III study of second-line treatment of patients with advanced non-small cell lung cancer.
Herbst, RS; Heymach, JV; Johnson, BE; Lockwood, SJ; Ryan, AJ, 2014
)
0.4
" Cell cycle and cell apoptosis were assessed by flow cytometry (FCM) combined with PI staining and annexin V-FITC/PI, respectively."( [Inhibitory effect of norcantharidin combined with evodiamine on the growth of human hepatic carcinoma cell line HepG2 in vitro].
Liao, H; Liu, Y; You, Z; Zahng, J, 2014
)
0.4
"EVO combined with NCTD showed synergetic effect on anti-proliferation and pro-apoptosis in HepG2 cells."( [Inhibitory effect of norcantharidin combined with evodiamine on the growth of human hepatic carcinoma cell line HepG2 in vitro].
Liao, H; Liu, Y; You, Z; Zahng, J, 2014
)
0.4
" Inhibition of PARP-1 is tested in combination with DNA damaging agents such as topoisomerase I inhibitors or ionizing radiations (RT) for the treatment of glioblastoma (GBM)."( Effect of p53 activity on the sensitivity of human glioblastoma cells to PARP-1 inhibitor in combination with topoisomerase I inhibitor or radiation.
Carlomagno, C; Della Vittoria Scarpati, G; Ferrone, S; Fusciello, C; Leonardi, A; Pacelli, R; Pepe, S; Pepin, D; Poudel, R; Sabbatino, F; Somma, D, 2014
)
0.4
"Neratinib in combination with capecitabine had a manageable toxicity profile and showed promising antitumor activity in patients with HER2-positive metastatic breast cancer pretreated with trastuzumab and lapatinib."( Safety and efficacy of neratinib in combination with capecitabine in patients with metastatic human epidermal growth factor receptor 2-positive breast cancer.
Baselga, J; Cortés, J; Garcia-Saenz, JA; Germa, C; Harb, W; Kiger, C; Kim, SB; Martin, M; Moroose, R; Pluard, T; Saura, C; Wang, K; Xu, B, 2014
)
0.4
"The purpose of this study is to compare the efficacy and safety of Gefitinib versus VMP in combination with three-dimensional conformal radiotherapy (3D-CRT) for multiple brain metastases from non-small cell lung cancer (NSCLC)."( Comparison of Gefitinib versus VMP in the combination with radiotherapy for multiple brain metastases from non-small cell lung cancer.
Chen, S; Hao, Y; Li, B; Li, L; Liu, C; Ning, F; Wang, F; Yu, Z, 2015
)
0.42
" FW-04-806, a novel Hsp90 N-terminal inhibitor that disassociates the Hsp90/Cdc37/client complex and degrades Hsp90 clients, was studied alone or in combination with the EGFR/HER2 tyrosine kinase inhibitor lapatinib in HER2+ breast cancer cells."( Novel Hsp90 inhibitor FW-04-806 displays potent antitumor effects in HER2-positive breast cancer cells as a single agent or in combination with lapatinib.
Cao, PR; Huang, W; Kong, YL; Wu, QD; Xu, JH; Ye, M; Zhang, M; Zheng, W, 2015
)
0.42
"0) mm(3) in the cetuximab treatment group and 0 mm(3) in the cetuximab combined with icotinib group."( [Cetuximab in combination with icotinib overcomes the acquired resistance caused by EGFR T790M mutation in non-small cell lung cancer].
Chen, Y; Liu, J; Wang, C; Wang, M; Zhang, L; Zhao, X, 2014
)
0.4
"To analyze the efficacy and survival associated factors of gefitinib combined with cisplatin and gemcitabine for advanced non-small cell lung cancer."( Efficacy and survival-associated factors with gefitinib combined with cisplatin and gemcitabine for advanced non- small cell lung cancer.
Fang, H; Lin, RY; Sun, MX; Tian, Y; Wang, Q; Wang, XY; Yu, JL; Zhao, YL, 2014
)
0.4
"A total of 57 patients with advanced non-small cell lung cancer (NSCLC), who received platinum-based chemotherapy regimens for more than 1 cycle, were treated with gefitinib combined with cisplatin and gemcitabine until disease progression."( Efficacy and survival-associated factors with gefitinib combined with cisplatin and gemcitabine for advanced non- small cell lung cancer.
Fang, H; Lin, RY; Sun, MX; Tian, Y; Wang, Q; Wang, XY; Yu, JL; Zhao, YL, 2014
)
0.4
"Gefitinib combined with cisplatin andgemcitabine, is effective for patients with IIIb~IV NSCLC who received multiple cycles of chemotherapy."( Efficacy and survival-associated factors with gefitinib combined with cisplatin and gemcitabine for advanced non- small cell lung cancer.
Fang, H; Lin, RY; Sun, MX; Tian, Y; Wang, Q; Wang, XY; Yu, JL; Zhao, YL, 2014
)
0.4
" Ad-p53 combined with gefitinib was used in vivo to explore their effect on tumor xenograft in nude mice."( [Effect of recombinant human p53 adenovirus (Ad-p53) combined with EGFR inhibitor gefitinib on the sensitivity of breast cancer MDA-MB-468 cells].
Guan, X; Liu, Q; Wang, L; Wang, X; Xie, L; Yu, Z, 2014
)
0.4
"This phase I study evaluated the maximum tolerated dose (MTD), safety, pharmacokinetics (PK), and pharmacodynamics of pilaralisib (SAR245408), an oral pan-class I phosphoinositide 3-kinase (PI3K) inhibitor, in combination with erlotinib, an epidermal growth factor receptor (EGFR) inhibitor."( Phase I dose-escalation study of pilaralisib (SAR245408, XL147), a pan-class I PI3K inhibitor, in combination with erlotinib in patients with solid tumors.
Bahleda, R; Burris, H; Jiang, J; Lager, J; Liu, L; LoRusso, P; Macé, S; Martini, JF; Soria, JC, 2015
)
0.42
" In this study, we investigated erlotinib in combination with shikonin and 14 shikonin derivatives in parental U87MG and transfected U87MG."( Shikonin and its derivatives inhibit the epidermal growth factor receptor signaling and synergistically kill glioblastoma cells in combination with erlotinib.
Bauer, R; Efferth, T; Kretschmer, N; Zhao, Q, 2015
)
0.42
" We conducted a phase II trial to investigate the efficacy and safety of gefitinib when combined with bevacizumab as first-line therapy in patients with advanced NSCLC harboring EGFR gene mutations."( Phase II trial of gefitinib in combination with bevacizumab as first-line therapy for advanced non-small cell lung cancer with activating EGFR gene mutations: the Okayama Lung Cancer Study Group Trial 1001.
Aoe, K; Bessho, A; Chikamori, K; Fujii, M; Harada, D; Hisamoto-Sato, A; Hosokawa, S; Hotta, K; Ichihara, E; Kishino, D; Kiura, K; Kozuki, T; Kubo, T; Kuyama, S; Nogami, N; Oze, I; Tabata, M; Takigawa, N; Tanimoto, M; Ueoka, H, 2015
)
0.42
"Gefitinib in combination with bevacizumab as first-line therapy seems to be a favorable and well-tolerated treatment for patients with advanced NSCLC with activating EGFR gene mutations, especially those with EGFR exon 19 deletion mutations, although the primary end point was not met because the lower limit of the CI was less than 40%."( Phase II trial of gefitinib in combination with bevacizumab as first-line therapy for advanced non-small cell lung cancer with activating EGFR gene mutations: the Okayama Lung Cancer Study Group Trial 1001.
Aoe, K; Bessho, A; Chikamori, K; Fujii, M; Harada, D; Hisamoto-Sato, A; Hosokawa, S; Hotta, K; Ichihara, E; Kishino, D; Kiura, K; Kozuki, T; Kubo, T; Kuyama, S; Nogami, N; Oze, I; Tabata, M; Takigawa, N; Tanimoto, M; Ueoka, H, 2015
)
0.42
"These findings suggest the potential roles of HM781-36B as the treatment for EGFR-overexpressing colon cancer, singly or in combination with chemotherapeutic agents."( Antitumor Activity of HM781-36B, alone or in Combination with Chemotherapeutic Agents, in Colorectal Cancer Cells.
Kang, MH; Kim, JH; Kim, JW; Lee, HS; Lee, JS; Lee, KW; Moon, SU; Sung, JH, 2016
)
0.43
" For the future, drug combination therapies, including letermovir, might be indicated under special medical conditions, such as the emergence of multidrug-resistant virus strains in transplant recipients or in HCMV-HIV-coinfected patients."( In vitro drug combination studies of Letermovir (AIC246, MK-8228) with approved anti-human cytomegalovirus (HCMV) and anti-HIV compounds in inhibition of HCMV and HIV replication.
Lischka, P; Wildum, S; Zimmermann, H, 2015
)
0.42
" This study was carried out to identify the contribution percentage of CYP450 to icotinib and use the results to develop a physiologically based pharmacokinetic (PBPK) model, which can help to predict drug-drug interaction (DDI)."( Relative contributions of the major human CYP450 to the metabolism of icotinib and its implication in prediction of drug-drug interaction between icotinib and CYP3A4 inhibitors/inducers using physiologically based pharmacokinetic modeling.
Chen, J; Hu, P; Jiang, J; Liu, D; Zhao, Q; Zheng, X, 2015
)
0.42
" The purpose of the present trial is to determine whether CHM (Fuzheng Kang'ai decoction (FZKA), a CHM formula) combined with gefitinib results in longer progression-free survival with less toxicity than gefitinib alone."( Fuzheng Kang'ai decoction combined with gefitinib in advanced non-small cell lung cancer patients with epidermal growth factor receptor mutations: study protocol for a randomized controlled trial.
Cai, JZ; Deng, H; He, WF; Li, QP; Liao, GY; Long, SQ; Pan, ZQ; Wu, WY; Xiao, SJ; Yang, XB; Zhou, YS, 2015
)
0.42
" This trial is designed to determine if CHM (FZKA) combined with gefitinib results in longer progression-free survival with less toxicity than gefitinib alone."( Fuzheng Kang'ai decoction combined with gefitinib in advanced non-small cell lung cancer patients with epidermal growth factor receptor mutations: study protocol for a randomized controlled trial.
Cai, JZ; Deng, H; He, WF; Li, QP; Liao, GY; Long, SQ; Pan, ZQ; Wu, WY; Xiao, SJ; Yang, XB; Zhou, YS, 2015
)
0.42
" This study will provide objective evidence to evaluate the efficiency of CHM combined with gefitinib in NSCLC patients with EGFR mutations, and may provide a novel regimen for patients with NSCLC."( Fuzheng Kang'ai decoction combined with gefitinib in advanced non-small cell lung cancer patients with epidermal growth factor receptor mutations: study protocol for a randomized controlled trial.
Cai, JZ; Deng, H; He, WF; Li, QP; Liao, GY; Long, SQ; Pan, ZQ; Wu, WY; Xiao, SJ; Yang, XB; Zhou, YS, 2015
)
0.42
"To evaluate the safety and maximum tolerated dose (MTD) of afatinib combined with nintedanib."( A Phase I dose-escalation study of afatinib combined with nintedanib in patients with advanced solid tumors.
Gordon, MS; LoRusso, PM; Ould-Kaci, M; Springett, GM; Su, YB; Wind, S; Zhao, Y, 2015
)
0.42
" We report the first bench-to-bedside evidence that RET inhibitor combined with an mTOR inhibitor is active against brain-metastatic RET-rearranged lung cancer and the first evidence of blood-brain barrier penetration."( Systemic and CNS activity of the RET inhibitor vandetanib combined with the mTOR inhibitor everolimus in KIF5B-RET re-arranged non-small cell lung cancer with brain metastases.
Ali, SM; Berry, J; Cascone, T; Guha-Thakurta, N; Heymach, JV; McMahon, C; Miller, V; Pai, S; Roxas, M; Subbiah, IM; Subbiah, V; Tang, Z, 2015
)
0.42
" We designed a study of cediranib, a vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor, combined with cilengitide, an integrin inhibitor."( A phase I study of cediranib in combination with cilengitide in patients with recurrent glioblastoma.
Ahluwalia, MS; Batchelor, TT; Duda, DG; Gerstner, ER; Grossman, S; Jain, RK; Kaley, TJ; Levine, MA; Mikkelsen, T; Nabors, BL; Olson, JJ; Wen, PY; Ye, X, 2015
)
0.42
"Cediranib did not improve the progression-free survival of patients with advanced biliary tract cancer in combination with cisplatin and gemcitabine, which remains the standard of care."( Cediranib or placebo in combination with cisplatin and gemcitabine chemotherapy for patients with advanced biliary tract cancer (ABC-03): a randomised phase 2 trial.
Anthoney, DA; Backen, AC; Beare, S; Bridgewater, JA; Corrie, P; Cunningham, D; Dive, C; Duggan, M; Lopes, A; Madhusudan, S; Maraveyas, A; Morris, K; Palmer, DH; Rees, C; Ross, PJ; Steward, WP; Valle, JW; Wasan, H; Waters, JS, 2015
)
0.42
" We aimed to investigate the apoptotic and antiproliferative effects of CuB as a single agent and in combination with Gef on both HT-29 and HCT-116 cell lines."( Treatment with cucurbitacin B alone and in combination with gefitinib induces cell cycle inhibition and apoptosis via EGFR and JAK/STAT pathway in human colorectal cancer cell lines.
Alp, E; Elmazoglu, Z; Menevse, S; Yar Saglam, AS, 2016
)
0.43
" Using a panel of eleven patient-derived ovarian cancer xenografts (EOC-PDX) growing orthotopically in the peritoneal cavity of nude mice we investigated the effect of cediranib as monotherapy or in combination with chemotherapy on overall survival (primary endpoint, at euthanasia), and tumor dissemination and metastasis in the peritoneal cavity (secondary endpoint, interim analysis)."( Cediranib combined with chemotherapy reduces tumor dissemination and prolongs the survival of mice bearing patient-derived ovarian cancer xenografts with different responsiveness to cisplatin.
Belotti, D; Bettolini, R; Bizzaro, F; Cesca, M; Decio, A; Giavazzi, R; Porcu, L; Taraboletti, G; Ubezio, P, 2015
)
0.42
" We explored multiple intermittent dose levels of pazopanib combined with continuous daily dosing of lapatinib in patients with solid tumors."( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors.
Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015
)
0.42
"Every other day dosing of pazopanib combined with daily lapatinib was tolerated at the established MTD, but no complete or partial tumor responses were observed at these dose levels."( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors.
Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015
)
0.42
"We conducted a phase I trial of erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor, combined with amrubicin, a topoisomerase II inhibitor."( Phase I and pharmacokinetic study of erlotinib administered in combination with amrubicin in patients with previously treated, advanced non-small cell lung cancer.
Asakuma, M; Fukui, T; Hamada, A; Hayashi, N; Hiyoshi, Y; Igawa, S; Ishihara, M; Kasajima, M; Katagiri, M; Katono, K; Kimura, M; Kubota, M; Maki, S; Masuda, N; Mitsufuji, H; Otani, S; Ryuge, S; Saito, H; Sasaki, J; Takakura, A; Toyooka, I; Wada, M; Yamamoto, M; Yokoba, M, 2015
)
0.42
" No drug-drug interactions between erlotinib and amrubicin were observed in this study."( Phase I and pharmacokinetic study of erlotinib administered in combination with amrubicin in patients with previously treated, advanced non-small cell lung cancer.
Asakuma, M; Fukui, T; Hamada, A; Hayashi, N; Hiyoshi, Y; Igawa, S; Ishihara, M; Kasajima, M; Katagiri, M; Katono, K; Kimura, M; Kubota, M; Maki, S; Masuda, N; Mitsufuji, H; Otani, S; Ryuge, S; Saito, H; Sasaki, J; Takakura, A; Toyooka, I; Wada, M; Yamamoto, M; Yokoba, M, 2015
)
0.42
" Both drugs are mainly metabolized by CYP3A4, and drug-drug interactions are a major concern."( Phase I dose-finding and pharmacokinetic study of docetaxel and gefitinib in patients with advanced or metastatic non-small-cell lung cancer: evaluation of drug-drug interaction.
Ando-Makihara, R; Hayashi, Y; Makino, Y; Motonaga, M; Ohe, Y; Takano, M; Yamamoto, N, 2015
)
0.42
"The tolerability of 60 mg/m(2) docetaxel with 250 mg/day gefitinib was confirmed, and we observed no drug-drug interaction in this combination."( Phase I dose-finding and pharmacokinetic study of docetaxel and gefitinib in patients with advanced or metastatic non-small-cell lung cancer: evaluation of drug-drug interaction.
Ando-Makihara, R; Hayashi, Y; Makino, Y; Motonaga, M; Ohe, Y; Takano, M; Yamamoto, N, 2015
)
0.42
"PET-CT imaging with [(18)F]-gefitinib is a powerful tool to non-invasively assess potential ABCB1- and ABCG2-mediated drug-drug interactions (DDIs) in vivo."( PET-CT imaging with [(18)F]-gefitinib to measure Abcb1a/1b (P-gp) and Abcg2 (Bcrp1) mediated drug-drug interactions at the murine blood-brain barrier.
DeGroot, J; Jansen, HT; Kivits, S; Läppchen, T; Sio, CF; Steinbach, OC; van de Steeg, E; van der Hoorn, JW; van Driel, A; Vlaming, ML, 2015
)
0.42
"Oral afatinib was combined with intravenous paclitaxel (80mg/m(2); days 1, 8 and 15 every four weeks) starting at 20mg once daily and escalated to 40 and 50mg in successive cohorts of ⩾3 patients."( A phase I study of daily afatinib, an irreversible ErbB family blocker, in combination with weekly paclitaxel in patients with advanced solid tumours.
Ang, JE; de Bono, J; Harris, D; Kristeleit, R; Kyle, F; Pelling, K; Pemberton, K; Rudman, S; Schnell, D; Solca, F; Spicer, J; Suder, A; Uttenreuther-Fischer, M, 2015
)
0.42
"The MTD and recommended phase II dose of once-daily afatinib combined with paclitaxel 80mg/m(2) (days 1, 8 and 15 every four weeks) was 40mg."( A phase I study of daily afatinib, an irreversible ErbB family blocker, in combination with weekly paclitaxel in patients with advanced solid tumours.
Ang, JE; de Bono, J; Harris, D; Kristeleit, R; Kyle, F; Pelling, K; Pemberton, K; Rudman, S; Schnell, D; Solca, F; Spicer, J; Suder, A; Uttenreuther-Fischer, M, 2015
)
0.42
" Preclinical evidence suggests that the scheduling of bevacizumab may be crucial to optimize its combination with chemo-radiotherapy."( Critical role of bevacizumab scheduling in combination with pre-surgical chemo-radiotherapy in MRI-defined high-risk locally advanced rectal cancer: Results of the BRANCH trial.
Aloj, L; Avallone, A; Bianco, F; Botti, G; Budillon, A; Caracò, C; Comella, P; Delrio, P; Granata, V; Iaffaioli, VR; Leone, A; Marone, P; Muto, P; Pecori, B; Petrillo, A; Romano, C; Romano, G; Tatangelo, F, 2015
)
0.42
"These results highlights the relevance of bevacizumab scheduling to optimize its combination with preoperative chemo-radiotherapy in the management of LARC."( Critical role of bevacizumab scheduling in combination with pre-surgical chemo-radiotherapy in MRI-defined high-risk locally advanced rectal cancer: Results of the BRANCH trial.
Aloj, L; Avallone, A; Bianco, F; Botti, G; Budillon, A; Caracò, C; Comella, P; Delrio, P; Granata, V; Iaffaioli, VR; Leone, A; Marone, P; Muto, P; Pecori, B; Petrillo, A; Romano, C; Romano, G; Tatangelo, F, 2015
)
0.42
" This study aimed to evaluate the effect of metformin in combination with EGFR-TKI on the prognosis of non-small cell lung cancer (NSCLC) patients with diabetes mellitus type 2 (DM2)."( Synergistic effects of metformin in combination with EGFR-TKI in the treatment of patients with advanced non-small cell lung cancer and type 2 diabetes.
Cao, M; Chen, H; Chu, Q; Han, R; He, Y; Sun, J; Wang, D; Wang, Y; Yao, W, 2015
)
0.42
"To determine the maximum tolerated dose (MTD) of volasertib, a Polo-like kinase inhibitor, combined with afatinib, an oral irreversible ErbB family blocker, in patients with advanced solid tumors (NCT01206816; Study 1230."( A phase I study of volasertib combined with afatinib, in advanced solid tumors.
De Smet, M; Herremans, C; Liu, D; Machiels, JP; Peeters, M; Pilz, K; Rottey, S; Specenier, P; Strelkowa, N; Surmont, V, 2015
)
0.42
"Patients with advanced non-resectable and/or metastatic disease following failure of conventional treatment received intravenous volasertib 150-300 mg on day 1 every 21 days, combined with oral afatinib 30-40 mg on days 2-21 of a 3-week cycle (Schedule A), or 50-90 mg on days 2-6 of a 3-week cycle (Schedule B)."( A phase I study of volasertib combined with afatinib, in advanced solid tumors.
De Smet, M; Herremans, C; Liu, D; Machiels, JP; Peeters, M; Pilz, K; Rottey, S; Specenier, P; Strelkowa, N; Surmont, V, 2015
)
0.42
"Volasertib combined with afatinib had manageable adverse effects and limited antitumor activity in this heavily pretreated population."( A phase I study of volasertib combined with afatinib, in advanced solid tumors.
De Smet, M; Herremans, C; Liu, D; Machiels, JP; Peeters, M; Pilz, K; Rottey, S; Specenier, P; Strelkowa, N; Surmont, V, 2015
)
0.42
"Lapatinib has proven efficacy as monotherapy and in combination with capecitabine in patients with metastatic breast cancer (MBC) overexpressing HER2 and/or EGFR."( Phase I and pharmacological trial of lapatinib in combination with gemcitabine in patients with advanced breast cancer.
Beijnen, JH; Boss, DS; Grob, M; Huitema, AD; Keessen, M; Rehorst, H; Rosing, H; Schellens, JH; Smit, WM; Tibben, MM; van der Noll, R; Wymenga, AN, 2015
)
0.42
" The drug-drug molecular salt may have some bearing on the treatment of patient suffering from anticancer and hypertension."( Drug-Drug Molecular Salt Hydrate of an Anticancer Drug Gefitinib and a Loop Diuretic Drug Furosemide: An Alternative for Multidrug Treatment.
Badiger, MV; Gonnade, RG; Patwadkar, MV; Sahu, SK; Thorat, SH, 2015
)
0.42
" The secondary target that can afford the highest potential for clinical translation is the one with the highest synergy against tumor cells in combination with HER2-inhibition, allowing the widest therapeutic index for clinical translation."( Chemical probing of HER2-amplified cancer cells identifies TORC2 as a particularly effective secondary target for combination with lapatinib.
Amin, DN; Gulizia, N; Moasser, MM; Ruiz-Saenz, A, 2015
)
0.42
" In this context, alternatives to the lapatinib (L) and capecitabine (C) regimen, evaluating L combined with other cytotoxic drugs, are warranted."( A Phase II Randomized Study of Lapatinib Combined With Capecitabine, Vinorelbine, or Gemcitabine in Patients With HER2-Positive Metastatic Breast Cancer With Progression After a Taxane (Latin American Cooperative Oncology Group 0801 Study).
Barrios, CH; Bines, J; Blajman, C; Capó, A; Fanelli, M; Fein, L; Gómez, HL; Ismael, G; Lerzo, G; Mano, M; Martínez-Mesa, J; Neciosup, S; Nerón, Y; Pinczowski, H; Sampaio, C; Santi, PX; Tosello, C; Varela, MS; Werutsky, G; Zarba, JJ, 2016
)
0.43
"In the present phase II, multicenter study, patients with HER2(+) MBC with progression after taxane were randomized between L, 1250 mg, combined with C, 2000 mg/m(2) on days 1 to 14 (LC), vinorelbine (V), 25 mg/m(2) on days 1 and 8 (LV), or gemcitabine (G), 1000 mg/m(2) on days 1 and 8 (LG), every 21 days."( A Phase II Randomized Study of Lapatinib Combined With Capecitabine, Vinorelbine, or Gemcitabine in Patients With HER2-Positive Metastatic Breast Cancer With Progression After a Taxane (Latin American Cooperative Oncology Group 0801 Study).
Barrios, CH; Bines, J; Blajman, C; Capó, A; Fanelli, M; Fein, L; Gómez, HL; Ismael, G; Lerzo, G; Mano, M; Martínez-Mesa, J; Neciosup, S; Nerón, Y; Pinczowski, H; Sampaio, C; Santi, PX; Tosello, C; Varela, MS; Werutsky, G; Zarba, JJ, 2016
)
0.43
" The aims of this study are to investigate the inhibitory effects of TKIs on UDP-glucuronosyltransferase (UGT) activities, and to quantitatively evaluate their potential to cause drug-drug interactions (DDIs)."( Drug-Drug Interaction Potentials of Tyrosine Kinase Inhibitors via Inhibition of UDP-Glucuronosyltransferases.
Jeong, H; Liu, Y; Zhang, N, 2015
)
0.42
"Here we investigated the activity of afatinib, a second-generation irreversible pan-EGFR family kinase inhibitor, alone or in combination with ionizing radiation, toward pancreatic cancer cells."( Afatinib, an Irreversible EGFR Family Inhibitor, Shows Activity Toward Pancreatic Cancer Cells, Alone and in Combination with Radiotherapy, Independent of KRAS Status.
Favaudon, V; Fernet, M; Giocanti, N; Huguet, F; Larsen, AK, 2016
)
0.43
"In this study, we examined the effect of cetuximab (epidermal growth factor receptor monoclonal antibody) combined with afatinib (epidermal growth factor receptorand human epidermal growth factor receptor 2 tyrosine kinase irreversible inhibitor) on the apoptosis of A549 cells and on kinase domain receptor (KDR) and aquaporin 1 (AQP1) expression in A549 cells."( Effects of cetuximab combined with afatinib on the expression of KDR and AQP1 in lung cancer.
Liu, YH; Zhu, WL, 2015
)
0.42
" This phase I study evaluated the safety profile of vandetanib in combination with standard doses of gemcitabine and capecitabine in order to determine the maximum tolerated dose (MTD)."( Phase I trial of vandetanib in combination with gemcitabine and capecitabine in patients with advanced solid tumors with an expanded cohort in pancreatic and biliary cancers.
Bradshaw-Pierce, EL; Eckhardt, SG; Eppers, S; Freas, E; Kane, MA; Kessler, ER; Leong, S; Lieu, CH; Messersmith, WA; Nallapreddy, S; O'byrant, CL; Pitts, TM; Spratlin, J; Weekes, C, 2016
)
0.43
" The present study was set out to evaluate the efficacy and safety of vinorelbine when combined with lapatinib, an anti-HER2 tyrosine-kinase inhibitor, as late-line regimen administered beyond previous disease progression on prior lapatinib in patients with HER-2/neu- positive MBC."( Phase II study on the efficacy and safety of Lapatinib administered beyond disease progression and combined with vinorelbine in HER-2/neu- positive advanced breast cancer: results of the CECOG LaVie trial.
Bartsch, R; Brodowicz, T; Knittelfelder, R; Kuhar, CG; Lang, I; Melichar, B; Petruzelka, L; Singer, CF; Thallinger, C; Zielinski, C, 2016
)
0.43
"MK-2206 combined with lapatinib can be tolerated with both drugs above biologically active single-agent doses."( Phase I Study of an AKT Inhibitor (MK-2206) Combined with Lapatinib in Adult Solid Tumors Followed by Dose Expansion in Advanced HER2+ Breast Cancer.
Bell, MC; Burkard, ME; Eickhoff, J; Flynn, C; Kolesar, JM; Liu, G; Rampurwala, M; Tevaarwerk, AJ; Wisinski, KB, 2016
)
0.43
" The effect of afatinib, as either a single agent or in combination with gemcitabine (GEM), on tumor growth was determined using NPC tumor xenografts in mice."( In vitro and in vivo efficacy of afatinib as a single agent or in combination with gemcitabine for the treatment of nasopharyngeal carcinoma.
Fang, W; Tian, Y; Xue, C; Zhan, J; Zhang, J; Zhang, L; Zhao, Y, 2016
)
0.43
" Afatinib in combination with GEM demonstrated significant antitumor effect in an NPC xenograft model."( In vitro and in vivo efficacy of afatinib as a single agent or in combination with gemcitabine for the treatment of nasopharyngeal carcinoma.
Fang, W; Tian, Y; Xue, C; Zhan, J; Zhang, J; Zhang, L; Zhao, Y, 2016
)
0.43
" Using NSCLC cell lines with differential EGFR status, we examined the potency of PA-MSHA (Pseudomonas aeruginosa-mannose-sensitive hemagglutinin) in combination with Gefitinib on proliferation, apoptosis, cell cycle arrest, EGFR signaling and tumor growth."( PA-MSHA in combination with EGFR tyrosine kinase inhibitor: A new strategy to overcome the drug resistance of non-small cell lung cancer cells.
Cai, XW; Chang, JH; Fu, XL; Huang, QL; Liu, Q; Liu, ZB; Lu, YN; Pan, SY; Wang, JL; Wu, XH; Zhao, XM, 2016
)
0.43
" Methods The study comprised a 3 + 3 dose-escalation part for LY2875358 monotherapy in patients with advanced malignancies (Part A) followed by an assessment of LY2875358 in combination with erlotinib or gefitinib in patients with non-small cell lung cancer (Part B)."( A phase I dose-escalation study of LY2875358, a bivalent MET antibody, given as monotherapy or in combination with erlotinib or gefitinib in Japanese patients with advanced malignancies.
Doi, T; Enatsu, S; Kojima, T; Nakamura, T; Ohmatsu, H; Takahashi, H; Turner, K; Uenaka, K; Wacheck, V; Yoh, K; Zenke, Y, 2016
)
0.43
"Patients were randomized 1:1:1 to receive daily anastrozole (1 mg) in combination with AZD8931 20 mg twice daily (bid), AZD8931 40 mg bid, or placebo."( Inhibition of EGFR, HER2, and HER3 signaling with AZD8931 in combination with anastrozole as an anticancer approach: Phase II randomized study in women with endocrine-therapy-naïve advanced breast cancer.
Basik, M; Clemons, M; Cristofanilli, M; Dreosti, L; Grzeda, L; Hegg, R; Johnston, S; Lausoontornsiri, W; Mann, H; Stuart, M, 2016
)
0.43
"At the interim analysis, 359 patients were randomized and received anastrozole in combination with AZD8931 20 mg (n = 118), 40 mg (n = 120), or placebo (n = 121); 39 % of patients (n = 141) had a progression event."( Inhibition of EGFR, HER2, and HER3 signaling with AZD8931 in combination with anastrozole as an anticancer approach: Phase II randomized study in women with endocrine-therapy-naïve advanced breast cancer.
Basik, M; Clemons, M; Cristofanilli, M; Dreosti, L; Grzeda, L; Hegg, R; Johnston, S; Lausoontornsiri, W; Mann, H; Stuart, M, 2016
)
0.43
"AZD8931, in combination with endocrine therapy, does not appear to enhance endocrine responsiveness and is associated with greater skin and gastrointestinal toxicity."( Inhibition of EGFR, HER2, and HER3 signaling with AZD8931 in combination with anastrozole as an anticancer approach: Phase II randomized study in women with endocrine-therapy-naïve advanced breast cancer.
Basik, M; Clemons, M; Cristofanilli, M; Dreosti, L; Grzeda, L; Hegg, R; Johnston, S; Lausoontornsiri, W; Mann, H; Stuart, M, 2016
)
0.43
" We assessed the clinical relevance of this potential drug-drug interaction (DDI) in a retrospective cohort of EGFR-mutant NSCLC patients."( EGFR kinase inhibitors and gastric acid suppressants in EGFR-mutant NSCLC: a retrospective database analysis of potential drug interaction.
Asmat, A; Kumarakulasinghe, NB; Loy, EY; Pang, B; Soo, RA; Soon, YY; Syn, N; Zheng, H, 2016
)
0.43
"Intestinal P-gp and CYP3A4 work coordinately to reduce the intracellular concentration of drugs, and drug-drug interactions (DDIs) based on this interplay are of clinical importance and require pre-clinical investigation."( The consequence of regional gradients of P-gp and CYP3A4 for drug-drug interactions by P-gp inhibitors and the P-gp/CYP3A4 interplay in the human intestine ex vivo.
de Graaf, IA; de Jager, MH; Groothuis, GM; Li, M; van de Steeg, E, 2017
)
0.46
"Co-administration of antineoplastics with ART is challenging due to potential drug-drug interactions (DDIs)."( Use of a physiologically based pharmacokinetic model to simulate drug-drug interactions between antineoplastic and antiretroviral drugs.
Back, D; Clotet, B; Miranda, C; Moltó, J; Owen, A; Rajoli, R; Siccardi, M; Valle, M, 2017
)
0.46
" Thirteen different TKIs were combined with or without SZU-101 and studied to determine their effects on immunocytes."( Immunomodulatory and Antitumor Effects of a Novel TLR7 Agonist Combined with Lapatinib.
Diao, Y; Gao, N; Jiang, W; Jin, G; Jin, Z; Li, W; Liu, Y; Wang, X; Wang, Z; Zhong, J, 2016
)
0.43
" Despite a clear potential in inhibiting these proteins in ovarian cancer, as a single agent or in combination with a carboplatin treatment, we need to target kinases in tandem because of their capacity to trigger compensatory pathways that synergize to promote drug resistance."( Dasatinib + Gefitinib, a non platinum-based combination with enhanced growth inhibitory, anti-migratory and anti-invasive potency against human ovarian cancer cells.
Jean-Claude, B; Thibault, B, 2017
)
0.46
"Here we target EGFR, c-Src and Met individually or in combination with carboplatin, using Gefitinib, Dasatinib and Crizotinib respectively, in a panel of carboplatin-sensitive (OVCAR-3, IGROV-1 and A2780) and carboplatin-resistant cells (SKOV-3 and EFO-21)."( Dasatinib + Gefitinib, a non platinum-based combination with enhanced growth inhibitory, anti-migratory and anti-invasive potency against human ovarian cancer cells.
Jean-Claude, B; Thibault, B, 2017
)
0.46
"Crizotinib, Dasatinib and Gefitinib, alone or in combination with carboplatin, showed a cell-specific cytotoxic synergy in ovarian cancer cells."( Dasatinib + Gefitinib, a non platinum-based combination with enhanced growth inhibitory, anti-migratory and anti-invasive potency against human ovarian cancer cells.
Jean-Claude, B; Thibault, B, 2017
)
0.46
" The primary end point established the maximum tolerated dose in combination with cisplatin-pemetrexed in a dose deescalation scheme."( Phase I Trial of Cediranib in Combination with Cisplatin and Pemetrexed in Chemonaive Patients with Unresectable Malignant Pleural Mesothelioma (SWOG S0905).
Gandara, DR; Kalemkerian, GP; Kelly, K; Moon, J; Redman, MW; Tsao, AS; Vogelzang, NJ; Wistuba, II, 2017
)
0.46
"Cediranib combined with cisplatin-pemetrexed has a reasonable toxicity profile and preliminary promising efficacy."( Phase I Trial of Cediranib in Combination with Cisplatin and Pemetrexed in Chemonaive Patients with Unresectable Malignant Pleural Mesothelioma (SWOG S0905).
Gandara, DR; Kalemkerian, GP; Kelly, K; Moon, J; Redman, MW; Tsao, AS; Vogelzang, NJ; Wistuba, II, 2017
)
0.46
" In MDA-MB-468 and HCC1806 orthotopic TNBC xenograft tumors in nude mice, the drug combination inhibited tumor growth and prolonged mouse survival, although this effect was not significant for the gefitinib-resistant cell line HCC70."( Inhibition of basal-like breast cancer growth by FTY720 in combination with epidermal growth factor receptor kinase blockade.
Baxter, RC; Boyle, FM; de Silva, HC; Julovi, SM; Lin, MZ; Martin, JL, 2017
)
0.46
"PIKHER2 phase IB study aimed primarily to determine a maximum tolerated dose (MTD) and propose a recommended phase II dose (RP2D) for buparlisib in combination with lapatinib in HER2-positive, trastuzumab-resistant, advanced breast cancer."( PIKHER2: A phase IB study evaluating buparlisib in combination with lapatinib in trastuzumab-resistant HER2-positive advanced breast cancer.
Autret, A; Bertucci, F; Boher, JM; Camerlo, J; Campone, M; Charafe-Jauffret, E; Extra, JM; Gonçalves, A; Guerin, M; Hervieu, A; Isambert, N; Lokiec, F; Pakradouni, J; Provansal, M; Rezai, K; Sabatier, R; Viens, P, 2017
)
0.46
" There was no significant evidence for drug-drug PK interaction."( PIKHER2: A phase IB study evaluating buparlisib in combination with lapatinib in trastuzumab-resistant HER2-positive advanced breast cancer.
Autret, A; Bertucci, F; Boher, JM; Camerlo, J; Campone, M; Charafe-Jauffret, E; Extra, JM; Gonçalves, A; Guerin, M; Hervieu, A; Isambert, N; Lokiec, F; Pakradouni, J; Provansal, M; Rezai, K; Sabatier, R; Viens, P, 2017
)
0.46
" To date, systematic studies on the pharmacokinetic drug-drug interaction of icotinib were limited."( Metabolic Pathway of Icotinib In Vitro: The Differential Roles of CYP3A4, CYP3A5, and CYP1A2 on Potential Pharmacokinetic Drug-Drug Interaction.
Li, Z; Lu, C; Ma, L; Wang, J; Zhang, K; Zhang, T; Zhang, Y; Zhu, M; Zhuang, X, 2018
)
0.48
" These results suggest that letermovir may be a perpetrator of CYP2C9/19-mediated drug-drug interactions."( Pharmacokinetics and Tolerability of Letermovir Coadministered With Azole Antifungals (Posaconazole or Voriconazole) in Healthy Subjects.
Butterton, JR; Cho, CR; de Haes, JIU; Drexel, M; Hulskotte, EGJ; Hussaini, A; Iwamoto, M; Jordan, HR; Kantesaria, BS; Liu, F; Macha, S; Marshall, WL; McCrea, JB; Menzel, K; Tsai, C; van Schanke, A, 2018
)
0.48
" These results were used to inform the US prescribing information in the absence of clinical drug-drug interaction studies."( PBPK Modeling Strategy for Predicting Complex Drug Interactions of Letermovir as a Perpetrator in Support of Product Labeling.
Chen, D; Cho, CR; Hartmann, G; Menzel, K; Wang, YH, 2019
)
0.51
" Tyrosine kinase inhibitors (TKIs), including erlotinib and gefitinib, which block the action of the human epidermal growth factor receptor type 1 receptor, provide small increases in patient survival when administered with gemcitabine."( Targeting retinoblastoma protein phosphorylation in combination with EGFR inhibition in pancreatic cancer cells.
Abraham, RG; Dedi, B; Krucher, NA; Thomas, NA, 2019
)
0.51
" This prospective, multicenter, open-label, phase I/II study determined the maximum tolerated dose (MTD) and evaluated the safety and efficacy of poziotinib combined with paclitaxel and trastuzumab in patients with HER2-positive advanced gastric cancer (GC)."( A phase I/II study of poziotinib combined with paclitaxel and trastuzumab in patients with HER2-positive advanced gastric cancer.
Bang, YJ; Cho, JY; Han, HS; Jung, SA; Kim, JS; Kim, TY; Kim, YH; Lee, KH; Lee, KW; Lee, N; Park, SH; Park, YI; Rha, SY; Song, EK; Zang, DY, 2019
)
0.51
"The MTD of poziotinib combined with paclitaxel and trastuzumab was 8 mg/day."( A phase I/II study of poziotinib combined with paclitaxel and trastuzumab in patients with HER2-positive advanced gastric cancer.
Bang, YJ; Cho, JY; Han, HS; Jung, SA; Kim, JS; Kim, TY; Kim, YH; Lee, KH; Lee, KW; Lee, N; Park, SH; Park, YI; Rha, SY; Song, EK; Zang, DY, 2019
)
0.51
"The impact of evodiamine in combination with histone deacetylase (HDAC) inhibitors on survival of thyroid carcinoma cells was identified."( Evodiamine in combination with histone deacetylase inhibitors has synergistic cytotoxicity in thyroid carcinoma cells.
Choi, MG; Ihm, SH; Kang, JG; Kim, CS; Kim, SH; Lee, SJ, 2019
)
0.51
" Moreover, repression of PI3K/Akt signaling synergistically reinforces cytotoxicity of evodiamine combined with HDAC inhibitors in thyroid carcinoma cells."( Evodiamine in combination with histone deacetylase inhibitors has synergistic cytotoxicity in thyroid carcinoma cells.
Choi, MG; Ihm, SH; Kang, JG; Kim, CS; Kim, SH; Lee, SJ, 2019
)
0.51
"Antiangiogenic agents combined with chemotherapy have efficacy in the treatment of unresectable malignant pleural mesothelioma (MPM)."( Phase II Trial of Cediranib in Combination With Cisplatin and Pemetrexed in Chemotherapy-Naïve Patients With Unresectable Malignant Pleural Mesothelioma (SWOG S0905).
Box-Noriega, B; Fossella, FV; Gadgeel, S; Gandara, DR; Heymach, JV; Hueftle, JG; Kelly, K; Lu, C; Miao, J; Redman, MW; Tsao, AS; Velasco, MR; Vogelzang, NJ; Wistuba, II, 2019
)
0.51
"AZD8931 (20 mg, 40 mg or 60 mg bd) was given with Xelox (oxaliplatin + capecitabine) for eight 21-day cycles, continuously or with intermittent schedule (4 days on/3 off every week; 14 days on/7 off, per cycle) in a rolling-six design."( Dual Erb B Inhibition in Oesophago-gastric Cancer (DEBIOC): A phase I dose escalating safety study and randomised dose expansion of AZD8931 in combination with oxaliplatin and capecitabine chemotherapy in patients with oesophagogastric adenocarcinoma.
Anthoney, DA; Collins, L; Eatock, M; Elhussein, L; Falk, S; Goff, M; Lord, SR; Love, S; Middleton, MR; Moschandreas, J; Thomas, A; Turkington, RC; Virdee, PS, 2020
)
0.56
" The primary aim is to assess progression-free survival after EGFR-TKIs treatment combined with apatinib 250 mg once daily."( Clinical study of apatinib combined with EGFR-TKI in the treatment of chronic progression after EGFR-TKI treatment in non-small cell lung cancer (ChiCTR1800019185).
Chen, J; Li, X; Liu, H; Liu, M; Zhang, H, 2020
)
0.56
" Inhibition of CYP1A1 may increase the concentration of ningetinib in target tissues, and the long-term safety and efficacy of ningetinib combined with gefitinib should be evaluated."( Drug interaction of ningetinib and gefitinib involving CYP1A1 and efflux transporters in non-small cell lung cancer patients.
Chen, X; Guo, Z; Hou, X; Li, J; Li, M; Liu, L; Sun, M; Wang, Q; Xi, N; Xie, C; Xie, N, 2021
)
0.62
" In this phase II study, we prospectively analyzed the efficacy and safety of raltitrexed combined with S-1 (RS regimen) in the treatment of mCRC after the failure of conventional chemotherapy."( A prospective phase II study of raltitrexed combined with S-1 as salvage treatment for patients with refractory metastatic colorectal cancer.
Chen, Z; Guo, W; Huang, M; Li, W; Qiu, L; Wang, C; Wang, Y; Yang, Y; Zhang, W; Zhang, X; Zhang, Z; Zhao, X; Zhu, X, 2021
)
0.62
" Our results suggest that voriconazole trough concentration decreases when voriconazole is combined with letermovir in allogeneic HCT recipients."( Drug interaction between letermovir and voriconazole after allogeneic hematopoietic cell transplantation.
Doke, Y; Fukuda, T; Fukushi, Y; Hashimoto, H; Inamoto, Y; Nakashima, T; Yamaguchi, M, 2021
)
0.62
" Hence, the purpose of this study was to investigate the efficacy and safety of icotinib combined with CRT in the treatment of locally advanced cervical cancer."( Outcomes of icotinib combined with concurrent chemoradiotherapy in locally advanced cervical cancer.
Chen, WJ; Ding, Y; Liu, H; Liu, YM; Sun, HL; Xu, YY; Ying, SP, 2021
)
0.62
"Bevacizumab combined with S-1 and raltitrexed demonstrated positive antitumor efficacy and acceptable toxicity."( Bevacizumab Combined with S-1 and Raltitrexed for Patients with Metastatic Colorectal Cancer Refractory to Standard Therapies: A Phase II Study.
Bi, F; Cao, D; Chen, Y; Cheng, K; Gou, HF; Li, Q; Li, ZP; Liu, JY; Luo, DY; Qiu, M; Shen, YL; Wang, X; Yang, Y; Zhou, YW, 2021
)
0.62
" In the present study, we assessed the activity and safety of bevacizumab combined with S-1 and raltitrexed."( Bevacizumab Combined with S-1 and Raltitrexed for Patients with Metastatic Colorectal Cancer Refractory to Standard Therapies: A Phase II Study.
Bi, F; Cao, D; Chen, Y; Cheng, K; Gou, HF; Li, Q; Li, ZP; Liu, JY; Luo, DY; Qiu, M; Shen, YL; Wang, X; Yang, Y; Zhou, YW, 2021
)
0.62
"Bevacizumab combined with S-1 and raltitrexed showed promising antitumor activity and safety in refractory mCRC."( Bevacizumab Combined with S-1 and Raltitrexed for Patients with Metastatic Colorectal Cancer Refractory to Standard Therapies: A Phase II Study.
