Page last updated: 2024-12-05

hydrazine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

diamine : Any polyamine that contains two amino groups. [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 CID9321
CHEMBL ID1237174
CHEBI ID15571
MeSH IDM0093828

Synonyms (84)

Synonym
hydrazin
CHEBI:15571 ,
h2nnh2
n2h4
diamine
nitrogen hydride
hdz ,
diazane
hsdb 544
rcra waste number u133
rcra waste no. u133
hydrazine (anhydrous)
ccris 335
einecs 206-114-9
hydrazine (hydrazine sulfate)
hydrazine base
hydrazine, anhydrous
hydrazines ,
un3293
oxytreat 35
levoxine
hydrazyna [polish]
un2029
hydrazine ,
C05361
302-01-2
hydrazine, anhydrous, 98%
hydrazine/hydrazine sulfate
AKOS000269060
H0172
H0204
NCGC00188947-01
CHEMBL1237174
H0697
STL281862
27rfh0gb4r ,
unii-27rfh0gb4r
hydrazyna
isoniazid impurity e [ep impurity]
hydrazine [mi]
h 70 (fuel)
hydrazine [hsdb]
hydrazine [who-dd]
allopurinol impurity f [ep impurity]
nitrogen hydride (n2h4)
hydrazine [iarc]
hydrazine anhydrous
hzn ,
amino nitrogen
CREXVNNSNOKDHW-UHFFFAOYSA-N
nh2nh2
nh2-nh2
zerox (salt/mix)
scav-ox ii (salt/mix)
amerzine (salt/mix)
nitrogen hydride, (n2h4)
catalyzed hydrazine (salt/mix)
un 2029 (salt/mix)
un 2030 (salt/mix)
DTXSID3020702 ,
mfcd00011417
J-017830
scav-ox ii
hydrazine (hydrazine sulphate)
zerox
amerzine
catalyzed hydrazine
BP-13613
119775-10-9
Q27110398
Q58447
diamine, hydrazine base
dtxcid30702
isoniazid impurity e (ep impurity)
hydrazine aqueous solution
hydrazine, (anhydrous)
hydrazine fume
(anhydrous)
hidrazine
hydrazine (iarc)
allopurinol impurity f (ep impurity)
diamidogen
hydrazine standard: n2h4 @ 1000 mg/l in 1% acetic acid
hydrazine standard: n2h4 @ 100 mg/l in 1% acetic acid

Research Excerpts

Overview

Hydrazine is a widely used but highly toxic chemical reagent. The development of a fluorescent probe for hydrazine detection is very meaningful. Hydrazine can cause DNA lesions and cancer.