Bi, F; Cao, D; Chen, Y; Cheng, K; Gou, HF; Li, Q; Li, ZP; Liu, JY; Luo, DY; Qiu, M; Shen, YL; Wang, X; Yang, Y; Zhou, YW, 2021
)
0.62
" This case suggests the re-challenge of the first-generation EGFR-TKIs combined with bevacizumab may overcome the tumor resistance and prolong survival of NSCLC patient."( Bevacizumab Combined with Icotinib Overcomes Osimertinib Resistance in a Patient of Non-Small Cell Lung Cancer.
Ji, YX; Mu, XY; Sun, L; Zhang, L, 2019
)
0.51
" Based on this, the COUP-1 trial aims at testing the toxicity and efficacy of copanlisib in combination with rituximab in treatment naive and relapsed MZL."( A phase II study of the PI3K inhibitor copanlisib in combination with the anti-CD20 monoclonal antibody rituximab for patients with marginal zone lymphoma: treatment rationale and protocol design of the COUP-1 trial.
Barth, TFE; Buske, C; Dreyhaupt, J; Grunenberg, A; Kaiser, LM; Kiesewetter, B; Möller, P; Muche, R; Raderer, M; Schmelzle, B; Viardot, A; Woelfle, S, 2021
)
0.62
"The COUP-1 trial evaluates the efficacy and toxicity of the treatment of copanlisib in combination with rituximab in patients with MZL and additionally offers the chance for translational research in this heterogenous type of lymphoma."( A phase II study of the PI3K inhibitor copanlisib in combination with the anti-CD20 monoclonal antibody rituximab for patients with marginal zone lymphoma: treatment rationale and protocol design of the COUP-1 trial.
Barth, TFE; Buske, C; Dreyhaupt, J; Grunenberg, A; Kaiser, LM; Kiesewetter, B; Möller, P; Muche, R; Raderer, M; Schmelzle, B; Viardot, A; Woelfle, S, 2021
)
0.62
" Moreover, when it used in combination with liposomal doxorubicin, it extended the time to end from 22."( Development of a stable and high loaded liposomal formulation of lapatinib with enhanced therapeutic effects for breast cancer in combination with Caelyx®: In vitro and in vivo evaluations.
Badiee, A; Jafari, MR; Karimi, M; Mansouri, A; Mehrabian, A; Nikpoor, AR; Sadri, K; Shokooh Saremi, S, 2021
)
0.62
" Preclinical data with cediranib, an inhibitor of all 3 VEGF receptors, in combination with selumetinib, an inhibitor of MEK 1/2, demonstrated improved tumor control experimentally."( Phase I study of cediranib, an oral VEGFR inhibitor, in combination with selumetinib, an oral MEK inhibitor, in patients with advanced solid malignancies.
Adjei, A; Costello, BA; Doyle, LA; Erlichman, C; Fiskum, J; Haluska, P; Hubbard, JM; Ivy, P; Lin, G; Menefee, M; Qin, R; Reid, JM; Schenk, EL; Strand, C; Yin, J, 2022
)
0.72
"This study aimed to evaluate the inhibitory effects and potential mechanisms of icotinib combined with antiangiogenic drugs on lung adenocarcinoma in vivo."( Inhibitory effects of icotinib combined with antiangiogenic drugs in human non-small cell lung cancer xenograft models are better than single target drugs.
Cui, J; Jiang, P; Li, Y; Wang, X; Zhang, Y, 2022
)
0.72
"Icotinib combined with bevacizumab or rh-endostatin has a stronger inhibitory effect on tumor growth than single-target drug in vivo, with no additional side effects."( Inhibitory effects of icotinib combined with antiangiogenic drugs in human non-small cell lung cancer xenograft models are better than single target drugs.
Cui, J; Jiang, P; Li, Y; Wang, X; Zhang, Y, 2022
)
0.72
" Cell lines treated with trametinib or AZD6244 in combination with AZD0424 had reduced EGFR, FAK and SRC compensatory activation, and cell viability was synergistically inhibited."( Pathway profiling of a novel SRC inhibitor, AZD0424, in combination with MEK inhibitors for cancer treatment.
Brunton, VG; Carragher, NO; Dawson, JC; Frame, M; Macleod, K; Muir, M; Munro, A; Timpson, P; Williams, RJ, 2022
)
0.72
" Peposertib (M3814) is a DNA-PK inhibitor that has shown preclinical activity in combination with DNA-damaging agents, including ionizing radiation (IR) and topoisomerase II inhibitors."( Pre-clinical activity of the oral DNA-PK inhibitor, peposertib (M3814), combined with radiation in xenograft models of cervical cancer.
Aghajanian, C; Chui, MH; Gardner, GJ; Gordhandas, SB; Grisham, RN; Henson, C; Iyer, G; Manning-Geist, B; Moore, KN; Sonoda, Y, 2022
)
0.72
" Understanding potential drug-drug interactions (DDIs) informs proper dosing when co-administering tucatinib with other therapies."( Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers.
Abdulrasool, LI; Endres, CJ; Lee, A; Mayor, JG; Rustia, EL; Sun, H; Topletz-Erickson, A; Walker, L, 2022
)
0.72
" This Phase I/II study examined the toxicity and efficacy of high-dose pulsed AZD8931, an EGFR/HER2/HER3 inhibitor, combined with chemotherapy, in metastatic colorectal cancer (CRC)."( PANTHER: AZD8931, inhibitor of EGFR, ERBB2 and ERBB3 signalling, combined with FOLFIRI: a Phase I/II study to determine the importance of schedule and activity in colorectal cancer.
Barber, PR; Forsyth, S; Gao, F; Hackett, LD; Hartley, JA; Hochhauser, D; Lopes, A; Lowe, HL; Ng, TT; Pearce, S; Propper, DJ; Sarker, D; Saunders, MP; Spanswick, VJ; Weitsman, GE; White, L, 2023
)
0.91
"Copanlisib dose selection was established under the maximum tolerated dose paradigm, and no dedicated dose-finding studies have investigated copanlisib dose selection when used in combination with rituximab."( Copanlisib population pharmacokinetics from phase I-III studies and exposure-response relationships in combination with rituximab.
Austin, R; Beckert, V; Childs, BH; Garmann, D; Hiemeyer, F; Mongay Soler, L; Morcos, PN; Moss, J; Zinzani, PL, 2023
)
0.91

Bioavailability

Quinazolines are NLRP3 agonists. Their chemical optimization to afford compounds with oral bioavailability in mice. NEU617, 23a is a highly potent, orally bioavailable inhibitor of trypanosome replication.

ExcerptReferenceRelevance
" Pharmacokinetic and biotransformation studies indicate that prazosin is well absorbed and is excreted principally in metabolized form with biliary excretion being the major route of elimination."( Prazosin: biochemistry and structure-activity studies.
Hess, HJ, 1975
)
0.25
" Oral bioavailability was 56."( Prazosin, pharmacokinetics and concentration effect.
Bateman, DN; Hobbs, DC; Rawlins, MD; Stevens, EA; Twomey, TM, 1979
)
0.26
" Changrolin could be well absorbed by oral administration."( Studies on a new antiarrhythmic drug changrolin-4-(3',5'-bis [(N-pyrrolidinyl) methyl]-4'-hydroxyanilino)-quinazoline.
Ding, GS; Hu, GJ; Li, LQ; Qu, ZX; Wang, ZM; Yang, XY; Zeng, YL, 1979
)
0.26
" The enhanced antihypertensive effect of prazosin in renal failure appears to reflect changes in the bioavailability or distribution of the drug, which result in higher drug concentrations for a given dose."( Responsiveness to prazosin in renal failure.
Frost, GW; MacCarthy, EP; Monaghan, JC; Stokes, GS, 1979
)
0.26
" The bioavailability of zenarestat was 93% in rats and 65% in dogs."( Absorption, distribution and excretion of zenarestat, a new aldose reductase inhibitor, in rats and dogs.
Esumi, Y; Katami, Y; Noda, K; Sawamoto, T; Sekiguchi, M; Tanaka, Y; Ueda, T, 1992
)
0.28
"), but its bioavailability following oral administration appeared to be low (approximately 10%-20%)."( The pharmacokinetics of the quinazoline antifolate ICI D 1694 in mice and rats.
Calvert, AH; Gibson, W; Hughes, LR; Jodrell, DI; Newell, DR, 1991
)
0.28
" Pelanserin bioavailability after oral dosing was about 30%, this could be due to a poor absorption from the gastrointestinal tract or to an important hepatic biotransformation by first pass effect."( [Pharmacokinetics and antihypertensive effect of pelanserin in dogs ].
Castañeda Hernández, G; Flores Murrieta, FJ; Hong, E,
)
0.13
"; this indicated a high bioavailability of RO 13-6438."( Dose-response following single administrations of a new cardiac performance enhancer RO 13-6438 in normal volunteers.
Belz, GG; Butzer, R; Stern, HC,
)
0.13
" Similarly, clinical myotonolytic activity of eperisone would only be expected at high doses unless its functional bioavailability were to be much better in man than in either the mouse or rabbit."( Comparison of the myotonolytic activity of tizanidine, eperisone and afloqualone in mouse and rabbit.
Coward, DM; White, TG,
)
0.13
" With oral administration, the mean bioavailability was 44% (range, 19 to 67%)."( Bioavailability of oral trimetrexate in patients with acquired immunodeficiency syndrome.
Allegra, CJ; Balis, FM; Chabner, BA; Drake, JC; Lane, HC; Masur, H; Murphy, RF; Parrillo, JE; Poplack, DG; Rogers, P, 1988
)
0.27
" Moreover, there was no evidence of unexpected accumulation of the drug in the plasma during multiple dosing and food did not appear to alter the bioavailability of tiacrilast to any clinically significant extent."( Pharmacokinetics of single and multiple ascending doses of the antiallergic agent tiacrilast in man.
Dunton, A; Keigher, N; Massarella, JW; Pao, J; Silvestri, TM, 1987
)
0.27
"The relative bioavailability of two different Prazosine preparations (Adversuten, VEB Arzneimittelwerk Dresden, GDR and Minipress, Pfizer GmbH, Karlsruhe, FRG) has been determined in 10 patients suffering from an essential hypertension by the cross-over test following a single oral application."( [Comparative study of the relative bioavailabilities of two prazosin preparations in patients with essential hypertension].
Faulhaber, HD; Günzel, R; Homuth, V; Prehm, C; Rostock, G; Unger, P, 1985
)
0.27
" Lacking an intravenous dosage form for use in human subjects, our study concentrated on the determination of the bioavailability and disposition parameters of tiodazosin in dogs, with a comparison to those parameters for prazosin, obtained from previous work in our laboratory."( The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride.
Baughman, RA; Benet, LZ; Mico, BA,
)
0.13
" The hypotensive action of prazosin is greater in patients with chronic renal failure, and the bioavailability or distribution of the drug is altered."( Clinical pharmacology of prazosin in hypertensive patients with chronic renal failure.
Aubert, P; Chaignon, M; Flouvat, B; Guedon, J; Le Roux, E; Lucsko, M; Safar, M,
)
0.13
"Prior to the introduction of an intravenous dosage form for use in humans, prazosin pharmacokinetic studies emphasizing clearance, hepatic extraction, and bioavailability were carried out in dogs."( Dose-dependent bioavailability of prazosin in beagle dogs.
Baughman, RA; Benet, LZ; Mico, BA; Sorgel, F,
)
0.13
" Our data suggest that the greater hypotensive activity of the combination results at least in part from a kinetic interaction that enhances the bioavailability of prazosin, but it is possible that a dynamic interaction at the level of vascular smooth muscle or compensatory cardiac activity also plays a role."( Combined alpha adrenoceptor antagonism and calcium channel blockade in normal subjects.
Elliott, HL; McSharry, DR; Meredith, PA; Pasanisi, F; Reid, JL, 1984
)
0.27
" Inhibitors of this enzyme can enhance the bioavailability of purine antagonists and in turn are helpful for the chemotherapy of cancer."( New guanine deaminase inhibitors.
Ahmad, S; Kishor, K; Saxena, AK; Shanker, K, 1984
)
0.27
" The rate of absorption of prazosin was identical in the two groups (t max: I,3 +/- 0,2 h and I,6 +/- 0,4 h)."( [Clinical pharmacology of prazosin in arterial hypertension with chronic renal insufficiency].
Aubert, P; Chaignon, M; Flouvat, B; Guédon, J; Le Roux, E; Lucsko, M, 1981
)
0.26
"Extractive alkylation was carried out on fenquizone, a sulphonamide diuretic, in order to devise a suitable method for its determination in pharmacokinetic and bioavailability studies."( Gas-liquid chromatographic evaluation of fenquizone in biological samples for pharmacokinetic investigations.
Marzo, A; Quadro, G; Treffner, E, 1983
)
0.27
" Oral bioavailability of prazosin ranges from 43."( Clinical pharmacokinetics of prazosin.
Jaillon, P,
)
0.13
" All patients did not respond in a similar way; two distinct patterns of BP and pulse response emerged, although there was no significant difference in the pharmacokinetic parameters, namely, absorption rate constant (Ka), maximum plasma concentration (Cpmax), time to reach the maximum concentration (Tmax), prazosin plasma half-life (T 1/2), elimination rate constant (kel), prazosin plasma concentration-time curve (AUC), and clearance."( Prazosin plasma concentration and blood pressure reduction.
Armstrong, J; du Souich, P; Hamet, P; Larochelle, P; Larocque, P,
)
0.13
" After oral doses bioavailability ranged between 55% and 82%."( Prazosin kinetics in hypertension.
Grahnén, A; Haglund, K; Lindström, B; Seideman, P; von Bahr, C, 1981
)
0.26
" The results suggest that these acrids have the capacity to increase the bioavailability of certain drugs."( Scientific evidence on the role of Ayurvedic herbals on bioavailability of drugs.
Atal, CK; Rao, PG; Zutshi, U, 1981
)
0.26
" The only effect of antacid, compared to fasting, was to slow the rate of absorption without appreciably altering the extent of absorption."( The effect of antacid and food on the absorption of proquazone (Biarison) in man.
Ohnhaus, EE, 1980
)
0.26
"9 mg/kg iv and 9 mg/kg po doses, systemic blood clearance (CLB) and bioavailability (F) of L-738,372 were species-dependent and inversely related (CLB = 48, 15, and 3 ml/min/kg; F = 6, 62 and 94%, in dogs, rats, and monkeys, respectively)."( Species differences in the metabolism of a potent HIV-1 reverse transcriptase inhibitor L-738,372. In vivo and in vitro studies in rats, dogs, monkeys, and human.
Balani, SK; Dwyer, LM; Ellis, JD; Kauffman, LR; Pitzenberger, SM; Prueksaritanont, T; Theoharides, AD; Varga, SL, 1995
)
0.29
" Ibopamine is well absorbed through the cornea, it is rapidly hydrolysed by esterases to epinine and the mydriatic effect is correlated with the concentration of epinine in the aqueous humor."( Ocular pharmacokinetics and pharmacodynamics in rabbits of ibopamine, a new mydriatic agent.
Galbiati, I; Gazzaniga, A; Gianesello, V; Soldati, L; Virno, M, 1993
)
0.29
" Previous drug design efforts based on co-factor analogues have produced good inhibitors of TS, but poor bioavailability and toxicity have limited their usefulness."( The complex of the anti-cancer therapeutic, BW1843U89, with thymidylate synthase at 2.0 A resolution: implications for a new mode of inhibition.
Stout, TJ; Stroud, RM, 1996
)
0.29
" Pharmacokinetic studies in normotensive volunteers showed that plasma peak concentration (Cmax) of bunazosin retard and bioavailability were approximately 50% and 81%, respectively, of the values of the standard non-retarded formulation."( Pharmacokinetic and pharmacodynamic properties and therapeutic use of bunazosin in hypertension. A review.
Weidinger, G, 1995
)
0.29
" The pharmacokinetics and bioavailability of 1954U89 were examined in male beagle dogs and male CD rats."( The pharmacokinetics of 1954U89, 1,3-diamino-7-(1-ethylpropyl)-8-methyl-7H-pyrrolo-(3,2-f)quinazoline, in dogs and rats after intravenous and oral administration.
Deangelis, DV; Studenberg, SD; Wargin, WA; Woolley, JL, 1997
)
0.3
" Pharmacokinetic studies suggested that SG-210 has a high bioavailability and possesses a long half-life in rats (ca."( Effect of SG-210, a novel aldose reductase inhibitor, on impaired polyol pathway in rats received diabetic manipulations.
Horie, S; Nagai, H; Nakajima, T; Nakamura, N; Narita, Y; Tsuda, Y; Yuuki, T,
)
0.13
" The bioavailability and pharmacokinetic and pharmacodynamic properties of oral nolatrexed were also studied."( Phase I studies with the nonclassical antifolate nolatrexed dihydrochloride (AG337, THYMITAQ) administered orally for 5 days.
Boddy, AV; Calvert, AH; Calvete, JA; Clendeninn, N; Griffin, MJ; Hughes, AN; Johnston, A; Newell, DR; Rafi, I, 1999
)
0.3
" As oral bioavailability is high (70-100%), nolatrexed was administered orally, 6 hourly for 10 days, at 3-week intervals, and dose escalated from 80 to 572 mg m(-2) day(-1) in 23 patients."( A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration.
Boddy, A; Bowman, A; Byrne, B; Clendeninn, NJ; Jodrell, DI; Johnston, A; Rafi, I; Rye, R; Taylor, GA, 1999
)
0.3
" bioavailability was 95% for rats, as well as for mice."( In vivo toxicity and pharmacokinetic features of the janus kinase 3 inhibitor WHI-P131 [4-(4'hydroxyphenyl)-amino-6,7- dimethoxyquinazoline.
Chen, CL; Ek, O; Liu, XP; Uckun, FM, 1999
)
0.3
" Alf was not due to the species difference in its bioavailability and biotransformation."( Selective effects of alfuzosin and doxazosin with intraduodenal administration on urethral pressure of cats.
Fu, SX; Li, YS; Ren, LM; Wu, ZJ; Yang, ZH, 1999
)
0.3
"1% when administered intravenously at 30 microg/kg to the chronically hypoxic rats and had an apparent oral bioavailability of about 19."( 4-(3-Chloro-4-methoxybenzyl)aminophthalazines: synthesis and inhibitory activity toward phosphodiesterase 5.
Adachi, H; Ishibashi, K; Ishihara, H; Kabasawa, Y; Kakiki, M; Kodama, K; Matsukura, M; Miyazaki, K; Nishino, M; Ozaki, H; Takase, Y; Watanabe, N, 2000
)
0.31
" The ability of halofuginone to interfere with key events in neovascularization, together with its oral bioavailability and safe use as an anti-parasitic agent, make it a promising drug for further evaluation in the treatment of a wide range of diseases associated with pathological angiogenesis."( Halofuginone: a potent inhibitor of critical steps in angiogenesis progression.
Aingorn, E; Dou, HL; Elkin, M; Hemo, I; Miao, HQ; Nagler, A; Pines, M; Reich, R; Vlodavsky, I, 2000
)
0.31
" On the basis of animal experiments, the oral bioavailability and penetration of raltitrexed into cerebrospinal fluid are both likely to be limited in the clinical setting."( Clinical and preclinical pharmacokinetics of raltitrexed.
Beale, PJ; Clarke, SJ; Rivory, LP, 2000
)
0.31
" The third study investigated the effect of food on the bioavailability of a single 50mg dose of ZD1839."( Pharmacokinetics and tolerability of the orally active selective epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 in healthy volunteers.
Dane, A; Jones, H; Laight, A; Morris, C; Stafford, L; Swaisland, H; Yates, R, 2001
)
0.31
" The best compounds are potent orally bioavailable inhibitors of both wild-type HIV-1 and its clinically relevant K103N mutant virus, but are highly protein-bound in human plasma."( 4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Bacheler, LT; Chidester, DR; Cocuzza, AJ; Cordova, BC; Diamond, S; Erickson-Viitanen, SK; Jeffrey, S; Klabe, RM; Ko, SS; Rodgers, JD; Weigelt, CA, 2001
)
0.31
"4) and good oral bioavailability in rat and dog (> 80 and > 50%, respectively)."( Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.
Curwen, JO; Dukes, M; Hennequin, LF; Johnstone, C; Kendrew, J; Ogilvie, DJ; Plé, PA; Stokes, ES; Thomas, AP; Wedge, SR, 2002
)
0.67
" This review traces the systematic development of the former Rhone-Poulenc Rorer factor Xa program from conception to the realization of potent, orally bioavailable inhibitors with exquisite selectivity against other serine proteases."( The design of competitive, small-molecule inhibitors of coagulation factor Xa.
Ewing, WR; Pauls, HW, 2001
)
0.31
" The present data demonstrate that BIBN4096BS is a very potent antagonist that could, depending on its bioavailability and in vivo affinity, be of potential benefit in the acute treatment of migraine headache by blocking and/or reversing the CGRP-mediated dilation of intracranial vessels induced by activation of trigeminovascular afferents."( Efficacy of the non-peptide CGRP receptor antagonist BIBN4096BS in blocking CGRP-induced dilations in human and bovine cerebral arteries: potential implications in acute migraine treatment.
Abounader, R; Doods, H; Hamel, E; Hébert, E; Moreno, MJ, 2002
)
0.31
" Results from Phase I trials, in healthy volunteers and in patients with advanced disease, have shown that ZD1839 has excellent bioavailability and an acceptable tolerability profile."( ZD1839: targeting the epidermal growth factor receptor in cancer therapy.
Herbst, RS, 2002
)
0.31
" Bioavailability with an unoptimized tablet formulation was 30% in fasted dogs and 86% in fed dogs."( Formulation and food effects on the oral absorption of a poorly water soluble, highly permeable antiretroviral agent.
Aungst, BJ; Bindra, DS; Nguyen, NH; Taylor, NJ, 2002
)
0.31
" Based on AUC(0-24) values corrected by the administered daily dose, the relative bioavailability of alfuzosin OD was 75."( Alfuzosin, an alpha1-adrenoceptor antagonist for the treatment of benign prostatic hyperplasia: once daily versus 3 times daily dosing in healthy subjects.
Ahtoy, P; Chrétien, P; Delfolie, A; Dupain, T; Rauch, C; Rouchouse, A, 2002
)
0.31
"Alfuzosin 10 mg once-daily provides a suitable pharmacokinetic profile for a once-daily administration, equivalent bioavailability between the 2 dosage regimens and a good safety profile justify the use of alfuzosin 10 mg in patients with BPH."( Alfuzosin, an alpha1-adrenoceptor antagonist for the treatment of benign prostatic hyperplasia: once daily versus 3 times daily dosing in healthy subjects.
Ahtoy, P; Chrétien, P; Delfolie, A; Dupain, T; Rauch, C; Rouchouse, A, 2002
)
0.31
" Derivatives of ML03 with lower metabolic clearance rate and higher bioavailability should be synthesized and their potential as anticancer drugs and PET bioprobes evaluated."( Labeled EGFr-TK irreversible inhibitor (ML03): in vitro and in vivo properties, potential as PET biomarker for cancer and feasibility as anticancer drug.
Ben-David, I; Chisin, R; Freedman, NM; Levitzki, A; Mishani, E; Ortu, G; Rozen, Y, 2002
)
0.31
" Gefitinib is orally bioavailable and is cleared via the cytochrome P450 3A4 pathway."( Gefitinib.
Culy, CR; Faulds, D, 2002
)
0.31
"The development of potent, orally bioavailable (in rat) and selective dihydroquinazolinone inhibitors of p38alpha MAP kinase is described."( Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Cameron, PM; Doherty, JB; Hop, CE; Liu, L; Nichols, EA; O'Keefe, SJ; O'Neill, EA; Patel, SB; Pivnichny, JV; Scapin, G; Schmatz, DM; Schwartz, CD; Singh, S; Stelmach, JE; Strauss, JR; Thompson, CM; Wang, Z; Zaller, DM, 2003
)
0.32
" Pigs in group 3 were used for bioavailability evaluation."( Pharmacokinetics studies and toxicity profile of raltitrexed used by intraperitoneal route in normothermia in a pig model.
Dube, P; Emond, C; Leclerc, Y; Nguyen, D; Sherman, I, 2003
)
0.32
" The 4-aminopentamethylpiperidine naphthyridinone 5, which was designed to block metabolism at major 'hot spots', combined excellent inhibitory potency with good oral bioavailability in the rat."( p38 Inhibitors: piperidine- and 4-aminopiperidine-substituted naphthyridinones, quinolinones, and dihydroquinazolinones.
Doherty, JB; Hop, CE; Hunt, JA; Ita, I; Kallashi, F; Kumar, S; McCormick, SX; O'Keefe, SJ; O'Neill, EA; Pivnichny, JV; Porter, G; Ruzek, RD; Sinclair, PJ; Thompson, JE; Wang, Z; Woods, A; Zaller, DM, 2003
)
0.32
" Following oral administration of T-5557, the absolute bioavailability in AA rats was increased by sixfold compared with normal rats."( Differences in pharmacokinetics and hepatobiliary transport of a novel anti-inflammatory agent between normal and adjuvant arthritis rats.
Achira, M; Kume, T; Totsuka, R, 2002
)
0.31
"Clinical development of ZD1839 (Iressa; AstraZeneca Pharmaceuticals LP, Wilmington, DE) was initiated based on strong preclinical studies that showed antitumor responses in a variety of solid tumor types and established its oral bioavailability and tolerability."( Phase I studies of ZD1839 in patients with common solid tumors.
Lorusso, PM, 2003
)
0.32
" ZD4190 is an orally bioavailable inhibitor of VEGF receptor-2 (KDR) tyrosine kinase activity, which elicits broad-spectrum antitumour activity in preclinical models following chronic once-daily dosing."( Dynamic contrast-enhanced MRI of vascular changes induced by the VEGF-signalling inhibitor ZD4190 in human tumour xenografts.
Checkley, D; Curry, B; Dukes, M; Kendrew, J; Middleton, B; Tessier, JJ; Waterton, JC; Wedge, SR, 2003
)
0.32
" The confirmed efficacy, proven bioavailability and good cardiovascular safety profile support the use of this drug for the management of lower urinary tract symptoms secondary to benign prostate hyperplasia (BPH)."( Alfuzosin for the management of benign prostate hyperplasia.
Lowe, FC; Weiner, DM, 2003
)
0.32
"These data indicate that the formation of O2- by the endothelial gp91phox-containing NADPH oxidase accounts for the reduced NO bioavailability in the 2K1C model and contributes to the development of renovascular hypertension and endothelial dysfunction."( gp91phox-containing NADPH oxidase mediates endothelial dysfunction in renovascular hypertension.
Brandes, RP; Busse, R; Geiger, H; Jung, O; Pedrazzini, T; Schreiber, JG, 2004
)
0.32
" However, gefitinib treatment dramatically increased the oral bioavailability of irinotecan after simultaneous oral administration."( Gefitinib enhances the antitumor activity and oral bioavailability of irinotecan in mice.
Cheshire, PJ; Daw, N; Germain, GS; Gilbertson, R; Harwood, FC; Houghton, PJ; Jenkins, JJ; Leggas, M; Panetta, JC; Peterson, J; Schuetz, JD; Stewart, CF, 2004
)
0.32
" Food has been found to exert a clinically important effect by enhancing the bioavailability of the ER formulation; thus, the drug should be taken on a full stomach."( Extended-release alfuzosin hydrochloride: a new alpha-adrenergic receptor antagonist for symptomatic benign prostatic hyperplasia.
Guay, DR, 2004
)
0.32
"The aim of the present study was to determine the relative bioavailability and safety profile of a single dose of gefitinib, an orally active inhibitor of epidermal growth factor receptor tyrosine kinase, when administered as a whole 250-mg tablet or as a dispersion preparation via drink or nasogastric tube in healthy male volunteers."( Relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers.
Bailey, C; Cantarini, MV; Marshall, AL; McFarquhar, T; Smith, RP, 2004
)
0.32
" The pharmacokinetic parameters of interest included AUC, C(max), and the relative bioavailability of the dispersion via drink or nasogastric tube compared with the standard tablet."( Relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers.
Bailey, C; Cantarini, MV; Marshall, AL; McFarquhar, T; Smith, RP, 2004
)
0.32
" The gefitinib dispersion preparation administered by drink had a mean bioavailability of 103."( Relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers.
Bailey, C; Cantarini, MV; Marshall, AL; McFarquhar, T; Smith, RP, 2004
)
0.32
" The 5-isoquinoline-containing compound 14a (hTRPV1 IC50 = 4 nM) exhibited 46% oral bioavailability and in vivo activity in animal models of visceral and inflammatory pain."( Novel transient receptor potential vanilloid 1 receptor antagonists for the treatment of pain: structure-activity relationships for ureas with quinoline, isoquinoline, quinazoline, phthalazine, quinoxaline, and cinnoline moieties.
Bayburt, EK; Didomenico, S; Drizin, I; Faltynek, CR; Gomtsyan, A; Hannick, SM; Honore, P; Jarvis, MF; Jinkerson, T; Koenig, JR; Lee, CH; Macri, BS; Marsh, KC; McDonald, HA; Oie, T; Perner, RJ; Schmidt, RG; Stewart, KD; Surowy, CS; Turner, S; Wetter, J; Wismer, CT; Zheng, GZ, 2005
)
0.33
"CF101, an A3 adenosine receptor (A3AR) agonist, is a small orally bioavailable molecule known to suppress in vitro the production of tumor necrosis factor-alpha (TNF-alpha)."( Antiinflammatory effect of A3 adenosine receptor agonists in murine autoimmune arthritis models.
Baharav, E; Bar-Yehuda, S; Fishman, P; Halpren, M; Madi, L; Ochaion, A; Rath-Wolfson, L; Silberman, D; Weinberger, A, 2005
)
0.33
" ZD6474 is an orally bioavailable inhibitor of VEGF receptor-2 tyrosine kinase activity that in preclinical studies has been shown to inhibit both VEGF-induced signalling in endothelial cells and tumour-induced angiogenesis."( ZD6474--a novel inhibitor of VEGFR and EGFR tyrosine kinase activity.
Ryan, AJ; Wedge, SR, 2005
)
0.33
"Study 1: Oral bioavailability of a gefitinib 250 mg dose was 57% in healthy volunteers."( Single-dose clinical pharmacokinetic studies of gefitinib.
Duvauchelle, T; Kerr, DJ; Laight, A; Ranson, M; Smith, RP; Swaisland, HC; Wilder-Smith, CH, 2005
)
0.33
"The gefitinib 250 mg tablet is orally bioavailable in both healthy volunteers and cancer patients; bioavailability is independent of dose and unaffected by food to any clinically significant extent."( Single-dose clinical pharmacokinetic studies of gefitinib.
Duvauchelle, T; Kerr, DJ; Laight, A; Ranson, M; Smith, RP; Swaisland, HC; Wilder-Smith, CH, 2005
)
0.33
"Gefitinib (Iressa, ZD 1839) is an orally bioavailable small molecule that selectively inhibits epidermal growth factor receptor(EGFR) tyrosine kinase activity."( [Molecular targeted therapy--non-small-cell lung cancer and gefitinib].
Horio, Y; Mitsudomi, T; Shimizu, J, 2005
)
0.33
"A randomized, open-label, 2-period crossover study was conducted to evaluate the bioequivalence of 6 tablets of erlotinib 25 mg and 1 tablet of erlotinib 150 mg (arm A, n = 42) and the oral bioavailability of the 150-mg tablet versus a 25-mg intravenous infusion (arm B, n = 20) in healthy subjects."( Evaluation of the absolute oral bioavailability and bioequivalence of erlotinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in a randomized, crossover study in healthy subjects.
Eppler, S; Frohna, P; Hamilton, M; Kenkare-Mitra, SR; Ling, J; Lu, J; Lum, BL; Rakhit, A; Wolf, J, 2006
)
0.33
"Our results show that YM-359445 is more potent than orally bioavailable VEGFR2 tyrosine kinase inhibitors, which leads to great expectations for clinical applicability."( YM-359445, an orally bioavailable vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor, has highly potent antitumor activity against established tumors.
Amino, N; Hisamichi, H; Ideyama, Y; Kudoh, M; Kuromitsu, S; Matsuhisa, A; Samizu, K; Shibasaki, M; Shirasuna, K; Tajinda, K; Yamano, M, 2006
)
0.33
" ATC0175 has adequate ADME profile (reasonable oral bioavailability and brain penetration) and potent oral activity in animal models."( ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety.
Chaki, S; Sekiguchi, Y; Semple, G; Thomsen, W; Tran, TA; Yamada, H; Yamaguchi, J, 2005
)
0.33
" The nearly equal inhibitory activities of 1 and 2, despite of their different binding modes at the active site, indicate that this 1-substituent is promising in improving the bioavailability of the inhibitor without compromising its inhibitory activity."( Binding mode of novel 1-substituted quinazoline derivatives to poly(ADP-ribose) polymerase-catalytic domain, revealed by X-ray crystal structure analysis of complexes.
Ishida, T; Kawashima, A; Kitamura, K; Kondo, K; Matsumoto, K; Ota, T, 2006
)
0.33
" Oral administration of 4-AQ molecules, such as gefitinib, inhibits ATP-binding cassette (ABC) transporter-mediated drug efflux and strongly increases the apparent bioavailability of coadministered drug molecules that are transporter substrates."( Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo.
Bai, F; Houghton, PJ; Johnston, B; Leggas, M; Panetta, JC; Schuetz, JD; Sorrentino, B; Stewart, CF; Zhou, S; Zhuang, Y, 2006
)
0.33
" When administered orally, sulfasalazine is poorly absorbed with an estimated bioavailability of 3-12%."( Breast cancer resistance protein (Bcrp/abcg2) is a major determinant of sulfasalazine absorption and elimination in the mouse.
Brayman, TG; Khan, AA; Palandra, J; Ware, JA; Yu, L; Zaher, H,
)
0.13
"5 microM genistein, a broad-spectrum tyrosine kinase inhibitor, virtually eliminates the CO(2) sensitivity of HCO(3)(-) absorption rate (J(HCO(3)))."( Role of a tyrosine kinase in the CO2-induced stimulation of HCO3- reabsorption by rabbit S2 proximal tubules.
Boron, WF; Bouyer, P; Zhou, Y, 2006
)
0.33
" Simulations exploring the effect of the rate of absorption, bioavailability after an extravascular administration and the rate of activation/inactivation of the anti-migraine effect were performed."( Modelling the anti-migraine effects of BIBN 4096 BS: a new calcitonin gene-related peptide receptor antagonist.
Roth, W; Schaefer, HG; Tillmann, C; Trocóniz, IF; Wolters, JM, 2006
)
0.33
" The resulting aminoquinazoline 70 represents a novel VR1 antagonist with improved in vitro potency and oral bioavailability vs the analogous compounds from the lead series."( From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Bakthavatchalam, R; Blum, CA; Blurton, P; Brian Jones, A; Brielmann, H; Burkamp, F; Chandrasekhar, J; Clarkson, R; Cortright, D; Crandall, M; De Lombaert, S; Hodgetts, KJ; Hutchison, A; Zheng, X, 2006
)
0.6
", Melville, NY) is a low molecular weight, orally bioavailable inhibitor of the EGFR that has been approved for both non-small cell lung cancer and pancreatic cancers."( Inactivation of Akt by the epidermal growth factor receptor inhibitor erlotinib is mediated by HER-3 in pancreatic and colorectal tumor cell lines and contributes to erlotinib sensitivity.
Buck, E; Cagnoni, P; Eyzaguirre, A; Gibson, NW; Haley, JD; Iwata, KK, 2006
)
0.33
" Optimized, orally bioavailable compounds 32 and 47 exhibit anti-inflammatory activity (ED(50) of 22 and 11 mg/kg, respectively) in the anti-CD3-induced production of interleukin-2 (IL-2) in mice."( Discovery of aminoquinazolines as potent, orally bioavailable inhibitors of Lck: synthesis, SAR, and in vivo anti-inflammatory activity.
Bemis, JE; Boucher, C; Buchanan, JL; Buckner, WH; Cee, VJ; Chai, L; Deak, HL; DiMauro, EF; Epstein, LF; Faust, T; Gallant, P; Geuns-Meyer, SD; Gore, A; Gu, Y; Henkle, B; Hodous, BL; Hsieh, F; Huang, X; Kim, JL; Lee, JH; Martin, MW; Masse, CE; McGowan, DC; Metz, D; Mohn, D; Morgenstern, KA; Newcomb, J; Nunes, JJ; Oliveira-dos-Santos, A; Patel, VF; Powers, D; Rose, PE; Schneider, S; Tomlinson, SA; Tudor, YY; Turci, SM; Welcher, AA; White, RD; Zhao, H; Zhu, L; Zhu, X, 2006
)
0.67
"A 2-compartment first-order absorption pharmacokinetic (PK) model with inter-subject variability (ISV) on the apparent oral elimination clearance (CL/F), apparent central volume of distribution (V1/F), apparent peripheral volume of distribution (V2/F), and first-order oral absorption rate constant (ka), interoccasion variability (IOV) on CL/F, and body weight (WT) as covariate on CL/F was developed."( Population pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors.
Guo, F; Letrent, SP; Sharma, A, 2007
)
0.34
" Two lead compounds are further shown to have low clearance and moderate bioavailability in rat."( The discovery of highly selective erbB2 (Her2) inhibitors for the treatment of cancer.
Arcari, J; Bhattacharya, S; Campbell, M; Chen, J; Hungerford, W; Kauffman, GS; Kwan, T; Lippa, B; Ma, L; Moyer, JD; Pustilnik, L; Steyn, S; Su, C; Williams, C; Xiao, J; Zhao, X, 2007
)
0.34
" Furthermore, the rutaecarpine-loaded microemulsion gave significantly higher AUC and Cmax than did suspension, suggesting that the oral bioavailability of rutaecarpine in this microemulsion system could be enhanced due to the enhanced solubility of rutaecarpine by microemulsion."( Short communication: in vivo evaluation of microemulsion system for oral and parenteral delivery of rutaecarpine to rats.
Bhamdari, K; Choi, HG; Jahng, Y; Kim, DH; Lee, MH; Park, BJ; Woo, JS; Yong, CS; Yoo, BK, 2007
)
0.34
" PK data indicated that the bioavailability of oral PQD-A4 was greatly limited at high dose levels, that PQD-A4 was slowly converted to PQD via a sequential three-step process of conversion, and that PQD-A4 was significantly less toxic than the one-step hydrolysis drug, PQD-BE."( Pharmacokinetics, safety, and hydrolysis of oral pyrroloquinazolinediamines administered in single and multiple doses in rats.
Anova, L; Kozar, MP; Li, Q; Lin, AJ; Milhous, WK; Shearer, TW; Si, Y; Skillman, DR; Smith, KS; Xie, LH; Zhang, J, 2007
)
0.34
" The kinetics of drug release, swelling and erosion, and dynamics of textural changes during dissolution for the designed composite systems offer a novel approach for developing gastro-retentive drug delivery system that has potential to enhance bioavailability and site-specific delivery to the proximal small intestine."( Zero-order delivery of a highly soluble, low dose drug alfuzosin hydrochloride via gastro-retentive system.
Fassihi, R; Liu, Q, 2008
)
0.35
"The aims of this study were to determine the relative bioavailability of a single dose of gefitinib when administered as 250 mg of a new granular formulation compared with the standard 250 mg tablet, and to assess the intra-subject variability of the granular formulation, in healthy subjects."( The relative bioavailability of gefitinib administered by granular formulation.
Bailey, CJ; Cantarini, MV; Collins, B; Smith, RP, 2008
)
0.35
" Although the clinical use of trastuzumab (Herceptin) has prolonged the survival of breast cancer patients with erbB2-overexpressing tumors, there is an urgent need for more potent and orally bioavailable small-molecule inhibitors."( Discovery and pharmacologic characterization of CP-724,714, a selective ErbB2 tyrosine kinase inhibitor.
Bhattacharya, SK; Campbell, M; Coleman, KG; Connell, RD; Currier, N; Emerson, EO; Finn, RS; Floyd, E; Harriman, S; Jani, JP; Kath, JC; Morris, J; Moyer, JD; Pustilnik, LR; Rafidi, K; Ralston, S; Rossi, AM; Steyn, SJ; Wagner, L; Winter, SM, 2007
)
0.34
" EGFR inhibition may be achieved either by small-molecule orally bioavailable tyrosine kinase inhibitors, such as gefitinib or erlotinib, or else by large-molecule receptor antibodies, such as cetuximab or panitumumab."( Tumor resensitization to erlotinib following brief substitution of cetuximab.
Epstein, RJ; Leung, TW, 2008
)
0.35
" This study illustrates the potential of BAS 100 to increase the low and variable oral bioavailability of erlotinib in cancer patients."( Modulation of erlotinib pharmacokinetics in mice by a novel cytochrome P450 3A4 inhibitor, BAS 100.
Baker, SD; Figg, WD; Gonzalez, FJ; Harris, JW; Smith, NF; Sparreboom, A, 2008
)
0.35
" In summary, this first phase I study indicates that DOP has linear and dose-proportional pharmacokinetics, satisfactory oral bioavailability and plasma half-life and renal excretion."( Phase I clinical trial with desoxypeganine, a new cholinesterase and selective MAO-A inhibitor: tolerance and pharmacokinetics study of escalating single oral doses.
Algorta, J; Alvarez-González, A; Maraschiello, C; Maruhn, D; Mucke, HA; Pena, MA; Windisch, M, 2008
)
0.35
" In the present study, we determined the effects of 3,3'-diindolylmethane (Bioresponse BR-DIM referred to as B-DIM), a formulated DIM with greater bioavailability on cell viability and apoptosis with erlotinib in vitro and in vivo using an orthotopic animal tumor model."( Apoptosis-inducing effect of erlotinib is potentiated by 3,3'-diindolylmethane in vitro and in vivo using an orthotopic model of pancreatic cancer.
Ahmad, A; Ali, S; Banerjee, S; El-Rayes, BF; Philip, PA; Sarkar, FH, 2008
)
0.35
"01) as well as bioavailability of erlotinib after oral administration (5 mg/kg) were statistically significantly increased in Bcrp1/Mdr1a/1b(-/-) knockout mice (60."( Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice.
Beijnen, JH; Bolijn, MJ; Buckle, T; de Vries, NA; Marchetti, S; Mazzanti, R; Schellens, JH; van Eijndhoven, MA; van Tellingen, O, 2008
)
0.35
" In vivo, absence of P-gp and Bcrp1 significantly affected the oral bioavailability of erlotinib."( Effect of the ATP-binding cassette drug transporters ABCB1, ABCG2, and ABCC2 on erlotinib hydrochloride (Tarceva) disposition in in vitro and in vivo pharmacokinetic studies employing Bcrp1-/-/Mdr1a/1b-/- (triple-knockout) and wild-type mice.
Beijnen, JH; Bolijn, MJ; Buckle, T; de Vries, NA; Marchetti, S; Mazzanti, R; Schellens, JH; van Eijndhoven, MA; van Tellingen, O, 2008
)
0.35
" BIBN4096 (olcegepant) is the first CGRP antagonist for the treatment of migraine which has been tested in clinical trials, but its principal limitation is that BIBN4096 presents low oral bioavailability and has only been tested through intravenous formulation."( Proinflammatory mediators and migraine pathogenesis: moving towards CGRP as a target for a novel therapeutic class.
Farinelli, I; Martelletti, P; Missori, S, 2008
)
0.35
" Here, we have summarized the progress made in recent years, including the identification and optimization of an orally bioavailable small molecule CGRP receptor antagonist."( The tortuous road to an ideal CGRP function blocker for the treatment of migraine.
Davis, CD; Xu, C, 2008
)
0.35
" The validated method was successfully employed for bioavailability study after oral administration of 10 mg of alfuzosin hydrochloride and 5mg of solifenacin succinate tablet formulations in eight healthy volunteers under fed condition."( Highly sensitive and rapid LC-ESI-MS/MS method for the simultaneous quantification of uroselective alpha1-blocker, alfuzosin and an antimuscarinic agent, solifenacin in human plasma.
Jangid, AG; Mistri, HN; Pudage, A; Rathod, DM; Shrivastav, PS, 2008
)
0.35
"To establish a methods based on high-performance liquid chromatogram-mass spectrum for measuring the plasma concentration of nolatrexed dihydrochloride and investigate the pharmacokinetic profile and absolute bioavailability of the drug in mice."( [Measurement of plasma concentration and bioavailability of nolatrexed dihydrochloride in mice].
Shao, CF; Wan, SH; Wang, GF; Wu, SY; Xu, W; Zhang, JJ; Zhang, JY, 2008
)
0.35
" The pharmacokinetic parameters were calculated using DAS software, and the absolute bioavailability of orally and intravenously administered was assessed according to the ratio of their area under the curve (AUC)."( [Measurement of plasma concentration and bioavailability of nolatrexed dihydrochloride in mice].
Shao, CF; Wan, SH; Wang, GF; Wu, SY; Xu, W; Zhang, JJ; Zhang, JY, 2008
)
0.35
" The absolute bioavailability of nolatrexed dihydrochloride in mice was 23."( [Measurement of plasma concentration and bioavailability of nolatrexed dihydrochloride in mice].
Shao, CF; Wan, SH; Wang, GF; Wu, SY; Xu, W; Zhang, JJ; Zhang, JY, 2008
)
0.35
"The absolute bioavailability of nolatrexed dihydrochloride in mice determined in this study provides an experimental basis for development of the oral preparation of the drug."( [Measurement of plasma concentration and bioavailability of nolatrexed dihydrochloride in mice].