ExcerptReferenceRelevance
"Hydrazine is a well-known RNA-specific reagent, already extensively used in the past for RNA sequencing and structural probing."( Analysis of pseudouridines and other RNA modifications using HydraPsiSeq protocol.
Bourguignon-Igel, V; Helm, M; Marchand, V; Motorin, Y, 2022
)
1.44
"Hydrazine is a widely used but highly toxic chemical reagent, and the development of a fluorescent probe for hydrazine detection is very meaningful. "( Coumarin 1,4-enedione for selective detection of hydrazine in aqueous solution and fluorescence imaging in living cells.
Hu, S; Li, Q; Luo, M; Shen, P; Su, Z; Wang, J; Wu, Z, 2021
)
2.32
"Hydrazine is a substrate for bacterial HAO, while phenylhydrazine is a suicide inhibitor of HAO."( Hydrazines as Substrates and Inhibitors of the Archaeal Ammonia Oxidation Pathway.
Crombie, AT; Lehtovirta-Morley, LE; Murrell, JC; Schatteman, A; Wright, CL, 2022
)
2.89
"Hydrazine is a genotoxic substance, which can cause DNA lesions and cancer"( Monitoring isoniazid metabolism
Ran, J; Wang, X; Xu, H; Yuan, Z; Zhang, J; Zhu, J, 2022
)
1.44
"As hydrazine is an environmental pollutant and highly toxic to living organisms, selective and rapid detection is highly needed for the benefit of living organisms as well as the environment. "( A benzothiazole-based dual reaction site fluorescent probe for the selective detection of hydrazine in water and live cells.
Banik, D; Halder, S; Jana, K; Karak, A; Mahapatra, AK; Maiti, A; Mandal, M; Manna, SK, 2022
)
1.56
"Hydrazine is an essential chemical in industries, but its high toxicity poses great threats to human health and environmental safety. "( A smartphone-adaptable chromogenic and fluorogenic sensor for rapid visual detection of toxic hydrazine in the environment.
Zeng, L; Zhang, J; Zuo, K, 2022
)
2.38
"Hydrazine is a rodent carcinogen and is classified as a probable human carcinogen by IARC. "( Exploring the molecular and functional cellular response to hydrazine via transcriptomics and DNA repair mutant cell lines.
Brayman, TG; Ciurlionis, R; Crosby, ME; Kondratiuk, A; Nicolette, JJ, 2022
)
2.41
"Hydrazine is an important catalyst and chemical raw material. "( A New Fluorescent Turn-on Dual Interaction Position Probe for Determination of Hydrazine.
Li, W; Li, X; Liu, W; Xu, W; Yang, Y; Yin, J, 2019
)
2.18
"Hydrazine is a kind of widely used industrial raw material and a toxic biochemical reagent. "( A coumarin-fused 'off-on' fluorescent probe for highly selective detection of hydrazine.
Guo, Z; Li, X; Ma, J; Wang, M; Wang, X; Wei, C; Yang, Z; Zhang, J, 2020
)
2.23
"Hydrazine is an important industrial chemical and fuel that has attracted considerable attention for use in liquid fuel cells. "( Electrochemical Strategy for Hydrazine Synthesis: Development and Overpotential Analysis of Methods for Oxidative N-N Coupling of an Ammonia Surrogate.
Bates, DM; Gerken, JB; Kim, YJ; Stahl, SS; Wang, F, 2020
)
2.29
"The hydrazine group serves as a great anchor for bioconjugation; however, the application of hydrazone ligation has been limited by poor product stability. "( Further Exploration of Hydrazine-Mediated Bioconjugation Chemistries.
Hymel, D; Liu, F; Mailig, M, 2020
)
1.43
"Hydrazine is a well-known genotoxic impurity which may be present in some important drugs, such as isoniazid and hydralazine. "( A selective and sensitive near-infrared fluorescent probe for in vivo real time tracking of exogenous and metabolized hydrazine, a genotoxic impurity.
Huang, W; Li, Z; Liu, J; Qi, Q; Song, L; Wang, S, 2020
)
2.21
"Hydrazine is a highly toxic and flammable liquid that can damage human liver, kidney, and central nervous system. "( A novel ESIPT fluorescent probe derived from 3-hydroxyphthalimide for hydrazine detection in aqueous solution and living cells.
Chen, X; Hou, Y; Hu, S; Luo, M; Wang, J; Wu, Z, 2021
)
2.3
"Hydrazine is a useful building block in the synthesis of organic pharmaceuticals but it is highly toxic so its determination at low ppm range is required. "( Hydrazine determination in allopurinol using derivatization and SPE for sample preparation.
Kormány, R; Tamás, K; Wachter-Kiss, E, 2018
)
3.37