Shao, CF; Wan, SH; Wang, GF; Wu, SY; Xu, W; Zhang, JJ; Zhang, JY, 2008
)
0.35
"The epidermal growth factor receptor (EGFR), an N-glycosylated transmembrane protein, is the target of erlotinib, an orally bioavailable agent approved for treatment of patients with non-small cell lung cancer (NSCLC)."( Activation of ER stress and inhibition of EGFR N-glycosylation by tunicamycin enhances susceptibility of human non-small cell lung cancer cells to erlotinib.
Haigentz, M; Li, T; Ling, YH; Perez-Soler, R, 2009
)
0.35
"This study was conducted to characterize the effect of food on the relative bioavailability of lapatinib."( Effects of food on the relative bioavailability of lapatinib in cancer patients.
Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009
)
0.35
" Increased bioavailability in the fed state did not significantly decrease relative variability."( Effects of food on the relative bioavailability of lapatinib in cancer patients.
Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009
)
0.35
"These large increases in lapatinib bioavailability and absolute variability support the recommendation for dosing in the fasted state to achieve consistent therapeutic exposure."( Effects of food on the relative bioavailability of lapatinib in cancer patients.
Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009
)
0.35
" This validated LC-MS/MS method was successfully applied to a bioavailability study of oral and intravenous administration of changrolin with 20mg/kg dosage in SD rats."( Liquid chromatography/tandem mass spectrometry for the determination of changrolin in rat plasma: application to a bioavailability study.
Li, S; Liu, G; Lu, Y; Wang, Y; Yang, D; Yu, C, 2009
)
0.35
" Pharmacokinetic studies were conducted to assess the effect of pancreatic enzyme deficiency and intestinal malabsorption secondary to cystic fibrosis on the bioavailability of orally administered erlotinib, a lipophilic drug."( Pharmacokinetics of erlotinib for the treatment of high-grade glioma in a pediatric patient with cystic fibrosis: case report and review of the literature.
Broniscer, A; Christiansen, SR; Panetta, JC; Stewart, CF, 2009
)
0.35
" To assess the effect of gefitinib on the pharmacokinetics of IV irinotecan and on the bioavailability of a single oral dose of irinotecan."( Tyrosine kinase inhibitor enhances the bioavailability of oral irinotecan in pediatric patients with refractory solid tumors.
Crews, KR; Daw, NC; Furman, WL; Gajjar, AJ; Houghton, PJ; McCarville, MB; McGregor, LM; Navid, F; Panetta, JC; Rodriguez-Galindo, C; Santana, VM; Spunt, SL; Stewart, CF; Wu, J, 2009
)
0.35
" Gefitinib significantly enhances the bioavailability of oral irinotecan."( Tyrosine kinase inhibitor enhances the bioavailability of oral irinotecan in pediatric patients with refractory solid tumors.
Crews, KR; Daw, NC; Furman, WL; Gajjar, AJ; Houghton, PJ; McCarville, MB; McGregor, LM; Navid, F; Panetta, JC; Rodriguez-Galindo, C; Santana, VM; Spunt, SL; Stewart, CF; Wu, J, 2009
)
0.35
" For the orally bioavailable CGRP antagonist telcagepant 300 mg, the headache relief was only 55% in one phase III study."( Is there an inherent limit to the efficacy of calcitonin gene-related peptide receptor antagonists in the acute treatment of migraine? A comment.
Tfelt-Hansen, PC, 2009
)
0.35
" This study sought to determine the maximum tolerated dose (MTD) of erlotinib administered as a single 30-min infusion in patients with advanced solid tumors and absolute bioavailability of erlotinib tablets at matched doses."( A phase I dose-escalation and bioavailability study of oral and intravenous formulations of erlotinib (Tarceva, OSI-774) in patients with advanced solid tumors of epithelial origin.
Dean, E; Hamilton, M; Judson, I; McCarthy, S; Ranson, M; Reid, A; Shaw, H; Wolf, J, 2010
)
0.36
"This was a two-center, open label, Phase I, dose-escalation and bioavailability study of single dose IV and oral erlotinib."( A phase I dose-escalation and bioavailability study of oral and intravenous formulations of erlotinib (Tarceva, OSI-774) in patients with advanced solid tumors of epithelial origin.
Dean, E; Hamilton, M; Judson, I; McCarthy, S; Ranson, M; Reid, A; Shaw, H; Wolf, J, 2010
)
0.36
" Median bioavailability of erlotinib tablets was 76%."( A phase I dose-escalation and bioavailability study of oral and intravenous formulations of erlotinib (Tarceva, OSI-774) in patients with advanced solid tumors of epithelial origin.
Dean, E; Hamilton, M; Judson, I; McCarthy, S; Ranson, M; Reid, A; Shaw, H; Wolf, J, 2010
)
0.36
"A 100 mg single IV dose of erlotinib, given as a 30-min infusion, was well tolerated with only minor adverse events and the high level of bioavailability of oral erlotinib was confirmed."( A phase I dose-escalation and bioavailability study of oral and intravenous formulations of erlotinib (Tarceva, OSI-774) in patients with advanced solid tumors of epithelial origin.
Dean, E; Hamilton, M; Judson, I; McCarthy, S; Ranson, M; Reid, A; Shaw, H; Wolf, J, 2010
)
0.36
" Our study led to the identification of compound 59 as a highly potent, orally bioavailable CDK inhibitor that exhibited significant in vivo efficacy on the A2780 ovarian carcinoma xenograft model."( Identification of potent pyrazolo[4,3-h]quinazoline-3-carboxamides as multi-cyclin-dependent kinase inhibitors.
Ballinari, D; Brasca, MG; Casale, E; Ciomei, M; Colombo, N; Croci, V; Fiorentini, F; Isacchi, A; Longo, A; Mercurio, C; Panzeri, A; Pastori, W; Pevarello, P; Roussel, P; Traquandi, G; Volpi, D; Vulpetti, A, 2010
)
0.36
" One promising therapeutic approach is to identify drugs that have been developed for other indications but that also correct the CFTR trafficking defect, thereby exploiting their known safety and bioavailability in humans and reducing the time required for clinical development."( Correction of the Delta phe508 cystic fibrosis transmembrane conductance regulator trafficking defect by the bioavailable compound glafenine.
Balghi, H; Carlile, GW; de Jonge, HR; Hanrahan, JW; Kus, B; Lesimple, P; Liao, J; Liu, N; Robert, R; Rotin, D; Scholte, BJ; Thomas, DY; Wilke, M, 2010
)
0.36
" We report on a novel small molecule inhibitor of Hsp90, SNX-2112, and an orally bioavailable prodrug analog, SNX-5422."( Targeting of multiple signaling pathways by the Hsp90 inhibitor SNX-2112 in EGFR resistance models as a single agent or in combination with erlotinib.
Barabasz, A; Fadden, P; Foley, B; Hall, S; Huang, K; Rice, JW; Scott, A; Steed, P; Veal, JM, 2009
)
0.35
" For example, the 1,8-naphthyridine 52 was characterized as an orally bioavailable and brain penetrant TRPV1 antagonist."( Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists.
Bakthavatchalam, R; Blum, CA; Boyce, S; Brielmann, H; Burnaby-Davies, N; Caldwell, T; Capitosti, S; Chenard, BL; Conley, R; Cortright, D; Crandall, M; De Lombaert, S; Hodgetts, KJ; Jones, AB; Kershaw, MT; Krause, JE; Martin, WJ; Mason, G; Matson, D; Murphy, BA; Perrett, H; Rycroft, W; Zheng, X, 2010
)
0.36
" Moreover, compound 1·2HCl has an oral bioavailability of 98% with LD(50) values of 693 mg/kg (p."( Antitumor activity of 3,4-dihydroquinazoline dihydrochloride in A549 xenograft nude mice.
Chang, SK; Choo, DJ; Jung, SY; Kang, HB; Kim, J; Kim, YD; Lee, JY; Lee, KT; Lee, SH; Oh, CR; Park, HA; Seo, JH, 2010
)
0.36
" Moreover, the in vivo study showed that the oral bioavailability of CH330331 was 82."( Absorption of CH330331, a novel 4-anilinoquinazoline inhibitor of epidermal growth factor receptor tyrosine kinase: comparative studies using in vitro, in situ and in vivo models.
Bi, H; Huang, M; Liu, D; Qin, Z; Sun, H, 2010
)
0.36
" The objectives of the study were to investigate the pharmacokinetics and pharmacodynamics after intravenous administration of linagliptin and to determine its absolute bioavailability (F)."( Pharmacokinetics and pharmacodynamics of single rising intravenous doses (0.5 mg-10 mg) and determination of absolute bioavailability of the dipeptidyl peptidase-4 inhibitor linagliptin (BI 1356) in healthy male subjects.
Dugi, KA; Duval, V; Graefe-Mody, U; Hüttner, S; Jaehde, U; Jungnik, A; Retlich, S; Ring, A; Staab, A, 2010
)
0.36
" The absolute bioavailability was estimated to be about 30% for the linagliptin 10 mg tablet."( Pharmacokinetics and pharmacodynamics of single rising intravenous doses (0.5 mg-10 mg) and determination of absolute bioavailability of the dipeptidyl peptidase-4 inhibitor linagliptin (BI 1356) in healthy male subjects.
Dugi, KA; Duval, V; Graefe-Mody, U; Hüttner, S; Jaehde, U; Jungnik, A; Retlich, S; Ring, A; Staab, A, 2010
)
0.36
" Because of the nonlinear pharmacokinetics, the standard approach of comparing the AUC after oral administration with the AUC after intravenous administration was inappropriate to determine the absolute bioavailability of linagliptin."( Pharmacokinetics and pharmacodynamics of single rising intravenous doses (0.5 mg-10 mg) and determination of absolute bioavailability of the dipeptidyl peptidase-4 inhibitor linagliptin (BI 1356) in healthy male subjects.
Dugi, KA; Duval, V; Graefe-Mody, U; Hüttner, S; Jaehde, U; Jungnik, A; Retlich, S; Ring, A; Staab, A, 2010
)
0.36
"75 mg/day × 1 day) on the relative bioavailability of either compound in healthy subjects (n = 20, age 18-55 years)."( Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects.
Graefe-Mody, U; Iovino, M; Ring, A; Rose, P; Woerle, HJ; Zander, K, 2011
)
0.37
" Here we report the identification and characterization of NMS-P715, a selective and orally bioavailable MPS1 small-molecule inhibitor, which selectively reduces cancer cell proliferation, leaving normal cells almost unaffected."( Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase.
Avanzi, N; Bertrand, JA; Bossi, RT; Caldarelli, M; Cappella, P; Colombo, R; Colotta, F; Cucchi, U; Depaolini, SR; Donati, D; Galvani, A; Giorgini, ML; Isacchi, A; Mennecozzi, M; Moll, J; Perrera, C; Pesenti, E; Rusconi, L; Sola, F, 2010
)
0.36
"The oral bioavailability of vasicine (1) was investigated in hard gelatin capsules of lyophilized Vasa Swaras (aqueous extract of Adhatoda vasica Nees."( Formulation and pharmacokinetic evaluation of hard gelatin capsule encapsulating lyophilized Vasa Swaras for improved stability and oral bioavailability of vasicine.
Anandjiwala, S; Dash, RP; Nivsarkar, M; Vyas, T, 2011
)
0.37
" Reduced toxicity, enhancement of bioavailability and counteraction of resistance are features desired by clinicians."( Newer antifungal agents.
Türel, O, 2011
)
0.37
"A nonoral alternative such as transdermal system is desired to improve bioavailability and to maintain a constant and prolonged drug level with reduced frequency of dosing."( Influence of chemical permeation enhancers on transdermal permeation of alfuzosin: an investigation using response surface modeling.
Bindhani, A; Mallick, S; Pattnaik, S; Swain, K, 2011
)
0.37
" Vandetanib reduces constitutive NO production and increases blood pressure, yet flow-stimulated NO bioavailability was preserved."( Contrary effects of the receptor tyrosine kinase inhibitor vandetanib on constitutive and flow-stimulated nitric oxide elaboration in humans.
Beckman, JA; Burstein, HJ; Dallabrida, SM; Hannagan, K; Ismail, NS; Mayer, EL; Redline, WM; Rupnick, MA, 2011
)
0.37
" They are characterized by a moderate rate of absorption after oral administration with peak plasma concentrations at several hours post-dose."( Clinical pharmacokinetics of tyrosine kinase inhibitors: focus on 4-anilinoquinazolines.
Di Gion, P; Doroshyenko, O; Fuhr, U; Scheffler, M; Wolf, J, 2011
)
0.6
"The objective of this study was to determine the relative bioavailability of the dipeptidyl-peptidase-4 (DPP-4) inhibitor linagliptin when administered with and without food, in accordance with regulatory requirements to support dosing recommendations for patients."( A randomized, open-label, crossover study evaluating the effect of food on the relative bioavailability of linagliptin in healthy subjects.
Giessmann, T; Graefe-Mody, U; Iovino, M; Ring, A; Woerle, HJ, 2011
)
0.37
" Relative bioavailability was assessed by the total area under the curve between 0 and 72 hours (AUC(0-72)) and maximum measured plasma concentration (C(max)) of linagliptin."( A randomized, open-label, crossover study evaluating the effect of food on the relative bioavailability of linagliptin in healthy subjects.
Giessmann, T; Graefe-Mody, U; Iovino, M; Ring, A; Woerle, HJ, 2011
)
0.37
"3 kg; male, 53%; white race, 100%), intake of a high-fat meal resulted in comparable bioavailability with regard to AUC(0-72) (geometric mean ratio [GMR] between the fed and fasted group means was 103."( A randomized, open-label, crossover study evaluating the effect of food on the relative bioavailability of linagliptin in healthy subjects.
Giessmann, T; Graefe-Mody, U; Iovino, M; Ring, A; Woerle, HJ, 2011
)
0.37
" Tryptanthrin was well absorbed across the Caco-2 monolayers, and its transepithelial transports were dominated by passive diffusion."( Transport characteristics of tryptanthrin and its inhibitory effect on P-gp and MRP2 in Caco-2 cells.
Ma, G; Wang, H; Yan, J; Yang, Q; Zhang, X; Zhu, X, 2011
)
0.37
"The bioavailability of Rut and Evo was increased along with the increasing of purity (16%-80%) in Wu-Chu-Yu extracts."( Pharmacokinetic comparisons of rutaecarpine and evodiamine after oral administration of Wu-Chu-Yu extracts with different purities to rats.
Chen, F; Ding, J; He, L; Li, Y; Peng, J; Xu, S; Zhang, J, 2012
)
0.38
" Two studies evaluated the role of P-gp-mediated transport in the bioavailability and intestinal secretion of linagliptin in rats."( Excretion of the dipeptidyl peptidase-4 inhibitor linagliptin in rats is primarily by biliary excretion and P-gp-mediated efflux.
Fuchs, H; Held, HD; Runge, F, 2012
)
0.38
" One triphenylbutanamine analogue and ispinesib possess very good bioavailability (51% and 45%, respectively), with the former showing in vivo antitumor growth activity in nude mice xenograft studies."( Triphenylbutanamines: kinesin spindle protein inhibitors with in vivo antitumor activity.
Good, JA; Kaan, HY; Kozielski, F; Mackay, SP; Rath, O; Sutcliffe, OB; Wang, F, 2012
)
0.38
" CEP-32496 is orally bioavailable in multiple preclinical species (>95% in rats, dogs, and monkeys) and has single oral dose pharmacodynamic inhibition (10-55 mg/kg) of both pMEK and pERK in BRAF(V600E) colon carcinoma xenografts in nude mice."( CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity.
Apuy, JL; Armstrong, RC; Ator, MA; Bhagwat, SS; Cheng, M; Cramer, MD; Dobrzanski, P; Dorsey, BD; Faraoni, R; Gardner, MF; Gitnick, D; Gunawardane, RN; Holladay, MW; Hunter, K; Insko, DE; James, J; Jones-Bolin, S; Nepomuceno, RR; Rowbottom, MW; Ruggeri, B; Williams, M; Yazdanian, M; Zhao, H, 2012
)
0.38
" NMS-P937, with its favorable pharmacologic parameters, good oral bioavailability in rodent and nonrodent species, and proven antitumor activity in different preclinical models using a variety of dosing regimens, potentially provides a high degree of flexibility in dosing schedules and warrants investigation in clinical settings."( NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies.
Alli, C; Alzani, R; Avanzi, N; Ballinari, D; Beria, I; Cappella, P; Caruso, M; Casolaro, A; Ciavolella, A; Cucchi, U; De Ponti, A; Felder, E; Fiorentini, F; Galvani, A; Gianellini, LM; Giorgini, ML; Isacchi, A; Lansen, J; Moll, J; Pesenti, E; Rizzi, S; Rocchetti, M; Sola, F; Valsasina, B, 2012
)
0.38
" SKLB1206 also showed a very good oral bioavailability (50."( SKLB1206, a novel orally available multikinase inhibitor targeting EGFR activating and T790M mutants, ErbB2, ErbB4, and VEGFR2, displays potent antitumor activity both in vitro and in vivo.
Cao, Z; Chen, X; Feng, S; Ji, P; Liu, J; Luo, S; Pan, Y; Wang, BL; Wang, L; Wang, X; Wang, Z; Wei, YQ; Xu, Y; Yang, HY; Yang, J; Yang, SY; Yu, Y; Zhang, S; Zheng, R; Zhong, L, 2012
)
0.38
"In recent years, new and effective therapeutic agents for blood glucose control have been added to standard diabetes therapies: dipeptidyl peptidase-4 (DPP-4) inhibitors, which prolong the bioavailability of the endogenously secreted incretin hormone glucagon-like peptide-1 (GLP-1)."( The dipeptidyl peptidase-4 inhibitor linagliptin attenuates inflammation and accelerates epithelialization in wounds of diabetic ob/ob mice.
Engelmann-Pilger, K; Frank, S; Klein, T; Linke, A; Mark, M; Pfeilschifter, J; Schürmann, C; Steinmetz, C, 2012
)
0.38
" The oral bioavailability of linagliptin estimated with this model is approximately 30%."( Clinical pharmacokinetics and pharmacodynamics of linagliptin.
Friedrich, C; Graefe-Mody, U; Retlich, S, 2012
)
0.38
"Vandetanib (an orally bioavailable VEGFR-2 and EGFR tyrosine kinases inhibitor) was combined at 100 mg, 200 mg, or 300 mg daily with standard dosed cetuximab and irinotecan (3+3 dose-escalation design)."( Phase I study of cetuximab, irinotecan, and vandetanib (ZD6474) as therapy for patients with previously treated metastastic colorectal cancer.
Abrams, TA; Ancukiewicz, M; Blaszkowsky, L; Chan, JA; Duda, DG; Elliott, M; Enzinger, PC; Goldstein, M; Jain, RK; Kulke, MH; Meyerhardt, JA; Regan, E; Schrag, D; Wolpin, BM; Zhu, AX, 2012
)
0.38
" Anagrelide is metabolized by cytochrome P450 (CYP) 1A2, and previous studies of the effect of food on the bioavailability and pharmacokinetics of anagrelide were conducted prior to the identification of the active metabolite, 3-hydroxyanagrelide."( Cardiovascular safety of anagrelide in healthy subjects: effects of caffeine and food intake on pharmacokinetics and adverse reactions.
Datino, T; Fernández-Avilés, F; Figueiras-Graillet, L; Franklin, R; Gama, JG; Jones, C; Martínez-Sellés, M, 2013
)
0.39
" Friend Leukemia Virus Strain B (FVB) mice were used to determine the bioavailability of elacridar after a 10 mg/kg dose of elacridar in the microemulsion, intraperitoneally (i."( Development and evaluation of a novel microemulsion formulation of elacridar to improve its bioavailability.
Elmquist, WF; Mittapalli, RK; Sane, R, 2013
)
0.39
" Those with the best potency and oral bioavailability were progressed to evaluations of efficacy against acute murine TB."( Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents.
Cho, SN; Franzblau, SG; Hwang, JM; Kaneko, T; Kim, P; Ma, Z; Oh, T; Upton, AM, 2013
)
0.39
" They have good oral bioavailability and pharmacokinetics and induced complete tumor regression in nude mice explanted with lung cancer patient xenografts."( Optimized S-trityl-L-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models.
Good, JA; Kaan, HY; Kozielski, F; MacKay, SP; Podgórski, D; Rath, O; Talapatra, SK; Wang, F, 2013
)
0.39
" Our compound optimization that has led to synthesis of several potent 4-anilinoquinazolines, including NEU617, 23a, a highly potent, orally bioavailable inhibitor of trypanosome replication."( Kinase scaffold repurposing for neglected disease drug discovery: discovery of an efficacious, lapatinib-derived lead compound for trypanosomiasis.
Behera, R; Edwards, P; Guyett, PJ; Karver, CE; Mensa-Wilmot, K; Patel, G; Pollastri, MP; Roncal, NE; Sullenberger, C, 2013
)
0.62
" Pharmacological inhibition of dipeptidylpeptidase-4 (DPP-4) to increase the bioavailability of glucagon-like peptide-1 is an emerging therapy for control of glycemia in type 2 diabetes patients."( Dipeptidylpeptidase inhibition is associated with improvement in blood pressure and diastolic function in insulin-resistant male Zucker obese rats.
Aroor, AR; Bender, SB; Demarco, VG; Garro, M; Hayden, MR; Johnson, MS; Mugerfeld, I; Nistala, R; Salam, M; Sowers, JR; Whaley-Connell, A, 2013
)
0.39
"The LUX-Lung 3 study investigated the efficacy of chemotherapy compared with afatinib, a selective, orally bioavailable ErbB family blocker that irreversibly blocks signaling from epidermal growth factor receptor (EGFR/ErbB1), human epidermal growth factor receptor 2 (HER2/ErbB2), and ErbB4 and has wide-spectrum preclinical activity against EGFR mutations."( Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations.
Bennouna, J; Boyer, M; Geater, SL; Gorbunova, V; Hirsh, V; Kato, T; Lee, KH; Massey, D; Mok, T; O'Byrne, K; Orlov, S; Schuler, M; Sequist, LV; Shah, R; Shahidi, M; Su, WC; Tsai, CM; Yamamoto, N; Yang, JC; Zazulina, V, 2013
)
0.39
"As the bioavailability of erlotinib is dependent on gastric pH, an increase in gastric pH via the concurrent use of gastric acid suppressive medications (AS) may reduce its bioavailability and efficacy."( An evaluation of the possible interaction of gastric acid suppressing medication and the EGFR tyrosine kinase inhibitor erlotinib.
Bradbury, PA; Hilton, JF; Seymour, L; Shepherd, FA; Tu, D, 2013
)
0.39
" Vandetanib, also known as ZD6474, is an orally bioavailable small molecule tyrosine kinase inhibitor of multiple growth factors that is an antagonist of the vascular endothelial growth factor receptor-2 (VEGFR-2)."( Specific binding of modified ZD6474 (Vandetanib) monomer and its dimer with VEGF receptor-2.
Kim, YS; Li, F; Li, Z; O'Neill, BE, 2013
)
0.39
" Its oral bioavailability is low and its intestinal absorption mechanism is not clear."( Intestinal absorption of raltitrexed and evaluation of the effects of absorption enhancers.
Li, X; Lu, Y; Yin, Z; Yu, Y; Zhao, X, 2013
)
0.39
"To improve the solubility, bioavailability and anti-tumor effect of lapatinib, lapatinib-incorporated lipid nanoparticles (LTNPs) were prepared and characterized."( In vivo behavior and safety of lapatinib-incorporated lipid nanoparticles.
Cao, S; Chen, C; Chen, J; Gao, H; Jiang, X; Xi, Z; Zhang, Q, 2014
)
0.4
"The objectives of the studies reported here were to determine the relative bioavailability of linagliptin and metformin when administered in a fixed-dose combination (FDC) tablet with and without food, and to investigate the relative bioavailability of linagliptin and metformin FDC tablets from two treatment batches with different dissolution behavior."( Effect of food and tablet-dissolution characteristics on the bioavailability of linagliptin fixed-dose combination with metformin: evidence from two randomized trials.
Friedrich, C; Hohl, K; Jungnik, A; Meinicke, T; Metzmann, K; Ring, A; Schnell, D; Theodor, R, 2014
)
0.4
"The administration of the FDC tablet with food had no influence on the relative bioavailability of linagliptin and metformin with regard to the extent of exposure as determined by AUC(0-72) (linagliptin) and AUC(0-inf) (metformin) compared with FDC tablet administration while fasting."( Effect of food and tablet-dissolution characteristics on the bioavailability of linagliptin fixed-dose combination with metformin: evidence from two randomized trials.
Friedrich, C; Hohl, K; Jungnik, A; Meinicke, T; Metzmann, K; Ring, A; Schnell, D; Theodor, R, 2014
)
0.4
"Food did not have a relevant impact on the bioavailability of linagliptin from the FDC tablet."( Effect of food and tablet-dissolution characteristics on the bioavailability of linagliptin fixed-dose combination with metformin: evidence from two randomized trials.
Friedrich, C; Hohl, K; Jungnik, A; Meinicke, T; Metzmann, K; Ring, A; Schnell, D; Theodor, R, 2014
)
0.4
" Pharmacokinetically, after oral administration, gefitinib is slowly absorbed with bioavailability of approximately 60% in human."( Gefitinib.
Kassem, MG; Korashy, HM; Rahman, AF, 2014
)
0.4
" It shows moderate oral bioavailability of 42-53 % and Tmax < 4 h in mouse, rat, dog and monkey, with exposure-dose linearity proved in rats and dogs."( Preclinical pharmacokinetics and disposition of a novel selective VEGFR inhibitor fruquintinib (HMPL-013) and the prediction of its human pharmacokinetics.
Gu, Y; Guo, L; Li, K; Ren, H; Sai, Y; Su, W; Wang, J; Zhang, L; Zhang, W, 2014
)
0.4
" It also showed a moderate oral bioavailability and good safety in vivo."( Novel N-substituted sophoridinol derivatives as anticancer agents.
Bi, CW; Deng, HB; Li, YH; Shao, RG; Song, DQ; Tang, S; Wang, Z; Zhang, CX; Zhao, WL, 2014
)
0.4
" Afatinib is a novel, orally bioavailable irreversible pan-HER inhibitor that has been evaluated in multiple tumor types."( Afatinib in the treatment of breast cancer.
Harbeck, N; Hurvitz, SA; Shatsky, R, 2014
)
0.4
" However, low bioavailability caused by its poor water solubility limits it anticancer efficacy in clinic."( Preparation, characterization, and anticancer efficacy of evodiamine-loaded PLGA nanoparticles.
Bao, J; Chen, F; Chen, M; He, C; Wang, L; Wang, S; Wang, Y; Zou, L, 2016
)
0.43
" The possible explanations for improved absorption and bioavailability were put forward here."( Supermolecular evodiamine loaded water-in-oil nanoemulsions: enhanced physicochemical and biological characteristics.
Fang, C; Hu, J; Sun, L; Tan, Q; Wang, H; Ye, M; Zhang, J; Zhang, L; Zhao, D, 2014
)
0.4
" Pharmacokinetic analysis confirms that co-administration of gefitinib increases irinotecan bioavailability leading to an increased SN-38 lactone systemic exposure."( Phase I dose escalation and pharmacokinetic study of oral gefitinib and irinotecan in children with refractory solid tumors.
Brennan, RC; Furman, W; Mao, S; McGregor, LM; Santana, V; Stewart, CF; Turner, DC; Wu, J, 2014
)
0.4
"Compared with EDA or conventional nanoemulsions containing EDA instead of evodiamine-phospholipid complex, NEEPN with its favorable in vivo kinetic characteristics clearly enhanced the gastrointestinal absorption and oral bioavailability of EDA; for example, the relative bioavailability of NEEPN to free EDA was calculated to be 630."( Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine-phospholipid nanocomplex.
Chen, D; Hu, J; Jiang, R; Tan, Q; Zhang, J; Zhu, B, 2014
)
0.4
"NEEPN markedly improved the oral bioavailability of EDA, which was probably due to its increased gastrointestinal absorption."( Improved absorption and in vivo kinetic characteristics of nanoemulsions containing evodiamine-phospholipid nanocomplex.
Chen, D; Hu, J; Jiang, R; Tan, Q; Zhang, J; Zhu, B, 2014
)
0.4
" In this article, we report the discovery of highly potent, selective, and orally bioavailable MMP-13 inhibitors as well as their detailed structure-activity data."( Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Kanzaki, N; Kori, M; Kuno, H; Mototani, H; Naito, T; Nara, H; Oki, H; Santou, T; Sato, K; Terauchi, J; Uchikawa, O; Yamamoto, Y, 2014
)
0.4
" The absorption rate constant was influenced by food."( Population pharmacokinetics of HM781-36 (poziotinib), pan-human EGF receptor (HER) inhibitor, and its two metabolites in patients with advanced solid malignancies.
Bae, KS; Jung, JA; Lim, HS; Noh, YH; Song, TH, 2015
)
0.42
" We evaluated the comparative bioavailability and tolerability of the test and reference formulations in healthy adult volunteers."( Pharmacokinetic properties of two erlotinib 150 mg formulations with a genetic effect evaluation in healthy Korean subjects.
Cho, SJ; Choi, HG; Im, YJ; Jeon, JY; Kim, MG; Kim, Y; Seo, YH; Song, EK, 2015
)
0.42
" Despite of poor physico-chemical properties of hit compound 1, our medicinal chemistry effort allowed the discovery and characterization of lead compound 33 (SEN461), with improved ADME profile, good bioavailability and active in vitro and in vivo in glioblastoma, gastric and sarcoma tumors."( Structure-activity relationship and properties optimization of a series of quinazoline-2,4-diones as inhibitors of the canonical Wnt pathway.
Andreini, M; Bakker, A; Benicchi, T; Cappelli, F; Caradonna, NP; De Robertis, A; Magnani, M; Mennillo, F; Nencini, A; Nibbio, M; Pratelli, C; Quinn, JM; Rossi, M; Salerno, M; Tunici, P; Turlizzi, E; Valensin, S; Varrone, M; Zanelli, U, 2015
)
0.42
" However, there was no clinically significant difference in bioavailability or toxicity between the two clinically used fed conditions at least in 14 days."( Comparison of the pharmacokinetics of erlotinib administered in complete fasting and 2 h after a meal in patients with lung cancer.
Fujiwara, Y; Goto, Y; Hamada, A; Horinouchi, H; Kanda, S; Katsuya, Y; Nokihara, H; Ohe, Y; Osawa, S; Sunami, K; Takashima, Y; Tamura, T; Utsumi, H; Yamamoto, N, 2015
)
0.42
" Typical value of clearance, distribution clearance, central volume of distribution, maximum absorption rate were 29."( Development of population pharmacokinetics model of icotinib with non-linear absorption characters in healthy Chinese volunteers to assess the CYP2C19 polymorphism and food-intake effect.
Chen, J; Hu, P; Jiang, J; Liu, D; Zhao, Q; Zheng, X, 2015
)
0.42
"To evaluate the relative bioavailability of single pill combination (SPC) tablets of linagliptin and metformin compared with separate tablets co-administered in healthy Chinese subjects."( Relative bioavailability study of linagliptin/metformin tablets in healthy Chinese subjects.
Cui, Y; Friedrich, C; Hohl, K; Meinicke, T; Pichereau, S; Zhao, S; Zhao, X, 2015
)
0.42
" Furthermore, the optimized compounds 7q and 8f also demonstrated good pharmacokinetic profiles, oral bioavailability as well as excellent in vivo efficacy in H1975 and HCC827 xenografts at a non-toxic dose."( Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors.
Chen, D; Fan, C; Li, Y; Yang, Y; Zhang, L; Zhao, S; Zheng, Q; Zheng, S; Zhou, H, 2015
)
0.42
" 23bb has a good pharmacokinetic profile with oral bioavailability of 47."( Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer.
Cao, D; Chen, L; Chen, X; Liu, Z; Long, C; Ma, L; Niu, T; Tang, M; Wang, F; Wang, T; Wang, X; Xiang, W; Yang, Z; Yi, Y; You, J, 2016
)
0.43
" (-)-Epicatechin prevented a compromised NO bioavailability and the development of oxidative stress produced by fructose overload essentially acting on superoxide anion metabolism."( Modifications in nitric oxide and superoxide anion metabolism induced by fructose overload in rat heart are prevented by (-)-epicatechin.
Calabró, V; Fischerman, L; Fraga, CG; Galleano, M; Piotrkowski, B; Vazquez Prieto, MA, 2016
)
0.43
" To minimize systemic exposure, a topically active PDE4 inhibitor with low transdermal bioavailability could be clinically useful."( Efficacy of a novel phosphodiesterase inhibitor, E6005, in patients with atopic dermatitis: An investigator-blinded, vehicle-controlled study.
Akama, H; Hojo, S; Imayama, S; Matsuguma, K; Matsuki, S; Nomoto, M; Ohba, F, 2016
)
0.43
" Unfortunately, the low oral bioavailability of lapatinib and drug efflux by blood-brain barrier have resulted in low drug delivery efficiency into the brain and limited therapeutic effects for patients with brain metastasis in clinical trials."( Lapatinib-loaded human serum albumin nanoparticles for the prevention and treatment of triple-negative breast cancer metastasis to the brain.
Jiang, T; Jiang, X; Pang, X; Pang, Z; Wan, X; Xu, W; Zhang, Q; Zhang, Z; Zhao, J; Zheng, X, 2016
)
0.43
" We have tested this hypothesis using an orally bioavailable Src inhibitor (saracatinib) in a rat model of cancer-induced bone pain."( Effects of Src-kinase inhibition in cancer-induced bone pain.
Andrew, D; De Felice, M; Escott, KJ; Holen, I; Lambert, D, 2016
)
0.43
" The relative bioavailability of evodiamine inclusion complex was 256."( [A preliminary study of pharmacokinetics of evodiamine hydroxypropyl-β-cyclodextrin inclusion complex].
Feng, J; Lei, TT; Liu, HM; Zhang, JQ; Zhang, X, 2016
)
0.43
" Additionally, there was no statistical difference in tlag or tmax , suggesting no difference in the absorption rate between treatments."( Bioequivalence study with lapatinib powder for oral suspension and the original tablet formulation in cancer patients.
Arya, N; Cartee, L; Curran, D; D'Amelio, AM; Ferron-Brady, G; Hollyfield, H; Koch, KM; Lemmon, C; Piepszak, A; Swaby, RF,
)
0.13
"Molecularly targeted agents that are designed to target specific lesions have been proven effective as clinical cancer therapies; however, most currently available therapeutic agents are poorly water-soluble and require oral administration, thereby resulting in low bioavailability and a high risk of side effects due to dose intensification."( iRGD-Decorated Polymeric Nanoparticles for the Efficient Delivery of Vandetanib to Hepatocellular Carcinoma: Preparation and in Vitro and in Vivo Evaluation.
Li, J; Liu, Z; Lu, D; Wang, H; Wang, J; Wei, X; Xie, H; Xu, X; Zheng, S; Zhuang, R, 2016
)
0.43
"We report the results of feasibility, phase I, and phase II studies of tandutinib (MLN518), an orally bioavailable inhibitor of type III receptor tyrosine kinases including PDGF receptor-β, Fms-like tyrosine kinase 3, and c-Kit in patients with recurrent glioblastoma."( Feasibility, phase I, and phase II studies of tandutinib, an oral platelet-derived growth factor receptor-β tyrosine kinase inhibitor, in patients with recurrent glioblastoma.
Batchelor, TT; Chowdhary, S; Desideri, S; Duda, DG; Gerstner, ER; Grossman, S; Lesser, GJ; Peereboom, D; Supko, JG; Wen, PY; Ye, X, 2017
)
0.46
"Lapatinib is an orally bioavailable dual inhibitor of the intracellular domain of both the HER2 protein and the epidermal growth factor receptor."( [A Case of Interstitial Pneumonitis Induced by Lapatinib plus Letrozole].
Yamamoto, C; Yamamoto, D; Yamamoto, M, 2016
)
0.43
"This open-label, randomized, phase 1 crossover study investigated the effect of elevated gastric pH level (>5) on the relative bioavailability and pharmacokinetic profile of the epidermal growth factor receptor tyrosine kinase inhibitor gefitinib."( Effect of Sustained Elevated Gastric pH Levels on Gefitinib Exposure.
Masson, E; Tang, W; Tomkinson, H, 2017
)
0.46
" The results revealed that a significant reduction in the oral bioavailability was recorded with both ERL and LAP following the ingestion of GTE particularly for short-term administration."( UPLC-ESI-MS/MS study of the effect of green tea extract on the oral bioavailability of erlotinib and lapatinib in rats: Potential risk of pharmacokinetic interaction.
Abahussain, AO; Alzoman, NZ; Maher, HM; Shehata, SM, 2017
)
0.46
" Bioavailability of AER was 55% of the CARP under fasting conditions and 60% under fed conditions."( Pharmacokinetics of a Novel Anagrelide Extended-Release Formulation in Healthy Subjects: Food Intake and Comparison With a Reference Product.
Jilma, B; Klade, CS; Petrides, PE; Schoergenhofer, C; Widmann, R, 2018
)
0.48
" It is an accepted opinion that modifying GEF strong hydrophobicity and poor bioavailability would not only enhance its antitumor effects, but also reduce its side effects."( In vitro and in vivo antitumor effect of gefitinib nanoparticles on human lung cancer.
Chen, LX; Chen, Y; Fu, SZ; Liu, J; Ni, XL; Wu, JB; Wu, M; Xu, S; Yang, B; Yang, LL; Zhang, H, 2017
)
0.46
" Oral area under the plasma concentration-time curve (AUC) and bioavailability of well known BCRP (sulfasalazine and rosuvastatin), P-glycoprotein (fexofenadine, aliskiren, and talinolol), and CYP3A (midazolam) substrates were investigated in the presence and absence of inhibitors."( Curcumin as an In Vivo Selective Intestinal Breast Cancer Resistance Protein Inhibitor in Cynomolgus Monkeys.
Abe, K; Ando, O; Imaoka, T; Karibe, T, 2018
)
0.48
" These ingredients are expected to have much better absorption and higher bioavailability than synthetic antitumor agents."( Improved delivery of natural alkaloids into lung cancer through woody oil-based emulsive nanosystems.
Hu, X; Li, Y; Liu, S; Yan, S; Yang, L; Zeng, M; Zhang, J; Zhang, Y; Zhao, H; Zhao, J, 2018
)
0.48
"Afatinib, a second-generation irreversible epidermal growth factor inhibitor receptor for the development of non-small cell lung cancer and secondary drug resistance, has low bioavailability and adverse reactions due to current oral administration."( [Formulation and Efficacy of Liposome-encapsulated Afatinib for Therapy of Non-small Cell Lung Cancer].
Liu, S; Lv, X; Sun, K; Yang, X; Yin, J, 2018
)
0.48
" DVAS exhibited linear dose-proportional pharmacokinetics at doses of 5, 15, and 45 mg/kg after oral administration, and the average oral absolute bioavailability of DVAS was 47."( In vivo and in vitro metabolism and pharmacokinetics of cholinesterase inhibitor deoxyvasicine from aerial parts of Peganum harmala Linn in rats via UPLC-ESI-QTOF-MS and UPLC-ESI-MS/MS.
Cao, N; Cheng, X; Deng, G; Ding, W; Guan, H; Liu, W; Ma, C; Rong, X; Wang, C; Wang, Y; Wu, C; Zhang, Y, 2019
)
0.51
"The overall bioavailability of the evaluated formulation of fruquintinib was not affected by the consumption of a high-fat, high-calorie meal prior to dosing."( Effects of a High-fat Meal on the Pharmacokinetics of the VEGFR Inhibitor Fruquintinib: A Randomized Phase I Study in Healthy Subjects.
Chen, Q; Fan, S; Jia, J; Li, K; Li, T; Liu, Y; Qian, H; Sai, Y; Su, W; Wang, W; Yu, C, 2019
)
0.51
" Previous findings demonstrate that evodiamine (Evo), an indolequinone alkaloid, is effective in combating CRC; however, its poor aqueous solubility and low oral bioavailability limit its application in the prevention of invasion and metastasis of CRC."( Development of EGFR-targeted evodiamine nanoparticles for the treatment of colorectal cancer.
Cai, G; Cai, J; Gao, R; Ji, Q; Li, C; Li, Q; Song, D; Sui, H; Teng, P; Wang, Y; Zhou, L, 2019
)
0.51
"The current work aimed to develop low-density gastroretentive sponges loaded with alfuzosin HCl (ALF) to sustain the rate of drug release, improve its oral bioavailability and deliver it to the main site of absorption."( Alfuzosin hydrochloride-loaded low-density gastroretentive sponges: development,
Abd El-Aziz, MF; Elnabarawi, MA; Ismail, S; Tadros, MI, 2020
)
0.56
" As BPR1K871 lacks oral bioavailability, we continued searching for orally bioavailable analogs through drug-like property optimization."( Drug-like property optimization: Discovery of orally bioavailable quinazoline-based multi-targeted kinase inhibitors.
Chang, CF; Chen, CH; Chen, PY; Coumar, MS; Hsieh, HP; Hsu, JTA; Kuo, FM; Kuo, PC; Li, AS; Li, MC; Lin, CY; Lin, SY; Lin, WH; Song, JS; Wang, SY; Yang, CM; Yeh, TK, 2020
)
0.56
"We assessed the pharmacokinetics and safety of a single oral administration of selatinib to healthy Chinese subjects and evaluated the potential bioavailability advantage of selatinib relative to lapatinib."( First-in-human, phase I single-ascending-dose study of the safety, pharmacokinetics, and relative bioavailability of selatinib, a dual EGFR-ErbB2 inhibitor in healthy subjects.
Cao, Y; Gong, LY; Guo, CX; Hua, Y; Huang, J; Kuang, Y; Pei, Q; Wang, MN; Yang, GP, 2020
)
0.56
" An orally bioavailable GRK2 inhibitor could offer unique therapeutic outcomes that cannot be attained by current heart failure treatments that directly target GPCRs or angiotensin-converting enzyme."( Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor.
DesJarlais, RL; Gaul, MD; Hermans, A; Huang, DZ; Krosky, D; Liu, Z; Lu, HR; Milligan, CM; Petrounia, I; Qi, J; Spurlino, JC; Wang, W; Xu, G; Xu, JZ, 2020
)
0.56
" Given the favorable safety profile and its oral bioavailability letermovir may be considered a valuable off-label option for secondary prophylaxis of GCV-resistant CMV in SOT recipients."( Emergence of letermovir resistance in solid organ transplant recipients with ganciclovir resistant cytomegalovirus infection: A case series and review of the literature.
Bittel, P; Dahdal, S; Hirzel, C; Hofmann, E; Manuel, O; Sidler, D; Suter-Riniker, F; Walti, LN, 2021
)
0.62
" These staged analyses indicate that letermovir PK in HSCT recipients and healthy participants differ only with respect to bioavailability and absorption rate."( Population pharmacokinetics of letermovir following oral and intravenous administration in healthy participants and allogeneic hematopoietic cell transplantation recipients.
Cho, CR; Davis, C; de Alwis, D; Dykstra, K; Fancourt, C; Iwamoto, M; Macha, S; Prohn, M; Sabato, P; Viberg, A; Zhang, D, 2021
)
0.62
" In vivo experimental results indicated that compared to intragastric administration of drug solution, the intranasal administration of hydrogel increased bioavailability of BBR and EVO, approximately 135 and 112 folds, respectively."( Intranasal co-delivery of berberine and evodiamine by self-assembled thermosensitive in-situ hydrogels for improving depressive disorder.
Cui, YL; Qiao, T; Qiu, C; Wang, Y; Xu, D, 2021
)
0.62
" 6c showed a favorable pharmacokinetic profile in vivo, with a bioavailability of 65."( Design of Orally-bioavailable Tetra-cyclic phthalazine SOS1 inhibitors with high selectivity against EGFR.
Chen, R; Fang, H; He, H; Liu, Y; Pan, W; Qing, L; Wang, Z; Zhang, S; Zhang, Y, 2023
)
0.91
" The hit compound showed a good bioavailability score (0."( Identification and exploration of quinazoline-1,2,3-triazole inhibitors targeting EGFR in lung cancer.
Ali, I; Azizov, S; Gupta, MK; Kumar, D; Kumar, S; Lalhlenmawia, H; Sengupta, S, 2023
)
0.91
" In this study, we report the discovery of quinazolines and 8-azaquinazolines as NLRP3 agonists and their chemical optimization to afford compounds with oral bioavailability in mice."( Discovery and characterisation of quinazolines and 8-Azaquinazolines as NLRP3 agonists with oral bioavailability in mice.
Baker, D; Ciotta, G; Degorce, SL; Demanze, S; Dockerill, M; Escudero-Ibarz, L; Ireland, L; Mao, Y; O' Donovan, DH; Packer, MJ; Robinson, J; Scarfe, G; Tang, H; Valge-Archer, V, 2023
)
1.45

Dosage Studied

ExcerptRelevanceReference
" There was a distinct improvement in the course of the 4 weeks' therapy with a mean dosage of 900 mg/day (it was in the meantime raised to a maximum of 1500 mg/day in isolated cases) especially in the pain, stiffness and functional capacity."( [Effect and tolerance of Biarison (proquazone) in rheumatoid arthritis (author's transl)].
Ghimicescu, R, 1978
)
0.26
" Dosage can be progressively increased up to 30 mg/day."( [Prazosine: a new vasodilator used for treatment of hypertension (author's transl)].
Bret, M; Fillastre, JP; Godin, M, 1978
)
0.26
" In contrast, BL-5111, an antihypertensive agent similar in chemical structure and shown in previous studies to be slightly less potent than prazosin but with appreciably less alpha-adrenergic receptor antagonist activity, had no effect on blood pressure at 12 hours after dosing (1 and 2 mg/kg po)."( Comparative first dose effects of prazosin and tiodazosin (BL-5111) in spontaneously hypertensive rats.
Buyniski, JP; Florczyk, AP; Roebel, LE, 1979
)
0.26
" Frusemide dosage was increased and the alpha adrenoreceptor blocking drug prazosin hydrochloride was added to the therapeutic regime."( The use of alpha blockade in the treatment of congestive heart failure associated with dirofilariasis and mitral valvular incompetence.
Atwell, RB, 1979
)
0.26
"In order to determine and compare the pharmacodynamic responses to single and multiple dose prazosin therapy in cardiac failure, 14 patients with severe low-output heart failure underwent central and regional hemodynamic measurements after random placement in one of two prazosin dosing schedules."( Development of pharmacodynamic tolerance to prozosin in congestive heart failure.
Blanford, MF; Desch, CE; Leier, CV; Magorien, RD; Triffon, DW; Unverferth, DV, 1979
)
0.26
"The pharmacokinetics and effects of prazosin have been studied after intravenous and oral dosing (1 mg) to 6 normal male volunteers."( Prazosin, pharmacokinetics and concentration effect.
Bateman, DN; Hobbs, DC; Rawlins, MD; Stevens, EA; Twomey, TM, 1979
)
0.26
" Examination of data from each subject on repeated dosing indicates considerable intrasubject consistency in pharmacokinetic response despite intersubject variability."( Pharmacokinetics of prazosin in man.
Hobbs, DC; Palmer, RF; Twomey, TM,
)
0.13
"In fifteen patients with hypertension, inadequately controlled during treatment with propranolol alone (mean dosage 333 mg/day), plasma volume (PV) and extracellular fluid volume (ECV) were determined."( Changes in plasma volume and extracellular fluid volume after addition of prazosin to propranolol treatment in patients with hypertension.
Ibsen, H; Jensen, HA; Leth, A; Rasmussen, K, 1978
)
0.26
" The dosage used was 1 mg TDS."( A phase II study of prazosin hydrochloride in hypertensive subjects.
Paul, RR; Sharma, PL; Wahi, PL, 1976
)
0.26
" Dosage increments were limited to 0-5 mg, beginning late in the evening."( Prazosin in the treatment of patients with hypertension and renal functional impairment.
Bailey, RR, 1977
)
0.26
" In patients with mild hypertension, prazosin in a dosage of 5 mg three or four times a day was consistently effective in lowering blood pressure to less than 100 mm Hg and often reduced it to less than 95 mm Hg."( Clinical evaluation of prazosin in 20 private practice patients.
Maher, PH, 1975
)
0.25
" The maximum useful dosage of prazosin was not defined, but increasing the dosage above 15 mg a day did not improve control of blood pressure."( Treatment of hypertension with a combination of prazosin and polythiazide.
Carroll, HJ; Cruz, WM; Lejano, RF; Oh, MS; Whang, ES, 1975
)
0.25
" The selective A1 receptor antagonist DPCPX also had no effect on release when administered at a low dosage (0."( Excitatory transmitter amino acid release from the ischemic rat cerebral cortex: effects of adenosine receptor agonists and antagonists.
O'Regan, MH; Perkins, LM; Phillis, JW; Simpson, RE, 1992
)
0.28
" Thus, these improvements were not correlated with the dosage of drug."( [The evaluation of the effects of bunazosin hydrochloride in the treatment of prostatic hyperplasia].
Asano, H; Fujita, T; Hirabayashi, S; Kato, N; Kinukawa, T; Ohshima, S; Ono, Y, 1992
)
0.28
" dosing to bile duct-cannulated rats, 96% of the radioactive dose was excreted in the bile."( Absorption, distribution and excretion of zenarestat, a new aldose reductase inhibitor, in rats and dogs.
Esumi, Y; Katami, Y; Noda, K; Sawamoto, T; Sekiguchi, M; Tanaka, Y; Ueda, T, 1992
)
0.28
" The dosage schedule was single-dose intravenous administration (single treatment), followed by one or two courses of 5-day intravenous administration (5-day treatment) at 3-week intervals."( [Phase I study of CI-898. CI-898 Study Group].
Ariyoshi, H; Furue, H; Hasegawa, K; Majima, H; Nakao, I; Niitani, H; Ohta, K; Taguchi, T; Tsukagoshi, S; Yasutomi, M, 1991
)
0.28
" At the late stage (within 8-11 hours of the perfusion period), the dose-response curve for guanabenz was shifted to the left and the maximum response became approximately 3-fold larger than that in the early stage."( Perfusion-time dependent enhancements of guanabenz- and KCl-induced vasoconstrictions in isolated and perfused dog pulmonary veins.
Chiba, S; Haniuda, M, 1990
)
0.28
"To determine the maximal tolerable dosage of trimetrexate for treatment of pneumocystis pneumonia, 25 patients were treated each day with 45 mg/m2 of trimetrexate and 80 mg/m2 of leucovorin; 10 received 60 mg/m2 and 80 mg/m2; 12 received 60 mg/m2 and 160 mg/m2; and 6 received 90 mg/m2 and 160 mg/m2, respectively."( Trimetrexate-leucovorin dosage evaluation study for treatment of Pneumocystis carinii pneumonia.
Akil, B; Allegra, CJ; Feinberg, J; Hughlett, C; Lane, HC; Ogata-Arakaki, D; Sattler, FR; Shelhamer, J; Tuazon, CU; Verdegem, TD, 1990
)
0.28
" Pelanserin bioavailability after oral dosing was about 30%, this could be due to a poor absorption from the gastrointestinal tract or to an important hepatic biotransformation by first pass effect."( [Pharmacokinetics and antihypertensive effect of pelanserin in dogs ].
Castañeda Hernández, G; Flores Murrieta, FJ; Hong, E,
)
0.13
" A dosage of 12 mg/day did not improve subjective symptoms more than did the 9 mg/day dose."( [Clinical study of bunazosin hydrochloride, an alpha 1-adrenergic blocker, in benign prostatic obstruction and neurogenic bladder dysfunction].
Kondo, A; Mitsuya, H; Otani, T; Takita, T, 1987
)
0.27
" Consequently, the stability of the chemotherapeutic agents can influence the dosing accuracy and ultimately the achievement of the desired therapeutic goal."( Stability of trimetrexate, a new non-classical antifolate, in infusion solutions.
Ensminger, WD; Shukla, UA; Stetson, PL, 1989
)
0.28
" At the dosage and schedule of trimetrexate used, no responses occurred in this population of patients with non-small-cell lung cancer."( Phase II trial of trimetrexate in patients with stage III and IV non-small-cell lung cancer.
Burke, MT; D'Acquisto, RW; Fanucchi, MP; Gralla, RJ; Heelan, RT; Kris, MG; Marks, LD, 1989
)
0.28
" The results indicated that the dosage of CRL and Lid generally used in anti-arrhythmic therapy basically exerted no harm to myocytes."( [Cytotoxic effects of changrolin, lidocaine and amiodarone on ultrastructure of cultured rat beating cardiac myocytes].
Chen, HZ; Chen, WZ; Gong, ZX; Guo, Q; Jin, PY; Pen, BZ; Shen, JY; Yang, XY; Yang, YZ, 1989
)
0.28
" The dosage chosen for the Phase 2 study, based only on the hematological dose limiting toxicity, was 10."( Trimetrexate and cyclophosphamide for metastatic inoperable nonsmall cell lung cancer.
Grove, W; Holsti, LR; Maasilta, P; Mattson, K; Tammilehto, L, 1988
)
0.27
" Courses were repeated at 3 week intervals with the trimetrexate dosage escalated according to patient tolerance."( Trimetrexate combined with cisplatin or etoposide in the treatment of non-small cell lung cancer: a pilot study.
Maroun, JA; Natale, RB; Robert, F, 1988
)
0.27
" An intraluminal injection of serotonin (5-HT) produced a marked vasoconstriction and the dose-response curve was bell-shaped."( Pharmacological analysis of 5-HT-induced vasoconstriction in isolated, perfused dog skeletal muscle arteries.
Chiba, S; Sinanović, O, 1987
)
0.27
" Two additional studies were done in rats dosed with 400 mg/kg, and with 90, 200, or 400 mg/kg, respectively."( Teratogenicity of the antiallergic Sm 857 SE in rats versus rabbits.
Kast, A; Kobayashi, S; Nishimura, M; Tsunenari, Y, 1988
)
0.27
" The increases in the requirement of 5-methyltetrahydrofolate (5-methyl-THF) by the resistant sublines were more pronounced than PGA requirement, moving the dose-response curve nearly 3 log orders in magnitude to the right."( Folate requirements of methotrexate-resistant human acute lymphoblastic leukemia cell lines.
Holland, JF; Kano, Y; Ohnuma, T, 1986
)
0.27
" Dosage adjustment may have to be considered for patients who have renal dysfunction."( Clinical pharmacology of trimetrexate.
Covington, WP; Ho, DH; Krakoff, IH; Legha, SS; Newman, RA, 1987
)
0.27
" TMTX plasma levels were measured by HPLC every 3 days prior to daily dosing in patients receiving 4 mg/m2 to determine whether drug accumulation occurred during this prolonged administration schedule."( A phase I study of trimetrexate, an analog of methotrexate, administered monthly in the form of nine consecutive daily bolus injections.
Eisenhauer, E; Jolivet, J; Landry, L; McCormack, JJ; Pinard, MF; Tong, WP, 1987
)
0.27
" While TMQ appeared to be more immunosuppressive than MTX following in vitro addition of the drugs, the converse appeared to be true when dosing was performed in vivo."( Comparative effects on the immune system of methotrexate and trimetrexate.
Ackermann, MF; Germolec, DR; Lamm, KR; Luster, MI; Rosenthal, GJ, 1987
)
0.27
" These results show that the dose-response curve for the inhibitory effect of prazosin on Ca2+ overload is complex, and that adding prazosin coincident with the reperfusion of isolated ischaemic hearts does not attenuate Ca2+ gain."( The protective effect of prazosin on the ischaemic and reperfused myocardium.
Gordon, M; Nayler, WG; Stephens, DJ; Sturrock, WJ, 1985
)
0.27
"The dose-response for the new cardiotonic agent RO13-6438 was studied in 6 patients with grade III or IV congestive heart failure."( RO 13-6438 in congestive heart failure: dose-response relationship after 3 single doses.
Elkik, F; Grosgogeat, Y; Komajda, M; Lechat, P, 1987
)
0.27
" Plasma samples were obtained at specified times after the initial dose, after 4 days of multiple dosing and after the last dose of tiacrilast."( Pharmacokinetics of single and multiple ascending doses of the antiallergic agent tiacrilast in man.
Dunton, A; Keigher, N; Massarella, JW; Pao, J; Silvestri, TM, 1987
)
0.27
" The dose-response curves for synaptosomal 22Na uptake and for the inotropic effect on guinea pig left atria are parallel for sulmazole and the quinazolone drug, with first an increase and then a decrease in activity."( Effect of some new cardiotonic agents on synaptosomal sodium uptake.
Decker, N; Grima, M; Schwartz, J, 1986
)
0.27
"A linear dose-response curve was produced by the addition of ouabain (10(-8)-10(-6) M) to the media bathing segments of porcine right coronary arteries."( Insurmountable antagonism of ouabain-induced coronary constriction by prazosin.
Fairfax, CA; Tanz, RD, 1985
)
0.27
" Dose-response studies revealed that 5 microM-carbachol significantly increased (16%) the accumulation of InsP3 whereas a significant increase in accumulation of InsP2 and InsP was observed only at agonist concentrations greater than 10 microM."( Carbachol causes rapid phosphodiesteratic cleavage of phosphatidylinositol 4,5-bisphosphate and accumulation of inositol phosphates in rabbit iris smooth muscle; prazosin inhibits noradrenaline- and ionophore A23187-stimulated accumulation of inositol pho
Abdel-Latif, AA; Akhtar, RA, 1984
)
0.27
" Only a few side-effects were reported and these occurred during the first 4 weeks whilst prazosin dosage was being adjusted."( Combined antihypertensive therapy: vasodilatation using prazosin in combination with beta-adrenoceptor blockers and diuretics.
Urban Waern, A, 1980
)
0.26
" Prazosin (PRZ), a selective alpha 1-receptor blocker, inhibited preferentially the positive phase of the inotropic response and displaced the dose-response curve of PE to the right in nanomolar concentrations, indicating a competitive mechanism of inhibition."( Competitive blockade of alpha-adrenergic receptors in rat heart by prazosin.
Osnes, JB; Oye, I; Skomedal, T, 1980
)
0.26
" Furthermore, at the end of the 52-day chronic dosing period tiodazosin caused appreciably less alpha-adrenergic receptor antagonist activity than prazosin as assessed by the norepinephrine dose-pressor response profiles."( Effects of tiodazosin, praxosin, trimazosin and phentolamine on blood pressure, heart rate and on pre- and postsynaptic alpha-adrenergic receptors in the rat.
Buyniski, JP; Campbell, JA; Pircio, AW; Schurig, JE, 1980
)
0.26
" The range of dosage varied widely and the side effects, although frequent, were not serious."( Prazosin in general practice.
Musgrove, JP, 1981
)
0.26
" In the isolated rabbit aorta, E-643 blocked noradrenaline-induced contraction of the aorta with a parallel shift of the dose-response curve to the right."( alpha-Adrenoceptor blocking properties of a new antihypertensive agent, 2-[4-(n-butyryl)-homopiperazine-1-yl]-4-amino-6,7-dimethoxyquinazoline (E-643).
Daiku, Y; Igarashi, T; Shoji, T, 1980
)
0.26
" (2) The dose-response pattern exhibits a plateau phase, beyond which higher doses cause little further effect."( Clinical, hemodynamic, and neuroendocrine effects of chronic prazosin therapy for congestive heart failure.
Braunwald, E; Colucci, WS; Williams, GH, 1981
)
0.26
" Clonidine followed by prazosin was added to their regimen on an outpatient basis to establish the dose-response for BP and catecholamines."( Clonidine and prazosin effects in hypernoradrenergic vasodilator-treated and beta-blocker-treated patients.
Mitchell, HC; Pettinger, WA, 1981
)
0.26
" The order of affinity (pA2) for presynaptic alpha-receptors, as assessed from parallel shift of the dose-response curve to clonidine, was: phentolamine greater than yohimbine greater than tolazoline greater than E-643 greater than or equal to prazosin."( Comparison of pre- and postsynaptic alpha-adrenoceptor blocking effects of E-643 in the isolated vas deferens of the rat.
Shoji, T, 1981
)
0.26
" Dose-response curves were constructed following increasing concentrations of prazosin."( A pharmacological analysis of the alpha-adrenoceptor antagonism by prazosin in arteries and veins.
Schulz, JC; Westfall, DP, 1982
)
0.26
" The pharmacodynamic response was a dose-related fall in the systemic arterial pressure, both supine and standing; dose-response effects were most evident in the upright posture."( The pharmacokinetic, pharmacodynamic and haemodynamic effects of acute and chronic alpha-adrenoceptor blockade in chronic heart failure.
Silke, B; Taylor, SH, 1981
)
0.26
" Lacking an intravenous dosage form for use in human subjects, our study concentrated on the determination of the bioavailability and disposition parameters of tiodazosin in dogs, with a comparison to those parameters for prazosin, obtained from previous work in our laboratory."( The bioavailability and disposition of tiodazosin levulinate in beagle dogs with a comparison to prazosin hydrochloride.
Baughman, RA; Benet, LZ; Mico, BA,
)
0.13
"alpha-Adrenoceptor antagonists have been compared for their effects on dose-response curves of fast and slow components of contraction of the rat aorta to noradrenaline (NA)."( Non-competitive antagonism of the alpha-adrenoceptor-mediated fast component of contraction of rat aorta, by doxazosin and prazosin.
Downing, OA; Wilson, KA; Wilson, VG, 1983
)
0.27
" A clear dose-response effect of the drug on both variables only became apparent during standing, when there was a significant correlation between dose, the postural fall in systolic and diastolic blood pressure, and the increase in heart rate."( Pharmacokinetic and pharmacodynamic studies with prazosin in chronic heart failure.
Lakhani, ZM; Silke, B; Taylor, SH,
)
0.13
" During chronic oral dosing (3--21 days), tolerance developed and blood pressure returned to base-line pretreatment levels."( Changes in alpha-adrenoceptors during long-term treatment of rabbits with prazosin.
Hamilton, CA; Reid, JL,
)
0.13
"Prior to the introduction of an intravenous dosage form for use in humans, prazosin pharmacokinetic studies emphasizing clearance, hepatic extraction, and bioavailability were carried out in dogs."( Dose-dependent bioavailability of prazosin in beagle dogs.
Baughman, RA; Benet, LZ; Mico, BA; Sorgel, F,
)
0.13
"We recorded intra-arterial ambulatory blood pressure in 13 patients with essential hypertension before and after long-term twice-daily prazosin therapy (mean dosage 13."( Prazosin alone and combined with a beta-adrenoreceptor blocker in treatment of hypertension.
Cashman, PM; Gould, BA; Hornung, RS; Kieso, HA; Raftery, EB,
)
0.13
"The effect of oral prazosin on blood pressure and antagonism of phenylephrine-induce blood pressure increase was investigated in six healthy subjects during a dosing interval after the first dose and 3 days after the first dose of the drug."( Alpha-receptor function changes after the first dose of prazosin.
Lindström, B; Seideman, P; von Bahr, C, 1982
)
0.26
" Dosages were titrated until the patient showed a sitting diastolic blood pressure less than or equal to 90 mm Hg or to a maximum dosage of 100 mg/day of hydrochlorothiazide, 320 mg of propranolol and 20 mg of prazosin."( Monotherapy in mild to moderate hypertension: comparison of hydrochlorothiazide, propranolol and prazosin.
Benowitz, N; Inouye, I; Loge, D; Massie, B; Simpson, P; Topic, N, 1984
)
0.27
" Dosage was adjusted to individual needs and a striking feature of the results was the decreasing dose requirement, a trend which was most marked after 2 years of treatment."( Prazosin ('Peripress'): a long-term study.
Melkild, A, 1984
)
0.27
" Long-term dosage requirements were predicted by the blood pressure response to a single 1-mg oral dose."( Pheochromocytoma and prazosin.
Artusio, J; Kleinert, HD; Laragh, JH; Lopez-Overjero, JA; Nicholson, JP; Pickering, TG; Resnick, LM; Vaughn, ED, 1983
)
0.27
") was administered at 30 min intervals on four experimental days: no pretreatment; after prazosin 1 mg/kg and infusion; after pharmacological 'total' autonomic effector block (TAB) and with repeated three point methoxamine dose-response lines."( Haemodynamic response to ketanserin in rabbits with Page hypertension: comparison with prazosin.
Angus, JA; Wright, CE, 1983
)
0.27
" For adequate intravenous dosing of the poorly water-soluble proquazone, advantage was taken of the high degree of protein binding of the drug."( Pharmacokinetics of the antirheumatic proquazone in healthy humans.
Hinderling, PH; Roos, A, 1984
)
0.27
"Halofuginone lactate, given once orally at a dosage rate of 1,2 mg/kg body mass on the 1st, 3rd or 5th days of fever, resulted in the recovery of only 1 out of 5 splenectomized cattle."( Chemotherapy of Theileria parva lawrencei infections in cattle with halofuginone.
De Vos, AJ; Roos, JA, 1983
)
0.27
" The metabolite pattern did not vary significantly among the 3 human subjects analyzed nor over the 5-day dosing period."( The biotransformation of fluproquazone in man and several animal species.
Bhuta, SI; Dugger, HA; Orwig, BA; Schwarz, HJ; Talbot, KC, 1981
)
0.26
" Both dosage were well tolerated during the short-term trial."( Fluproquazone in the management of strains and sprains.
Jaegemann, V; Kolb, E; Lataste, X; Pabst, J, 1981
)
0.26
" Although more investigation is needed to define prazosin kinetics in congestive heart failure and chronic renal failure, the available information about prolongation of elimination half-life, decreased protein binding and increased peak plasma concentrations suggest that prazosin dosage should be titrated cautiously in such patients."( Clinical pharmacokinetics of prazosin.
Jaillon, P,
)
0.13
" Each dosage level of proquazone and aspirin provided significant analgesia compared to placebo and was well tolerated."( An evaluation of the analgesic efficacy of proquazone and aspirin in postoperative dental pain.
Forbes, JA; Hughes, MK; White, EH; White, RW, 1980
)
0.26
" The difference between the 2 groups, however, was not statistically significant, indicating an advantage for the lower daily dosage regimen over the high daily dosage regimen."( Proquazone ('Biarison') in osteoarthritis of the knee: a double-blind, dose comparison trial.
Serry, MM, 1980
)
0.26
") there was a parallel shift to the right of the dose-response curve of R 28935 (v."( Centrally induced impairment of the hypotensive effects of R 28935 and R 29814 by prazosin in anaesthetized cats.
Timmermans, PB; Van Zwieten, PA, 1980
)
0.26
" The dosage was increased, as necessary, by 1 tablet every 2 weeks to a maximum of 4 tablets daily to provide an adequate blood pressure response."( Treatment of Essential hypertension with single daily doses of a prazosin-polythiazide combination: a multicentre study with Minizide.
Gordon, AJ; Woeltjen, AE, 1981
)
0.26
" It is concluded that the drug combination, Minizide, is effective and well tolerated as initial and long-term therapy in hypertension and that the convenient dosage regimen will lead to enhanced treatment compliance for this chronic condition."( Sustained antihypertensive response with Minizide: long-term follow-up in a multicentre study.
Gordon, AJ; Woeltjen, AE, 1981
)
0.26
" 5 It was concluded that reduced venous return to the heart, due to significant suppression of sympathetically mediated venoconstriction by small initial oral dosage of prazosin, contributes to the pathophysiology of the orthostatic hypotension and faintness, described as the 'first-dose phenomenon'."( The effect of a single oral dose of prazosin on venous reflex response, blood pressure and pulse rate in normal volunteers.
Betts, WH; Schapel, GJ, 1981
)
0.26
" Effect on blood pressure was significantly better at the dosage range of 3 to 8 mg/day than at higher doses of 9 to 20 mg/day."( Prazosin kinetics and effectiveness in renal failure.
Affrime, MB; Hobbs, D; Lowenthal, DT; Martinez, EW; Onesti, G; Twomey, TM, 1980
)
0.26
" Some compounds also proved to be effective inhibitors of stimulated acid secretion in both the rat and dog when dosed intravenously."( Reversible inhibitors of the gastric (H+/K+)-ATPase. 5. Substituted 2,4-diaminoquinazolines and thienopyrimidines.
Blurton, P; Brown, TH; Ife, RJ; Keeling, DJ; Leach, CA; Meeson, ML; Parsons, ME; Theobald, CJ, 1995
)
0.52
" A significant decrease in both systolic and diastolic BP was observed after consecutive dosing of bunazosin compared to baseline values over 24 h in the NRF and for 8 h in the IRF."( Pharmacokinetics and pharmacodynamics of the alpha 1-adrenergic antagonist bunazosin retard in hypertensives.
Gotoh, E; Ishii, M; Minamisawa, K; Minamisawa, M; Shionoiri, H; Sugimoto, K; Takasaki, I; Takizawa, T; Ueda, S, 1994
)
0.29
" Dosage was of 3 and 6 mg/day per os; after 2 weeks' treatment, if DBP in clinostatism > or = 95 mmHg, the dose was doubled."( [Dose-response study of bunazosin in the treatment of light-to-moderate arterial hypertension].
De Luca, N; Fontana, D; Lamenza, F; Marchegiano, R; Sarno, D; Tozzi, N, 1993
)
0.29
" In fact, this range of daily dosage led to a fall in pressure values, without causing clinically significant alterations of heart rate, electrocardiograph traces and laboratory parameters."( [Dose-response study of bunazosin in the treatment of light-to-moderate arterial hypertension].
De Luca, N; Fontana, D; Lamenza, F; Marchegiano, R; Sarno, D; Tozzi, N, 1993
)
0.29
"In conclusions, in mild/moderate arterial hypertension, bunazosin in monotherapy at the dosage of 3-6 mg/day, is an effective and safe treatment."( [Dose-response study of bunazosin in the treatment of light-to-moderate arterial hypertension].
De Luca, N; Fontana, D; Lamenza, F; Marchegiano, R; Sarno, D; Tozzi, N, 1993
)
0.29
" As there was a close correlation between plasma levels and antihypertensive activity of bunazosin in the present study, dosage adjustment of the alpha 1-receptor blocker in patients with impaired liver and kidney function appears to be mandatory."( Bunazosin in patients with impaired hepatic or renal function.
Halabi, A; Kirch, W; Nokhodian, A,
)
0.13
" The dose-response curves for clonidine and NA were shifted to the right by bunazosin (a selective alpha 1-adrenoceptor antagonist), but were not affected by midaglizole (a selective alpha 2-adrenoceptor antagonist)."( Characteristics of the responses of isolated and perfused canine splenic arteries to vasoactive substances and to periarterially electrical stimulation.
Chiba, S; Nakane, T; Ren, LM, 1994
)
0.29
" Changes in hepatic enzymes have been seen with both drugs, and are also seen with other anti-folates including MTX, but these changes settle with repeat dosing and with cessation of treatment."( The history of the development and clinical use of CB 3717 and ICI D1694.
Clarke, SJ; Jackman, AL; Judson, IR, 1993
)
0.29
" Patients who received Tomudex spent a substantially shorter time in hospital for dosing and had significantly lower rates of grade 3 and 4 toxicities such as leucopenia and mucositis."( 'Tomudex' (ZD1694): results of a randomised trial in advanced colorectal cancer demonstrate efficacy and reduced mucositis and leucopenia. The 'Tomudex' Colorectal Cancer Study Group.
Cunningham, D; Harper, P; Kerr, D; Olver, I; Perez-Manga, G; Rath, U; Seitz, JF; Svensson, C; Van Cutsem, E; Zalcberg, JR, 1995
)
0.29
" Prolonged dosing periods of 5 or 10 days were required for activity, and efficacy was improved with twice-daily dose administration."( AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies.
Bartlett, CA; Boritzki, TJ; Hillard, JA; Howland, EF; Johnston, AL; Kosa, M; Margosiak, SA; Morse, CA; Shetty, BV; Webber, S, 1996
)
0.29
" In addition, Tomudex has an acceptable toxicity profile and a convenient dosing schedule (single intravenous injection every 3 weeks) and thus appears to offer real potential as a novel agent for the treatment of patients with advanced CRC."( ZD1694: A novel thymidylate synthase inhibitor with substantial activity in the treatment of patients with advanced colorectal cancer. Tomudex Colorectal Study Group.
Adenis, A; Azab, M; Cunningham, D; Francois, E; Green, M; Iveson, A; Schornagel, J; Seymour, I; Van Cutsem, E; Zalcberg, JR, 1996
)
0.29
" Because current dosing guidelines for anagrelide are scarce, the dosing method of the Anagrelide Study Group that published the largest study to date on the drug's efficacy in thrombocytosis was followed."( Precipitous fall in platelet count with anagrelide: case report and critique of dosing recommendations.
Liles, D; Lindley, C; McCune, JS,
)
0.13
" Another advantage compared with alfuzosin (and prazosin) is the once-daily dosing regimen of tamsulosin."( Comparison of tamsulosin with alfuzosin in the treatment of patients with lower urinary tract symptoms suggestive of bladder outlet obstruction (symptomatic benign prostatic hyperplasia). The European Tamsulosin Study Group.
Buzelin, JM; Fonteyne, E; Khan, A; Kontturi, M; Witjes, WP, 1997
)
0.3
" One of these toxic findings was cataract, and we have found that cataract appeared in rats dosed orally with FK506 for 13 weeks and more."( Cataract development induced by repeated oral dosing with FK506 (tacrolimus) in adult rats.
Fukuhara, Y; Hisatomi, A; Ishida, H; Mitamura, T; Murato, K; Ohara, K; Takahashi, Y, 1997
)
0.3
" Elevated transaminases were frequently reported with raltitrexed but were usually reversible with continued dosing and were not associated with clinical sequelae."( Overview of the tolerability of 'Tomudex' (raltitrexed): collective clinical experience in advanced colorectal cancer.
Zalcberg, J, 1997
)
0.3
" It has a convenient dosing schedule and a potential for lower toxicity which represent important advantages over existing treatments."( 'Tomudex' (raltitrexed) development: preclinical, phase I and II studies.
Judson, IR, 1997
)
0.3
" A North American study (study 10) was originally set up to compare two raltitrexed dosage arms (3."( Mature results from three large controlled studies with raltitrexed ('Tomudex').
Cunningham, D, 1998
)
0.3
" To date, the role of varying dosing regimens in responding patients has not been well studied."( Intermittent alpha-blocker therapy in the treatment of men with lower urinary tract symptoms.
Cologna, A; Kaplan, SA; Kohn, IJ; Martins, AC; Reis, RB; Suaid, HJ; Te, AE, 1998
)
0.3
"In men with LUTS who responded to alfuzosin, changing the dosing regimen from daily to once every other day resulted in similar efficacy and safety at 3 and 6 months."( Intermittent alpha-blocker therapy in the treatment of men with lower urinary tract symptoms.
Cologna, A; Kaplan, SA; Kohn, IJ; Martins, AC; Reis, RB; Suaid, HJ; Te, AE, 1998
)
0.3
" Raltitrexed, a thymidylate synthase inhibitor, offers similar antitumoral activity together with a tolerability in comparison to standard 5-fluorouracil based chemotherapy and its simple dosage schedule also contributes to better quality of life."( [Drug clinics. How I treat. II. Therapeutic approaches to metastatic colorectal cancer].
Bours, V; Fillet, G; Jerusalem, G, 1998
)
0.3
" Raltitrexed has the added convenience of an every 3 weeks dosing schedule."( Open, randomized, multicenter trial of raltitrexed versus fluorouracil plus high-dose leucovorin in patients with advanced colorectal cancer. Tomudex Colorectal Cancer Study Group.
Cocconi, G; Cunningham, D; Francois, E; Gustavsson, B; Hietschold, SM; Kerr, D; Possinger, K; Van Cutsem, E; van Hazel, G, 1998
)
0.3
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, and dosage and administration of anagrelide are reviewed."( Anagrelide, a selective thrombocytopenic agent.
Oertel, MD, 1998
)
0.3
" Based on these results, the recommended dosage and administration for the phase II study of ZD-1694 was 3 n (3."( [Phase I study of raltitrexed (ZD-1694)].
Aiba, K; Akazawa, S; Fukuoka, M; Furue, H; Furuse, K; Horikoshi, N; Kanamaru, R; Konishi, T; Kotake, T; Kudoh, S; Kurihara, M; Niitani, H; Ota, K; Sakata, Y; Taguchi, T; Tsukagoshi, S; Wakui, A; Yoshida, S, 1998
)
0.3
" Nolatrexed plasma concentrations 1 h after dosing were 6-16 microg ml(-1), and trough 3-8 microg ml(-1), at 572 mg m(-2) day(-1)."( A phase I study of the lipophilic thymidylate synthase inhibitor Thymitaq (nolatrexed dihydrochloride) given by 10-day oral administration.
Boddy, A; Bowman, A; Byrne, B; Clendeninn, NJ; Jodrell, DI; Johnston, A; Rafi, I; Rye, R; Taylor, GA, 1999
)
0.3
" At the peak approximately 30% of the administered dose was in the deep tissue compartment, and 24 h after the dosing >20% of the administered dose remained in the body with >99% in the deep tissue compartment."( The plasma pharmacokinetics and cerebrospinal fluid penetration of the thymidylate synthase inhibitor raltitrexed (Tomudex) in a nonhuman primate model.
Adamson, PC; Balis, FM; Godwin, KS; McCully, C; Widemann, BC, 1999
)
0.3
" Oral administration of selected compounds to mice produced total plasma levels 6 h after dosing of between 3 and 49 microM."( Design and structure-activity relationship of a new class of potent VEGF receptor tyrosine kinase inhibitors.
Curwen, JO; Dukes, M; Hennequin, LF; Johnstone, C; Kendrew, J; Lambert-van der Brempt, C; Lohmann, JJ; Ogilvie, DJ; Plé, PA; Stokes, ES; Thomas, AP; Wedge, SR, 1999
)
0.3
" Chronic once-daily oral dosing of ZD4190 to young rats produced a dose-dependent increase in the femoral epiphyseal growth plate area, which may be attributed to the inhibition of VEGF signaling in vivo because vascular invasion of cartilage is a prerequisite to the process of ossification."( ZD4190: an orally active inhibitor of vascular endothelial growth factor signaling with broad-spectrum antitumor efficacy.
Curry, B; Curwen, JO; Dukes, M; Hennequin, LF; Kendrew, J; Ogilvie, DJ; Richmond, GH; Stokes, ES; Thomas, AP; Wadsworth, PF; Wedge, SR, 2000
)
0.31
"To assess the efficacy and safety of a new prolonged release formulation of the uroselective alpha(1)-blocker alfuzosin for a once-daily dosing regimen in patients with lower urinary tract symptoms (LUTS) suggestive of symptomatic benign prostatic hyperplasia (BPH)."( Efficacy and safety of a new prolonged release formulation of alfuzosin 10 mg once daily versus alfuzosin 2.5 mg thrice daily and placebo in patients with symptomatic benign prostatic hyperplasia. ALFORTI Study Group.
Jardin, A; Laval, KU; van Cangh, P; van Kerrebroeck, P, 2000
)
0.31
" Just 16 patients (3%) developed adverse events; measures undertaken were to modify the dosage or to interrupt the treatment (2 cases)."( [Prostatic benign hypertrophy: review of effectiveness, tolerance, and impact on quality of life of prolonged treatment with alfuzosin].
Ausín, I; Barajas, R; Gabriel, R; Vela Navarrete, R, 2000
)
0.31
" The stability of the DPC 961 and 963 in the dosing formulation was followed over a 24-h period using a stability indicating HPLC method."( In-use testing of extemporaneously prepared suspensions of second generation non-nucleoside reversed transcriptase inhibitors in support of phase I clinical studies.
Aubry, AF; Gray, V; Hobson, T; Rabel, S; Sebastian, D; Xie, M; Xu, JQ, 2000
)
0.31
" Body-surface area did not correlate with drug clearance; therefore, fixed daily dosing of 25 mg/d was studied and found to be tolerable, with two of 12 dose-limiting events."( Phase I study of ZD9331 on short daily intravenous bolus infusion for 5 days every 3 weeks with fixed dosing recommendations.
Averbuch, S; Bertucci, D; Douglass, E; Goh, BC; Hutchison, M; Mani, S; Ratain, MJ; Schilsky, RL; Smith, M; Smith, R; Vogelzang, NJ, 2001
)
0.31
" Faecal samples were collected on the first day of dosing and four, seven, 14 and 21 days later, and Cryptosporidium parvum oocysts were counted and faecal indices for diarrhoea were determined after a clinical examination."( Efficacy of halofuginone lactate in the prevention of cryptosporidiosis in suckling calves.
Chermette, R; Lefay, D; Naciri, M; Poirier, P, 2001
)
0.31
" Dose-response relationships for evodiamine, rutaecarpine and capsaicin were obtained."( The positive inotropic and chronotropic effects of evodiamine and rutaecarpine, indoloquinazoline alkaloids isolated from the fruits of Evodia rutaecarpa, on the guinea-pig isolated right atria: possible involvement of vanilloid receptors.
Hoshikuma, K; Kamiya, T; Kobayashi, Y; Nakano, Y; Yokoo, Y, 2001
)
0.31
" Anticipatory changes in hydroxyurea dosage or the maintenance of a constant dose did not abolish periodicity, but a change in therapy to the non-cycle-specific drug anagrelide dampened and abolished the cycling."( Hydroxyurea and periodicity in myeloproliferative disease.
Bennett, M; Grunwald, AJ, 2001
)
0.31
"Anagrelide was introduced with gradually higher dosage, while the dosage of hydroxyurea was gradually reduced."( [Anagrelide in primary thrombocythemia].
Hysing, J; Knutsen, H, 2001
)
0.31
" In contrast, dosing with 60 mg/kg of CW252053 produced a cure rate against tumor growth of 37."( In vivo antitumor efficacy of CW252053, a folate-based thymidylate synthase inhibitor.
Baek, DJ; Ha, JR; Oh, SW, 2001
)
0.31
" A once-daily formulation of alfuzosin administered through a novel prolonged-release system has been recently developed to improve the convenience of dosing and to provide optimal pharmacokinetic coverage over 24 hours."( Alfuzosin: overview of pharmacokinetics, safety, and efficacy of a clinically uroselective alpha-blocker.
Roehrborn, CG, 2001
)
0.31
" dosing and 15-16% and 16% of the administered dose within 24 and 48 h, respectively, after oral dosing."( Pharmacokinetics and tissue distribution of halofuginone (NSC 713205) in CD2F1 mice and Fischer 344 rats.
Covey, JM; Egorin, MJ; Eiseman, JL; Hamburger, DR; Parise, RA; Stecklair, KP, 2001
)
0.31
" As with other cytotoxic agents, serious and potentially life-threatening side-effects can occur; nevertheless, adherence to simple patient guidelines should minimise the incidence of serious side-effects with raltitrexed; these include the assessment of renal function before each and every treatment, dosage adjustment in the presence of renal impairment and close monitoring with prompt treatment of toxicities, particularly diarrhoea and neutropenia."( Efficacy, tolerability and management of raltitrexed (Tomudex) monotherapy in patients with advanced colorectal cancer. a review of phase II/III trials.
Clarke, S; Cunningham, D; Facchini, T; González Barón, M; James, R; Maroun, J; Maughan, TS; Schulz, J; Vincent, M; Zalcberg, J, 2002
)
0.31
" No dosage titration is required."( Alfuzosin: a review of the therapeutic use of the prolonged-release formulation given once daily in the management of benign prostatic hyperplasia.
McKeage, K; Plosker, GL, 2002
)
0.31
") formulation of alfuzosin has recently been developed in order to improve the convenience of dosing and to provide optimal pharmacokinetic coverage over a 24-h period."( Alfuzosin: a clinically uroselective alpha1-blocker.
Höfner, K; Jonas, U, 2002
)
0.31
" To accomplish this, groups of four to six dogs were dosed with various formulations of DPC 961 under fasted or fed conditions, and DPC 961 pharmacokinetics were examined."( Formulation and food effects on the oral absorption of a poorly water soluble, highly permeable antiretroviral agent.
Aungst, BJ; Bindra, DS; Nguyen, NH; Taylor, NJ, 2002
)
0.31
"Alfuzosin 10 mg once-daily provides a suitable pharmacokinetic profile for a once-daily administration, equivalent bioavailability between the 2 dosage regimens and a good safety profile justify the use of alfuzosin 10 mg in patients with BPH."( Alfuzosin, an alpha1-adrenoceptor antagonist for the treatment of benign prostatic hyperplasia: once daily versus 3 times daily dosing in healthy subjects.
Ahtoy, P; Chrétien, P; Delfolie, A; Dupain, T; Rauch, C; Rouchouse, A, 2002
)
0.31
" dosing might be a suitable therapeutic regimen."( ZD1839 (Iressa): an orally active inhibitor of epidermal growth factor signaling with potential for cancer therapy.
Ashton, SE; Barker, AJ; Curry, BJ; Gibson, KH; Guy, SP; Wakeling, AE; Woodburn, JR, 2002
)
0.31
" In conclusion, once-daily alfuzosin, 10 mg, could be safely administered to patients with impaired renal function, and dosage adjustment does not seem necessary."( Pharmacokinetics and safety of a single oral dose of once-daily alfuzosin, 10 mg, in male subjects with mild to severe renal impairment.
Blum, RA; Marbury, TC; Pinquier, JL; Rauch, C, 2002
)
0.31
" Intermittent and continuous dosing schedules with ZD1839 were well tolerated by these patients for up to 6 months or more."( Phase I studies of ZD1839 in patients with common solid tumors.
Lorusso, PM, 2003
)
0.32
" Anagrelide offers the advantage of oral dosing and long-term effectiveness at managing platelet counts."( Indications for lowering platelet numbers in essential thrombocythemia.
Barbui, T, 2003
)
0.32
" Mean terminal half-life following multiple dosing was 50."( Phase I pharmacokinetic trial of the selective oral epidermal growth factor receptor tyrosine kinase inhibitor gefitinib ('Iressa', ZD1839) in Japanese patients with solid malignant tumors.
Dong, RP; Fukuoka, M; Hirose, M; Kudoh, S; Nakagawa, K; Nakatani, I; Negoro, S; Swaisland, H; Takeda, K; Tamura, T; Yamamoto, N, 2003
)
0.32
" Alfuzosin prostate and blood concentrations at 12 hours post dosing on day 4 were significantly correlated (r=0."( Prostatic tissual distribution of alfuzosin in patients with benign prostatic hyperplasia following repeated oral administration.
Bressolle, F; Costa, P; Delmas, V; Mottet, N; Robert, M, 2003
)
0.32
" This includes defining dosing schedules and appropriate combination partners, identifying predictive markers of response, developing techniques to accurately assess antitumor activity, and determining whether it is possible to preselect patients before therapy."( Challenges and opportunities for Erlotinib (Tarceva): what does the future hold?
Hortobagyi, GN; Sauter, G, 2003
)
0.32
"0 mL volume) human prostate (PC-3), lung (Calu-6) and breast (MDA-MB-231) tumor xenografts, were dosed with ZD4190 (p."( Dynamic contrast-enhanced MRI of vascular changes induced by the VEGF-signalling inhibitor ZD4190 in human tumour xenografts.
Checkley, D; Curry, B; Dukes, M; Kendrew, J; Middleton, B; Tessier, JJ; Waterton, JC; Wedge, SR, 2003
)
0.32
" No dosage titration is needed for ER alfuzosin, and its onset of peak action is within days of the start of treatment."( Alfuzosin hydrochloride for the treatment of benign prostatic hyperplasia.
Lee, M, 2003
)
0.32
" The base model employed for modeling dose-response effect is the four parameter Hill equation [1]."( A new nonlinear mixture response surface paradigm for the study of synergism: a three drug example.
Brun, Y; Greco, WR; Slocum, HK; White, DB; Wrzosek, C, 2003
)
0.32
" Initially, patients were dosed at 130 mg/m2 (Regimen 1); however, following a protocol amendment, the starting dose was reduced to 65 mg/m2 (Regimen 2)."( Phase II multicentre trial of ZD9331 monotherapy as first-line treatment for gastric cancer.
Petruzelka, L, 2003
)
0.32
" However, since the tumor in this animal model was EGFR positive and because tumor growth tended to be suppressed in mice with higher immune activity, it seems likely that additional studies of this therapy will contribute to identifying the optimum drugs to be combined with gefitinib and the optimum method of dosing that will lead to satisfactory efficacy and safety of gefitinib combined with immunotherapy."( [Significance of gefitinib combined with immunotherapy in tumor-bearing mice].
Maruyama, S; Sukegawa, Y; Yagita, A, 2003
)
0.32
" Ongoing investigation will help to determine optimal dosing and dose frequency of erlotinib in various cancers in the clinical setting."( Erlotinib: preclinical investigations.
Hidalgo, M, 2003
)
0.32
" Dosing erlotinib at the maximum tolerated dose, which is associated with more frequent and more severe rash, may improve response rates and survival durations."( Can rash associated with HER1/EGFR inhibition be used as a marker of treatment outcome?
Pérez-Soler, R, 2003
)
0.32
" Dose-response studies for this compound against HT-29 human colon adeno carcinoma xenografts at 100, 200 and 400mg/kg doses were performed."( Synthesis and biological evaluation of [4-(2-phenylethenesulfonylmethyl)phenyl]-quinazolin-4-yl-amines as orally active anti-cancer agents.
Adi Seshu, KV; Ajaykumar, R; Babu, PA; Chandra Sekhar, V; Kumar, TS; Madan, S; Rajagopal, S; Ravi Krishna, V; Sharma, VM; Sreenu, J; Vamsee Krishna, C; Venkateswarlu, A; Vishnu, B, 2004
)
0.32
" Gefitinib was investigated clinically by a single dose ascending study and 3-day multiple dosing study in male volunteers in the UK initially."( [Development of novel molecular targeted drug, "Iressa", for the treatment of malignant diseases--its basic and clinical studies].
Mikami, O; Tsukagoshi, S, 2003
)
0.32
" Patient characteristics, lack of patient selection, dosing schedule, and trial design may all have played roles."( HER1/EGFR targeting: refining the strategy.
Pérez-Soler, R, 2004
)
0.32
" In contrast, continuous treatment of mice bearing established GEO xenografts with ZD6474 resulted in efficient tumor growth inhibition for the entire duration of dosing (up to 150 days)."( Antitumor activity of ZD6474, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in human cancer cells with acquired resistance to antiepidermal growth factor receptor therapy.
Bianco, AR; Bianco, R; Caputo, R; Ciardiello, F; Damiano, V; De Placido, S; De Vita, F; Melisi, D; Tortora, G; Troiani, T, 2004
)
0.32
" The use of influential covariates to guide anticancer dosage selection may result in less variability in drug exposure and potentially a better clinical outcome."( Population pharmacokinetics of raltitrexed in patients with advanced solid tumours.
Blair, EY; Clarke, SJ; McLachlan, AJ; Rivory, LP, 2004
)
0.32
" Gefitinib, which can be given at doses below the maximum tolerated dose, is associated with slightly lower rates of adverse events than erlotinib, which is dosed at the maximum tolerated dose."( Rationale and clinical validation of epidermal growth factor receptor as a target in the treatment of head and neck cancer.