"Hydrazine is an important industrial material yet highly toxic and extremely harmful to people's health when over-exposed in the environment, thus monitoring hydrazine is of great significance. "( A new quinoline-derived highly-sensitive fluorescent probe for the detection of hydrazine with excellent large-emission-shift ratiometric response.
Liang, W; Stadler, FJ; Wang, J; Wu, Q; Zhang, W; Zheng, J, 2019
)
2.18
"Hydrazine is an intermediate product of the anaerobic ammonium oxidation (Anammox) process where both ammonium and nitrite in wastewater are converted to nitrogen gas by bacteria. "( Effect of external hydrazine addition on anammox reactor start-up time.
Ganesan, S; Vadivelu, VM, 2019
)
2.29
"Hydrazine is a substance harmful to humans and the environment, necessitating the development of a sensitive and specific detection method. "( A novel chemiluminescent probe for hydrazine detection in water and HeLa cells.
Dou, Y; Jiang, J; Liu, J; Liu, X; Qu, J; Zhang, F; Zhu, Q, 2019
)
2.23
"Hydrazine (N2H4) is a known genotoxic impurity that typically needs to be controlled down to low ppm level in pharmaceutical development. "( A simple and sensitive method to analyze genotoxic impurity hydrazine in pharmaceutical materials.
Wang, J; Yang, S; Zhang, K, 2016
)
2.12
"Hydrazine (N(2)H(4)) is a clear, inorganic colourless liquid. "( Multiple basal cell carcinomas after long-term exposure to hydrazine: case report and review of the literature.
Aigner, BA; Darsow, U; Grosber, M; Plötz, SG; Ring, J, 2010
)
2.05
"Hydrazine is an important industrial chemical but also very toxic thus requiring rapid detection agents. "( An ICT-based ratiometric probe for hydrazine and its application in live cells.
Cao, J; Cheng, G; Dong, H; Fan, J; Hu, M; Liu, Y; Peng, X; Song, K; Sun, S; Sun, W, 2012
)
2.1
"Hydrazine (HzN) is an aircraft fuel and propellant used by the U.S. "( Cellular toxicity of hydrazine in primary rat hepatocytes.
Frazier, JM; Hussain, SM, 2002
)
2.08
"Hydrazine is a relatively poor substrate for the wild-type (alpha-70(Val)) MoFe protein."( Substrate interaction at an iron-sulfur face of the FeMo-cofactor during nitrogenase catalysis.
Barney, BM; Dean, DR; Dos Santos, PC; Igarashi, RY; Seefeldt, LC, 2004
)
1.04
"Hydrazine is a model toxin that induces both hepatotoxic and neurotoxic effects in experimental animals. "( Integrated metabonomic analysis of the multiorgan effects of hydrazine toxicity in the rat.
Bollard, ME; Connelly, J; Connor, SC; Garrod, S; Holmes, E; Nicholls, AW; Nicholson, JK, 2005
)
2.01
"Hydrazine sulfate is an in vitro mutagen that induces lung and liver tumours in mice."( Evidence for in vivo non-mutagenicity of the carcinogen hydrazine sulfate in target tissues of lacZ transgenic mice.
Douglas, GR; Gingerich, JD; Soper, LM, 1995
)
1.26
"Hydrazine sulfate is a controversial agent that was originally studied in cancer patients approximately 20 years ago. "( Randomized placebo-controlled evaluation of hydrazine sulfate in patients with advanced colorectal cancer.
Cobau, CD; Gerstner, JB; Gesme, DH; Goldberg, RM; Kuross, SA; Loprinzi, CL; O'Fallon, JR; Rospond, RM, 1994
)
1.99
"Hydrazine is a more potent acute toxicant in the neonate than in the adult rat."( Hydrazine genotoxicity in the neonatal rat.
Leakakos, T; Shank, RC, 1994
)
2.45
"Hydrazine sulfate is a genotoxic hepatocarcinogen for the hamster. "( Changes in methyl-sensitive restriction sites of liver DNA from hamsters chronically exposed to hydrazine sulfate.
Shank, RC; Zheng, H, 1996
)
1.95
"Hydrazine reagents are a well-known group of derivatizing agents for the determination of aldehydes and ketones in liquid and gaseous samples. "( Hydrazine reagents as derivatizing agents in environmental analysis--a critical review.
Büldt, A; Karst, U; Vogel, M, 2000
)
3.19
"Hydrazine is an aircraft fuel and propellant used by the US Air Force. "( In vitro toxicity assessment of a new series of high energy compounds.
Frazier, JM; Hussain, SM, 2001
)
1.75
"Hydrazine sulfate is an anticachexia agent which interrupts host energy wasting as a result of the malignant process. "( Hydrazine sulfate: a current perspective.
Gold, J, 1987
)
3.16

Effects

Hydrazine has a wide range of industrial applications, but it is also a toxic and explosive chemical substance, which brings potential risks to human health and environmental safety. It has been described as a mutagenic, probable human carcinogen.

ExcerptReferenceRelevance
"Hydrazine has a wide range of industrial applications, but it is also a toxic and explosive chemical substance, which brings potential risks to human health and environmental safety. "( Design of a ratiometric near-infrared fluorescent probe with double excitation for hydrazine detection in vitro and in vivo.
Lai, Y; Lin, W; Zhang, T, 2022
)
2.39
"Hydrazine has a wide range of industrial applications, but it is also a toxic and explosive chemical substance, which brings potential risks to human health and environmental safety. "( Design of a ratiometric near-infrared fluorescent probe with double excitation for hydrazine detection in vitro and in vivo.
Lai, Y; Lin, W; Zhang, T, 2022
)
2.39
"Hydrazine has been described as a mutagenic, probable human carcinogen. "( In vitro and in vivo mammalian mutation assays support a nonmutagenic mechanism of carcinogenicity for hydrazine.
Crosby, M; Kondratiuk, A; Murray, J; Nicolette, J; Sonders, P, 2021
)
2.28
"Hydrazine has been applied diffusely in most of the chemical industry; however, it is a hazardous environmental pollutant and highly toxic to organisms. "( Naked-eye and near-infrared fluorescence probe for hydrazine and its applications in in vitro and in vivo bioimaging.
Liu, J; Liu, X; Ning, L; Wang, J; Yao, X; Yu, B; Zhang, H; Zhang, J; Zhang, Z, 2015
)
2.11
"Hydrazine (N2H4), which has been categorized as a weak carcinogen, is a chemical with the one of the largest production rates in Japan. "( Evidence on N-acetyltransferase allele-associated metabolism of hydrazine in Japanese workers.
Imamiya, S; Koizumi, A; Miyauchi, H; Nomiyama, T; Omae, K; Sakurai, H; Tanaka, S; Tsukada, M; Wada, Y, 1998
)
1.98
"Hydrazine has been reported to be metabolised by NADPH cytochrome P-450 reductase (reductase) to reactive and potentially toxic intermediates."( The role of l-thyroxine and hepatic reductase activity in isoniazid-induced hepatotoxicity in rabbits.
Adams, SP; Sarich, TC; Wright, JM, 1998
)
1.02
"Hydrazine has been used to remove organic components and to isolate the mineral(s) from human calculus. "( A micro-Raman spectroscopic study of hydrazine-treated human dental calculus.
Arends, J; Jongebloed, WL; Stokroos, I; Tsuda, H, 1996
)
2.01
"Hydrazines have been found naturally in tobacco and mushrooms. "( Hydrazines as mutagens in a histidine-requiring auxotroph of Salmonella typhimurium.
Hoffmann, D; Schmeltz, I; Tosk, J, 1979
)
3.15
"Hydrazine has been identified by gas chromatography-mass spectrometry in the 0- to 24-hr urine of patients administered hydralazine. "( Identification and quantitation of hydrazine in the urine of patients treated with hydralazine.
Harland, SJ; Timbrell, JA, 1979
)
1.98
"Hydrazine has not previously been shown to have any carcinogenic action in man. "( On the question of the carcinogenic action of hydrazine--evaluation on the basis of new experimental results.
Mohr, U; Schmidt, WM; Steinhoff, D, 1990
)
1.98
"Hydrazine has been shown to be a specific inhibitor of gluconeogenesis, causing a metabolic crossover at the step catalyzed by phosphoenolpyruvate carboxykinase."( Modulation of endotoxin lethality in mice by hydrazine sulfate.
Christoffersen, CA; Morrison, DC; Silverstein, R, 1989
)
1.26

Actions

Hydrazine plays an important role in chemistry, pharmaceuticals, agriculture and aerospace. Hydrazine can cause mitochondrial injury, which can lead to mitochondrial oxidant stress and impairment of energy homeostasis.

ExcerptReferenceRelevance
"Hydrazine plays an important role in chemistry, pharmaceuticals, agriculture and aerospace. "( A novel colorimetric and ratiometric fluorescence probe based on 'C-CN' for detection of hydrazine and its imaging in living cells and mouse.
He, Q; Jiang, C; Yan, LJ; Yao, C; Ye, AY, 2022
)
2.39
"hydrazine) can cause mitochondrial injury, which can lead to mitochondrial oxidant stress and impairment of energy homeostasis."( Mechanisms of isoniazid-induced idiosyncratic liver injury: emerging role of mitochondrial stress.
Boelsterli, UA; Lee, KK, 2014
)
1.12
"Hydrazine is known to cause cancer in animals after skin exposure and is used to induce angiosarcomas in mice after cutaneous exposure."( Epithelioid sarcoma of the thumb associated with hydrazine fuel exposure: a case report.
Helmers, S; Jacob, LN; Ruland, RT, 2004
)
1.3
"Hydrazine does not produce detectable single-strand breaks or alkali-labile sites in the treated DNA nor gaps in DNA newly synthesized after treatment."( Fixation and loss of hydrazine-induced premutational damage in Haemophilus influenzae.
Hirsch, BF; Kimball, RF, 1976
)
1.3
"Hydrazine was able to produce chlorophyll mutations in the M1-generation itself if applied alone, in a mixture or as a last treatment in a sequence."( Mutagenic activity of hydrazine and its combinations with maleic mydrazide and X-rays in barley.
Kak, SN; Kaul, BL, 1975
)
1.29
"Hydrazine was found to cause a dose-dependent depletion of hepatic ATP in vivo 3 h after dosing."( Course of ATP depletion in hydrazine hepatotoxicity.
Ghatineh, S; Preece, NE; Timbrell, JA, 1990
)
1.3
"Hydrazine did not cause either ethane expiration or MDA formation."( Investigation of lipid peroxidation induced by hydrazine compounds in vivo in the rat.
Preece, NE; Timbrell, JA, 1989
)
1.26
"The hydrazine-induced increase in PAP activity and TG accumulation was completely prevented by adrenalectomy."( The effects of hydrazine on the phosphatidate phosphohydrolase activity in rat liver.
Haghighi, B; Honarjou, S, 1987
)
1.11
"4. Hydrazine does not inhibit monoamine oxidase unless a substrate and oxygen are present."( Inhibition of monoamine oxidase by substituted hydrazines.
Tipton, KF, 1972
)
1.02