Caponigro, F, 2004
)
0.32
" Gefitinib is administered orally at a dosage of 250 mg/day."( Gefitinib: a new antineoplastic for advanced non-small-cell lung cancer.
Cersosimo, RJ, 2004
)
0.32
"Nineteen patients were treated with 71 cycles of ZD9331 and docetaxel (ZD9331/docetaxel) at dose levels that encompassed dosing iterations of ZD9331 ranging from 65 to 260 mg/m(2) and docetaxel doses in the range of 50 to 75 mg/m(2)."( A phase I and pharmacokinetic study of the nonpolyglutamatable thymidylate synthase inhibitor ZD9331 plus docetaxel in patients with advanced solid malignancies.
Garrison, M; Jones, CB; McCreery, H; Patnaik, A; Rowinsky, EK; Schwartz, GH; Skinner, M; Takimoto, C; Tolcher, AW, 2004
)
0.32
" Gefitinib represents a significant advance in the treatment of this population; a once-daily, oral dosage of 250 mg/day was well tolerated, produced objective tumour responses and disease stabilisation, and improved disease-related symptoms and quality of life."( Gefitinib: a review of its use in the management of advanced non-small-cell lung cancer.
Easthope, SE; Frampton, JE, 2004
)
0.32
" Gefitinib was found to be generally well tolerated at the approved dosage of 250 mg/day; the most commonly reported adverse drug reactions (ADRs) were mild to moderate skin rash and diarrhoea, which were manageable and non-cumulative."( Overview of the tolerability of gefitinib (IRESSA) monotherapy : clinical experience in non-small-cell lung cancer.
Faulkner, K; Forsythe, B, 2004
)
0.32
"This article reviews data on the pharmacodynamics, pharmacokinetics, efficacy, tolerability, drug-interaction potential, and dosing of alfuzosin ER."( Extended-release alfuzosin hydrochloride: a new alpha-adrenergic receptor antagonist for symptomatic benign prostatic hyperplasia.
Guay, DR, 2004
)
0.32
" Plasma samples obtained before dosing to 240 hours after dosing were analyzed for gefitinib using reverse-phase high-performance liquid chromatography with tandem mass-spectrometric detection."( Relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers.
Bailey, C; Cantarini, MV; Marshall, AL; McFarquhar, T; Smith, RP, 2004
)
0.32
" No dosage adjustment is required for patient age, body weight, gender, ethnicity or moderate to severe hepatic impairment due to liver metastases."( Gefitinib: current status in the treatment of non-small cell lung cancer.
Alfaro, V; Tanović, A, 2004
)
0.32
" The anti-EGFR mAbs and TKIs have partially overlapping toxicity profiles, but distinct routes of administration, serum half-lives and therefore dosing schedules."( Epidermal growth factor receptor inhibition strategies in oncology.
Harari, PM, 2004
)
0.32
" After 25 minutes of perfusion, peritoneal fluid, portal and systemic blood were harvested and prepared for dosage of Raltitrexed."( A study of the effect of temperature on the pharmacokinetic profile of raltitrexed administered by intraperitoneal route in the rat.
Bendavid, Y; Dubé, P; Leblond, FA, 2005
)
0.33
" This provokes a problem for correct dosage finding in formulations for the treatment of Alzheimer's disease and in the therapy of alcoholism and nicotine dependence."( Biotransformation of desoxypeganine by microsomal enzymes of the rabbit liver.
Illgner, S; Matusch, R, 2005
)
0.33
" PK demonstrated steady state within the first 2 weeks of dosing and dose dependent exposure."( A phase I study of oral ZD 1839 given daily in patients with solid tumors: IND.122, a study of the Investigational New Drug Program of the National Cancer Institute of Canada Clinical Trials Group.
Batist, G; Douglas, L; Friedmann, J; Goss, G; Hanna, P; Hirte, H; Lorimer, IA; Mathews, S; Miller, WH; Parolin, DA; Seymour, LK; Stafford, S; Stewart, D; Walsh, W, 2005
)
0.33
" Eleven patients required dosing modification (hold or reduction), while 3 patients discontinued therapy because of toxicity."( A phase II trial of ZD1839 (Iressa) 750 mg per day, an oral epidermal growth factor receptor-tyrosine kinase inhibitor, in patients with metastatic colorectal cancer.
Batist, G; Douglas, L; Glenwood, G; Goel, R; Hirte, HW; Jean, M; Lorimer, IA; Mackenzie, MJ; Major, PP; Matthews, S; Miller, WH; Panasci, L; Seymour, L, 2005
)
0.33
" Dosage was titrated to achieve a platelet count < 600 x 10(9) L(-1) and ideally between 130 and 450 x 10(9) L(-1)."( Anagrelide: analysis of long-term efficacy, safety and leukemogenic potential in myeloproliferative disorders.
Fiddler, G; Fruchtman, SM; Gilbert, HS; Lyne, A; Petitt, RM, 2005
)
0.33
" We observed preliminary evidence of antileukemia activity using this weekly dosing schedule and these observations support further evaluation of raltitrexed in this population."( Phase I trial and pharmacokinetic study of raltitrexed in children with recurrent or refractory leukemia: a pediatric oncology group study.
Berg, SL; Bernstein, M; Blaney, SM; Horton, TM; Kamen, B; Kuhn, J; Langevin, AM; Weitman, S, 2005
)
0.33
" Furthermore, we hypothesized that intermittent dosing would allow for dose escalation and greater inhibition of EGFR-dependent antiapoptotic pathways."( Pulsatile administration of the epidermal growth factor receptor inhibitor gefitinib is significantly more effective than continuous dosing for sensitizing tumors to paclitaxel.
Kris, MG; Lobo, J; Rosen, N; Scher, HI; She, Y; Sirotnak, FM; Solit, DB, 2005
)
0.33
"To test these assertions, we compared combinations of paclitaxel and gefitinib using either intermittent or continuous dosing schedules in mice."( Pulsatile administration of the epidermal growth factor receptor inhibitor gefitinib is significantly more effective than continuous dosing for sensitizing tumors to paclitaxel.
Kris, MG; Lobo, J; Rosen, N; Scher, HI; She, Y; Sirotnak, FM; Solit, DB, 2005
)
0.33
" Following intravenous dosing (5 mg kg(-1), gefitinib plasma half-life was 3-6h in rats and dogs, although studies using a more sensitive HPLC-MS assay produced longer estimates of half-life (7-14h)."( Pharmacokinetics of gefitinib, an epidermal growth factor receptor tyrosine kinase inhibitor, in rat and dog.
Bardsley, J; Hutchison, M; McKillop, D; Parry, AC; Partridge, EA; Rhead, SA; Swaisland, HC; Woodman, HM, 2004
)
0.32
" Gefitinib represents a significant advance in the treatment of this population; a once-daily oral dosage of 250 mg/day was well tolerated, produced objective tumour responses and disease stabilization, and improved disease-related symptoms and quality of life."( Spotlight on gefitinib in non-small-cell lung cancer.
Easthope, SE; Frampton, JE, 2005
)
0.33
"Once-daily oral dosing of ZD6474 at 300 mg/day is generally well tolerated in patients with advanced solid tumors, and this dose is being investigated in phase II trials."( Clinical evaluation of ZD6474, an orally active inhibitor of VEGF and EGF receptor signaling, in patients with solid, malignant tumors.
Barge, A; Basser, R; de Boer, R; Eckhardt, SG; Green, M; Holden, SN; Hurwitz, HI; Rischin, D; Rosenthal, MA; Wheeler, C, 2005
)
0.33
" The major challenges on the clinical development of targeted therapy include the proper selection of patients, the identification of the optimal dosage and schedule of administration, the combinations with conventional treatments and the more appropriate therapeutic strategy."( Therapy of breast cancer with molecular targeting agents.
Gasparini, G; Longo, R; Morabito, A; Torino, F, 2005
)
0.33
" Consistent with inhibition of angiogenesis, once-daily oral dosing of ZD6474 produced significant broad-spectrum antitumour activity in a panel of histologically diverse human tumour xenografts."( ZD6474--a novel inhibitor of VEGFR and EGFR tyrosine kinase activity.
Ryan, AJ; Wedge, SR, 2005
)
0.33
" The assay was applied to a pharmacokinetic study in mice to determine dosing schedules that would approximate therapeutic ZD6474 levels determined in humans."( Rapid and sensitive LC/MS/MS analysis of the novel tyrosine kinase inhibitor ZD6474 in mouse plasma and tissues.
Bradshaw, EL; Gustafson, DL; Long, ME; Zirrolli, JA, 2005
)
0.33
"This study (EGF10004) assessed the safety/tolerability, pharmacokinetics, and clinical activity of daily oral dosing with lapatinib (GW572016) in patients with ErbB1-expressing and/or ErbB2-overexpressing advanced-stage refractory solid tumors."( Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas.
Blackwell, KL; Burris, HA; Dees, EC; Dowlati, A; Ellis, MJ; Harris, JL; Hurwitz, HI; Jones, SF; Koch, KM; Mangum, S; Marcom, PK; O'Neil, B; Overmoyer, B; Smith, DA; Spector, NL; Stead, A, 2005
)
0.33
" Because of the potentially serious consequences of this interaction, close monitoring of the International Normalized Ratio and warfarin dosage adjustment are recommended for patients receiving warfarin together with gefitinib."( Drug interaction between gefitinib and warfarin.
Abe, T; Hagiri, S; Ishii, K; Katagiri, M; Kato, E; Kobayashi, H; Kuboto, M; Masuda, N; Mitsufuji, H; Onoda, S; Ryuge, S; Takada, N; Tanaka, N; Wada, M; Yamamoto, M; Yanaihara, T; Yanase, N; Yokoba, M, 2005
)
0.33
" The possibility that this skin toxicity correlates with anti-tumour activity offers the potential to titrate dosing on a case-by-case basis."( The management of skin reactions in cancer patients receiving epidermal growth factor receptor targeted therapies.
Chosidow, O; Dirschka, T; Elsner, J; Layton, A; Mancini, L; Maughan, T; Morere, JF; Santoro, A; Segaert, S; Sobrero, A; Tabernero, J; Van Cutsem, E, 2005
)
0.33
" Cell growth was analyzed by the MTS assay, with differences between dose-response curves analyzed nonparametrically."( Differential effects of gefitinib and cetuximab on non-small-cell lung cancers bearing epidermal growth factor receptor mutations.
Cantley, LC; Engelman, JA; Halmos, B; Hanna, NH; Jänne, PA; Johnson, BE; Kobayashi, S; Lindeman, N; Mukohara, T; Pearlberg, J; Tenen, DG; Tsuchihashi, Z; Yeap, BY, 2005
)
0.33
" Exposure to gefitinib is increased by coadministration with CYP3A4 inhibitors, but since gefitinib is known to have a good tolerability profile, a dosage reduction is not recommended."( Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol.
Laight, A; Leadbetter, J; McKillop, D; Ranson, M; Smith, RP; Swaisland, HC; Wild, MJ, 2005
)
0.33
"A novel slow release formulation of alfuzosin should improve compliance by reducing dosing to one 10 mg tablet per day."( Early symptom improvement of benign prostatic hyperplasia (BPH) treated with once daily alfuzosin.
Casey, R; Elhilali, M; Kuzmarov, I; Nickel, JC; Saad, F; Valiquette, L, 2005
)
0.33
" Highly potent inhibition, high selectivity and physical properties suitable for oral dosing were achieved within this series: 23d and 42 were identified as sub-0."( New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors.
Barlaam, B; Costello, G; Fennell, M; Germain, H; Green, T; Hennequin, L; Morgentin, R; Olivier, A; Plé, P; Vautier, M, 2005
)
0.57
" Further investigations of dosing regimens using EGFR tyrosine kinase inhibitors and radioimmunotherapy in the treatment of EGFR expressing tumors are warranted."( Enhanced efficacy of radioimmunotherapy with 90Y-CHX-A''-DTPA-hu3S193 by inhibition of epidermal growth factor receptor (EGFR) signaling with EGFR tyrosine kinase inhibitor AG1478.
Brechbiel, MW; Burgess, AW; Hall, C; Johns, TG; Kelly, MP; Lee, FT; Mountain, AJ; Nice, EC; Rigopoulos, A; Scott, AM; Smyth, FE, 2005
)
0.33
" Thus, the microemulsion system composed of castor oil, PEG 400, Tween 80, and water could be a stable dosage form for rutaecarpine."( Physicochemical characterization of rutaecarpine-loaded microemulsion system.
Choi, HG; Jahng, Y; Kim, JK; Kim, JO; Park, BJ; Park, YJ; Rhee, JD; Yong, CS; Yoo, BK, 2005
)
0.33
") dosing in rats, six of eight drugs produced dose- and time-related antinociception on both the tail flick and hot plate tests over a nearly eight-fold range of potencies."( Antinociceptive, brain-penetrating derivatives related to improgan, a non-opioid analgesic.
Hough, LB; Lu, Q; Montero, MJ; Nalwalk, JW; Shan, Z; Svokos, K; Wentland, MP, 2005
)
0.33
" Gefitinib undergoes rapid plasma clearance and has an extensive volume of distribution, resulting in a pharmacokinetic profile supportive of a once-daily dosage regimen."( Single-dose clinical pharmacokinetic studies of gefitinib.
Duvauchelle, T; Kerr, DJ; Laight, A; Ranson, M; Smith, RP; Swaisland, HC; Wilder-Smith, CH, 2005
)
0.33
" A dose-response relationship may exist for this agent in SCCHN and grade of cutaneous toxicity attributable to gefitinib is a clinical predictor of better outcome."( Phase II trial of gefitinib 250 mg daily in patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck.
Brockstein, BE; Cohen, EE; Dekker, A; Huo, D; Kane, MA; List, MA; Mauer, AM; Mehrotra, B; Pierce, C; Vokes, EE, 2005
)
0.33
"Parallel dose-response effects were found in both CD41(+) number and TPO-specific pTyr activity."( A preliminary investigation into the action of anagrelide: thrombopoietin-c-Mpl receptor interactions.
Dessypris, EN; Kanamori, D; McCarty, JM; Melone, PD; Simanis, JP; Warshamana-Greene, GS, 2006
)
0.33
"7%); previous radiotherapy dosage ranged between 30 and 55 Gy (median, 50."( Preoperative hyperfractionated chemoradiation for locally recurrent rectal cancer in patients previously irradiated to the pelvis: A multicentric phase II study.
Bolzicco, G; Coco, C; Dalla Palma, M; De Paoli, A; Di Russo, A; Doglietto, GB; Gambacorta, MA; Mohiuddin, M; Morganti, AG; Rossi, C; Valentini, V; Valvo, F, 2006
)
0.33
" Cumulative dose-response study with acetylcholine and histamine indicated for its non-specific direct effect on smooth muscles."( Synthesis and bronchodilator activity of new quinazolin derivative.
Bhagat, A; Dhar, KL; Gupta, BD; Gupta, OP; Qazi, GN; Satti, NK; Singh, GD; Suri, KA; Suri, OP; Youssouf, MS; Zabeer, A, 2006
)
0.33
" In study 1, CV alpha1-adrenoceptor antagonism was assessed by measuring the inhibition of phenylephrine (PE)-induced increases in diastolic blood pressure (DBP) and total peripheral resistance (TPR) before and after dosing with placebo, tamsulosin OCAS, and alfuzosin XL in 18 young subjects."( Comparison of the cardiovascular effects of tamsulosin oral controlled absorption system (OCAS) and alfuzosin prolonged release (XL).
Chapple, CR; Michel, MC, 2006
)
0.33
"In study 1, tamsulosin OCAS induced statistically significantly less inhibition of PE-induced increases in DBP at 2 h after dosing and in TPR at 2 and 4 h after dosing than alfuzosin XL."( Comparison of the cardiovascular effects of tamsulosin oral controlled absorption system (OCAS) and alfuzosin prolonged release (XL).
Chapple, CR; Michel, MC, 2006
)
0.33
"Gefitinib and sirolimus were administered on a continuous daily dosing schedule at dose levels that were escalated in successive cohorts of malignant glioma patients at any recurrence who were stratified based on concurrent use of CYP3A-inducing anticonvulsants [enzyme-inducing antiepileptic drugs, (EIAED)]."( Phase 1 trial of gefitinib plus sirolimus in adults with recurrent malignant glioma.
Bigner, DD; Desjardins, A; Dowell, JM; Friedman, AH; Friedman, HS; Gururangan, S; Herndon, JE; Lyons, P; McLendon, RE; Ochs, JS; Provenzale, JM; Quinn, JA; Reardon, DA; Rich, JN; Sampson, JH; Sathornsumetee, S; Smith, RP; Swaisland, AJ; Tourt-Uhlig, S; Vredenburgh, JJ, 2006
)
0.33
"We show that gefitinib plus sirolimus can be safely coadministered on a continuous, daily dosing schedule, and established the recommended dose level of these agents in combination for future phase 2 clinical trials."( Phase 1 trial of gefitinib plus sirolimus in adults with recurrent malignant glioma.
Bigner, DD; Desjardins, A; Dowell, JM; Friedman, AH; Friedman, HS; Gururangan, S; Herndon, JE; Lyons, P; McLendon, RE; Ochs, JS; Provenzale, JM; Quinn, JA; Reardon, DA; Rich, JN; Sampson, JH; Sathornsumetee, S; Smith, RP; Swaisland, AJ; Tourt-Uhlig, S; Vredenburgh, JJ, 2006
)
0.33
" Comparative studies to assess the therapeutic indices of PQD-A4, PQD-BE, and PQD were conducted in Plasmodium berghei-infected rats following daily intragastric dosing for three consecutive days."( New potential antimalarial agents: therapeutic-index evaluation of pyrroloquinazolinediamine and its prodrugs in a rat model of severe malaria.
Li, Q; Lin, AJ; Skillman, DS; Smith, K; Xie, LH; Zhang, J, 2006
)
0.33
" The incorporation of an empirical approach to dosing in mouse models of cancer in preclinical studies may allow for better prediction of clinical efficacy for ZD6474 alone and in combination with other therapeutic modalities based on equivalent drug exposure."( Tissue distribution and metabolism of the tyrosine kinase inhibitor ZD6474 (Zactima) in tumor-bearing nude mice following oral dosing.
Bradshaw-Pierce, EL; Gustafson, DL; Merz, AL; Zirrolli, JA, 2006
)
0.33
"Epidermal growth factor receptor (EGFR) mRNA expression and EGFR gene dosage by quantitative PCR in tumor samples obtained from patients with gefitinib-treated non-small cell lung cancer were analyzed in order to determine the association with treatment outcome, clinical, and biological features [EGFR copy number by fluorescent in situ hybridization (FISH), EGFR tyrosine kinase mutations, and EGFR protein expression]."( Epidermal growth factor receptor messenger RNA expression, gene dosage, and gefitinib sensitivity in non-small cell lung cancer.
Barón, AE; Bunn, PA; Cappuzzo, F; Crino, L; Danenberg, KD; Danenberg, PV; Dziadziuszko, R; Franklin, WA; Hirsch, FR; Park, S; Tanaka, K; Varella-Garcia, M; Witta, SE, 2006
)
0.33
"EGFR mRNA expression was measured by real-time quantitative reverse transcription-PCR in 64 patients, and EGFR gene dosage was analyzed by real-time quantitative PCR in 82 patients from paraffin-embedded specimens."( Epidermal growth factor receptor messenger RNA expression, gene dosage, and gefitinib sensitivity in non-small cell lung cancer.
Barón, AE; Bunn, PA; Cappuzzo, F; Crino, L; Danenberg, KD; Danenberg, PV; Dziadziuszko, R; Franklin, WA; Hirsch, FR; Park, S; Tanaka, K; Varella-Garcia, M; Witta, SE, 2006
)
0.33
" EGFR gene dosage is neither predictive for response nor progression-free nor overall survival."( Epidermal growth factor receptor messenger RNA expression, gene dosage, and gefitinib sensitivity in non-small cell lung cancer.
Barón, AE; Bunn, PA; Cappuzzo, F; Crino, L; Danenberg, KD; Danenberg, PV; Dziadziuszko, R; Franklin, WA; Hirsch, FR; Park, S; Tanaka, K; Varella-Garcia, M; Witta, SE, 2006
)
0.33
" Although higher exposure to gefitinib occurs in individuals who are poor CYP2D6 metabolisers, genotyping prior to initiation of therapy and dosage adjustment are not warranted."( Exploring the relationship between expression of cytochrome P450 enzymes and gefitinib pharmacokinetics.
Cantarini, MV; Fuhr, R; Holt, A; Swaisland, HC, 2006
)
0.33
" The objective of the current study is to develop a population pharmacokinetic/pharmacodynamic model resembling the mechanism of action of BIBN 4096 BS, and to extract by model-based simulations dosage formulations and pharmacodynamic properties that can assist in the development of CGRP receptor antagonists."( Modelling the anti-migraine effects of BIBN 4096 BS: a new calcitonin gene-related peptide receptor antagonist.
Roth, W; Schaefer, HG; Tillmann, C; Trocóniz, IF; Wolters, JM, 2006
)
0.33
" However, the response rates of IFN-alpha therapy frequently have been hampered by high dropout rates due to side effects and inconvenient dosing schedules."( Pegylated interferon therapy for patients with Philadelphia chromosome-negative myeloproliferative disorders.
Giles, F; Kantarjian, HM; Quintás-Cardama, A; Verstovsek, S, 2006
)
0.33
"The long half-life of erlotinib supports the current once-daily dosing regimen at 150 mg/d."( Clinical pharmacokinetics of erlotinib in patients with solid tumors and exposure-safety relationship in patients with non-small cell lung cancer.
Bruno, R; Eppler, SM; Hamilton, M; Lu, JF; Lum, BL; Rakhit, A; Wolf, J, 2006
)
0.33
" The actin remodeling effect was more prominent at lower dosage levels (1/8-1/4 of IC(50)), which was accompanied by an increased cell adhesion and decreased motility."( Effect of an epidermal growth factor receptor tyrosine kinase inhibitor on actin remodeling in an in vitro bladder cancer carcinogenesis model.
Belldegrun, A; Figlin, R; Iwata, KK; Jin, Y; Lieberman, R; Pantuck, A; Rao, J; Zhang, ZF, 2006
)
0.33
" Although both classes of anti-EGFR agents target the same receptor, substantial distinctions regarding their mechanism significantly affect dosing requirements, toxicity profiles, and their use as combination agents."( Clinical implications of the mechanism of epidermal growth factor receptor inhibitors.
Marshall, J, 2006
)
0.33
" AZD0530 is a potent inhibitor of tumor growth in a c-Src-transfected 3T3-fibroblast xenograft model in vivo and led to a significant increase in survival in a highly aggressive, orthotopic model of human pancreatic cancer when dosed orally once daily."( N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
Allen, J; Breed, J; Costello, G; Curwen, J; Fennell, M; Green, TP; Hennequin, LF; Lambert-van der Brempt, C; Morgentin, R; Norman, RA; Olivier, A; Otterbein, L; Plé, PA; Warin, N, 2006
)
0.33
" In the escalating phase of the trial, patients were enrolled in sequential cohorts using 100 or 150 mg oral daily dosing of erlotinib."( Erlotinib plus gemcitabine in patients with unresectable pancreatic cancer and other solid tumors: phase IB trial.
Dragovich, T; Hage, G; Hamilton, M; Huberman, M; Nadler, P; Patnaik, A; Rowinsky, EK; Von Hoff, DD; Wolf, J; Wood, D, 2007
)
0.34
" These EGFR mutations were associated with increased EGFR gene dosage and conferred anchorage-independent growth and tumorigenicity to NIH-3T3 cells."( Epidermal growth factor receptor activation in glioblastoma through novel missense mutations in the extracellular domain.
Beroukhim, R; Cloughesy, T; DeBiasi, RM; Feng, WL; Gabriel, S; Getz, G; Glatt, KA; Greulich, H; Huang, JH; Kawaguchi, T; Khan, H; King, JC; Leahy, DJ; Lee, JC; Levine, RL; Liau, LM; Linhart, DJ; Mellinghoff, IK; Meyerson, M; Mischel, P; Nelson, SF; Nghiemphu, P; O'Neill, K; Onofrio, R; Paez, JG; Peck, TC; Pieper, RO; Rao, PN; Sawyers, CL; Sellers, WR; Thomas, RK; Vivanco, I; Xu, Q; Yoshimoto, K; Yuza, Y; Ziaugra, L, 2006
)
0.33
" Dosing at 400 mg twice daily and 250 mg thrice daily was not feasible due to reversible, cholestatic liver dysfunction."( First study of the safety, tolerability, and pharmacokinetics of CP-724,714 in patients with advanced malignant solid HER2-expressing tumors.
Britten, CD; Denis, L; Gelmon, K; Guo, F; Letrent, SP; Minton, SE; Mita, M; Moulder, S; Munster, PN; Slamon, DJ; Tolcher, AW, 2007
)
0.34
" This study aimed to evaluate the schedule-dependent interaction of clinically relevant dosing of vandetanib with RT in human head and neck cancer models that had been characterized as EGFR positive (EGFR+) or negative (EGFR-) in order to begin differentiating vandetanib and RT interactions at the level of antitumor (EGFR) or antivascular (VEGFR2) activities."( Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
Frederick, B; Gustafson, DL; Merz, AL; Raben, D, 2008
)
0.35
" Vandetanib was dosed at 30 mg kg(-1) day(-1) based on pharmacokinetic studies in nude mice showing that this dose results in drug exposure similar to that seen in humans at clinical doses."( Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
Frederick, B; Gustafson, DL; Merz, AL; Raben, D, 2008
)
0.35
" Both effects depend on the dosage of the drug, which shows saturation kinetics."( relocating job wise? A mathematical model separates quantitatively the cytostatic and cytotoxic effects of a HER2 tyrosine kinase inhibitor.
Arteaga, CL; Hinow, P; Wang, SE; Webb, GF, 2007
)
0.34
" Due to difficulties in crystalline identification in the jejunal fluid samples, only the same crystalline form as the dosed form was identified."( Pharmacokinetics of gefitinib in humans: the influence of gastrointestinal factors.
Bergman, E; Cantarini, MV; Dickinson, P; Farmer, MR; Forsell, P; Knutson, L; Lennernäs, H; Persson, EM; Smith, R; Swaisland, H, 2007
)
0.34
" Thus, our results indicated that the microemulsion system composed of castor oil, polyethylene glycol 400, Tween 80, and water could be a more effective oral and parenteral dosage form for rutaecarpine."( Short communication: in vivo evaluation of microemulsion system for oral and parenteral delivery of rutaecarpine to rats.
Bhamdari, K; Choi, HG; Jahng, Y; Kim, DH; Lee, MH; Park, BJ; Woo, JS; Yong, CS; Yoo, BK, 2007
)
0.34
"Patients with measurable and nonmeasurable disease were treated with erlotinib 150 mg/d on days 1 through 28 of each 28-day dosing cycle."( Phase II study of erlotinib in patients with malignant pleural mesothelioma: a Southwest Oncology Group Study.
Altomare, DA; Borden, EC; Gandara, DR; Garland, LL; Klein-Szanto, AJ; Nagle, RB; Rankin, C; Rivkin, SE; Scott, KM; Testa, JR, 2007
)
0.34
" AZD1152 was dosed via several parenteral (s."( AZD1152, a selective inhibitor of Aurora B kinase, inhibits human tumor xenograft growth by inducing apoptosis.
Barrass, NC; Bigley, A; Boyle, FT; Brady, MC; Brown, E; Byth, KF; Crafter, C; Foote, KM; Foster, JR; Green, S; Heaton, SP; Heron, NM; Jung, FH; Keen, NJ; Mortlock, AA; Mundt, KE; Odedra, R; Wedge, SR; Wilkinson, RW, 2007
)
0.34
" A representative quinazolinimine (MD212) showed attenuation of cognitive deficits at a low dosage (0."( In vivo investigations on the cholinesterase-inhibiting effects of tricyclic quinazolinimines: scopolamine-induced cognitive impairments in rats are attenuated at low dosage and reinforced at higher dosage.
Appenroth, D; Decker, M; Fleck, C; Lehmann, J; Mohr, K; Tränkle, C, 2008
)
0.35
"Patients (n = 30) with advanced malignant HER2 positive solid tumors were enrolled in this open label dose-escalation study, and treated with daily oral dosing of CP-724,714 in 21-day cycles at the following dose levels: 250 mg QD, 250 mg BID, 400 mg BID, and 250 mg TID."( Pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors: correlations with clinical characteristics and safety.
Britten, CD; Gelmon, K; Guo, F; Letrent, SP; Munster, PN; Sharma, A; Tolcher, AW, 2008
)
0.35
" When various dosing schedules were applied, MP-412 showed significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound."( Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptor and ErbB2 tyrosine kinase inhibitor.
Abe, D; Amano, Y; Fujii, A; Kitano, Y; Nakamura, H; Ohya, J; Suzuki, T, 2007
)
0.34
"The study design includes two different dosage arms and a placebo group with a total sample size of 150 patients and is powered to detect a modest reduction in the mean tumor size burden in the high-dose sorafenib arm compared with a slight increase in the placebo group."( Design of phase II cancer trials using a continuous endpoint of change in tumor size: application to a study of sorafenib and erlotinib in non small-cell lung cancer.
Karrison, TG; Maitland, ML; Ratain, MJ; Stadler, WM, 2007
)
0.34
" Healthy male subjects (n = 18) received either a single gefitinib 250 mg tablet (once), or a 250 mg granular formulation of gefitinib (on two separate occasions) over the three dosing periods, in randomized order."( The relative bioavailability of gefitinib administered by granular formulation.
Bailey, CJ; Cantarini, MV; Collins, B; Smith, RP, 2008
)
0.35
" These dosing schedules resulted in significant effects on tumor vasculature, with decreased volume transfer constants, area under the curve, and permeability surface factor as well as increased gadolinium clearance after 30 days of treatment."( Investigation of two dosing schedules of vandetanib (ZD6474), an inhibitor of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling, in combination with irinotecan in a human colon cancer xenograft model.
Ciardiello, F; Eckhardt, SG; Gustafson, DL; Henthorn, TK; Lockerbie, O; Long, M; Merz, A; Morrow, M; Serkova, NJ; Troiani, T, 2007
)
0.34
" We detected no antitumor activity of ispinesib in RMHNSC on this dosing schedule."( Phase II study of ispinesib in recurrent or metastatic squamous cell carcinoma of the head and neck.
Chen, EX; Chia, S; Colevas, AD; Hotte, SJ; Johnson, C; Pond, GR; Schwarz, JK; Siu, LL; Synold, TW; Tang, PA; Vasist, LS; Winquist, E, 2008
)
0.35
" Its extended half-life probably permits dosing less frequently than once a day."( New and emerging treatments for fungal infections.
Denning, DW; Pasqualotto, AC, 2008
)
0.35
"These studies provide a rationale for intermittent dosing of EGFR TKIs with chemotherapy in order to enhance cytotoxicity."( Schedule-dependent apoptosis in K-ras mutant non-small-cell lung cancer cell lines treated with docetaxel and erlotinib: rationale for pharmacodynamic separation.
Davies, AM; Gandara, DR; Gumerlock, PH; Holland, W; Lara, PN; Mack, PC; Mahaffey, CM; Pryde, B, 2007
)
0.34
" This case suggests that, in some patients with NSCLC, even short-term administration of gefitinib may bring about clinical benefits and disease response comparable to the standard long-term daily dosing schedule."( Short-term gefitinib treatment brought about a long-term regression of bronchioloalveolar carcinoma without EGFR gene alterations: a case report.
Goya, S; Kawase, I; Kijima, T; Kumagai, T; Matsuoka, H; Minami, S; Osaki, T; Suzuki, M; Tachibana, I; Takeda, Y; Ueda, K; Yokota, S; Yoshida, M, 2007
)
0.34
" Compound 11a possessed desirable pharmaceutical properties, including excellent brain exposure and long brain half-life following oral dosing to mice."( Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy.
Andresson, T; Bedell, L; Bjornsson, JM; Bragason, G; Burghes, AH; Butchbach, ME; Coovert, DD; Gurney, ME; Haraldsson, M; Keyvan, M; Mishra, R; Pai, G; Palomo, M; Pease, B; Rao, M; Singh, J; Thosteinsdottir, M; Thurmond, J, 2008
)
0.35
" In contrast, systemic exposure of lapatinib after oral dosing was unchanged when efflux by Pgp and BCRP was absent from the gastrointestinal tract."( The role of efflux and uptake transporters in [N-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine (GW572016, lapatinib) disposition and drug interactions.
Castellino, S; Harmon, KA; Humphreys, JE; John-Williams, LS; Koch, KM; O'Mara, MJ; Olson, KL; Polli, JW; Serabjit-Singh, CJ, 2008
)
0.35
" Three treatment cohorts were assessed, using different dosing regimens."( Erlotinib in combination with capecitabine and docetaxel in patients with metastatic breast cancer: a dose-escalation study.
Baselga, J; De Rosa, F; Fettner, S; Jones, R; Rakhit, A; Trigo, JM; Twelves, C; Wright, T, 2008
)
0.35
" The goal of this investigation was to cast the combined PG/PK/PD variables into models that could be used to design equivalent PK/PD dosing regimens for gefitinib in genetically distinct tumor models."( Preclinical pharmacokinetic/pharmacodynamic models of gefitinib and the design of equivalent dosing regimens in EGFR wild-type and mutant tumor models.
Gallo, JM; Guo, P; Wang, S; Wang, X; Zhou, Q, 2008
)
0.35
"Although no maximum tolerated dose was reached in cycle 1 with 35 mg/m(2) docetaxel, repetitive dosing proved intolerable in a substantial number of patients; thus, the recommended phase II dose of weekly docetaxel is 30 mg/m(2) when combined with 150 mg of daily erlotinib."( A phase I and pharmacokinetic trial of erlotinib in combination with weekly docetaxel in patients with taxane-naive malignancies.
Al Omari, AS; Chiorean, EG; Fife, KL; Foster, AE; Jones, DR; Murry, DJ; Porter, JM; Strother, RM; Sweeney, CJ; Yoder, CA; Yu, M, 2008
)
0.35
"Our present results imply that (1) mutation analyses of EGFR and KRAS provide valuable information about whether or not to apply treatments targeting against EGFR and the selection of dosage for such treatments, and (2) siRNA-mediated knockdown is effective in lung adenocarcinomas with EGFR mutation, probably in those with resistance to gefitinib by acquired mutation in EGFR."( siRNA targeting against EGFR, a promising candidate for a novel therapeutic application to lung adenocarcinoma.
Fujisaki, R; Gu, Z; Horii, A; Inomata, K; Inoue, A; Kondo, T; Nukiwa, T; Sakurada, A; Sato, M; Yamanaka, S, 2008
)
0.35
" Our findings suggest that HKI-272 treatment at maximally tolerated dosing may lead to the emergence of T790M-mediated resistance, whereas treatment with a more potent irreversible inhibitor could yield a resistance mutation at EGFR C797."( The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor.
Brannigan, BW; Godin-Heymann, N; Haber, DA; Lamb, J; Maheswaran, S; McDermott, U; Settleman, J; Ulkus, L, 2008
)
0.35
" Treatment arms with gefitinib 250mg/day and platinum-based doublets chemotherapy irrespective of dosage and schedule were combined to calculate the pooled estimates for efficacy and safety outcomes of interest."( The safety and efficacy of gefitinib versus platinum-based doublets chemotherapy as the first-line treatment for advanced non-small-cell lung cancer patients in East Asia: a meta-analysis.
Chan, KA; Chang, CH; Chen, KY; Kurth, T; Orav, EJ; Yang, PC; Young-Xu, Y, 2008
)
0.35
" There were no significant differences in clinical activity or the AE profile between the dosing schedules."( Efficacy and safety of lapatinib as first-line therapy for ErbB2-amplified locally advanced or metastatic breast cancer.
Ang, PC; Arbushites, MC; Aziz, Z; Berger, MS; Casey, MA; Chavez, MA; Chow, LW; Doval, DC; Franco, SX; Gomez, HL; Nag, S; Ng, C; Sledge, GW; Stein, SH, 2008
)
0.35
" Dosing 3 mg/kg/d cediranib for 4 days induced a marked hypertension of 35 to 50 mmHg."( Inhibition of vascular endothelial growth factor-a signaling induces hypertension: examining the effect of cediranib (recentin; AZD2171) treatment on blood pressure in rat and the use of concomitant antihypertensive therapy.
Curwen, JO; Kendrew, J; Musgrove, HL; Ogilvie, DJ; Richmond, GH; Wedge, SR, 2008
)
0.35
" Phase I studies have established that it is suitable for once-daily oral dosing at a dose of up to 300 mg."( Dual targeting of the vascular endothelial growth factor receptor and epidermal growth factor receptor pathways with vandetinib (ZD6474) in patients with advanced or metastatic non-small cell lung cancer.
Natale, RB, 2008
)
0.35
" Multiplex ligation-dependent probe amplification and fluorescence in situ hybridization analysis revealed increased EGFR dosage in 28% of MPNSTs."( EGFR and erbB2 in malignant peripheral nerve sheath tumors and implications for targeted therapy.
Holtkamp, N; Malzer, E; Mautner, VF; Mawrin, C; Mucha, J; Okuducu, AF; Schildhaus, HU; von Deimling, A; Zietsch, J, 2008
)
0.35
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug and food interactions, dosage and administration, and role in therapy of lapatinib in metastatic breast cancer are reviewed."( Lapatinib: a dual tyrosine kinase inhibitor for metastatic breast cancer.
Paul, B; Thompson, J; Trovato, JA, 2008
)
0.35
" This is likely to be due to lack of radical corrections in the dosage of the drug for different reasons."( [What is the current treatment of patients with essential thrombocytopenia and other myeloproliferations accompanied with thrombocythemia [corrected] and what can be the predictive sign of the risk of thrombosis in such patients--a report from the registr
Brychtová, Y; Cerná, O; Doubek, M; Dulícek, P; Dusek, L; Hadacová, I; Hlusi, A; Hochová, I; Kissová, J; Pavlík, T; Penka, M; Pytiĺk, R; Schutzová, M; Schwarz, J; Seghetová, J; Szotkowski, T; Voglová, J; Volková, Z; Vozobulová, V,
)
0.13
" Docetaxel may exert antiangiogenic effects if dosed so plasma levels are maintained at low nanomolar concentrations over a prolonged time."( Pharmacokinetic-directed dosing of vandetanib and docetaxel in a mouse model of human squamous cell carcinoma.
Bradshaw-Pierce, EL; Gustafson, DL; Raben, D; Steinhauer, CA, 2008
)
0.35
" The approved dosing of lapatinib is 1,250 mg PO QD given continuously in combination with capecitabine 2,000 mg/m(2) daily administered in 2 divided doses on days 1 to 14 of a 21-day cycle."( Lapatinib: a dual inhibitor of human epidermal growth factor receptor tyrosine kinases.
Goodin, S; Medina, PJ, 2008
)
0.35
" Cediranib (3 mg/kg per day) or vehicle was then dosed orally (2, 26 and 50 h after the baseline scan; 12 rats per group) and a second scan acquired 2 h after the final dosing event."( Examining the acute effects of cediranib (RECENTIN, AZD2171) treatment in tumor models: a dynamic contrast-enhanced MRI study using gadopentate.
Bradley, DP; Jürgensmeier, JM; Kilburn, L; Lacey, T; Mills, J; Odedra, R; Scott, M; Tessier, JJ; Wedge, SR, 2009
)
0.35
" The effect of 1 to 2 months of chronic dosing of BI 1356 in two different animal models was investigated."( Chronic treatment with the dipeptidyl peptidase-4 inhibitor BI 1356 [(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione] increases basal glucagon-like peptide-1 and improves glycemic contro
Mark, M; Tadayyon, M; Thomas, L, 2009
)
0.35
" It was concluded that a change of the dosage from the crude drug to solid dispersion could improve significantly the efficiency of rutaecarpine absorption and increase its plasma concentration."( Solid dispersion of rutaecarpine improved its antihypertensive effect in spontaneously hypertensive rats.
Ding, JS; Gao, R; Li, D; Li, YJ; Peng, J; Ran, LL, 2008
)
0.35
" Gefitinib was administrated orally at a dosage of 250mg/day during the radiation course and was continued for each 28-day treatment cycle until progression of the disease, unacceptable toxicity, or withdrawal of consent."( Treatment of brain metastasis from non-small cell lung cancer with whole brain radiotherapy and Gefitinib in a Chinese population.
Deng, Q; Ma, S; Xu, Y; Yu, X, 2009
)
0.35
" Additionally, 57 inhibited the related receptor, VEGF receptor I (VEGFR-1), and showed excellent exposure when dosed orally to female CD-1 mice."( Arylphthalazines as potent, and orally bioavailable inhibitors of VEGFR-2.
Balagtas, C; Bohlen, P; Doody, JF; Duncton, MA; Hadari, YR; Katoch-Rouse, R; Kawakami, JK; Kiselyov, AS; Kussie, P; Milligan, DL; Mitelman, S; Patel, SN; Piatnitski Chekler, EL; Rolster, RL; Sherman, D; Smith, LM; Surguladze, D; Tonra, JR; Wang, Y; Wong, WC, 2009
)
0.35
"Five dosage levels (70, 90, 120, 160, and 200 mg/m(2) per day) were planned in this phase I study."( Phase I and pharmacokinetic studies of erlotinib administered concurrently with radiotherapy for children, adolescents, and young adults with high-grade glioma.
Baker, SJ; Broniscer, A; Ellison, DW; Endersby, R; Gajjar, A; Kocak, M; Laningham, FH; Merchant, TE; Morris, EB; Schaiquevich, P; Stewart, CF, 2009
)
0.35
" However, there was no relationship between erlotinib dosage and drug exposure."( Phase I and pharmacokinetic studies of erlotinib administered concurrently with radiotherapy for children, adolescents, and young adults with high-grade glioma.
Baker, SJ; Broniscer, A; Ellison, DW; Endersby, R; Gajjar, A; Kocak, M; Laningham, FH; Merchant, TE; Morris, EB; Schaiquevich, P; Stewart, CF, 2009
)
0.35
"Lapatinib was dosed at 1,500 mg/day orally continuously."( A phase II study of lapatinib in patients with advanced biliary tree and hepatocellular cancer.
Belani, CP; Dancey, J; Gandara, DR; Gandour-Edwards, R; Iqbal, S; Kindler, HL; Lenz, HJ; Longmate, J; Lurje, G; Mack, PC; Ramanathan, RK; Singh, DA; Tanaka, M; Yen, Y, 2009
)
0.35
"These large increases in lapatinib bioavailability and absolute variability support the recommendation for dosing in the fasted state to achieve consistent therapeutic exposure."( Effects of food on the relative bioavailability of lapatinib in cancer patients.
Beelen, AP; Cohen, RB; Koch, KM; Lewis, LD; Lewis, NL; Mackay, K; Reddy, NJ; Stead, A; Whitehead, B, 2009
)
0.35
" These data suggest that the inhibition of aurora B kinase may be a useful therapeutic strategy in the treatment of AML and that further exploration of dosing and treatment schedules is warranted in clinical trials."( AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo.
Bonnet, D; Cavenagh, J; Crafter, C; Fitzgibbon, J; Joel, S; Lister, AT; Odedra, R; Oke, A; Pearce, D; Wilkinson, RW, 2009
)
0.35
" We think that in our case, the adverse response of anagrelide therapy was determined, by accumulated dosage of the drug, through an intensive inotropic stimulation and a sympathetic hyperactivation in a vulnerable myocardium."( Atypical Takotsubo syndrome during anagrelide therapy.
Ardizzone, F; Maccio, S; Proietti, R; Rognoni, A; Rognoni, G; Santagostino, A, 2009
)
0.35
" This validated LC-MS/MS method was successfully applied to a bioavailability study of oral and intravenous administration of changrolin with 20mg/kg dosage in SD rats."( Liquid chromatography/tandem mass spectrometry for the determination of changrolin in rat plasma: application to a bioavailability study.
Li, S; Liu, G; Lu, Y; Wang, Y; Yang, D; Yu, C, 2009
)
0.35
"The clinical records were assessed for the patients who started treatment with erlotinib, on a compassionate-use basis, with an oral dosage of 150 mg/day until June 2008."( [Effectiveness and safety of erlotinib in 2 patients with carcinoma of the cervix].
Albornoz López, R; Fernández García, I; Pérez Rodrigo, I; Soto Rojas, M; Torres Degayón, V,
)
0.13
" x 15 days, respectively, as dictated by the equivalent PK/PD dosing strategy."( Demonstration of the equivalent pharmacokinetic/pharmacodynamic dosing strategy in a multiple-dose study of gefitinib.
Gallo, JM; Wang, S; Zhou, Q, 2009
)
0.35
" The steady-state pharmacokinetics of linagliptin and metformin and the inhibition of DPP-4 activity were determined at the end of each dosing period."( Evaluation of the potential for steady-state pharmacokinetic and pharmacodynamic interactions between the DPP-4 inhibitor linagliptin and metformin in healthy subjects.
Dugi, KA; Graefe-Mody, EU; Padula, S; Ring, A; Withopf, B, 2009
)
0.35
"An isocratic reversed phase high-performance liquid chromatographic (HPLC) method with ultraviolet detection at 245 nm has been developed for the determination of alfuzosin hydrochloride in dosage formulation."( Quantitation of alfuzosin hydrochloride in pharmaceutical formulations by RP-HPLC.
Ganesh, M; Gangully, S; Kamalakannan, K; Rathinavel, G; Sivakumar, T; Tivari, R; Uppatyay, S, 2009
)
0.35
" dosing of [(14)C]-radio labeled BI 1356."( Tissue distribution of the novel DPP-4 inhibitor BI 1356 is dominated by saturable binding to its target in rats.