Treatment

Hydrazine treatment is used to release mucin-type O-glycans from glycoproteins. Treatment induced altered expression of proteins related to lipid metabolism, Ca(2+) homeostasis, thyroid hormone pathways and stress response.

ExcerptReferenceRelevance
"Hydrazine treatment is frequently used for releasing mucin-type O-glycans (O-glycans) from glycoproteins because the method provides O-glycans that retain a reducible GalNAc at their reducing end, which is available for fluorescent labeling. "( Malonic acid suppresses mucin-type O-glycan degradation during hydrazine treatment of glycoproteins.
Goso, Y, 2016
)
2.12
"Hydrazine treatment induced altered expression of proteins related to lipid metabolism, Ca(2+) homeostasis, thyroid hormone pathways and stress response."( Mechanisms of hydrazine toxicity in rat liver investigated by proteomics and multivariate data analysis.
Baunsgaard, D; Jensen, ON; Kjeldal, HØ; Klenø, TG; Laursen, SM; Leonardsen, LR, 2004
)
1.41
"Hydrazine treatment, however, elevated the pyridoxal level in liver, while kidney pyridoxal level remained unaltered under the same condition."( Regulation of formation in vivo of pyridoxal phosphate in hydrazine-treated rats.
Chatterjee, AK; Sengupta, K, 1980
)
1.23
"Hydrazine sulfate pretreatment has previously been shown in our laboratory to protect normal mice against endotoxin and D-galactosamine-sensitized mice against both exogenous tumor necrosis factor (TNF) and endotoxin. "( Contribution of tumor necrosis factor-alpha and glucocorticoid in hydrazine sulfate-mediated protection against endotoxin lethality.
Freudenberg, MA; Galanos, C; Gonzalez, JC; Jia, F; Johnson, DC; Morrison, DC; Silverstein, R, 1994
)
1.97
"The hydrazine treatment did not produce such an effect."( A critical evaluation of the purification of biominerals by hypochlorite treatment.
Brown, WE; Eanes, ED; Tomazic, BB, 1993
)
0.77
"Hydrazine-hydrate treatment (inactivation of C3 of the complement system) and exposure of fresh human serum to dithiothreitol completely abolished serum bactericidal activity."( Further characterization of "promptly" and "delayed" human serum-sensitive strains of Serratia marcescens.
Fukushima, PI; Traub, WH, 1979
)
0.98
"Hydrazine treatment also increased the incorporation of [1,3-14C]glycerol into hepatic triacylglycerol by the intact animal."( Effect of hydrazine exposure on hepatic triacylglycerol biosynthesis.
Banks, WL; Lamb, RG, 1979
)
1.38
"Hydrazine sulfate pretreatment also protects D-galactosamine-sensitized mice against the lethal effects of injected tumor necrosis factor/cachectin."( Hydrazine sulfate protects D-galactosamine-sensitized mice against endotoxin and tumor necrosis factor/cachectin lethality: evidence of a role for the pituitary.
Christoffersen, CA; Johnson, DC; Morrison, DC; Silverstein, R; Turley, BR, 1991
)
2.45
"The hydrazine treatment was performed for 10 minutes in order to remove the levulinyl group on controlled pore glass."( 5'-Levulinyl and 2'-tetrahydrofuranyl protection for the synthesis of oligoribonucleotides by the phosphoramidite approach.
Iwai, S; Ohtsuka, E, 1988
)
0.76
"Hydrazine treatment of 4 hr duration stimulated equally kidney ornithine decarboxylase activities of nondiabetic and diabetic rats."( Hydrazine stress in the diabetic: ornithine decarboxylase activity.
Chan, W; Higgins, ES; Rogers, KS, 1988
)
2.44
"The treatment with hydrazine sulfate (60 mg/kg) plus thiophosphamide (1 mg/kg) resulted in suppression of tumor growth up to 90%, the dosage of thiophosphamide being therapeutically ineffective."( [Selective action of hydrazine sulfate in combination with thiophosphamide on tumor cell mitochondria].
Filov, VA; Golovatova, VA; Tret'iakov, AV, 1982
)
0.9
"Rats treated with hydrazine and pharmacological doses of alpha-tocopherol accumulated higher concentrations of vitamin E in all studied tissues compared with the alpha-tocopherol-only treated rats."( Content and redistribution of vitamin E in tissues of Wistar rats under oxidative stress induced by hydrazine.
Antosiewicz, J; Kaczor, JJ; Matuszkiewicz, A; Olek, RA; Popinigis, J; Wakabayashi, T; Ziółkowski, W, 2002
)
0.85