Binder, R; Fuchs, H; Greischel, A, 2009
)
0.35
"This was a multicenter, open-label, single-arm trial evaluating the toxicity and efficacy of oral erlotinib at an initial dosage of 150 mg daily until progressive disease or adverse effects prohibited further therapy."( A phase II trial of erlotinib in recurrent squamous cell carcinoma of the cervix: a Gynecologic Oncology Group Study.
Lee, YC; Mannel, R; Schilder, RJ; Sill, MW, 2009
)
0.35
" Data further indicated that the modified USP method provided for complete matrix hydration and swelling as the dosage form remained fully submerged, allowing for more reliable release mimicking the in-vivo conditions."( Application of a novel symmetrical shape factor to gastroretentive matrices as a measure of swelling synchronization and its impact on drug release kinetics under standard and modified dissolution conditions.
Fassihi, R; Liu, Q, 2009
)
0.35
", increasing the dosage until a rash appears) as a rational management strategy."( Expert consensus on the management of erlotinib-associated cutaneous toxicity in the u.k.
Dunlop, J; Eaby, B; Groves, RW; McPhelim, J; Nicolson, M; Nijjar, R; Steele, J; Thatcher, N; Ukachukwu, I, 2009
)
0.35
" Medical information, including the indication for warfarin use, warfarin dosing and dosing changes, and exposure to gefitinib were collected from computerized databases and medical records."( Effect of gefitinib on warfarin antithrombotic activity.
Arai, S; Fukui, T; Hataishi, R; Iwasaki, M; Katagiri, M; Katono, K; Kobayashi, H; Kubota, M; Masuda, N; Mitsufuji, H; Nishii, Y; Onoda, S; Otani, S; Ryuge, S; Takakura, A; Wada, M; Yamamoto, M; Yanaihara, T; Yanase, N; Yokoba, M, 2009
)
0.35
" The applicability of the method was demonstrated by successful determination of AZD1152 and hQPA in human plasma and in plasma, brain, liver, kidney and ileum samples from mice dosed with AZD1152."( Simultaneous determination of AZD1152 (prodrug) and AZD1152-hydroxyquinazoline pyrazol anilide by reversed phase liquid chromatography.
Beijnen, JH; Pluim, D; Schellens, JH; van Tellingen, O, 2009
)
0.35
" Individually, the selection and dosing of erlotinib for the treatment of lung cancer patients who continue to smoke is a clinical challenge."( Using erlotinib to treat patients with non-small cell lung cancer who continue to smoke.
Miller, AA; Petty, WJ; Waller, LL, 2010
)
0.36
" Dosing levels of saracatinib ascended by cohort (60 to 250 mg)."( Effects of the Src kinase inhibitor saracatinib (AZD0530) on bone turnover in healthy men: a randomized, double-blind, placebo-controlled, multiple-ascending-dose phase I trial.
Clack, G; Eastell, R; Finkelman, RD; Hannon, RA; Lockton, JA; Rimmer, M; Swaisland, A, 2010
)
0.36
" However, recent data reported elevated liver transaminases when telcagepant was dosed twice daily for three months for the prevention of migraine rather than acutely."( The role of CGRP in the pathophysiology of migraine and efficacy of CGRP receptor antagonists as acute antimigraine drugs.
Olesen, J; Villalón, CM, 2009
)
0.35
" Twice-daily dosing was implemented to further explore tolerability, and was limited by diarrhea to 500 mg twice daily."( A phase I and pharmacokinetic study of oral lapatinib administered once or twice daily in patients with solid malignancies.
Arya, N; Burris, HA; Fleming, RA; Jones, SF; Koch, KM; Pandite, L; Smith, DA; Spector, N; Taylor, CW; Versola, MJ; Wilding, G, 2009
)
0.35
" This review summarizes the background, scientific rationale and early clinical data in support of intercalation of intermittent erlotinib dosing with pemetrexed as a means of achieving pharmacodynamic separation."( Intercalation of erlotinib and pemetrexed in the treatment of non-small cell lung cancer.
Gandara, DR; Lara, PN; Li, T; Mack, PC; Perez-Soler, R, 2010
)
0.36
" The current analysis focused mainly on evaluation of anagrelide dosage needed to achieve a complete response in high-risk patients: reduction in platelet count to below 400 x 10(9)/l, which was also considered as reaching the therapeutic goal."( [The results of patients with essentials thrombocythemia and other myeloproliferation-related thrombocythemia--a report of patients treated with Thromboreductin].
Bodzásová, C; Brychtová, Y; Cerná, O; Doubek, M; Dulícek, P; Dusek, L; Hadacová, I; Hlusí, A; Hochová, I; Indrák, K; Jelínková, P; Jonásová, A; Kissová, J; Korístek, Z; Nováková, L; Pavlík, T; Penka, M; Pospísilová, D; Schutzová, M; Schwarz, J; Segethová, J; Voglová, J; Vozobulová, V; Walterová, L, 2009
)
0.35
"Principles of experimental design have been exploited to develop the dosage form."( Alfuzosin hydrochloride transdermal films: evaluation of physicochemical, in vitro human cadaver skin permeation and thermodynamic parameters.
Acharya, PK; Choudhury, P; Mallick, S; Pattnaik, S; Swain, K,
)
0.13
" Key aspects of erlotinib clinical pharmacology, dosing in special populations (e."( A review of erlotinib--an oral, selective epidermal growth factor receptor tyrosine kinase inhibitor.
Bharthuar, A; Iyer, R, 2010
)
0.36
" The reader will also understand the pharmacologic bases for the recent change in dosing guidelines of erlotinib, and the current knowledge of clinical and laboratory correlates that can serve as surrogates of response."( A review of erlotinib--an oral, selective epidermal growth factor receptor tyrosine kinase inhibitor.
Bharthuar, A; Iyer, R, 2010
)
0.36
" More studies to individualize therapy and optimize dosing are needed."( A review of erlotinib--an oral, selective epidermal growth factor receptor tyrosine kinase inhibitor.
Bharthuar, A; Iyer, R, 2010
)
0.36
" All other treatments were continued with some dosage adjustments."( Management of refractory essential thrombocythemia with anagrelide in a patient undergoing hemodialysis.
Demulder, AC; Malarme, M; Mesquita, Mdo C; Noubouossie, D; Sol, EB, 2009
)
0.35
" The CSF concentration of EGFR-TKIs achieved by standard daily dosing may be insufficient for therapeutic effect."( High dose weekly erlotinib achieves therapeutic concentrations in CSF and is effective in leptomeningeal metastases from epidermal growth factor receptor mutant lung cancer.
Clarke, JL; Lassman, AB; Miller, VA; Pao, W; Wu, N, 2010
)
0.36
"It was shown that AZD1152 is an effective antineoplastic agent for breast cancer, and our results define a novel mechanism for posttranscriptional regulation of Aurora B after AZD1152 treatment and provide insight into dosing regimen design for this kinase inhibitor in metastatic breast cancer treatment."( Antineoplastic effects of an Aurora B kinase inhibitor in breast cancer.
Chen, J; Gully, CP; Lee, MH; Velazquez-Torres, G; Wang, E; Yeung, JA; Yeung, SC; Zhang, F, 2010
)
0.36
" Toxicity studies in animals and phase I/II clinical trials have indicated that RVX-208 is safe and well tolerated in multiple dosing regimens."( RVX-208, a stimulator of apolipoprotein AI gene expression for the treatment of cardiovascular diseases.
McNeill, E, 2010
)
0.36
" Dose-response curves were generated to determine sensitivity to lapatinib, erlotinib, and trastuzumab."( Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo.
Anghel, A; Ayala, R; Desai, AJ; Fejzo, MS; Finn, RS; Hecht, JR; Luo, T; Safran, B; Slamon, DJ; Wainberg, ZA, 2010
)
0.36
" Wistar rats were orally administered with a daily dosage of 200 mg kg(-1) Erlotinib-HCl either as free drug or as Poly(D,L-lactic-co-glycolic acid) (PLGA) encapsulated nanoparticles."( Poly(D,L-lactic-co-glycolic acid) nanoencapsulation reduces Erlotinib-induced subacute toxicity in rat.
Franklin, G; Kalaichelvan, VK; Manavalan, R; Marslin, G; Reddy, PN; Sheeba, CJ, 2009
)
0.35
" Adverse events were similar across dosing regimens."( Randomized phase II multicenter trial of two schedules of lapatinib as first- or second-line monotherapy in patients with advanced or metastatic non-small cell lung cancer.
Aisner, J; Allen, KE; Blumenschein, GR; Damjanov, N; Dowlati, A; Garst, J; Hassani, H; Leopold, L; Rigas, JR; Ross, HJ; Shepherd, FA; Smylie, M; Zaks, TZ, 2010
)
0.36
" The proposed method is applied to time course microarray data of lung cells treated by stimulating EGF receptors and dosing an anticancer drug, Gefitinib."( A state space representation of VAR models with sparse learning for dynamic gene networks.
Gotoh, N; Higuchi, T; Imoto, S; Kojima, K; Miyano, S; Nagasaki, M; Shimamura, T; Ueno, K; Yamaguchi, R; Yamauchi, M; Yoshida, R, 2010
)
0.36
"Given the marked toxicity in our patient population, the combination of vinflunine and erlotinib cannot be recommended for further study with these dosing schemas."( A phase I evaluation of the combination of vinflunine and erlotinib in patients with refractory solid tumors.
Buie, L; Chiu, WK; Davies, JM; Dees, EC; Irvin, W; Ivanova, A; Keller, K; O'Neil, BH; Sanoff, HK; Stinchcombe, TE; Walko, C, 2011
)
0.37
" Blood samples were collected before dosing and on days 7, 14, 21, and 28."( The relationship between drug exposure and clinical outcomes of non-small cell lung cancer patients treated with gefitinib.
Guo, Y; Jiang, W; Li, S; Liao, H; Shi, YX; Xue, C; Zhang, L; Zhang, Y; Zhao, HY; Zhao, YY, 2011
)
0.37
" In 24 patients, the mean Cmax and AUC erlotinib values increased with dose and following cumulative dosing (days 7 and 8 vs."( Phase I and pharmacokinetic study of erlotinib (OSI-774) in combination with docetaxel in squamous cell carcinoma of the head and neck (SSCHN).
Agrawal, A; Aimiumu, J; Chan, KK; Chen, P; Cheng, H; Dancey, J; Grever, MR; Kraut, EH; Lang, J; Rhoades, C; Young, DC; Zhang, Y, 2011
)
0.37
" Dosing for phase II trials was docetaxel 35 mg/m² and erlotinib 50 mg."( Phase I and pharmacokinetic study of erlotinib (OSI-774) in combination with docetaxel in squamous cell carcinoma of the head and neck (SSCHN).
Agrawal, A; Aimiumu, J; Chan, KK; Chen, P; Cheng, H; Dancey, J; Grever, MR; Kraut, EH; Lang, J; Rhoades, C; Young, DC; Zhang, Y, 2011
)
0.37
" The synergy with docetaxel depended on the treatment sequence; a schedule of MK-2206 dosed before docetaxel was not effective."( MK-2206, an allosteric Akt inhibitor, enhances antitumor efficacy by standard chemotherapeutic agents or molecular targeted drugs in vitro and in vivo.
Hatch, H; Hirai, H; Kotani, H; Majumder, PK; Miyama, K; Nakatsuru, Y; Pan, BS; Sootome, H; Taguchi, S; Tsujioka, K; Ueno, Y, 2010
)
0.36
" The accumulation ratio with multiple dosing was <1."( Linagliptin, a dipeptidyl peptidase-4 inhibitor in development for the treatment of type 2 diabetes mellitus: a Phase I, randomized, double-blind, placebo-controlled trial of single and multiple escalating doses in healthy adult male Japanese subjects.
Dugi, KA; Graefe-Mody, EU; Hayashi, N; Horie, Y; Nakashima, M; Sarashina, A; Sesoko, S; Taniguchi, A; Woerle, HJ, 2010
)
0.36
" Multiple dosing of linagliptin for 12 days was well tolerated and exhibited a pharmacokinetic/pharmacodynamic profile consistent with a once-daily regimen."( Linagliptin, a dipeptidyl peptidase-4 inhibitor in development for the treatment of type 2 diabetes mellitus: a Phase I, randomized, double-blind, placebo-controlled trial of single and multiple escalating doses in healthy adult male Japanese subjects.
Dugi, KA; Graefe-Mody, EU; Hayashi, N; Horie, Y; Nakashima, M; Sarashina, A; Sesoko, S; Taniguchi, A; Woerle, HJ, 2010
)
0.36
" Patients were stratified by platinum sensitivity and were treated with erlotinib 150 mg daily on a continuous dosing schedule, and carboplatin at an AUC of 5 every 21 days."( A phase II study of erlotinib (OSI-774) given in combination with carboplatin in patients with recurrent epithelial ovarian cancer (NCIC CTG IND.149).
Ellard, SL; Fisher, B; Grimshaw, R; Hirte, H; Oza, A; Seymour, L; Swenerton, K; Tsao, M, 2010
)
0.36
" Although some patients may benefit from the treatment, other dosing regimens and novel taxanes such as Nab-paclitaxel should be explored in this setting."( Docetaxel second-line therapy in patients with advanced pancreatic cancer: a retrospective study.
Kaley, K; Penney, R; Saif, MW; Syrigos, K, 2010
)
0.36
" The initial gefitinib dosage was 100mg/m(2)/d commencing with radiation therapy and the dose-finding period extended until 2 weeks post-radiation."( A phase I and biology study of gefitinib and radiation in children with newly diagnosed brain stem gliomas or supratentorial malignant gliomas.
Banerjee, A; Blaney, SM; Boyett, JM; Broniscer, A; Douglas, JG; Geyer, JR; Gilbertson, RJ; Gururangan, S; Kieran, MW; Kocak, M; Kun, LE; Packer, RJ; Phillips, P; Stewart, CF, 2010
)
0.36
" Lapatinib dosage was related linearly to area under the [concentration-time] curve from start time to 12 hours later (AUC(0-12)) and dose-normalized maximum serum concentration and AUC values for patients in stratum II were both significantly higher (P = ."( Phase I trial of lapatinib in children with refractory CNS malignancies: a Pediatric Brain Tumor Consortium study.
Blaney, SM; Boyett, JM; Fouladi, M; Gajjar, A; Gilbertson, RJ; Kun, LE; Onar-Thomas, A; Packer, RJ; Schaiquevich, P; Stewart, CF, 2010
)
0.36
" The patient's warfarin dosage was adjusted to reach a target INR of 2-3."( Elevated international normalized ratio associated with concomitant warfarin and erlotinib.
Amarshi, N; Billingsley, A; Nair, BA; Thomas, KS, 2010
)
0.36
" A 7-day intrathecal treatment with morphine (15 μg/day) produced tolerance to its analgesic effects as well as a rightward shift in the dose-response curve to its antinociceptive effects."( Morphological evidence for the involvement of microglial p38 activation in CGRP-associated development of morphine antinociceptive tolerance.
Chabot, JG; Ma, W; Quirion, R; Wang, Z, 2010
)
0.36
" Saracatinib accumulated 4- to 5-fold on once-daily dosing to reach steady-state exposure after 10 to 17 days of dosing."( Phase I safety, pharmacokinetics, and inhibition of SRC activity study of saracatinib in patients with solid tumors.
Baselga, J; Casado, E; Cervantes, A; Chirivella, I; Elvin, P; Hamberg, P; Hoekman, K; Hurwitz, HI; Iacona, R; Jodrell, DI; Martinelli, E; Swaisland, A; Tabernero, J, 2010
)
0.36
" Dose modification including dose reduction and dosing schedule modification may be utilized to manage toxicities, but this must be based on careful hematologic, neurologic, and liver function monitoring."( Optimizing ixabepilone treatment schedules in patients with advanced or metastatic breast cancer.
Egerton, N, 2010
)
0.36
"To determine, for each of two dosing schedules, the dose-limiting toxicity (DLT) and maximum-tolerated dose (MTD) of AZD1152, an Aurora B kinase inhibitor, and to evaluate its safety, biologic activity and pharmacokinetics (PK)."( Clinical evaluation of AZD1152, an i.v. inhibitor of Aurora B kinase, in patients with solid malignant tumors.
Ataman, O; Boss, DS; Das, S; Lolkema, MP; Schellens, JH; Stockman, PK; van der Sar, J; Voest, EE; Wilson, D; Witteveen, PO, 2011
)
0.37
" However, this was not seen as clinically relevant due to the absence of a reliable dose-response relationship and the known large pharmacokinetic interindividual variability of glyburide."( Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects.
Graefe-Mody, U; Iovino, M; Ring, A; Rose, P; Woerle, HJ; Zander, K, 2011
)
0.37
" This study evaluated the effect of food on the pharmacokinetics of cediranib and compared the administration of continual cediranib via two dosing strategies using this as a platform to investigate pharmacodynamic imaging biomarkers."( A two-part phase II study of cediranib in patients with advanced solid tumours: the effect of food on single-dose pharmacokinetics and an evaluation of safety, efficacy and imaging pharmacodynamics.
Cheung, S; Evans, J; Fielding, A; Harris, A; Jackson, A; Jayson, GC; Kelly, C; Middleton, M; Mitchell, CL; O'Connor, JP; Parker, GJ; Roberts, C; Rudman, S; Spicer, J; Tessier, J; Watson, Y; Young, H, 2011
)
0.37
" In continual dosage phase (Part B), patients were randomised to a fixed-dose or dose-escalation arm."( A two-part phase II study of cediranib in patients with advanced solid tumours: the effect of food on single-dose pharmacokinetics and an evaluation of safety, efficacy and imaging pharmacodynamics.
Cheung, S; Evans, J; Fielding, A; Harris, A; Jackson, A; Jayson, GC; Kelly, C; Middleton, M; Mitchell, CL; O'Connor, JP; Parker, GJ; Roberts, C; Rudman, S; Spicer, J; Tessier, J; Watson, Y; Young, H, 2011
)
0.37
" L + T for short duration (14 and 42 days), intermittent administration (14 days on/off), and reduced dosing (half dose) was also investigated."( Reduced dose and intermittent treatment with lapatinib and trastuzumab for potent blockade of the HER pathway in HER2/neu-overexpressing breast tumor xenografts.
Arpino, G; Gutierrez, C; Hilsenbeck, SG; Huang, C; Massarweh, S; Migliaccio, I; Osborne, CK; Rimawi, MF; Schiff, R; Soliz, R; Wang, YC; Ward, R; Wiechmann, LS; Wu, MF, 2011
)
0.37
"6 μg/mL, and area under the drug concentration-time curve over a dosing interval (AUC) was 12."( Pharmacokinetics of sotrastaurin combined with tacrolimus or mycophenolic acid in de novo kidney transplant recipients.
Arns, W; Budde, K; Dantal, J; Grinyo, JM; Kovarik, JM; Proot, P; Rostaing, L; Steiger, JU, 2011
)
0.37
" Furthermore, we advise to monitor closely erlotinib plasma concentrations and adjust the erlotinib dose accordingly when a clinically relevant interaction is suspected and no proper dosing guidelines are available."( Erlotinib and pantoprazole: a relevant interaction or not?
Beijnen, JH; Fanggiday, JC; Lankheet, NA; Malingré, MM; Staaks, GH; Ter Heine, R; Van Der Westerlaken, MM, 2010
)
0.36
" Treatment durations and dosing were derived from randomized controlled trials, FDA labeling, and National Comprehensive Cancer Network guidelines."( Budget impact of erlotinib for maintenance therapy in advanced non-small cell lung cancer.
Carlson, JJ; Reyes, C; Veenstra, DL; Wong, WB, 2011
)
0.37
" The recommended dosage is not dependent on body weight either."( Lapatinib in breast cancer - the predictive significance of HER1 (EGFR), HER2, PTEN and PIK3CA genes and lapatinib plasma level assessment.
Bouchalova, K; Cizkova, M; Cwiertka, K; Friedecky, D; Hajduch, M; Trojanec, R, 2010
)
0.36
" First, we provide advances into administration schedules and dosing regimens for the combination treatment in in vivo pancreatic tumour."( Aurora B kinase inhibitor AZD1152: determinants of action and ability to enhance chemotherapeutics effectiveness in pancreatic and colon cancer.
Azzariti, A; Bocci, G; Chiarappa, P; Del Bufalo, D; Del Tacca, M; Fioravanti, A; Mangia, A; Paradiso, A; Porcelli, L; Quatrale, AE; Sebastian, S; Simone, GM; Sini, P, 2011
)
0.37
" At the end of the 24-h dosing interval, inhibition was still high (82-90%)."( The oral DPP-4 inhibitor linagliptin significantly lowers HbA1c after 4 weeks of treatment in patients with type 2 diabetes mellitus.
Dugi, KA; Forst, T; Graefe-Mody, U; Ring, A; Ritzhaupt, A; Uhlig-Laske, B, 2011
)
0.37
" PEG-IFNα was dosed subcutaneously once weekly (initially 6 μg/kg/week, later reduced to 4 μg/kg/week) for 12 weeks."( A phase II trial of gefitinib and pegylated IFNα in previously treated renal cell carcinoma.
Frankel, P; Gandara, DR; Lara, PN; Longmate, J; Margolin, KA; Pan, CX; Quinn, DI; Shek, D; Twardowski, P, 2011
)
0.37
" It shows highly selective, potent, dose-dependent inhibition of DPP-4, with ≥ 80% inhibition of DPP-4 throughout the 24-hour dosing interval."( Linagliptin: in type 2 diabetes mellitus.
Scott, LJ, 2011
)
0.37
" In Study 2, the geometric mean gefitinib steady-state AUC during the 24-h dosing interval was slightly, but not significantly, higher in patients with moderate hepatic impairment; there were, however, no significant differences between groups in gefitinib and metabolite pharmacokinetic parameters."( The effect of different etiologies of hepatic impairment on the pharmacokinetics of gefitinib.
Cantarini, M; Carmichael, J; Harris, AL; Holt, A; Horak, J; Macpherson, M; Swaisland, A; Swaisland, H; Twelves, C; Verrill, M; White, J, 2011
)
0.37
" We applied ImageRail to collect and analyze drug dose-response landscapes in human cell lines at single-cell resolution."( Adaptive informatics for multifactorial and high-content biological data.
Menden, MP; Millard, BL; Muhlich, JL; Niepel, M; Sorger, PK, 2011
)
0.37
" Cediranib was dosed at 3 mg/kg daily five times a week orally for 2 weeks."( Cediranib enhances control of wild type EGFR and EGFRvIII-expressing gliomas through potentiating temozolomide, but not through radiosensitization: implications for the clinic.
Andersen, B; Dicker, AP; Lawrence, RY; Liu, Y; Wachsberger, PR; Xia, X, 2011
)
0.37
"Coadministration of linagliptin did not alter the pharmacokinetics or pharmacodynamics of R- or S-warfarin, indicating that no dosage adjustment for warfarin is necessary when co-administered with linagliptin."( Effect of linagliptin on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers.
Brand, T; Graefe-Mody, EU; Iovino, M; Ring, A; Stangier, J; Withopf, B; Woerle, HJ, 2011
)
0.37
" The number of pain episodes, analgesic dosage and the number of days of spontaneous passage of the calculi through the ureter were also recorded."( Efficacy of three different alpha 1-adrenergic blockers and hyoscine N-butylbromide for distal ureteral stones.
Canat, L; Caskurlu, T; Gurbuz, MC; Kilic, M; Polat, H,
)
0.13
" In this report, it was observed that combined treatment of a low dosage of curcumin (5-10 µM) with a low concentration (0."( Combined treatment of curcumin and small molecule inhibitors suppresses proliferation of A549 and H1299 human non-small-cell lung cancer cells.
Chuu, CP; Kuo, LK; Lin, HP, 2012
)
0.38
" The initial cohort was dosed at 100 mg every other day."( Pharmacokinetics and tolerability of vandetanib in Chinese patients with solid, malignant tumors: an open-label, phase I, rising multiple-dose study.
Guan, Z; Jiang, Y; Li, S; Liao, H; Martin, PD; Smith, R; Zhan, J; Zhang, L; Zhang, Y; Zou, BY, 2011
)
0.37
" Taken together, this non-clinical study shows that lapatinib and capecitabine modulate each other's molecular determinants of response and that concomitant dosing seems to be the optimal way to combine these drugs."( Positive interaction between lapatinib and capecitabine in human breast cancer models: study of molecular determinants.
Chefrour, M; Ciccolini, J; Denden, A; Fischel, JL; Formento, P; Giacometti, S; Iliadis, A; Milano, G; Renée, N, 2012
)
0.38
"The two-stage approach could have been applied safely to define starting doses for alternative dosing strategies with barasertib."( Two-stage model-based design of cancer phase I dose escalation trials: evaluation using the phase I program of barasertib (AZD1152).
Beijnen, JH; Huitema, AD; Keizer, RJ; Schellens, JH; Zandvliet, AS, 2012
)
0.38
" The pharmacokinetic parameters measured were maximum steady-state plasma concentration during a dosage interval (C(max,ss)), time to reach maximum plasma concentration following administration at steady state (t(max,ss)) and area under the plasma concentration-time curve during a dosage interval (τ) at steady state (AUC(τ,ss))."( Effect of multiple oral doses of linagliptin on the steady-state pharmacokinetics of a combination oral contraceptive in healthy female adults: an open-label, two-period, fixed-sequence, multiple-dose study.
Friedrich, C; Giessmann, T; Graefe-Mody, U; Iovino, M; Port, A; Ring, A; Woerle, HJ, 2011
)
0.37
" Because both drugs were developed to target wild-type EGFR, we hypothesized that current dosing schedules were not optimized for mutant EGFR or to prevent resistance."( Optimization of dosing for EGFR-mutant non-small cell lung cancer with evolutionary cancer modeling.
Amato, KR; Arcila, M; Chmielecki, J; de Stanchina, E; Foo, J; Ginsberg, MS; Hutchinson, K; Inoue, A; Kris, MG; Ladanyi, M; Michor, F; Miller, VA; Ohashi, K; Oxnard, GR; Pao, W; Socci, ND; Somwar, R; Sos, ML; Thomas, RK; Viale, A; Wang, L, 2011
)
0.37
"The objective of this study was to determine the relative bioavailability of the dipeptidyl-peptidase-4 (DPP-4) inhibitor linagliptin when administered with and without food, in accordance with regulatory requirements to support dosing recommendations for patients."( A randomized, open-label, crossover study evaluating the effect of food on the relative bioavailability of linagliptin in healthy subjects.
Giessmann, T; Graefe-Mody, U; Iovino, M; Ring, A; Woerle, HJ, 2011
)
0.37
" Plasma samples for pharmacokinetic analysis were collected before dosing and at prespecified time points after dosing."( A randomized, open-label, crossover study evaluating the effect of food on the relative bioavailability of linagliptin in healthy subjects.
Giessmann, T; Graefe-Mody, U; Iovino, M; Ring, A; Woerle, HJ, 2011
)
0.37
" Since adequate drug exposure for inhibition of DPP-4 was still given for the entire 24-hour dosing interval, this result was considered to be of no clinical relevance."( A randomized, open-label, crossover study evaluating the effect of food on the relative bioavailability of linagliptin in healthy subjects.
Giessmann, T; Graefe-Mody, U; Iovino, M; Ring, A; Woerle, HJ, 2011
)
0.37
" Combined dosing with gefitinib and AZ12253801 similarly delayed the onset of symptoms, and at 200 days suppressed small intestinal tumourigenesis more effectively than either treatment alone (median small intestinal adenoma volume (47 mm(3) (comb) vs 248 mm(3) (AZ12253801), P=0."( Dual inhibition of epidermal growth factor and insulin-like 1 growth factor receptors reduce intestinal adenoma burden in the Apc(min/+) mouse.
Clarke, AR; Maughan, TS; Shaw, PH, 2011
)
0.37
"AEB071 combined with a smaller dosage of Tac may be clinically possible to establish calcineurin inhibitor (CNI) minimization protocol in solid organ transplantation."( The effects of AEB071 (sotrastaurin) with tacrolimus on rat heterotopic cardiac allograft rejection and survival.
Fang, YH; Huh, KH; Joo, DJ; Kim, MS; Kim, YS; Lim, BJ; Suh, H, 2011
)
0.37
"A total of 143 patients were randomly assigned to either erlotinib 150 mg daily orally until disease progression (PD) occurred or to chemotherapy with paclitaxel 200 mg/m(2) intravenously (IV) and carboplatin dosed by creatinine clearance (AUC 6) IV on day 1 intercalated with erlotinib 150 mg orally on days 2 through 15 every 3 weeks for four cycles followed by erlotinib 150 mg orally until PD occurred (CT + erlotinib)."( A randomized, phase II, biomarker-selected study comparing erlotinib to erlotinib intercalated with chemotherapy in first-line therapy for advanced non-small-cell lung cancer.
Bunn, PA; Camidge, DR; Camidge, R; Dziadziuszko, R; Eisen, T; Franklin, WA; Hirsch, FR; Kabbinavar, F; Martins, R; Richardson, F; Richardson, K; Rusk, J; Schnell, FM; Sternberg, DW; Varella-Garcia, M; Wacker, B, 2011
)
0.37
"Erlotinib is effective for epidermal growth factor receptor (EGFR) mutant lung cancer, but CNS penetration at standard daily dosing is limited."( "Pulsatile" high-dose weekly erlotinib for CNS metastases from EGFR mutant non-small cell lung cancer.
Clarke, JL; Grommes, C; Holodny, AI; Kris, MG; Lassman, AB; Miller, VA; Oxnard, GR; Pao, W, 2011
)
0.37
"Our group applied mathematical modeling to capecitabine dosing and predicted 7 days of treatment followed by 7 days of rest (7-7) would improve efficacy and minimize toxicity."( Phase II trial of a novel capecitabine dosing schedule in combination with lapatinib for the treatment of patients with HER2-positive metastatic breast cancer.
Chen, C; D'Andrea, G; Drullinsky, P; Feigin, K; Gajria, D; Gonzalez, J; Hudis, CA; Lake, D; Norton, L; Patil, S; Theodoulou, M; Traina, TA, 2012
)
0.38
" Erlotinib was dosed at 150 mg daily, and 5-azacytidine was escalated by increasing the number of daily doses of 75 mg/m(2) per cycle."( A phase I study of 5-azacytidine and erlotinib in advanced solid tumor malignancies.
Bauman, J; Belinsky, S; Fekrazad, M; Jones, D; Lee, SJ; Muller, C; Ravindranathan, M; Rutledge, T; Verschraegen, C, 2012
)
0.38
" Irinotecan dosing started at 50 mg m(-2) and was escalated in patients by 25 mg m(-2) increments up to a maximum dose of 150 mg m(-2)."( Phase I study of irinotecan and gefitinib in patients with gefitinib treatment failure for non-small cell lung cancer.
Horai, T; Horiike, A; Kasahara, K; Kudo, K; Miyauchi, E; Nishio, M; Ohyanagi, F, 2011
)
0.37
"MET gene dosage of the tumor tissues from 208 NSCLC patients was investigated by real time quantitative polymerase chain reaction and compared with molecular and clinical features, including EGFR mutations, KRAS mutations, EGFR gene copy numbers, and patient survivals."( Clinical implications of high MET gene dosage in non-small cell lung cancer patients without previous tyrosine kinase inhibitor treatment.
Chang, JW; Chen, YR; Chen, YT; Chiu, YT; Hsieh, JJ; Huang, SF; Liu, HP; Wu, HD; Yu, TF, 2011
)
0.37
"The proportion of high MET gene dosage was 10."( Clinical implications of high MET gene dosage in non-small cell lung cancer patients without previous tyrosine kinase inhibitor treatment.
Chang, JW; Chen, YR; Chen, YT; Chiu, YT; Hsieh, JJ; Huang, SF; Liu, HP; Wu, HD; Yu, TF, 2011
)
0.37
"High MET gene dosage was not related to primary TKI resistance and the incidence was increased after chemotherapy, suggesting high MET gene dosage may also be related to chemotherapy resistance."( Clinical implications of high MET gene dosage in non-small cell lung cancer patients without previous tyrosine kinase inhibitor treatment.
Chang, JW; Chen, YR; Chen, YT; Chiu, YT; Hsieh, JJ; Huang, SF; Liu, HP; Wu, HD; Yu, TF, 2011
)
0.37
" Adequate monitoring and early intervention are recommended to prevent debilitating toxicity and suboptimal dosing of EGFRI."( The risk of nail changes with epidermal growth factor receptor inhibitors: a systematic review of the literature and meta-analysis.
Garden, BC; Lacouture, ME; Wu, S, 2012
)
0.38
" Since linagliptin is mostly eliminated via the enterohepatic system (80%) and not to a significant extent through renal excretion, dosage adjustment is not necessary in patients with renal impairment."( Linagliptin: the newest dipeptidyl peptidase-4 inhibitor for type 2 diabetes mellitus.
Aletti, R; Cheng-Lai, A,
)
0.13
" In addition, significant oral efficacy was observed in a 14-day BRAF(V600E)-dependent human Colo-205 tumor xenograft mouse model, upon dosing at 30 and 100 mg/kg BID."( Identification of 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea hydrochloride (CEP-32496), a highly potent and orally efficacious inhibitor of V-RAF murine sarcoma viral oncogene homologue B1 (B
Abraham, S; Apuy, JL; Armstrong, RC; Ator, MA; Bhagwat, S; Campbell, BT; Chao, Q; Cramer, MD; Dorsey, BD; Ezawa, M; Faraoni, R; Gardner, MF; Ghose, AK; Gibney, M; Gitnick, D; Gunawardane, RN; Herbertz, T; Holladay, MW; Hua, H; Insko, DE; James, J; Jones-Bolin, S; Lai, AG; Nepomuceno, RR; Rowbottom, MW; Ruggeri, B; Setti, E; Sprankle, KG; Struss, B; Tran, L; Valenta, I; Williams, M, 2012
)
0.38
" was administered on days 1, 8, 15, and erlotinib 150 mg was dosed orally on days 2-7, 9-14, 16-28 of each 28-day cycle."( Phase II trial of erlotinib and docetaxel in advanced and refractory hepatocellular and biliary cancers: Hoosier Oncology Group GI06-101.
Bufill, JA; Chiorean, EG; Coleman, N; Currie, C; Johnston, EL; Loehrer, PJ; Picus, J; Ramasubbaiah, R; Tong, Y; Yu, M, 2012
)
0.38
" Therefore, a potential effect of hepatic impairment on the elimination of linagliptin may have important implications for dosing recommendations."( Pharmacokinetics of linagliptin in subjects with hepatic impairment.
Cinca, R; Graefe-Mody, U; Retlich, S; Ring, A; Rose, P; Waldhauser, L; Woerle, HJ, 2012
)
0.38
"• This study shows that mild, moderate or severe hepatic impairment did not result in an increase in linagliptin exposure after single and multiple dosing as compared with normal hepatic function."( Pharmacokinetics of linagliptin in subjects with hepatic impairment.
Cinca, R; Graefe-Mody, U; Retlich, S; Ring, A; Rose, P; Waldhauser, L; Woerle, HJ, 2012
)
0.38
"Mild, moderate or severe hepatic impairment did not result in an increase in linagliptin exposure after single and multiple dosing compared with normal hepatic function."( Pharmacokinetics of linagliptin in subjects with hepatic impairment.
Cinca, R; Graefe-Mody, U; Retlich, S; Ring, A; Rose, P; Waldhauser, L; Woerle, HJ, 2012
)
0.38
" Bone turnover markers were measured in serum and urine samples collected before dosing on days 1, 2, 3, 17 and 28."( Effects of Src kinase inhibition by saracatinib (AZD0530) on bone turnover in advanced malignancy in a Phase I study.
Baselga, J; Clack, G; Eastell, R; Finkelman, RD; Gossiel, F; Hannon, RA; Iacona, RB; Rimmer, M, 2012
)
0.38
" Of 14 recruited subjects enrolled, nine completed the study (three in each dosage tier)."( Phase I evaluation of intravenous ascorbic acid in combination with gemcitabine and erlotinib in patients with metastatic pancreatic cancer.
Bazzan, AJ; Deshmukh, S; Levine, M; Littman, S; Mitchell, E; Monti, DA; Newberg, AB; Pillai, MV; Yeo, CJ; Zabrecky, G, 2012
)
0.38
" It contrasts with other agents in its class by not requiring dosage adjustment in patients with renal or hepatic impairment."( Pharmacology, efficacy, and safety of linagliptin for the treatment of type 2 diabetes mellitus.
Neumiller, JJ, 2012
)
0.38
" NMS-P937, with its favorable pharmacologic parameters, good oral bioavailability in rodent and nonrodent species, and proven antitumor activity in different preclinical models using a variety of dosing regimens, potentially provides a high degree of flexibility in dosing schedules and warrants investigation in clinical settings."( NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies.
Alli, C; Alzani, R; Avanzi, N; Ballinari, D; Beria, I; Cappella, P; Caruso, M; Casolaro, A; Ciavolella, A; Cucchi, U; De Ponti, A; Felder, E; Fiorentini, F; Galvani, A; Gianellini, LM; Giorgini, ML; Isacchi, A; Lansen, J; Moll, J; Pesenti, E; Rizzi, S; Rocchetti, M; Sola, F; Valsasina, B, 2012
)
0.38
" Scheduling of docetaxel before selumetinib was more beneficial than when selumetinib was dosed before docetaxel and demonstrated a pro-apoptotic phenotype."( The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models.
Alferez, D; Davies, BR; Heaton, SP; Heier, A; Holt, SV; Logié, A; Odedra, R; Smith, PD; Wilkinson, RW, 2012
)
0.38
"From May 2005 to August 2006, 15 patients received a 250 mg/day dosage of gefitinib after having disease progression while taking erlotinib at a dose of 150 mg/day."( The administration of gefitinib in patients with advanced non-small-cell lung cancer after the failure of erlotinib.
Barletta, G; Boldrini, L; Brianti, A; Cosso, M; Dal Bello, MG; Defferrari, C; Fontanini, G; Genova, C; Grossi, F; Murolo, C; Pronzato, P; Rijavec, E; Truini, M, 2012
)
0.38
" For a real data application, our proposed approach is applied to time series data from normal Human lung cells and Human lung cells treated by stimulating EGF-receptors and dosing an anticancer drug termed Gefitinib."( Identifying regulational alterations in gene regulatory networks by state space representation of vector autoregressive models and variational annealing.
Fujita, A; Gotoh, N; Imoto, S; Kojima, K; Miyano, S; Yamaguchi, R; Yamauchi, M, 2012
)
0.38
" On the other hand, the optimal combination and dosage of these drugs, selection of the apropriate biomarker and better understanding of the conflicting role of PDGFR and FGFR signaling in angiogenesis remain future challenges."( [Possibilities for inhibiting tumor-induced angiogenesis: results with multi-target tyrosine kinase inhibitors].
Döme, B; Török, S, 2012
)
0.38
" We demonstrate that dasatinib plus erlotinib can be safely co-administered on a continuous, daily dosing schedule with erlotinib, and established the recommended dose level of this combination."( Phase 1 trial of dasatinib plus erlotinib in adults with recurrent malignant glioma.
Coan, A; Desjardins, A; Friedman, HS; Herndon, JE; McLendon, RE; McSherry, F; Peters, KB; Reardon, DA; Rich, JN; Sampson, JH; Sathornsumetee, S; Threatt, S; Vredenburgh, JJ; Zhang, S, 2012
)
0.38
" Patients received continuous once-daily oral dosing with saracatinib starting 7 days after a single dose in ascending dose cohorts until dose-limiting toxicity (DLT) or disease progression."( First report of the safety, tolerability, and pharmacokinetics of the Src kinase inhibitor saracatinib (AZD0530) in Japanese patients with advanced solid tumours.
Boku, N; Fujisaka, Y; Goto, I; Kurata, T; Machida, N; Onozawa, Y; Shi, X; Shimada, H; Watanabe, J; Yamazaki, K; Yasui, H, 2013
)
0.39
"The purpose of this article is to review the pharmacology, pharmacokinetic properties, efficacy, tolerability including drug-drug interactions, contraindications/precautions, and dosage and administration of linagliptin, and the potential role of linagliptin in the management of glycemia in adults with T2DM."( Review of linagliptin for the treatment of type 2 diabetes mellitus.
Neumiller, JJ; Setter, SM, 2012
)
0.38
" Dosage adjustments based on renal or hepatic function are not required."( Review of linagliptin for the treatment of type 2 diabetes mellitus.
Neumiller, JJ; Setter, SM, 2012
)
0.38
" Dosage adjustment of linagliptin is not required in patients with renal impairment."( Review of linagliptin for the treatment of type 2 diabetes mellitus.
Neumiller, JJ; Setter, SM, 2012
)
0.38
" Follow-up dose-response studies revealed that 12 of the 13 known EGFR inhibitors in the library were confirmed as hits."( A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery.
Antczak, C; Bhinder, B; Calder, PA; Djaballah, H; Mahida, JP, 2012
)
0.38
" This study aimed to establish the recommended dosing of the erlotinib and pertuzumab combination; assess safety, preliminary efficacy, and pharmacokinetics; and analyze biomarkers."( A phase Ib, dose-finding study of erlotinib in combination with a fixed dose of pertuzumab in patients with advanced non-small-cell lung cancer.
Brewster, M; Cedrés, S; Dean, E; Felip, E; Galdermans, D; Martínez, P; McNally, V; Ranson, M; Ross, G, 2012
)
0.38
"The purpose of this study was to determine the maximum-tolerated dose (MTD), pharmacokinetics and safety profile for two different dosing regimens of barasertib, a selective inhibitor of Aurora B Kinase."( Phase I study of barasertib (AZD1152), a selective inhibitor of Aurora B kinase, in patients with advanced solid tumors.
Ataman, O; Carvajal, RD; Das, S; Midgley, R; Rodig, SJ; Schwartz, GK; Shapiro, GI; Stockman, PK; Wilson, D, 2013
)
0.39
"Vandetanib (an orally bioavailable VEGFR-2 and EGFR tyrosine kinases inhibitor) was combined at 100 mg, 200 mg, or 300 mg daily with standard dosed cetuximab and irinotecan (3+3 dose-escalation design)."( Phase I study of cetuximab, irinotecan, and vandetanib (ZD6474) as therapy for patients with previously treated metastastic colorectal cancer.
Abrams, TA; Ancukiewicz, M; Blaszkowsky, L; Chan, JA; Duda, DG; Elliott, M; Enzinger, PC; Goldstein, M; Jain, RK; Kulke, MH; Meyerhardt, JA; Regan, E; Schrag, D; Wolpin, BM; Zhu, AX, 2012
)
0.38
" The large (n=331), randomized, double-blind, multinational ZETA trial compared vandetanib at a dosage of 300 mg once daily with placebo in patients with unresectable, locally advanced or metastatic, hereditary or sporadic, medullary thyroid cancer."( Vandetanib: in medullary thyroid cancer.
Frampton, JE, 2012
)
0.38
" Two dosing schedules were evaluated; in the "intermittent 5 & 9 dosing" cohort, XL647 350 mg for 5 days every 14 days was given; and in the "daily dosing" cohort, XL647 300 mg daily for 28 days was administered."( Phase II study of the multitargeted tyrosine kinase inhibitor XL647 in patients with non-small-cell lung cancer.
Azzoli, CG; Beumer, JH; Dowlati, A; Gadgeel, SM; Kris, MG; Krug, LM; Lynch, TJ; Miller, VA; Mitchell, B; Pietanza, MC; Price, KA; Riely, GJ; Rizvi, NA; Rowland, KM; Salgia, R; Tonda, M; Wertheim, MS, 2012
)
0.38
" The adverse-event profile was similar for the two dosing schedules."( Phase II study of the multitargeted tyrosine kinase inhibitor XL647 in patients with non-small-cell lung cancer.
Azzoli, CG; Beumer, JH; Dowlati, A; Gadgeel, SM; Kris, MG; Krug, LM; Lynch, TJ; Miller, VA; Mitchell, B; Pietanza, MC; Price, KA; Riely, GJ; Rizvi, NA; Rowland, KM; Salgia, R; Tonda, M; Wertheim, MS, 2012
)
0.38
"A dosage of sunitinib 37."( Sunitinib plus erlotinib for the treatment of advanced/metastatic non-small-cell lung cancer: a lead-in study.
Blumenschein, GR; Chao, RC; Ciuleanu, T; Groen, HJ; Juhasz, E; Robert, F; Ruiz-Garcia, A; Tye, L; Usari, T, 2012
)
0.38
"Multiparticulate floating drug delivery systems have proven potential as controlled-release gastroretentive drug delivery systems that avoid the "all or none" gastric emptying nature of single-unit floating dosage forms."( Statistical approach for assessing the influence of calcium silicate and HPMC on the formulation of novel alfuzosin hydrochloride mucoadhesive-floating beads as gastroretentive drug delivery systems.
Fahmy, RH, 2012
)
0.38
"5 mg twice-daily dosing of linagliptin has comparable efficacy and safety to 5 mg once-daily dosing when given in addition to metformin twice daily in patients with inadequate glycaemic control."( Efficacy and safety of linagliptin 2.5 mg twice daily versus 5 mg once daily in patients with type 2 diabetes inadequately controlled on metformin: a randomised, double-blind, placebo-controlled trial.
Meinicke, T; Rafeiro, E; Ross, SA; Toorawa, R; Weber-Born, S; Woerle, HJ, 2012
)
0.38
" Low solubility of BAT in water, high toxicity and necessity of high drug dosing are major limitations of its use as a chemotherapeutic drug."( Novel approaches in the synthesis of batracylin and its analogs: rebirth of an old player?