Toxicity

Hydrazines are highly toxic inorganic liquids that are used as propellants in military and aviation industries, such as the U.S. Air Force. Despite recent research efforts to generate less toxic alternatives to hydrazine fuel, it will likely continue to have a role in military or aviation industries.

ExcerptReferenceRelevance
" The overall effect of isoniazid in vivo was to increase metabolism of acetylhydrazine through the microsomal pathway leading to increased covalent binding of the toxic reactive intermediate to liver protein."( Studies on the role of acetylhydrazine in isoniazid hepatotoxicity.
Timbrell, JA, 1979
)
0.78
" The findings clearly showed that all four chemicals exerted a stronger toxic effect in male than in female mice."( Sex dependent toxicity of four chemicals.
Erickson, J; Issenberg, P; Shimizu, H; Sornson, H; Toth, B, 1975
)
0.25
" The generalized conception of the toxic effect of the derivatives is suggested."( [New molecular criteria for assessing the toxic action of hydrazine derivatives. Active forms of oxygen as the key agents in the mechanism of toxicity].
Avakian, AKh,
)
0.38
" Toxic effects included depression of growth, decreased feed intake, and increased feed conversion."( Toxicity of 1,2-diethylhydrazine fed to turkey poults.
Czarnecki, CM, 1989
)
0.59
" The inner salts were appreciably less toxic than the hydrazinium diiodides in brine shrimp testing."( 2,2'-Phthaloyl-,2,2'-isophthaloyl-, and 2,2'-terephthaloylbis[1,1,1-trimethylhydrazinium] dihydroxide, bis(inner salts): synthesis, partition coefficients, toxicity and effect on ganglionic transmission.
Alkadhi, KA; Basrur, JP; Cates, LA; Li, VS, 1986
)
0.27
" Toxic effects of hydrazine fuels on humans and animals as well as in vitro studies are discussed with emphasis on recent findings and USAF studies."( Toxicity assessment of hydrazine fuels.
Keller, WC, 1988
)
0.92
" All chemicals were toxic to strain TA1538."( Mutagenicity and toxicity of carcinogenic and other hydrazine derivatives: correlation between toxic potency in animals and toxic potency in Salmonella typhimurium TA1538.
Malca-Mor, L; Stark, AA, 1982
)
0.51
" The threshold dose for the toxic effect is around 10 mg/kg, and the optimal effect is seen after a dose of 40 mg/kg."( Studies on hydrazine hepatotoxicity. 2. Biochemical findings.
Scales, MD; Streeter, AJ; Timbrell, JA, 1982
)
0.65
" The possible adverse effects of RH-5992 on nontarget aquatic organisms were studied in two test systems."( Toxicity of a new molt-inducing insecticide (RH-5992) to aquatic macroinvertebrates.
Capell, SS; Eichenberg, DC; Kreutzweiser, DP; Wainio-Keizer, KL, 1994
)
0.29
"Intracellular killing of Leishmania parasites within activated murine macrophages is thought to result from the toxic activities of nitrogen oxidation products (referred to as NO) released by the activated cells."( Leishmania spp.: mechanisms of toxicity of nitrogen oxidation products.
Mauël, J; Ransijn, A, 1997
)
0.3
"Several hydrazine derivatives (HD) tested so far have pharmacological activities, but many also have toxic side effects, including carcinogenesis."( Contribution of hydrazines-derived alkyl radicals to cytotoxicity and transformation induced in normal c-myc-overexpressing mouse fibroblasts.
Armelin, MC; Cidade, MR; Gamberini, M; Leite, LC; Valotta, LA, 1998
)
1.08
" Three carbon sugars, such as glyceraldehyde and dihydroxy acetone, and the two carbon sugar glycolaldehyde, were similarly toxic in an O-2-dependent manner."( Superoxide dependence of the toxicity of short chain sugars.
Benov, L; Fridovich, I, 1998
)
0.3