Dzierzbicka, K; Januchta, W; Skladanowski, A, 2012
)
0.38
" Initial cediranib dosing was 45 mg daily during a 28-day cycle."( Cediranib in patients with malignant mesothelioma: a phase II trial of the University of Chicago Phase II Consortium.
Agamah, E; Campbell, NP; Gandara, DR; Gitlitz, BJ; Kindler, HL; Koczywas, M; Kunnavakkam, R; Leighl, N; Stadler, WM; Thomas, SP; Vincent, MD; Vokes, EE, 2012
)
0.38
"The PK profile of barasertib is similar to previous studies using the same dosing regimen in patients with AML."( Phase I study of the Aurora B kinase inhibitor barasertib (AZD1152) to assess the pharmacokinetics, metabolism and excretion in patients with acute myeloid leukemia.
D'Souza, R; Davies, M; Dennis, M; Oliver, S; Pike, L; Stockman, P, 2012
)
0.38
" Additional trials and subgroup analyses of pooled data suggest that linagliptin improves glycaemic control regardless of factors such as age, duration of type 2 diabetes, ethnicity and renal function, and as linagliptin is eliminated primarily via a nonrenal route, it can be used without dosage adjustment in patients with renal impairment of any degree."( Linagliptin: a review of its use in the management of type 2 diabetes mellitus.
Deeks, ED, 2012
)
0.38
"To ascertain the role of patient age as an influencing factor in the pharmacokinetics of anagrelide and to clarify whether different dosing is required in young (18 - 50 years) vs."( Pharmacokinetics and tolerability of anagrelide hydrochloride in young (18 - 50 years) and elderly (≥ 65 years) patients with essential thrombocythemia.
Alvarez-Larrán, A; Besses, C; Coll, R; Freitag, C; Martin, P; Purkayastha, J; Troy, S; Zeller, W, 2012
)
0.38
" Three days prior to pharmacokinetic assessment, patients divided their normal daily anagrelide into a structured twice-daily dosing (BID) schedule."( Pharmacokinetics and tolerability of anagrelide hydrochloride in young (18 - 50 years) and elderly (≥ 65 years) patients with essential thrombocythemia.
Alvarez-Larrán, A; Besses, C; Coll, R; Freitag, C; Martin, P; Purkayastha, J; Troy, S; Zeller, W, 2012
)
0.38
"To conclude, the differences observed in anagrelide and 3-hydroxy-anagrelide pharmacokinetics do not justify using a different dosing regimen in young vs."( Pharmacokinetics and tolerability of anagrelide hydrochloride in young (18 - 50 years) and elderly (≥ 65 years) patients with essential thrombocythemia.
Alvarez-Larrán, A; Besses, C; Coll, R; Freitag, C; Martin, P; Purkayastha, J; Troy, S; Zeller, W, 2012
)
0.38
" Assuming no dose limiting toxicities were observed, dosage was maintained at 150 mg BID for 10 more cycles."( Phase I/II study of oral erlotinib for treatment of relapsed/refractory glioblastoma multiforme and anaplastic astrocytoma.
Boockvar, JA; Christos, P; Kaplan, R; Kesavabhotla, K; Lavi, E; Mubita, L; Pannullo, SC; Scheff, R; Schlaff, CD; Shin, B; Tsiouris, AJ, 2012
)
0.38
" The lack of direct comparison PFS and treatment dosage modification data were the main limitations."( Budget impact analysis of the use of oral and intravenous anti-cancer drugs for the treatment of HER2-positive metastatic breast cancer.
Benjamin, L; Buthion, V; Farah, B; Iskedjian, M; Rioufol, C; Vidal-Trécan, G, 2013
)
0.39
"We used mathematical modeling and available clinical trial data to predict how different pharmacokinetic parameters (fast versus slow metabolism) and dosing schedules (low dose versus high dose; missed doses with and without make-up doses) might affect the evolution of T790M-mediated resistance in mixed populations of tumor cells."( Effects of pharmacokinetic processes and varied dosing schedules on the dynamics of acquired resistance to erlotinib in EGFR-mutant lung cancer.
Chmielecki, J; Foo, J; Michor, F; Pao, W, 2012
)
0.38
"For existing and new kinase inhibitors, this novel framework can be used to rationally and rapidly design optimal dosing strategies to minimize the development of acquired resistance."( Effects of pharmacokinetic processes and varied dosing schedules on the dynamics of acquired resistance to erlotinib in EGFR-mutant lung cancer.
Chmielecki, J; Foo, J; Michor, F; Pao, W, 2012
)
0.38
" Animals were then dosed with vehicle or linagliptin (3 mg/kg PO) orally once-daily for a 28 day period."( Effects of the DPP-4 inhibitor, linagliptin, in diet-induced obese rats: a comparison in naive and exenatide-treated animals.
Birmingham, GD; Cheetham, SC; Dickinson, K; Grempler, R; Headland, KR; Hocher, B; Klein, T; Mark, M; Rowley, HL; Vickers, SP, 2012
)
0.38
" Similar dose-response lapatinib experiments were conducted with varying concentrations of 5-FU or GEM and isobolograms were constructed to evaluate therapeutic synergy."( Dual ErbB1 and ErbB2 receptor tyrosine kinase inhibition exerts synergistic effect with conventional chemotherapy in pancreatic cancer.
Drebin, JA; Pippin, JA; Singla, S, 2012
)
0.38
" Multiple dosing levels were studied, combining pazopanib up to 800 mg/day with lapatinib up to 1,500 mg/day."( Phase I and pharmacokinetic study of pazopanib and lapatinib combination therapy in patients with advanced solid tumors.
Arumugham, T; de Jonge, MJ; Hamberg, P; Hodge, J; Hurwitz, HI; Pandite, LN; Savage, S; Suttle, AB; Verweij, J, 2013
)
0.39
" Thirty-two patients with recurrent glioblastoma multiforme (GBM) and 32 patients with recurrent anaplastic gliomas (AGs) were treated in the phase II trial, at a dosage of 300 mg/day on 28-day cycles."( A phase I/II trial of vandetanib for patients with recurrent malignant glioma.
Fine, HA; Iwamoto, FM; Kreisl, TN; McNeill, KA; Shih, J; Sul, J, 2012
)
0.38
"Patients with advanced solid tumors received three weekly AVE1642 dosed at 6 mg/kg, chosen following previous study, with 75 (cohort A) or 100 mg/m(2) (B) docetaxel, 1250 mg/m(2) gemcitabine/100 mg erlotinib (C1), or 60 mg/m(2) doxorubicin (D1)."( Phase I study of humanized monoclonal antibody AVE1642 directed against the type 1 insulin-like growth factor receptor (IGF-1R), administered in combination with anticancer therapies to patients with advanced solid tumors.
Bahleda, R; Blay, JY; Dieras, V; LoRusso, P; Macaulay, VM; Mery-Mignard, D; Middleton, MR; Protheroe, AS; Sessa, C; Soria, JC; Tolcher, A, 2013
)
0.39
" Double dosage of gefitinib (500 mg per day) together with pemetrexed were given as the second-line therapy after the patient developed new brain lesions and leptomeningeal metastasis during the maintenance therapy of gefitinib."( Activity of pemetrexed and high-dose gefitinib in an EGFR-mutated lung adenocarcinoma with brain and leptomeningeal metastasis after response to gefitinib.
Fang, X; Hu, Y; Li, M; Ma, S; Shen, H; Tan, C; Yuan, Y, 2012
)
0.38
"Twenty-three patients received oral saracatanib on a continuous daily dosing regimen."( Phase II study of the Src kinase inhibitor saracatinib (AZD0530) in metastatic melanoma.
Clark, JI; Gajewski, TF; Gangadhar, TC; Karrison, T, 2013
)
0.39
"A Phase I study to determine the maximum tolerated dose (MTD) and pharmacokinetics of afatinib (BIBW 2992), a novel irreversible ErbB Family Blocker, administered orally once daily in a 3-week-on/1-week-off dosing schedule."( A Phase I, open-label, dose escalation study of afatinib, in a 3-week-on/1-week-off schedule in patients with advanced solid tumors.
Burger, H; Cohen, RB; Eskens, FA; Hwang, J; Lewis, NL; Malik, S; Marshall, J; Ould-Kaci, M; Stopfer, P; Uttenreuther-Fischer, M, 2013
)
0.39
"To increase knowledge about lung tumor tissue levels of erlotinib and its primary active metabolite, and about erlotinib plasma levels in intercalated dosing schedules, a sensitive and accurate method for determination of erlotinib and O-desmethyl erlotinib (OSI-420) in human plasma and lung tumor tissue has been developed."( Quantitative determination of erlotinib and O-desmethyl erlotinib in human EDTA plasma and lung tumor tissue.
Beijnen, JH; Burgers, JA; Huitema, AD; Lankheet, NA; Rosing, H; Schaake, EE; Schellens, JH, 2012
)
0.38
" In this phase I, open-label, parallel-group study, adults with advanced solid tumours received a single 45 mg dose of cediranib, followed by 30 mg continuous once-daily oral dosing for 21 days after a 7-day washout period (clinicaltrials."( Pharmacokinetics and tolerability of cediranib, a potent VEGF signalling inhibitor, in cancer patients with hepatic impairment.
Brown, KH; de Jonge, MJ; Desar, IM; Lassen, U; Marotti, M; van Herpen, CM, 2013
)
0.39
" Two compounds exhibiting suitable mouse PK were profiled in in vivo tumor models and were shown to suppress mTORC1 and mTORC2 signaling for over 12 h when dosed orally."( Potent, selective, and orally bioavailable inhibitors of the mammalian target of rapamycin kinase domain exhibiting single agent antiproliferative activity.
Bergeron, P; Blackwood, E; Bowman, KK; Chen, YH; Deshmukh, G; Ding, X; Epler, J; Koehler, MF; Lau, K; Lee, L; Liu, L; Ly, C; Lyssikatos, JP; Malek, S; Nonomiya, J; Oeh, J; Ortwine, DF; Pei, Z; Sampath, D; Sideris, S; Trinh, L; Truong, T; Wu, J, 2012
)
0.38
" However, these inhibitors have yet to prove clinically efficacious, and their toxicity in skin, reflecting activity against wild-type EGFR, may limit dosing required to effectively suppress EGFR T790M in vivo."( Noncovalent wild-type-sparing inhibitors of EGFR T790M.
Chan, E; Heffron, TP; La, H; Lee, HJ; Malek, S; Merchant, M; Pirazzoli, V; Politi, K; Schaefer, G; Settleman, J; Shao, L; Sideris, S; Ubhayakar, S; Yauch, RL; Ye, X, 2013
)
0.39
" On detection of epidermal growth factor receptor(EGFR)mutations, we administered gefitinib, an EGFR tyrosine kinase inhibitor, at a dosage of 250 mg daily."( [Efficacy of low-dose erlotinib against gefitinib-induced hepatotoxicity in a patient with lung adenocarcinoma harboring EGFR mutations].
Hokkoku, K; Igarashi, S; Kitade, H; Mori, M; Nakai, M; Sagawa, M; Shintaku, K; Yamada, T; Yano, S, 2013
)
0.39
" We intended to identify the optimum dosage of anagrelide in treatment-naïve Japanese patients with ET and assess its long-term safety and efficacy."( Open-label, dose-titration and continuation study to assess efficacy, safety, and pharmacokinetics of anagrelide in treatment-naïve Japanese patients with essential thrombocythemia.
Abhyankar, B; Hodgson, I; Kanakura, Y; Miyakawa, Y; Okamoto, S; Smith, J; Troy, S, 2013
)
0.39
" Although daily dosing with erlotinib is effective, weekly dosing may reduce toxicity and have advantages, particularly for prevention."( Effect of intermittent dosing regimens of erlotinib on methylnitrosourea-induced mammary carcinogenesis.
Bode, A; Gill, SC; Grubbs, CJ; Iwata, KK; Juliana, MM; Lubet, RA; Nicastro, HL; Steele, VE; Szabo, E; Tucker, C, 2013
)
0.39
" The optimum dosing combination of these two agents has yet to be determined however, and in many patients it is likely that greater overall survival will be achieved by using them in successive lines rather than in combination."( New oxaliplatin-based combinations in the treatment of colorectal cancer.
Cassidy, J; Hochster, H, 2003
)
0.32
"Patients received AZD8931 as a single oral dose followed by 4 days of observation, then twice-daily dosing for 21 consecutive days."( Phase I, dose-finding study of AZD8931, an inhibitor of EGFR (erbB1), HER2 (erbB2) and HER3 (erbB3) signaling, in patients with advanced solid tumors.
Keilholz, U; Learoyd, M; Manikhas, G; Moiseyenko, V; Saunders, A; Semiglazov, V; Stuart, M; Tjulandin, S, 2014
)
0.4
" However, frequent repeated dosing is required, and hepatic and cardiac adverse events may occur."( A phase II, randomized, double-blind, placebo-controlled, parallel group, dose-ranging study to investigate the efficacy and safety of 4 dose regimens of oral albaconazole in patients with distal subungual onychomycosis.
Malahias, S; Raterink, K; Sigurgeirsson, B; van Rossem, K, 2013
)
0.39
" In 2B/- SMA mice, RG3039 provided a >600% survival benefit (median 18 days to >112 days) when dosing began at P4, highlighting the importance of early intervention."( The DcpS inhibitor RG3039 improves survival, function and motor unit pathologies in two SMA mouse models.
Bail, S; Barlow, C; Cardona, H; DiDonato, CJ; Durens, M; Emery, C; Gogliotti, RG; Heier, CR; Jacques, V; Jarecki, J; Jorgensen, M; Kiledjian, M; Kuntz, N; Plasterer, HL; Rusche, J; Singh, J; Xia, B, 2013
)
0.39
" However, linagliptin is the first DPP-4 inhibitor to be approved as a once-daily, 5-mg dose and, due to its primarily non-renal route of excretion, no dosage adjustment is required for patients with renal or hepatic impairment."( Clinical utility of the dipeptidyl peptidase-4 inhibitor linagliptin.
Grunberger, G, 2013
)
0.39
" The approved dosage is 250 mg/body/day without adjustment for physical size such as body surface area (BSA), and the impact of physical size on the efficacy of gefitinib has not been evaluated."( Impact of physical size on gefitinib efficacy in patients with non-small cell lung cancer harboring EGFR mutations.
Hayakawa, H; Honda, Y; Hotta, K; Ichihara, E; Kato, Y; Kiura, K; Kudo, K; Minami, D; Sato, A; Tabata, M; Takigawa, N; Tanimoto, M, 2013
)
0.39
" We investigated the toxicities and recommended phase 2 dosing (RP2D) of the combination of cediranib, a multitargeted inhibitor of vascular endothelial growth factor receptor (VEGFR)-1/2/3 and olaparib, a PARP-inhibitor (NCT01116648)."( A Phase 1 trial of the poly(ADP-ribose) polymerase inhibitor olaparib (AZD2281) in combination with the anti-angiogenic cediranib (AZD2171) in recurrent epithelial ovarian or triple-negative breast cancer.
Birrer, M; Buss, MK; Dahlberg, SE; Fleming, GF; Ivy, P; Lee, H; Liu, JF; Matulonis, UA; Tolaney, SM; Tyburski, K; Whalen, C; Winer, E, 2013
)
0.39
" Maximum plasma concentration (C(max)) values were achieved 2-5 h after dosing and thereafter declined at least bi-exponentially."( Pharmacokinetics of afatinib, a selective irreversible ErbB family blocker, in patients with advanced solid tumours.
Erhardt, J; Goeldner, RG; Schmid, M; Stopfer, P; Wind, S, 2013
)
0.39
"The pharmacokinetic profile of afatinib supports a once-daily dosage regimen."( Pharmacokinetics of afatinib, a selective irreversible ErbB family blocker, in patients with advanced solid tumours.
Erhardt, J; Goeldner, RG; Schmid, M; Stopfer, P; Wind, S, 2013
)
0.39
"Based on the convenient oral dosing of erlotinib and the promising results of biologic therapy, we undertook a phase II study with 21 patients with locally advanced (T3-4) lesions combining radiation with intra-arterial (IA) cisplatin and oral daily erlotinib for a 7-week therapy."( A phase II study of intra-arterial cisplatin with concurrent radiation and erlotinib for locally advanced head and neck cancer.
Chalasani, P; Clausen, C; Dhiwakar, M; Kalapurakal, S; Malone, J; Rao, K; Robbins, KT; Robinson, K; Ronen, O; Shevlin, B, 2013
)
0.39
" Despite the slightly faster clearance compared with typical bivalent mAbs, the PK of onartuzumab support dosing regimens of 15 mg/kg every 3 weeks or doses equivalent to achieve the target minimum tumoristatic concentration in patients."( Population pharmacokinetic analysis from phase I and phase II studies of the humanized monovalent antibody, onartuzumab (MetMAb), in patients with advanced solid tumors.
Bai, S; Bothos, J; Damico-Beyer, LA; Davis, JD; Eppler, S; Jin, D; Joshi, A; Kaur, S; Nijem, I; Patel, P; Peterson, A; Xin, Y, 2013
)
0.39
" Further clinical evaluation is warranted to investigate whether a low dosage of these antifolates can elicit immunosuppressive effects equivalent to MTX, and whether they are superior to MTX in patients who fail to respond to MTX."( Methotrexate analogues display enhanced inhibition of TNF-α production in whole blood from RA patients.
Assaraf, YG; Dijkmans, BA; Gerards, AH; Jansen, G; Lems, WF; Oerlemans, R; Scheper, RJ; van der Heijden, JW, 2014
)
0.4
" Hypertensive animals entered a 16-week dosing period."( Effects of telmisartan and linagliptin when used in combination on blood pressure and oxidative stress in rats with 2-kidney-1-clip hypertension.
Alter, ML; Chaykovska, L; Hocher, B; Hohmann, M; Klein, T; Kraft, R; Kutil, B; Reichetzeder, C; Tsuprykov, O; von Websky, K, 2013
)
0.39
"The pharmacokinetic/pharmacodynamic properties of erlotinib in a human tumor xenograft model were described by the indirect response model and integrated model, which will be helpful in understanding the detailed processes of erlotinib activity and determining an appropriate dosing regimen in clinical studies."( Pharmacokinetic-pharmacodynamic modeling of the anticancer effect of erlotinib in a human non-small cell lung cancer xenograft mouse model.
Deng, CH; Li, HQ; Li, L; Li, MY; Lu, W; Wu, Q; Zhou, TY, 2013
)
0.39
"5 mg twice-daily provided bioequivalent exposure and similar inhibition of dipeptidyl peptidase-4 over the whole dosing interval."( Bioequivalence of Linagliptin 5 mg once daily and 2.5 mg twice daily: pharmacokinetics and pharmacodynamics in an open-label crossover trial.
Friedrich, C; Jungnik, A; Meinicke, T; Retlich, S; Ring, A, 2014
)
0.4
"Because of the complexity derived from the existence of various phosphoinositide 3-kinase (PI3K) isoforms and their differential roles in cancers, development of PI3K inhibitors with differential pharmacologic and pharmacokinetic profiles would allow best exploration in different indications, combinations, and dosing regimens."( BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110α and p110δ activities in tumor cell lines and xenograft models.
Bull, CO; Fracasso, PR; Haegebarth, A; Hentemann, M; Liu, N; Mumberg, D; Rowley, BR; Schatz, CA; Schneider, C; Scott, WJ; Wilhelm, SM; Wilkie, DP; Ziegelbauer, K, 2013
)
0.39
" The convenient, once-daily dosing does not need adjustment in patients with hepatic and/or renal impairment."( Linagliptin as add-on therapy to insulin for patients with type 2 diabetes.
Hocher, B; Reichetzeder, C; von Websky, K, 2013
)
0.39
" This allows the usage of p110α-specific PI3K inhibitors and thus may spare patients the toxicities of pan-PI3K inhibition to allow maximal dosage and efficacy."( Enhanced PI3K p110α signaling confers acquired lapatinib resistance that can be effectively reversed by a p110α-selective PI3K inhibitor.
Brady, SW; Seok, D; Wang, H; Yu, D; Zhang, J, 2014
)
0.4
" The method was successfully applied to pharmacokinetic study of CUDC-101 after intravenous administration of single dosage 5 mg/kg in rats."( Determination of CUDC-101 in rat plasma by liquid chromatography mass spectrometry and its application to a pharmacokinetic study.
Ma, J; Wang, X; Wen, C; Xiang, Z; Zhang, Q, 2014
)
0.4
"These findings suggest that the pharmacokinetics and metabolism of erlotinib are related to skin toxicity and may support further studies where erlotinib dosing is tailored according to pharmacokinetic parameters."( Correlation between erlotinib pharmacokinetics, cutaneous toxicity and clinical outcomes in patients with advanced non-small cell lung cancer (NSCLC).
Andreoli, R; Ardizzoni, A; Azzoni, C; Bartolotti, M; Bortesi, B; De Palma, G; Gelsomino, F; Goldoni, M; Mozzoni, P; Mutti, A; Silini, EM; Tiseo, M, 2014
)
0.4
" Twelve phase I patients treated at the maximum tolerated dosage were included in the phase II cohort for analysis."( Phase I/II study of erlotinib and temsirolimus for patients with recurrent malignant gliomas: North American Brain Tumor Consortium trial 04-02.
Aldape, KD; Chang, SM; Cloughesy, TF; Dancey, J; Drappatz, J; Gilbert, MR; Groves, MD; Kuhn, JG; Lamborn, KR; Lieberman, FS; Ligon, AH; Ligon, KL; Mehta, MP; Norden, AD; Prados, MD; Robins, HI; Santagata, S; Wen, PY; Wright, JJ; Yung, WK, 2014
)
0.4
"Because of increased toxicity, the maximum tolerated dosage of temsirolimus in combination with erlotinib proved lower than expected."( Phase I/II study of erlotinib and temsirolimus for patients with recurrent malignant gliomas: North American Brain Tumor Consortium trial 04-02.
Aldape, KD; Chang, SM; Cloughesy, TF; Dancey, J; Drappatz, J; Gilbert, MR; Groves, MD; Kuhn, JG; Lamborn, KR; Lieberman, FS; Ligon, AH; Ligon, KL; Mehta, MP; Norden, AD; Prados, MD; Robins, HI; Santagata, S; Wen, PY; Wright, JJ; Yung, WK, 2014
)
0.4
"Erlotinib exposure (AUC0-∞ and C max) was reduced after pre- or concomitant dosing with rifampicin."( The effect of rifampicin, a prototypical CYP3A4 inducer, on erlotinib pharmacokinetics in healthy subjects.
Drolet, DW; Fettner, SH; Hamilton, M; Lum, BL; Rakhit, AK; Witt, K; Wolf, JL, 2014
)
0.4
" After dosing 400 mg of Icotinib with high-fat and high-calorie meal, mean Cmax and AUC were significantly increased by 59 and 79 %, respectively."( Clinical pharmacokinetics of Icotinib, an anti-cancer drug: evaluation of dose proportionality, food effect, and tolerability in healthy subjects.
Hu, P; Jiang, J; Liu, D; Tan, F; Wang, Y; Zhang, D; Zhang, L, 2014
)
0.4
" Plasma concentration-time data for up to 7 months dosing were analyzed using nonlinear mixed-effects modeling."( Population pharmacokinetics of afatinib, an irreversible ErbB family blocker, in patients with various solid tumors.
Fleury, A; Freiwald, M; Schmid, U; Staab, A; Stopfer, P; Wind, S, 2014
)
0.4
" Male Zucker Diabetic Fatty (ZDF) rats were dosed for 3 days, fasted overnight and a sucrose/glucose tolerance test was performed."( Effect of linagliptin, alone and in combination with voglibose or exendin-4, on glucose control in male ZDF rats.
Cheetham, SC; Headland, KR; Jones, RB; Klein, T; Mark, M; Vickers, SP, 2014
)
0.4
" Testing of biological activity revealed limited potential for resistance to these agents, low toxicity, and highly effective in vivo activity, even with low dosing regimens."( Antibacterial activity of a series of N2,N4-disubstituted quinazoline-2,4-diamines.
Burda, WN; Fleeman, R; Manetsch, R; Shaw, LN; Van Horn, KS, 2014
)
0.4
"Cigarette smoking dosage of ≥ 30 pack-years is an independent negative predictive factor of EGFR-TKI treatment outcome in lung adenocarcinoma patients with activating EGFR mutations."( Impact of cigarette smoking on response to epidermal growth factor receptor (EGFR)-tyrosine kinase inhibitors in lung adenocarcinoma with activating EGFR mutations.
Bae, MK; Cho, BC; Kang, DR; Kim, EY; Kim, HR; Kim, JH; Kim, MH; Lee, CY; Lee, JS, 2014
)
0.4
" The VEGF signal inhibitors significantly elevated blood pressure (BP) in rats within a few days of the initiation of dosing, and levels recovered after dosing ended."( Estimating the clinical risk of hypertension from VEGF signal inhibitors by a non-clinical approach using telemetered rats.
Honda, M; Isobe, T; Komatsu, R; Kuramoto, S; Shindoh, H; Tabo, M, 2014
)
0.4
" donovani in the BALB/c mouse model of infection; dosing on days 7-11 with a 50 mg/kg oral dose of sunitinib, lapatinib or sorafenib reduced liver amastigote burdens by 41%, 36% and 30%, respectively, compared with untreated control mice."( Activity of anti-cancer protein kinase inhibitors against Leishmania spp.
Croft, SL; Sanderson, L; Yardley, V, 2014
)
0.4
" Lapatinib dose was escalated to 7,000 mg per day in twice-daily dosing with no DLTs; however, plasma lapatinib concentrations plateaued in this dose range."( Phase I dose-escalation study of 5-day intermittent oral lapatinib therapy in patients with human epidermal growth factor receptor 2-overexpressing breast cancer.
Auerback, G; Chien, AJ; Goga, A; Khanafshar, E; Koch, KM; Melisko, ME; Moasser, MM; Munster, PN; Ordovas, K; Park, JW; Rugo, HS, 2014
)
0.4
"Lapatinib exposure can be safely and significantly increased through intermittent dosing but reaches a ceiling that currently impedes clinical translation of the treatment hypothesis."( Phase I dose-escalation study of 5-day intermittent oral lapatinib therapy in patients with human epidermal growth factor receptor 2-overexpressing breast cancer.
Auerback, G; Chien, AJ; Goga, A; Khanafshar, E; Koch, KM; Melisko, ME; Moasser, MM; Munster, PN; Ordovas, K; Park, JW; Rugo, HS, 2014
)
0.4
" The median time from dosing to the maximum concentration of linagliptin in plasma (t(max)) was similar under both conditions."( Effect of food and tablet-dissolution characteristics on the bioavailability of linagliptin fixed-dose combination with metformin: evidence from two randomized trials.
Friedrich, C; Hohl, K; Jungnik, A; Meinicke, T; Metzmann, K; Ring, A; Schnell, D; Theodor, R, 2014
)
0.4
" Low incidence of toxicity and low erlotinib exposure suggest standardized and maximum-allowable dosing may be suboptimal in African Americans."( Erlotinib in African Americans with advanced non-small cell lung cancer: a prospective randomized study with genetic and pharmacokinetic analyses.
Aimiuwu, J; Blachly, JS; Gao, Y; Hicks, WJ; Li, J; Otterson, GA; Papp, A; Phelps, MA; Poi, M; Schaaf, LJ; Socinski, MA; Starrett, SL; Stinchcombe, TE; Villalona-Calero, MA; Wang, D; Wei, L; Zhao, W, 2014
)
0.4
" PI4KIIα knockdown greatly prolonged the effects and decreased the effective dosage of AG-1478, a specific inhibitor of EGFR."( Dual inhibition of EGFR at protein and activity level via combinatorial blocking of PI4KIIα as anti-tumor strategy.
Chen, C; Gao, Z; Kang, H; Li, J; Rong, G; Zhang, L; Zhang, X, 2014
)
0.4
"Erlotinib is currently marketed at fixed standard dosage against pancreatic cancer and non-small-cell lung carcinoma."( Erlotinib: another candidate for the therapeutic drug monitoring of targeted therapy of cancer? A pharmacokinetic and pharmacodynamic systematic review of literature.
Buclin, T; Decosterd, LA; Gairard-Dory, AC; Gourieux, B; Guidi, M; Petit-Jean, E; Quoix, E; Ubeaud-Séquier, G; Widmer, N, 2015
)
0.42
"2% of the patients developed side effects resulting in dosage reductions."( Chemotherapy for advanced pancreatic adenocarcinoma in elderly patients (≥70 years of age): a retrospective cohort study at the National Center for Tumor Diseases Heidelberg.
Abel, U; Berger, AK; Harig, S; Jäger, D; Komander, C; Springfeld, C,
)
0.13
" To investigate the antitumor effect of erlotinib at different dosing times and the underlying molecular mechanism via the PI3K/AKT pathway, we established a mouse model of Lewis lung cancer xenografts."( Chronopharmacology and mechanism of antitumor effect of erlotinib in Lewis tumor-bearing mice.
An, F; Li, M; Lin, P; Liu, J; Liu, L; Wang, P; Zhang, B; Zhao, L; Zhuang, X, 2014
)
0.4
" With a therapeutic dosing regimen in which mice were fed Western diet for 10 weeks to develop lesions followed by switching to a low fat diet and concurrent treatment with RVX-208 for 14 weeks, RVX-208 similarly reduced lesion formation by 39% in the whole aorta without significant changes in the plasma lipid parameters."( A novel BET bromodomain inhibitor, RVX-208, shows reduction of atherosclerosis in hyperlipidemic ApoE deficient mice.
Attwell, S; Azhar, S; Hansen, HC; Jahagirdar, R; Johansson, J; McLure, KG; Srivastava, RA; Tobin, J; Wagner, GS; Wong, NC; Wu, J; Young, PR; Yu, R; Zhang, H, 2014
)
0.4
" Pulsed dosing conferred no apparent safety or dose advantage."( A phase I, dose-escalation trial of continuous- and pulsed-dose afatinib combined with pemetrexed in patients with advanced solid tumors.
Chand, VK; Chu, QS; Hirte, HW; Hotte, SJ; Sangha, R; Schnell, D; Sergenson, G, 2014
)
0.4
"To review the pharmacology, pharmacokinetics, efficacy, adverse effects, drug-drug interactions, dosage and administration, and formulary considerations for ado-trastuzumab emtansine."( Ado-trastuzumab emtansine: a HER2-positive targeted antibody-drug conjugate.
Auten, JJ; Cicci, TA; Corrigan, PA; Lowe, DK, 2014
)
0.4
" In phase II, participants were randomized (stratified by age and KPS) to receive A, T or AT; A was dosed at 40 mg/day and T at 75 mg/m(2) for 21 of 28 days."( Phase I/randomized phase II study of afatinib, an irreversible ErbB family blocker, with or without protracted temozolomide in adults with recurrent glioblastoma.
Cong, J; Cseh, A; Eisenstat, DD; Fu, Y; Kavan, P; Mason, WP; Mathieu, D; Nabors, LB; Perry, JR; Phuphanich, S; Reardon, DA; Shapiro, W; Wind, S, 2015
)
0.42
" Further greenhouse experiments indicated that compounds 11d and 11 h displayed strong and broad-spectrum post-emergent herbicidal activity even at a dosage as low as 37."( Design, synthesis and herbicidal activity of novel quinazoline-2,4-diones as 4-hydroxyphenylpyruvate dioxygenase inhibitors.
Cao, RJ; Chen, T; Hao, GF; Lin, HY; Ming, ZZ; Wang, DW; Yang, GF; Yang, WC, 2015
)
0.42
" Because tasisulam is highly albumin-bound, patients in the tumor-specific confirmation arms were dosed targeting specific albumin-corrected exposure ranges (AUCalb) identified during dose-escalation (3,500 h*μg/mL [75th percentile] for docetaxel, temozolomide, and cisplatin; 4,000 h*μg/mL for gemcitabine and erlotinib)."( An innovative, multi-arm, complete phase 1b study of the novel anti-cancer agent tasisulam in patients with advanced solid tumors.
Becerra, CR; Braiteh, F; Chen, J; Chow, KH; Conkling, PR; Garbo, L; Ilaria, R; Jotte, RM; Richards, DA; Robert-Vizcarrondo, F; Smith, DA; Stephenson, J; Tai, DF; Turner, PK; Von Hoff, DD, 2015
)
0.42
"To determine the more effective dosing sequence of intermittent erlotinib and docetaxel for treating chemotherapy-naive patients with advanced Non-Small Cell Lung Cancer (NSCLC)."( Docetaxel and intermittent erlotinib in patients with metastatic Non-Small Cell Lung Cancer; a phase II study from the Hellenic Cooperative Oncology Group.
Boukovinas, I; Briasoulis, E; Dimopoulos, MA; Fountzilas, G; Kalogera-Fountzila, A; Karavasilis, V; Klouvas, G; Kosmidis, P; Kotoula, V; Mavropoulou, P; Papandreou, CN; Pectasides, D; Syrigos, KN, 2014
)
0.4
" Linagliptin is the first DPP-4 inhibitor to be eliminated primarily via a nonrenal route, enabling its use without dosage adjustment in patients with any degree of renal impairment."( Linagliptin: an update of its use in patients with type 2 diabetes mellitus.
McKeage, K, 2014
)
0.4
"The pharmacology, pharmacokinetics, clinical efficacy, safety, adverse effects, dosage and administration, and role in therapy of afatinib in the management of non-small-cell lung cancer (NSCLC) are reviewed."( Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.
Engle, JA; Kolesar, JM, 2014
)
0.4
" The recommended dosage is 40 mg once daily."( Afatinib: A first-line treatment for selected patients with metastatic non-small-cell lung cancer.
Engle, JA; Kolesar, JM, 2014
)
0.4
" It would require high potency (low effective drug concentrations) and sufficient drug exposures at tolerated doses so that the drug concentration can be maintained above effective drug concentration for target inhibition within the dosing period."( Discovery of fruquintinib, a potent and highly selective small molecule inhibitor of VEGFR 1, 2, 3 tyrosine kinases for cancer therapy.
Cai, H; Cui, Y; Gu, Y; Guo, M; Hong, M; Liang, J; Long, J; Ni, L; Qing, W; Ren, Y; Sai, Y; Su, W; Sun, J; Sun, Q; Yang, H; Yang, Z; Yin, F; Zhang, M; Zhang, W; Zhang, Z; Zhou, F; Zhou, J, 2014
)
0.4
" Central lead shield was used if the dose reached 30 Gy to produce a total dosage of 50 Gy."( The role of raltitrexed/cisplatin with concurrent radiation therapy in treating advanced cervical cancer.
Li, XY; Liu, L; Xie, XM; Zhou, C, 2014
)
0.4
" Vandetanib and sirolimus were orally administered on a continuous daily dosing schedule in escalating dose cohorts."( Vandetanib plus sirolimus in adults with recurrent glioblastoma: results of a phase I and dose expansion cohort study.
Batchelor, TT; Beroukhim, R; Betensky, RA; Chheda, MG; Chi, AS; Drappatz, J; Eichler, AF; Gerstner, ER; Hochberg, FH; Norden, AD; Wen, PY; Yang, D, 2015
)
0.42
" Inhibitory concentrations on cell proliferation were calculated by non-linear regression analysis using sigmoidal fitting of dose-response curves."( Calcitriol and its analogues enhance the antiproliferative activity of gefitinib in breast cancer cells.
Díaz, L; Esparza-López, J; García-Becerra, R; García-Quiroz, J; González-González, ME; Ibarra-Sánchez, MJ; Larrea, F; Martínez-Reza, I; Prado-Garcia, H; Segovia-Mendoza, M, 2015
)
0.42
" Pharmacokinetic evaluation suggested low accumulation with this dosing regimen."( A Phase I Study of CUDC-101, a Multitarget Inhibitor of HDACs, EGFR, and HER2, in Combination with Chemoradiation in Patients with Head and Neck Squamous Cell Carcinoma.
Atoyan, R; Bauman, JE; Burtness, B; Colevas, AD; Galloway, TJ; Gilbert, J; Jimeno, A; Ma, AW; Mehra, R; Raben, D; Saba, NF; Wang, J; Wirth, LJ, 2015
)
0.42
" Our own data as well as data from the literature was used to calculate those R levels revealing that the formation of 5'-DFUR - the immediate precursor of 5-fluorouracil - was not affected by concomitant medication within the dosing range investigated."( A simple method for comparing enzymatic capecitabine activation in various mono- and combination chemotherapies.
Baroian, N; Buchner, P; Czejka, M; Dittrich, C; Sahmanovic, A; Schreiber, V, 2015
)
0.42
" In the ranitidine study, on day 13, participants were randomized to either concomitant dosing (treatment B) or staggered administration (treatment C) of erlotinib and ranitidine and crossed over to the other treatment starting on day 27."( Effect of gastric pH on erlotinib pharmacokinetics in healthy individuals: omeprazole and ranitidine.
Abt, M; Ducray, PS; Giraudon, M; Hamilton, M; Kletzl, H; Lum, BL, 2015
)
0.42
" After 4 weeks of treatment, AZD0530 dosing of APP/PS1 transgenic mice fully rescues spatial memory deficits and synaptic depletion, without altering APP or Aß metabolism."( Fyn inhibition rescues established memory and synapse loss in Alzheimer mice.
Gunther, EC; Haas, LT; Jeng, AT; Kaufman, AC; Kostylev, MA; Nygaard, HB; Robinson, SA; Salazar, SV; Strittmatter, SM; van Dyck, CH; Yang, J, 2015
)
0.42
"This phase I open-label trial of a novel gefitinib dosing schedule employed a 3+3 design."( A phase I trial of high dose gefitinib for patients with leptomeningeal metastases from non-small cell lung cancer.
Cioffredi, LA; Jackman, DM; Jacobs, L; Johnson, BE; Kesari, S; Lucca, J; Lynch, TJ; Marcoux, PJ; Morse, LK; Plotkin, SR; Rabin, MS; Sharmeen, F, 2015
)
0.42
" To investigate the influence of dosing time on the ability of erlotinib to inhibit tumor growth and the underlying molecular mechanisms via the PI3K/AKT and ERK/MAPK pathway, we established nude mice HCC827 tumor xenografts models."( Chronopharmacodynamics and mechanisms of antitumor effect induced by erlotinib in xenograft-bearing nude mice.
An, F; Li, M; Lin, P; Liu, J; Liu, L; Liu, N; Wang, L; Wang, P; Xu, X; Zhao, L, 2015
)
0.42
" LC-MS-SPE-NMR is a technique that allows complete structure identification, but is difficult to apply to complex in vivo samples (such as bile collected during in vivo drug metabolism studies) due to the presence, at high concentrations, of interfering endogenous components, and potentially also dosage excipient components (e."( Micropreparative isolation and NMR structure elucidation of metabolites of the drug candidate 1-isopropyl-4-(4-isopropylphenyl)-6-(prop-2-yn-1-yloxy) quinazolin-2(1H)-one from rat bile and urine.
Aichholz, R; Blanz, J; Braun, E; Dayer, J; Délémonté, T; Desrayaud, S; Gertsch, W; Luneau, A; Pearson, D; Ramstein, P; Ritzau, M, 2015
)
0.42
" Kinase inhibitors preferentially targeting growth of fulvestrant resistant cells were identified and the growth inhibitory effect verified by dose-response cell growth experiments."( Aurora kinase B is important for antiestrogen resistant cell growth and a potential biomarker for tamoxifen resistant breast cancer.
Bak, M; Duun-Henriksen, AK; Kirkegaard, T; Laenkholm, AV; Larsen, SL; Lykkesfeldt, AE; Rasmussen, BB; Yde, CW, 2015
)
0.42
" UNC0638 inhibition of G9a caused dosed accumulation of HbF up to 30% of total hemoglobin in differentiated cells."( Inhibition of G9a methyltransferase stimulates fetal hemoglobin production by facilitating LCR/γ-globin looping.
Byrnes, C; de Vasconcellos, JF; Dean, A; Kaushal, M; Krivega, I; Lee, YT; Miller, JL, 2015
)
0.42
" To determine whether inhibition of HER2 could increase the efficacy of AZD5363, a novel AKT inhibitor, a panel of breast cancer cells was dosed with AZD5363 in combination with AZD8931, an inhibitor of EGFR/HER2/HER3 signalling."( Combining AZD8931, a novel EGFR/HER2/HER3 signalling inhibitor, with AZD5363 limits AKT inhibitor induced feedback and enhances antitumour efficacy in HER2-amplified breast cancer models.
Crafter, C; Davies, BR; Dudley, P; James, NH; Klinowska, T; Tang, E; Vincent, JP, 2015
)
0.42
" Our results suggest that the use of a hybrid system may allow a decrease in the dosage regimen without the loss of therapeutic effect."( Novel nanosystem to enhance the antitumor activity of lapatinib in breast cancer treatment: Therapeutic efficacy evaluation.
Huo, ZJ; Liu, K; Liu, P; Pang, B; Wang, SJ; Wang, ZQ; Zuo, WS, 2015
)
0.42
" Clinically, continuous dosing of pazopanib/lapatinib combination was associated with a higher response rate than with lapatinib monotherapy, with poor tolerance."( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors.
Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015
)
0.42
"The present study used a phase 1, modified 3 + 3, dose-escalation design to evaluate the safety and tolerability of the combination of orally received pazopanib once every other day with continuous daily dosing of lapatinib for 28 days."( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors.
Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015
)
0.42
"Every other day dosing of pazopanib combined with daily lapatinib was tolerated at the established MTD, but no complete or partial tumor responses were observed at these dose levels."( A phase 1 study of intermittently administered pazopanib in combination with continuous daily dosing of lapatinib in patients with solid tumors.
Fu, S; George, GC; Henary, H; Hong, DS; Kurzrock, R; Mistry, R; Naing, A; Piha-Paul, S; Wheler, J; Zinner, R, 2015
)
0.42
" Dose-response studies, biochemical and cytometric assessment of the effect of OOS on cell cycle and apoptosis, and drug combination analyses were performed on BT474 and SKBR3 cells, 2 HER2-overexpressing breast cancer cell lines."( Effect of Oncoxin Oral Solution in HER2-Overexpressing Breast Cancer.
González, V; Hernández-García, S; Pandiella, A; Sanz, E, 2015
)
0.42
" It was dosed daily with gemcitabine (1,000 mg/m2 on days 1, 8 and 15) and cisplatin (70 mg/m2 on day 2) every 28 days."( Results from a Phase I Study of Lapatinib with Gemcitabine and Cisplatin in Advanced or Metastatic Bladder Cancer: EORTC Trial 30061.
Agerbaek, M; Cerbone, L; Collette, S; Daugaard, G; Marreaud, S; Sengeløv, L; Sternberg, CN; Van Herpen, C; Zhang, J, 2016
)
0.43
" Eligible patients were randomized to one of the following treatment arms: PCG, P 175 mg/m(2), and C AUC 5 administered intravenously on day 1 intercalated with G 250 mg orally on days 2 through 15 every 3 weeks for four cycles followed by G 250 mg orally until progressive disease; or PC, same dosing schedule for four cycles only."( Randomized phase II study of paclitaxel/carboplatin intercalated with gefitinib compared to paclitaxel/carboplatin alone for chemotherapy-naïve non-small cell lung cancer in a clinically selected population excluding patients with non-smoking adenocarcino
Ahn, JH; Choi, CM; Choi, YJ; Kim, SW; Lee, DH; Lee, JS; Lee, SJ, 2015
)
0.42
" Optimal dosing is currently determined using concentrations of tyrosine kinase inhibitors in plasma as a surrogate for tumor concentrations."( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor.
Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015
)
0.42
"Mice bearing BT474 HER2+ human breast cancer xenografts were dosed once or twice daily (BID) with lapatinib."( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor.
Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015
)
0.42
" Tumor concentrations exceeded the in vitro IC90 (~ 900 nM or 500 ng/mL) for inhibition of HER2 phosphorylation throughout the 12-hour dosing interval."( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor.
Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015
)
0.42
"Plasma lapatinib concentrations underestimated tumor drug levels, suggesting that optimal dosing should be focused on the site of action to avoid to inappropriate dose escalation."( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor.
Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015
)
0.42
"Plasma lapatinib concentrations underestimated tumor drug levels, suggesting that optimal dosing should be focused on the site of action to avoid to inappropriate dose escalation."( Lapatinib Plasma and Tumor Concentrations and Effects on HER Receptor Phosphorylation in Tumor.
Avisar, E; Bacus, S; Beitsch, P; Blackwell, K; Cartee, L; Gittelman, M; Glenn, K; Harris, J; Kimbrough, CL; Koch, KM; Robertson, FC; Smith, DA; Spector, NL, 2015
)
0.42
" The therapeutic window of erlotinib is narrow, and the recommended dosage is close to the maximum tolerable dosage."( Evaluation of Three Small Molecular Drugs for Targeted Therapy to Treat Nonsmall Cell Lung Cancer.
Ni, J; Zhang, L, 2016
)
0.43
"Purpose The approval history, pharmacology, pharmacokinetics, clinical trials, efficacy, dosing recommendations, drug interactions, safety, place in therapy, and economic considerations of gefitinib are reviewed."( Flipped script for gefitinib: A reapproved tyrosine kinase inhibitor for first-line treatment of epidermal growth factor receptor mutation positive metastatic nonsmall cell lung cancer.
Bogdanowicz, BS; Hartranft, ME; Hoch, MA, 2017
)
0.46
" However, the use of daily dosing of ERBB2 tyrosine kinase inhibitors (TKIs)-including afatinib-has been fraught with plasma concentrations that barely achieve preclinical model inhibition, significant patient-reported toxicities, and limited clinical activity."( Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.