" Hydrazine has been reported to be metabolised by NADPH cytochrome P-450 reductase (reductase) to reactive and potentially toxic intermediates."( The role of l-thyroxine and hepatic reductase activity in isoniazid-induced hepatotoxicity in rabbits.
Adams, SP; Sarich, TC; Wright, JM, 1998
)
1.21
" Methoxyfenozide was the most toxic followed by tebufenozide, halofenozide, and RH-5849."( Significance of absorption, oxidation, and binding to toxicity of four ecdysone agonists in multi-resistant cotton leafworm.
Carton, B; Decombel, L; Smagghe, G; Tirry, L, 2001
)
0.31
" Although HECs are reliable constituents of powered propellant systems, they constitute an important class of toxic agents to which military and civilian personnel can be exposed."( In vitro toxicity assessment of a new series of high energy compounds.
Frazier, JM; Hussain, SM, 2001
)
0.31
" While two of the bisacylhydrazines (coded as RH-5992 and RH-2485) are predominantly toxic to lepidopteran pests, RH-5849, which has not been commercialized, has a broader spectrum of toxicity."( Comparative toxicity and ecdysone receptor affinity of non-steroidal ecdysone agonists and 20-hydroxyecdysone in Chironomus tentans.
Dhadialla, TS; Lezzi, M; Smagghe, G, 2002
)
0.62
" Descriptors comprising the QSARs for MTT were consistent with the biophysical mechanism of toxic response found experimentally for hydrazine derivatives."( Risk assessment of high-energy chemicals by in vitro toxicity screening and quantitative structure-activity relationships.
Frazier, JM; Hussain, SM; Pachter, R; Trohalaki, S; Zellmer, RJ, 2002
)
0.52
" Based on viability data, exposure to 50 mM HzN for 2 h is a marginally toxic dose while 75 mM is a significantly toxic dose."( Involvement of apoptosis in hydrazine induced toxicity in rat primary hepatocytes.
Frazier, JM; Hussain, SM, 2003
)
0.61
"5-fold less toxic in terms of LD50 values against last-instar larvae of a greenhouse-selected strain of the beet armyworm Spodoptera exigua (Hübner) that was collected in July 2001 in an experimental greenhouse for resistance at Murcia in southern Spain, in comparison with a laboratory susceptible strain."( Toxicity and kinetics of methoxyfenozide in greenhouse-selected Spodoptera exigua (Lepidoptera: Noctuidae).
Budia, F; Carton, B; Del Estal, P; Pineda, S; Smagghe, G; Viñuela, E, 2003
)
0.32
" The absolute toxic dose was 50 mg/kg/day and the level at which no adverse effects were observed was 2 mg/kg/day for male and female dogs."( Subacute toxicity and toxicokinetics of CJ-10882, a type IV phosphodiesterase inhibitor, after 4-week repeated oral administration in dogs.
Han, J; Kim, B; Kim, JC; Shin, HC, 2004
)
0.32
" The MN test and comet assay revealed potential adverse effects of the two pesticides on DNA in the erythrocytes of amphibians in aquatic and agricultural ecosystems."( Acute toxicity and genotoxicity of two novel pesticides on amphibian, Rana N. Hallowell.
Feng, S; Kong, Z; Peng, P; Wang, X; Zhao, L, 2004
)
0.32
" The abundance of mRNA was investigated on cDNA microarrays containing 699 rat-specific genes involved in toxic responses."( Combination of 'omics' data to investigate the mechanism(s) of hydrazine-induced hepatotoxicity in rats and to identify potential biomarkers.
Baunsgaard, D; Kiehr, B; Klenø, TG; Sidelmann, UG,
)
0.37
" By 168 h postdose, NMR spectral profiles of treated rats appeared similar to those of matched controls for all tissue types indicative of recovery from toxic insult."( Integrated metabonomic analysis of the multiorgan effects of hydrazine toxicity in the rat.
Bollard, ME; Connelly, J; Connor, SC; Garrod, S; Holmes, E; Nicholls, AW; Nicholson, JK, 2005
)
0.57