Costa, DB; Freed, JA; Huberman, MS; Jorge, SE; Kobayashi, SS; Moran, JP; Zerillo, JA, 2016
)
0.43
"Pulse afatinib at a weekly dosing scheme induced antitumor activity in ERBB2 exon 20 insertion-mutated lung adenocarcinomas."( Pulse Afatinib for ERBB2 Exon 20 Insertion-Mutated Lung Adenocarcinomas.
Costa, DB; Freed, JA; Huberman, MS; Jorge, SE; Kobayashi, SS; Moran, JP; Zerillo, JA, 2016
)
0.43
" Patients received once-daily vandetanib (planned dosing levels of 100, 200, and 300 mg) with concomitant daily radiotherapy (1."( Induction Therapy for Locally Advanced, Resectable Esophagogastric Cancer: A Phase I Trial of Vandetanib (ZD6474), Paclitaxel, Carboplatin, 5-Fluorouracil, and Radiotherapy Followed by Resection.
Astsaturov, IA; Berger, AC; Boland, PM; Burtness, BA; Cheng, JD; Cohen, SJ; Cooper, HS; Davey, M; Lebenthal, A; Meyer, JE; Neuman, T; Olszanski, AJ; Scott, WJ, 2017
)
0.46
"The dose escalation cohort enrolled adults with advanced solid tumors, who received MK-2206 dosed 30 to 60 mg every other day and lapatinib 1,000 to 1,500 mg daily continuously, escalated using a 3+3 design."( Phase I Study of an AKT Inhibitor (MK-2206) Combined with Lapatinib in Adult Solid Tumors Followed by Dose Expansion in Advanced HER2+ Breast Cancer.
Bell, MC; Burkard, ME; Eickhoff, J; Flynn, C; Kolesar, JM; Liu, G; Rampurwala, M; Tevaarwerk, AJ; Wisinski, KB, 2016
)
0.43
" A higher dosage of r-TNC induced cerebral arterial constriction more severely, which continued for 48 hours."( Epidermal growth factor-like repeats of tenascin-C-induced constriction of cerebral arteries via activation of epidermal growth factor receptors in rats.
Fujimoto, M; Imanaka-Yoshida, K; Kawakita, F; Liu, L; Nakasaki, A; Shiba, M; Shimojo, N; Suzuki, H; Yoshida, T, 2016
)
0.43
"This study aimed to evaluate the safety, tolerability and pharmacokinetics of the combination of oral vinorelbine with erlotinib using the conventional (CSV) and metronomic (MSV) dosing schedules in patients with advanced non-small cell lung cancer (NSCLC)."( Phase I Study of Oral Vinorelbine in Combination with Erlotinib in Advanced Non-Small Cell Lung Cancer (NSCLC) Using Two Different Schedules.
Ang, MK; Chowbay, B; Lim, WT; Ng, QS; Sutiman, N; Tan, EH; Tan, SW; Toh, CK; Zhang, Z, 2016
)
0.43
" This study was an open-label, randomized, adaptive design, two-period crossover bioequivalence study of the powder for suspension relative to the commercial tablet at steady state following once daily dosing for 7 days in patients with advanced cancer."( Bioequivalence study with lapatinib powder for oral suspension and the original tablet formulation in cancer patients.
Arya, N; Cartee, L; Curran, D; D'Amelio, AM; Ferron-Brady, G; Hollyfield, H; Koch, KM; Lemmon, C; Piepszak, A; Swaby, RF,
)
0.13
" In comparison to capsaicin, coadministration of 1 and capsaicin increased the half-maximal effective concentration (EC50) of capsaicin-activated TRPV1 currents as shown by a right shift in the dose-response curve, whereas coadministration of 1 with protons failed to inhibit the proton-induced current."( Partial Activation and Inhibition of TRPV1 Channels by Evodiamine and Rutaecarpine, Two Major Components of the Fruits of Evodia rutaecarpa.
Dai, Y; Kogure, Y; Noguchi, K; Wang, S; Yamamoto, S; Zhang, W, 2016
)
0.43
"[(14) C]-AZD1152 (barasertib) drug substance was prepared in order to support a hADME study that was to be dosed as an intravenous infusion to patients with acute myeloid leukaemia."( [(14) C]-AZD1152 drug substance manufacture: challenges of an IV-infusion dosed human mass balance study in patients.
Bergin, J; Bushby, N; Harding, J, 2016
)
0.43
" As such, the development of PI3K inhibitors from novel compound classes should lead to differential pharmacological and pharmacokinetic profiles and allow exploration in various indications, combinations, and dosing regimens."( Discovery and SAR of Novel 2,3-Dihydroimidazo[1,2-c]quinazoline PI3K Inhibitors: Identification of Copanlisib (BAY 80-6946).
Brands, M; Bull, CO; Bullion, AM; Esler, W; Fracasso, RP; Garrison, T; Hamilton, M; Hentemann, MF; Jenkins, S; Johnson, J; Lefranc, J; Levy, J; Liu, N; Michels, M; Redman, A; Robbins, AH; Rowley, RB; Schaefer, M; Scott, WJ; Stasik, E; Wilkie, DP; Wood, JE; Xiao, H, 2016
)
0.43
"The stability of extemporaneously prepared erlotinib, lapatinib, and imatinib oral liquid dosage forms using two commercially available vehicles when stored at 4 and 25 °C was evaluated."( Stability of extemporaneous erlotinib, lapatinib, and imatinib oral suspensions.
Griffith, N; Kolli, S; Li, Q; Liu, Z; Poi, MJ; Wetz, K, 2016
)
0.43
" More importantly, compound 3k also strongly blocked tumor growth with the dosage of 30 mg/kg/day, and subsequent mechanism exploration suggested that this series of compounds took effect mainly through angiogenesis signaling pathways."( Discovery and Optimization of N-Substituted 2-(4-pyridinyl)thiazole carboxamides against Tumor Growth through Regulating Angiogenesis Signaling Pathways.
Chen, Y; Dong, Y; Jiang, Z; Li, Y; Pei, H; Peng, Y; Shao, T; Sun, Z; Tang, W; Wang, J; Yi, Z; Zhou, W, 2016
)
0.43
" Different risk factors, including malnourishment, sarcopenia, and low body surface might be associated with a higher toxicity risk, and these groups of patients could begin treatment with a low dose of afatinib followed by a close evaluation on tolerability and toxicity in order to slowly increase the dosage of afatinib."( The safety of afatinib for the treatment of non-small cell lung cancer.
Arrieta, O; Barron, F; Cardona, AF; de la Torre-Vallejo, M; Luna-Palencia, RL, 2016
)
0.43
" We confirmed the diagnosis by evaluating the total radiation dosage and by excluding target therapy-induced maculopathy based on a review of the medical literature."( Rapid onset of radiation maculopathy after whole-brain radiation therapy: A case report.
Chang, YH; Chien, KH; Hsu, CR; Tai, MC, 2016
)
0.43
"Whether a full dosage of afatinib is tolerable and effective for elderly or low performance status (PS) patients with advanced refractory non-small-cell lung cancer (NSCLC) is unclear."( Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.
Fujii, S; Kashiwabara, K; Semba, H; Tsumura, S, 2016
)
0.43
" Afatinib was administered at a starting dosage of 20 or 30mg/day, followed by 10mg increases in dose up to a maximum dosage of 40mg/day."( Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.
Fujii, S; Kashiwabara, K; Semba, H; Tsumura, S, 2016
)
0.43
" Eight patients did not receive the 40mg/day dosage because of patient refusal due to grade 2 diarrhea (n=6) or the judgment of the doctor (n=2)."( Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.
Fujii, S; Kashiwabara, K; Semba, H; Tsumura, S, 2016
)
0.43
"A low starting dosage of afatinib might enable elderly or low PS patients with advanced refractory NSCLC to receive this drug as salvage therapy."( Tolerability and efficacy of afatinib at a low starting dosage in 10 elderly or low performance status patients with advanced refractory non-small-cell lung cancer.
Fujii, S; Kashiwabara, K; Semba, H; Tsumura, S, 2016
)
0.43
"8 mg/kg, dosed intermittently on days 1, 8, and 15 of a 28-day cycle."( A Phase I study of intravenous PI3K inhibitor copanlisib in Japanese patients with advanced or refractory solid tumors.
Bando, H; Doi, T; Fuse, N; Kaneko, M; Kojima, T; Miyamoto, H; Ohtsu, A; Osada, M; Yoshino, T, 2017
)
0.46
" Based on our predictions, dose-adjustment strategies may consist of once-daily dosing erlotinib at 25 mg and gefitinib at 125 mg with darunavir/ritonavir; or erlotinib at 200 mg and gefitinib at 375 mg with etravirine."( Use of a physiologically based pharmacokinetic model to simulate drug-drug interactions between antineoplastic and antiretroviral drugs.
Back, D; Clotet, B; Miranda, C; Moltó, J; Owen, A; Rajoli, R; Siccardi, M; Valle, M, 2017
)
0.46
" Moreover, this study revealed that CBZ dosage was related to toxicity in mice."( Evaluating the Effectiveness of GTM-1, Rapamycin, and Carbamazepine on Autophagy and Alzheimer Disease.
Che, H; Fu, P; Gao, Y; Pan, Y; Wang, L; Wang, R; Zhang, L, 2017
)
0.46
" Dosage reduction is recommended in patients with intolerable adverse events; however, data regarding the efficacy of low-dose afatinib are limited."( Complete Tumor Response with Afatinib 20 mg Daily in EGFR-Mutated Non-small Cell Lung Cancer: A Case Report.
Giusti, R; Iacono, D; Lauro, S; Marchetti, P; Mazzotta, M, 2017
)
0.46
"A highly sensitive, cheap, simple and accurate spectrofluorimetric method has been developed and validated for the determination of alfuzosin hydrochloride and terazosin hydrochloride in their pharmaceutical dosage forms and in human plasma."( Utility of Hantzsch reaction for development of highly sensitive spectrofluorimetric method for determination of alfuzosin and terazosin in bulk, dosage forms and human plasma.
Hammad, MA; Omar, MA; Salman, BI, 2017
)
0.46
" These highly selective IRAK4 compounds show activity in vivo via oral dosing in a TLR7 driven model of inflammation."( Identification of quinazoline based inhibitors of IRAK4 for the treatment of inflammation.
Altman, MD; Andresen, B; Baker, J; Brubaker, JD; Chen, H; Chen, Y; Childers, M; Donofrio, A; Ferguson, H; Fischer, C; Fischmann, TO; Gibeau, C; Hicks, A; Jin, S; Kattar, S; Kleinschek, MA; Leccese, E; Lesburg, C; Li, C; Lim, J; Liu, D; Maclean, JKF; Mansoor, F; Moy, LY; Mulrooney, EF; Necheva, AS; Northrup, A; Presland, J; Rakhilina, L; Smith, GF; Torres, L; Yang, R; Zhang-Hoover, J, 2017
)
0.46
"Standard 3+3 dose escalation scheme using two different dosing schedules were studied: once daily, 14-day on, and 7-day off (intermittent schedule); and once daily continuous dosing with food effect."( Phase 1 Studies of Poziotinib, an Irreversible Pan-HER Tyrosine Kinase Inhibitor in Patients with Advanced Solid Tumors.
Bang, YJ; Han, H; Han, SW; Im, SA; Kim, DW; Kim, JH; Kim, TM; Kim, TY; Kim, WH; Kim, YJ; Lee, JS; Lee, KW; Oh, DY, 2018
)
0.48
" Doselimiting toxicities were grade 3 diarrhea in the intermittent schedule and grade 3 anorexia and diarrhea in the continuous dosing schedule."( Phase 1 Studies of Poziotinib, an Irreversible Pan-HER Tyrosine Kinase Inhibitor in Patients with Advanced Solid Tumors.
Bang, YJ; Han, H; Han, SW; Im, SA; Kim, DW; Kim, JH; Kim, TM; Kim, TY; Kim, WH; Kim, YJ; Lee, JS; Lee, KW; Oh, DY, 2018
)
0.48
" The average dosage of EGFR-TKI was 56±22% of the standard dosage."( Effects of an Alkaline Diet on EGFR-TKI Therapy in EGFR Mutation-positive NSCLC.
Hamaguchi, R; Hasegawa, M; Okamoto, T; Sato, M; Wada, H, 2017
)
0.46
" Subgroup analysis suggested that the increased risk of all-grade rash was clear across all subgroups, including first-line/second-line therapy, phase 2/phase 3 trial, sample size 200, a dosage of 100 or 300 mg, and monotherapy/combination therapy."( Risk of rash associated with vandetanib treatment in non-small-cell lung cancer patients: A meta-analysis of 9 randomized controlled trials.
Hou, S; Li, Y; Liu, Q; Liu, Y; Qi, M; Shao, L; Zhang, J, 2017
)
0.46
" Here, we developed a computational approach to model the in vitro cellular dynamics of the EGFR-mutant cell line SF268 in response to different lapatinib concentrations and dosing schedules."( Mathematical modeling identifies optimum lapatinib dosing schedules for the treatment of glioblastoma patients.
Haeno, H; Michor, F; Stein, S; Vivanco, I; Zhao, R, 2018
)
0.48
"A new, selective and sensitive spectrofluorimetric method was designed for the quantitation of doxazosin (DOX), terazosin (TER) and alfuzosin (ALF) in their dosage forms and human plasma."( An efficient spectrofluorimetric method adopts doxazosin, terazosin and alfuzosin coupling with orthophthalaldehyde: Application in human plasma.
Derayea, SM; Hammad, MA; Mohamed, AA; Mohamed, AI; Omar, MA, 2018
)
0.48
" The results demonstrate that the xenobiotic metabolism conferred by transfection of CYP-encoding mRNAs shifts the dose-response relationship for some of the tested chemicals such as aflatoxin B1 (bioactivation) and fenazaquin (detoxification)."( mRNA transfection retrofits cell-based assays with xenobiotic metabolism.
Carmichael, PL; DeGroot, DE; Lee, MY; Simmons, SO; Strynar, M; Swank, A; Thomas, RS,
)
0.13
" weekly dosing with EGFR inhibitors (gefitinib and lapatinib) and an AKT inhibitor (MK2206) were compared in two rodent breast cancer models."( Daily or weekly dosing with EGFR inhibitors, gefitinib and lapatinib, and AKt inhibitor MK2206 in mammary cancer models.
Bode, A; Grubbs, CJ; Juliana, MM; Lubet, RA; Moeinpour, F; Steele, VE, 2018
)
0.48
" Alternatively, the concept of prior dosing allows for the application of dialyzable chemotherapeutic drugs using a normal dose, with an HD followed shortly after to mimic normal renal function."( Chemotherapeutic agents eligible for prior dosing in pancreatic cancer patients requiring hemodialysis: a systematic review
.
Egger, J; Hann, A; Hermann, PC; Keller, F; Nosalski, E; Seufferlein, T, 2018
)
0.48
" Letermovir is available both orally and intravenously in 480-mg and 240-mg dosage forms, and is approved for use in the prophylaxis of CMV infection and disease in CMV-seropositive recipients of allogeneic hematopoietic stem cell transplant (HSCT) over the age of 18."( Letermovir for prophylaxis of cytomegalovirus in allogeneic hematopoietic stem cell recipients.
Cho, JC; Le, AD; Locke, SC, 2018
)
0.48
"To evaluate the safety, tolerability, and pharmacokinetics of XL647 and determine the maximum tolerated dose (MTD) of oral XL647 once-daily using intermittent or continuous dosing schedules."( A safety, tolerability, and pharmacokinetic analysis of two phase I studies of multitargeted small molecule tyrosine kinase inhibitor XL647 with an intermittent and continuous dosing schedule in patients with advanced solid malignancies.
Adjei, A; Das, M; Frymoyer, A; Lensing, JL; Miles, D; Molina, J; Padda, SK; Sikic, BI; Wakelee, HA, 2018
)
0.48
"Patients with advanced solid malignancies were enrolled in successive cohorts to receive escalating dose levels of oral once-daily XL647 using two different dosing schedules: 5 consecutive days of every 14-day cycle (study XL647-001) or continuously over 28-day cycles (study XL647-002)."( A safety, tolerability, and pharmacokinetic analysis of two phase I studies of multitargeted small molecule tyrosine kinase inhibitor XL647 with an intermittent and continuous dosing schedule in patients with advanced solid malignancies.
Adjei, A; Das, M; Frymoyer, A; Lensing, JL; Miles, D; Molina, J; Padda, SK; Sikic, BI; Wakelee, HA, 2018
)
0.48
" Estimated growth rate and dose-response was found to be comparable between brain metastasis and subcutaneous mouse models."( Pharmacodynamic modelling of resistance to epidermal growth factor receptor inhibition in brain metastasis mouse models.
Aarons, L; Martin, EC; Yates, JWT, 2018
)
0.48
" This model suggests changes to dosing and dosing schedule may not prevent resistance to treatment developing, and that additional treatments would need to be used in combination to overcome resistance."( Pharmacodynamic modelling of resistance to epidermal growth factor receptor inhibition in brain metastasis mouse models.
Aarons, L; Martin, EC; Yates, JWT, 2018
)
0.48
" The developed method was successfully applied to determine the studied drugs in dosage forms and human plasma samples and the results were satisfactory as revealed by statistical analysis of the data."( Simultaneous HPLC determination of alfuzosin, tamsulosin and vardenafil in human plasma and pharmaceutical formulations using time programmed fluorescence detection.
Belal, F; Borg, H; Fathy, M; Walash, MI; Zayed, S, 2019
)
0.51
"Once-daily dosing of epertinib at 800 mg was well-tolerated and demonstrated promising antitumour activity in patients with heavily pretreated HER2-positive breast and upper GI cancer, including those with brain metastases."( An extended phase Ib study of epertinib, an orally active reversible dual EGFR/HER2 tyrosine kinase inhibitor, in patients with solid tumours.
Adenis, A; Arimura, A; Arkenau, HT; Baird, RD; Deva, S; Donaldson, K; Flynn, M; Forster, M; Garcia-Corbacho, J; Italiano, A; Kawabata, I; Mak, G; Plummer, R; Posner, J; Spicer, J; Tosi, D; Toulmonde, M; Wilson, RH, 2018
)
0.48
" Here we describe the identification of potent pan-KIT mutant kinase inhibitors that can be dosed without being limited by the tolerability issues seen with multitargeted agents."( Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.
Anjum, R; Barry, E; Bhavsar, D; Boyd, S; Brown, C; Campbell, A; Goldberg, K; Grondine, M; Guichard, S; Hardy, CJ; Hunt, T; Jones, RDO; Kettle, JG; Li, X; Moleva, O; Ogg, D; Overman, RC; Packer, MJ; Pearson, S; Schimpl, M; Shao, W; Smith, A; Smith, JM; Stead, D; Stokes, S; Tucker, M; Ye, Y, 2018
)
0.48
" Fatigue is a common adverse event during treatment with these and other TKIs and a common cause of drug discontinuation or dosage reduction."( Primary Adrenal Insufficiency During Lenvatinib or Vandetanib and Improvement of Fatigue After Cortisone Acetate Therapy.
Colombo, C; De Leo, S; Di Stefano, M; Fugazzola, L; Persani, L; Vannucchi, G, 2019
)
0.51
"We show that the occurrence of PAI may be a common cause of fatigue during lenvatinib and vandetanib treatment, and we therefore recommend testing adrenal function for a prompt start of replacement therapy to avoid treatment discontinuation, dosage reduction, and potentially severe PAI complications."( Primary Adrenal Insufficiency During Lenvatinib or Vandetanib and Improvement of Fatigue After Cortisone Acetate Therapy.
Colombo, C; De Leo, S; Di Stefano, M; Fugazzola, L; Persani, L; Vannucchi, G, 2019
)
0.51
" Mice were examined in the Barnes maze at the end of the dosing period, and brain tissue and optic nerves were examined immunohistochemically or biochemically for changes in MT density, axonal dystrophy, and tau pathology."( A brain-penetrant triazolopyrimidine enhances microtubule-stability, reduces axonal dysfunction and decreases tau pathology in a mouse tauopathy model.
Ballatore, C; Brunden, KR; Cornec, AS; James, MJ; Koivula, P; Lee, VM; Oukoloff, K; Smith, AB; Trojanowski, JQ; Yao, Y; Zhang, B, 2018
)
0.48
" For pharmacokinetic studies, 32 Sprague-Dawley rats were randomly divided into four groups, namely, intravenous dosage group (2 mg/kg DVAS) and three oral dosage groups (5, 15, and 45 mg/kg DVAS)."( In vivo and in vitro metabolism and pharmacokinetics of cholinesterase inhibitor deoxyvasicine from aerial parts of Peganum harmala Linn in rats via UPLC-ESI-QTOF-MS and UPLC-ESI-MS/MS.
Cao, N; Cheng, X; Deng, G; Ding, W; Guan, H; Liu, W; Ma, C; Rong, X; Wang, C; Wang, Y; Wu, C; Zhang, Y, 2019
)
0.51
" These data support the reduction in clinical dosage of letermovir (to 240 mg) upon coadministration with cyclosporine."( Pharmacokinetic Drug-Drug Interactions Between Letermovir and the Immunosuppressants Cyclosporine, Tacrolimus, Sirolimus, and Mycophenolate Mofetil.
Adedoyin, A; Cho, CR; Iwamoto, M; Kraft, WK; Levine, V; Liu, F; Macha, S; Marshall, W; McCrea, JB; Menzel, K; Panebianco, D; Stoch, SA; Yoon, E; Zhao, T, 2019
)
0.51
"5 mL; n = 7), dosed once every 24 hours for 21 days."( Long-term cardiovascular effects of vandetanib and pazopanib in normotensive rats.
Carter, JJ; Cooper, SL; March, J; Woolard, J, 2019
)
0.51
" Detailed information on therapeutic-drug-monitoring measures and dosage adjustments for letermovir is provided."( Compassionate Use of Letermovir in a 2-Year-Old Immunocompromised Child With Resistant Cytomegalovirus Disease.
Andre, P; Asner, SA; Buclin, T; Decosterd, LA; Gengler, C; Jaton-Ogay, K; Mercier, T; Meylan, P; Murray, K; Natterer, J; Opota, O; Pérez Marín, M; Perez, MH; Rizzi, M, 2020
)
0.56
" However, traditional Body Surface Area (BSA)-based dosing is unsafe or ineffective, and a more accurate model-based approach is required."( Hepatic Artery and Peripheral Vein Pharmacokinetics of Raltitrexed in Swine After the Administration of a Hepatic Arterial Infusion.
Li, X; Zhang, X; Zheng, N; Zhu, L, 2019
)
0.51
"The pharmacokinetic model could be helpful in quantitatively describing the detailed processes of raltitrexed activity administered by HAI and determining an appropriate dosing regimen for preclinical and clinical studies."( Hepatic Artery and Peripheral Vein Pharmacokinetics of Raltitrexed in Swine After the Administration of a Hepatic Arterial Infusion.
Li, X; Zhang, X; Zheng, N; Zhu, L, 2019
)
0.51
" These results provide a foundation for loading RTX in a nanoparticle formulation, and establish a combined radiation and drug dosing schedule to determine optimal tumor growth delay and subsequent treatment efficacy."( Enhancing chemoradiation of colorectal cancer through targeted delivery of raltitrexed by hyaluronic acid coated nanoparticles.
Landry, MR; Rosch, JG; Sun, C; Thomas, CR, 2019
)
0.51
" Further study of the dosing and efficacy of letermovir for CMV prophylaxis or treatment in thoracic organ transplant recipients is warranted."( Single-center experience with use of letermovir for CMV prophylaxis or treatment in thoracic organ transplant recipients.
Ahmad, K; Aryal, S; Brown, AW; Chun, J; Cochrane, A; Desai, S; Fregoso, M; Katugaha, SB; King, C; Marinak, L; Nathan, SD; Shlobin, OA, 2019
)
0.51
" The pediatric dosing was 30% lower compared to the adult dosing, which may have contributed to response differences."( Cediranib phase-II study in children with metastatic alveolar soft-part sarcoma (ASPS).
Chen, AP; Cohen, JW; Derdak, J; Dombi, E; Dompierre, J; Glod, J; Goodwin, A; Kummar, S; O'Sullivan Coyne, G; Onukwubiri, U; Steinberg, SM; Widemann, BC, 2019
)
0.51
" The drug effect score (DES) was calculated from the dose-response of each drug for comparison among drugs or samples."( Aurora B kinase as a therapeutic target in acute lymphoblastic leukemia.
Goto, H; Goto, S; Hamanoue, S; Inukai, T; Ito, M; Iwasaki, F; Keino, D; Kumamoto, T; Miyagawa, N; Nagai, J; Sakurai, Y; Shiomi, M; Yokosuka, T; Yoshino, Y, 2020
)
0.56
"AZD3229 drives inhibition of phosphorylated KIT in an exposure-dependent manner, and optimal efficacy is observed when >90% inhibition of KIT phosphorylation is sustained over the dosing interval."( The Pharmacokinetic-Pharmacodynamic (PKPD) Relationships of AZD3229, a Novel and Selective Inhibitor of KIT, in a Range of Mouse Xenograft Models of GIST.
Anjum, R; Banks, E; Barry, E; Bhavsar, D; Brown, C; Grondine, M; Guichard, SM; Jones, RDO; Kettle, JG; Pilla Reddy, V; Shao, W; Smith, A, 2020
)
0.56
" While this technique produces dose-response data which fit very well to a linear-quadratic model for exposures to low linear energy transfer (LET) radiation and for doses up for 5 Gy, limitations to the accuracy of this method arise at larger doses."( Cytogenetically-based biodosimetry after high doses of radiation.
Brenner, DJ; Cunha, L; Garty, G; Harken, A; Perrier, JR; Pujol-Canadell, M; Shuryak, I, 2020
)
0.56
"Although ECT was the most accurate imaging method, its high cost and large radiation dosage limit its widespread application."( Diagnostic accuracy of MR, CT, and ECT in the differentiation of neoplastic from nonneoplastic spine lesions.
Bian, C; Dong, J; Hu, A; Jiang, L; Liang, Y; Liu, P; Wang, H; Zhou, X, 2020
)
0.56
"Data on the efficacy, dosing and safety of letermovir for the compassionate therapeutic use of CMV infections are limited."( Letermovir for the compassionate therapeutic use of cytomegalovirus infection.
Burgmann, H; Fisecker, L; Schubert, L; Steininger, C; Thalhammer, F, 2021
)
0.62
" Radiation was prescribed at 60 Gy in 30 fractions in both groups, and icotinib was administered at a dosage of 125 mg 3 times a day in the RT plus icotinib group."( Icotinib With Concurrent Radiotherapy vs Radiotherapy Alone in Older Adults With Unresectable Esophageal Squamous Cell Carcinoma: A Phase II Randomized Clinical Trial.
Chen, P; Ding, L; Du, D; Fang, M; Hua, Y; Jiang, W; Jing, Z; Luo, H; Ma, L; Song, Y; Tian, Z; Wang, J; Wu, S; Xie, R; Zhou, R, 2020
)
0.56
" Additional dose-response analyses were carried out."( Association of Glycolysis-Enhancing α-1 Blockers With Risk of Developing Parkinson Disease.
Liu, L; Narayanan, NS; Pottegård, A; Simmering, JE; Welsh, MJ, 2021
)
0.62
" The intravenous route of administration and intermittent dosing schedule of copanlisib may support a favorable tolerability profile over continually administered oral alternatives."( Copanlisib for the Treatment of Malignant Lymphoma: Clinical Experience and Future Perspectives.
Follows, GA; Munoz, J; Nastoupil, LJ, 2021
)
0.62
" Further studies on combination therapy or alternative LET dosing are needed."( Letermovir treatment of cytomegalovirus infection or disease in solid organ and hematopoietic cell transplant recipients.
Avery, R; Clark, NM; Gonzalez, AA; Hakki, M; Kaul, DR; Kotton, CN; Kovacs, C; La Hoz, RM; Limaye, AP; Linder, KA; Malinis, M; Mishkin, A; Mullane, KM; Ostrander, D; Prono, MD; Smith, J; Wolfe, C, 2021
)
0.62
" This method was successfully applied to pure form, tablet dosage form, spiked human (urine and plasma)."( Development of novel univariate and multivariate validated chemometric methods for the analysis of dasatinib, sorafenib, and vandetanib in pure form, dosage forms and biological fluids.
Abdelhameed, AS; Alanazi, AM; AlRabiah, H; Alruqi, OS; Attia, MI; Attwa, MW, 2022
)
0.72
" Cediranib and selumetinib were dosed using a toxicity-adaptive isotonic design for the dose escalation/de-escalation of each agent."( Phase I study of cediranib, an oral VEGFR inhibitor, in combination with selumetinib, an oral MEK inhibitor, in patients with advanced solid malignancies.
Adjei, A; Costello, BA; Doyle, LA; Erlichman, C; Fiskum, J; Haluska, P; Hubbard, JM; Ivy, P; Lin, G; Menefee, M; Qin, R; Reid, JM; Schenk, EL; Strand, C; Yin, J, 2022
)
0.72
" Due to the high toxicity of Foscarnet (FOS) and Cidofovir (CDV), Letermovir (LMV) monotherapy at the dosage of 480 mg per day was administered, with a gradual viral load reduction."( Emergence of Letermovir-resistant HCMV UL56 mutant during rescue treatment in a liver transplant recipient with ganciclovir-resistant infection HCMV: a case report.
Baldanti, F; Campanini, G; Cassaniti, I; Fratini, A; Girelli, F; Meini, A; Novazzi, F; Palumbo, L; Paolucci, S; Plebani, A; Tebaldi, A, 2021
)
0.62
" These results support current dosing recommendations in several countries and regions, including the United States and European Union."( Exposure-Response Analyses of Letermovir Following Oral and Intravenous Administration in Allogeneic Hematopoietic Cell Transplantation Recipients.
Badshah, C; Cho, CR; Davis, C; Dykstra, K; Fancourt, C; Leavitt, R; Macha, S; Murata, Y; Prohn, M; Sabato, P; Stone, J; Viberg, A, 2022
)
0.72
" We found that the survival in RA-treated NSCLC cells was significantly decreased by treatment with 500 nM AZD3759 and osimertinib at the RA dosage of 8 Gy."( AZD3759 enhances radiation effects in non-small-cell lung cancer by a synergistic blockade of epidermal growth factor receptor and Janus kinase-1.
Deng, Q; Ma, S; Mao, Y; Yin, W; Yu, Q; Zhang, K; Zhao, R, 2022
)
0.72
" These drug concentrations were selected using physiologically-based pharmacokinetic simulation considering patient dosing regimens."( A Transcriptomic Approach to Elucidate the Mechanisms of Gefitinib-Induced Toxicity in Healthy Human Intestinal Organoids.
Chung, SW; Coyle, L; de Kok, TM; Ferreira, S; Fisher, C; Herpers, B; Jennen, DGJ; Jo, H; Kleinjans, JCS; Rodrigues, D, 2022
)
0.72
" Efficacy of the tucatinib/trastuzumab combination matched that induced by current standard-of-care trastuzumab/pertuzumab/docetaxel combination, with the exception that the chemotherapy-sparing tucatinib/trastuzumab combination did not require a dosing holiday to achieve the same efficacy."( Tucatinib has Selective Activity in HER2-Positive Cancers and Significant Combined Activity with Approved and Novel Breast Cancer-Targeted Therapies.
Ayala, R; Gong, KW; Huang, HKT; Issakhanian, S; Lu, M; Luo, T; Madrid, AM; McDermott, MSJ; O'Brien, NA; Slamon, DJ; Zhang, J, 2022
)
0.72
" In a dose-response analysis, intranasal administration of 1 µg compound 31 together with an inactivated vaccine (0."( The efficacy of a 2,4-diaminoquinazoline compound as an intranasal vaccine adjuvant to protect against influenza A virus infection in vivo.
An, T; Han, SB; Jeong, EJ; Kim, H; Kim, M; Noh, K; Shin, JS, 2022
)
0.72
" Dose-response analysis using defined daily doses of drug (DDDs) was conducted."( Use of α1-adrenoceptor antagonists tamsulosin and alfuzosin and the risk of Alzheimer's disease.
Hartikainen, S; Latvala, L; Murtola, TJ; Tiihonen, M; Tolppanen, AM, 2022
)
0.72
" Understanding potential drug-drug interactions (DDIs) informs proper dosing when co-administering tucatinib with other therapies."( Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers.
Abdulrasool, LI; Endres, CJ; Lee, A; Mayor, JG; Rustia, EL; Sun, H; Topletz-Erickson, A; Walker, L, 2022
)
0.72
" As CI is a central player of cellular bioenergetics, a finely tuned dosing of targeting drugs is required to avoid side effects."( NDUFS3 knockout cancer cells and molecular docking reveal specificity and mode of action of anti-cancer respiratory complex I inhibitors.
Cavina, B; De Luise, M; Fornasa, A; Gasparre, G; Ghelli, A; Iommarini, L; Iorio, M; Kurelac, I; Lama, E; Miglietta, S; Musiani, F; Nasiri, HR; Porcelli, AM; Sollazzo, M; Traversa, D, 2022
)
0.72
" The follow-up included 3 visits: visit of inclusion in the program of patients with a previously prescribed drug of Alfuprost MR in a dosage of 10 mg once a day (visit "0"), visit 1 at 30 days (+/-5 days) later, and visit 2 at 90 days (+/-5 days) after inclusion in the study."( [The influence of alfuzosin monotherapy on the sexual function of patients with benign prostatic hyperplasia in real clinical practice (results of a Russian multicenter study)].
Bernikov, AN; Loran, OB; Pushkar, DY, 2022
)
0.72
"after 3 months of therapy with Alfuprost MR in a dosage of 10 mg once a day, significant (p<0."( [The influence of alfuzosin monotherapy on the sexual function of patients with benign prostatic hyperplasia in real clinical practice (results of a Russian multicenter study)].
Bernikov, AN; Loran, OB; Pushkar, DY, 2022
)
0.72
" Considering minimal and clinically insignificant vasodilatory effects observed during 3 months of therapy, it is possible to prescribe Alfuprost MR in a dosage of 10 mg once daily, including comorbid patients."( [The influence of alfuzosin monotherapy on the sexual function of patients with benign prostatic hyperplasia in real clinical practice (results of a Russian multicenter study)].
Bernikov, AN; Loran, OB; Pushkar, DY, 2022
)
0.72
" These outcomes substantiate the current intermittent dosing regimen of copanlisib 60 mg on days 1, 8, and 15 of a 28-day cycle and support the observed clinical results of copanlisib in combination with rituximab in the iNHL population."( Copanlisib population pharmacokinetics from phase I-III studies and exposure-response relationships in combination with rituximab.
Austin, R; Beckert, V; Childs, BH; Garmann, D; Hiemeyer, F; Mongay Soler, L; Morcos, PN; Moss, J; Zinzani, PL, 2023
)
0.91
" Steady-state was achieved after 14 days of QD dosing with systemic exposure four-fold higher than that after a single dose."( Phase 1/1b open-label, dose-escalation study of fruquintinib in patients with advanced solid tumors in the United States.
Chien, C; Gonzalez, M; Kania, M; Schelman, W; Ukrainskyj, S; Wang-Gillam, A; Yang, Z; Yeckes-Rodin, H, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (4)

ClassDescription
mancude organic heterobicyclic parent
quinazolinesAny organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
azaarene
ortho-fused heteroareneAn ortho-fused compound in which at least one of the rings contains at least one heteroatom.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Epidermal growth factor receptorHomo sapiens (human)IC50 (µMol)0.02700.00000.536910.0000AID1795547; AID69425
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (89)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
MAPK cascadeEpidermal growth factor receptorHomo sapiens (human)
ossificationEpidermal growth factor receptorHomo sapiens (human)
embryonic placenta developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein phosphorylationEpidermal growth factor receptorHomo sapiens (human)
hair follicle developmentEpidermal growth factor receptorHomo sapiens (human)
translationEpidermal growth factor receptorHomo sapiens (human)
signal transductionEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
activation of phospholipase C activityEpidermal growth factor receptorHomo sapiens (human)
salivary gland morphogenesisEpidermal growth factor receptorHomo sapiens (human)
midgut developmentEpidermal growth factor receptorHomo sapiens (human)
learning or memoryEpidermal growth factor receptorHomo sapiens (human)
circadian rhythmEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell population proliferationEpidermal growth factor receptorHomo sapiens (human)
diterpenoid metabolic processEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
cerebral cortex cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell growthEpidermal growth factor receptorHomo sapiens (human)
lung developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cell migrationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of superoxide anion generationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
response to cobalaminEpidermal growth factor receptorHomo sapiens (human)
response to hydroxyisoflavoneEpidermal growth factor receptorHomo sapiens (human)
cellular response to reactive oxygen speciesEpidermal growth factor receptorHomo sapiens (human)
peptidyl-tyrosine autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
ERBB2-EGFR signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of epidermal growth factor receptor signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
negative regulation of protein catabolic processEpidermal growth factor receptorHomo sapiens (human)
vasodilationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphorylationEpidermal growth factor receptorHomo sapiens (human)
ovulation cycleEpidermal growth factor receptorHomo sapiens (human)
hydrogen peroxide metabolic processEpidermal growth factor receptorHomo sapiens (human)
negative regulation of apoptotic processEpidermal growth factor receptorHomo sapiens (human)
positive regulation of MAP kinase activityEpidermal growth factor receptorHomo sapiens (human)
tongue developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA repairEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA replicationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of bone resorptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of DNA-templated transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of vasoconstrictionEpidermal growth factor receptorHomo sapiens (human)
negative regulation of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIEpidermal growth factor receptorHomo sapiens (human)
regulation of JNK cascadeEpidermal growth factor receptorHomo sapiens (human)
symbiont entry into host cellEpidermal growth factor receptorHomo sapiens (human)
protein autophosphorylationEpidermal growth factor receptorHomo sapiens (human)
astrocyte activationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of fibroblast proliferationEpidermal growth factor receptorHomo sapiens (human)
digestive tract morphogenesisEpidermal growth factor receptorHomo sapiens (human)
positive regulation of smooth muscle cell proliferationEpidermal growth factor receptorHomo sapiens (human)
neuron projection morphogenesisEpidermal growth factor receptorHomo sapiens (human)
epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
positive regulation of epithelial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
regulation of peptidyl-tyrosine phosphorylationEpidermal growth factor receptorHomo sapiens (human)
protein insertion into membraneEpidermal growth factor receptorHomo sapiens (human)
response to calcium ionEpidermal growth factor receptorHomo sapiens (human)
regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of synaptic transmission, glutamatergicEpidermal growth factor receptorHomo sapiens (human)
positive regulation of glial cell proliferationEpidermal growth factor receptorHomo sapiens (human)
morphogenesis of an epithelial foldEpidermal growth factor receptorHomo sapiens (human)
eyelid development in camera-type eyeEpidermal growth factor receptorHomo sapiens (human)
response to UV-AEpidermal growth factor receptorHomo sapiens (human)
positive regulation of mucus secretionEpidermal growth factor receptorHomo sapiens (human)
regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeEpidermal growth factor receptorHomo sapiens (human)
cellular response to amino acid stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to mechanical stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to cadmium ionEpidermal growth factor receptorHomo sapiens (human)
cellular response to epidermal growth factor stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to estradiol stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to xenobiotic stimulusEpidermal growth factor receptorHomo sapiens (human)
cellular response to dexamethasone stimulusEpidermal growth factor receptorHomo sapiens (human)
positive regulation of canonical Wnt signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
liver regenerationEpidermal growth factor receptorHomo sapiens (human)
cell-cell adhesionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein kinase C activityEpidermal growth factor receptorHomo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleEpidermal growth factor receptorHomo sapiens (human)
positive regulation of non-canonical NF-kappaB signal transductionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of prolactin secretionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of miRNA transcriptionEpidermal growth factor receptorHomo sapiens (human)
positive regulation of protein localization to plasma membraneEpidermal growth factor receptorHomo sapiens (human)
negative regulation of cardiocyte differentiationEpidermal growth factor receptorHomo sapiens (human)
neurogenesisEpidermal growth factor receptorHomo sapiens (human)
multicellular organism developmentEpidermal growth factor receptorHomo sapiens (human)
positive regulation of kinase activityEpidermal growth factor receptorHomo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathwayEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (24)

Processvia Protein(s)Taxonomy
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
virus receptor activityEpidermal growth factor receptorHomo sapiens (human)
chromatin bindingEpidermal growth factor receptorHomo sapiens (human)
double-stranded DNA bindingEpidermal growth factor receptorHomo sapiens (human)
MAP kinase kinase kinase activityEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane signaling receptor activityEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor receptor activityEpidermal growth factor receptorHomo sapiens (human)
integrin bindingEpidermal growth factor receptorHomo sapiens (human)
protein bindingEpidermal growth factor receptorHomo sapiens (human)
calmodulin bindingEpidermal growth factor receptorHomo sapiens (human)
ATP bindingEpidermal growth factor receptorHomo sapiens (human)
enzyme bindingEpidermal growth factor receptorHomo sapiens (human)
kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein kinase bindingEpidermal growth factor receptorHomo sapiens (human)
protein phosphatase bindingEpidermal growth factor receptorHomo sapiens (human)
protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
transmembrane receptor protein tyrosine kinase activator activityEpidermal growth factor receptorHomo sapiens (human)
ubiquitin protein ligase bindingEpidermal growth factor receptorHomo sapiens (human)
identical protein bindingEpidermal growth factor receptorHomo sapiens (human)
cadherin bindingEpidermal growth factor receptorHomo sapiens (human)
actin filament bindingEpidermal growth factor receptorHomo sapiens (human)
ATPase bindingEpidermal growth factor receptorHomo sapiens (human)
epidermal growth factor bindingEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (26)

Processvia Protein(s)Taxonomy
endosomeEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
ruffle membraneEpidermal growth factor receptorHomo sapiens (human)
Golgi membraneEpidermal growth factor receptorHomo sapiens (human)
extracellular spaceEpidermal growth factor receptorHomo sapiens (human)
nucleusEpidermal growth factor receptorHomo sapiens (human)
cytoplasmEpidermal growth factor receptorHomo sapiens (human)
endosomeEpidermal growth factor receptorHomo sapiens (human)
endoplasmic reticulum membraneEpidermal growth factor receptorHomo sapiens (human)
plasma membraneEpidermal growth factor receptorHomo sapiens (human)
focal adhesionEpidermal growth factor receptorHomo sapiens (human)
cell surfaceEpidermal growth factor receptorHomo sapiens (human)
endosome membraneEpidermal growth factor receptorHomo sapiens (human)
membraneEpidermal growth factor receptorHomo sapiens (human)
basolateral plasma membraneEpidermal growth factor receptorHomo sapiens (human)
apical plasma membraneEpidermal growth factor receptorHomo sapiens (human)
cell junctionEpidermal growth factor receptorHomo sapiens (human)
clathrin-coated endocytic vesicle membraneEpidermal growth factor receptorHomo sapiens (human)
early endosome membraneEpidermal growth factor receptorHomo sapiens (human)
nuclear membraneEpidermal growth factor receptorHomo sapiens (human)
membrane raftEpidermal growth factor receptorHomo sapiens (human)
perinuclear region of cytoplasmEpidermal growth factor receptorHomo sapiens (human)
multivesicular body, internal vesicle lumenEpidermal growth factor receptorHomo sapiens (human)
intracellular vesicleEpidermal growth factor receptorHomo sapiens (human)
protein-containing complexEpidermal growth factor receptorHomo sapiens (human)
receptor complexEpidermal growth factor receptorHomo sapiens (human)
Shc-EGFR complexEpidermal growth factor receptorHomo sapiens (human)
basal plasma membraneEpidermal growth factor receptorHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID422946Inhibition of NADH fumarate reductase in Echinococcus multilocularis protoscolece2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
Anaerobic NADH-fumarate reductase system is predominant in the respiratory chain of Echinococcus multilocularis, providing a novel target for the chemotherapy of alveolar echinococcosis.
AID58159The concentration required to inhibit dihydrofolate reductase in rat liver1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
General distance geometry three-dimensional receptor model for diverse dihydrofolate reductase inhibitors.
AID1145385Inhibition of liver dihydrofolate reductase (unknown origin)1976Journal of medicinal chemistry, May, Volume: 19, Issue:5
Inhibition of dihydrofolate reductase. Structure-activity correlations of quinazolines.
AID69425Inhibitory potency against isolated epidermal growth factor receptor (EGFR) from human A431 carcinoma cells1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor.
AID1795547Kinase Inhibition Assay from Article 10.1021/jm9508651: \\Tyrosine Kinase Inhibitors. 10. Isomeric 4-[(3-Bromophenyl)amino]pyrido[d]- pyrimidines Are Potent ATP Binding Site Inhibitors of the Tyrosine Kinase Function of the Epidermal Growth Factor Receptor1996Journal of medicinal chemistry, Apr-26, Volume: 39, Issue:9
Tyrosine kinase inhibitors. 10. Isomeric 4-[(3-bromophenyl)amino]pyrido[d]-pyrimidines are potent ATP binding site inhibitors of the tyrosine kinase function of the epidermal growth factor receptor.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (18,579)

TimeframeStudies, This Drug (%)All Drugs %
pre-19902214 (11.92)18.7374
1990's1157 (6.23)18.2507
2000's5498 (29.59)29.6817
2010's8573 (46.14)24.3611
2020's1137 (6.12)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 46.16

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index46.16 (24.57)
Research Supply Index9.98 (2.92)
Research Growth Index5.00 (4.65)
Search Engine Demand Index79.95 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (46.16)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials2,417 (12.57%)5.53%
Reviews2,030 (10.55%)6.00%
Case Studies1,137 (5.91%)4.05%
Observational40 (0.21%)0.25%
Other13,611 (70.76%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]