" Metabolic principal component (PC) trajectories highlighted the greater degree of toxic response in the rat."( Comparative metabonomics of differential hydrazine toxicity in the rat and mouse.
Antti, H; Beckonert, O; Bollard, ME; Cantor, GH; Ebbels, TM; Holmes, E; Keun, HC; Lindon, JC; Nicholls, AW; Nicholson, JK; Shockcor, JP; Stevens, G, 2005
)
0.59
" The cytogenetic techniques and comet assay revealed potential adverse effects of both imidacloprid and RH-5849 in human peripheral blood lymphocytes in vitro."( Assessing the genotoxicity of imidacloprid and RH-5849 in human peripheral blood lymphocytes in vitro with comet assay and cytogenetic tests.
Feng, S; Kong, Z; Peng, P; Wang, X; Zeng, EY, 2005
)
0.33
" These results indicate that radiolabeled melanin-binding peptides are efficient and safe in treatment of melanoma and could be potentially useful against this tumor."( Radiolabeled melanin-binding peptides are safe and effective in treatment of human pigmented melanoma in a mouse model of disease.
Bryan, RA; Casadevall, A; Dadachova, E; Huang, X; Mints, L; Moadel, T; Nosanchuk, JD; Nosanchuk, JS; Ortiz, G; Revskaya, E; Schweitzer, AD; Zhang, T, 2006
)
0.33
" All of these effects of ATR were observed at levels that were not toxic to the tissue, as LDH release into the medium (lactate dehydrogenase, an index of non-specific cytotoxicity) was not affected by ATR."( Dopaminergic toxicity of the herbicide atrazine in rat striatal slices.
Carr, RL; Filipov, NM; Sistrunk, SC; Stewart, MA, 2007
)
0.34
" Endosulfan and cypermethrin were highly toxic towards eggs and larvae with mortality rates ranging from 80% to 100%."( Side effects of conventional and non-conventional insecticides on eggs and larvae of Chrysoperla externa (Hagen) (Neuroptera: Chrysopidae) in Argentine.
Pineda, P; Schneider, MI; Smagghe, G, 2006
)
0.33
" In addition, a short-term toxicity assessment in rats was also conducted for the identification of certain toxic effects of AG after heat processing."( Increase in the free radical scavenging activities of American ginseng by heat processing and its safety evaluation.
Kang, KS; Kim, HY; Okamoto, T; Sei, Y; Yamabe, N; Yokozawa, T, 2007
)
0.34
" These results implicated H2O2, a cellular mediator of inflammation, as a potential risk factor for the manifestation of adverse drug reactions, particularly those caused by hydrazine containing drugs."( Role of hydrazine in isoniazid-induced hepatotoxicity in a hepatocyte inflammation model.
Mashregi, M; O'Brien, PJ; Tafazoli, S, 2008
)
0.97
" Metabolism and the formation of toxic metabolites of the TB drugs may play an important role in the development of ATDH."( Isoniazid and its toxic metabolite hydrazine induce in vitro pyrazinamide toxicity.
Aarnoutse, RE; Boeree, MJ; Dekhuijzen, PN; Peters, WH; Roelofs, HM; Tostmann, A; van der Ven, AJ, 2008
)
0.62
" Patients and the public expect that safe and cost-effective cataract medical care with N-acetylcarnosine therapeutic platform should be commissioned for them."( State of the art clinical efficacy and safety evaluation of N-acetylcarnosine dipeptide ophthalmic prodrug. Principles for the delivery, self-bioactivation, molecular targets and interaction with a highly evolved histidyl-hydrazide structure in the treatm
Babizhayev, MA; Kasus-Jacobi, A, 2009
)
0.35
" Toxicity was more severe in germ-free rats compared with conventional rats for equivalent exposures indicating that bacterial presence altered the nature or extent of response to hydrazine and that the toxic response can vary markedly in the absence of a functional microbiome."( Gut microbiome modulates the toxicity of hydrazine: a metabonomic study.
Abecia, L; Costabile, A; Gibson, G; Holmes, E; Jones, H; Nicholson, J; Roberts, D; Sidaway, J; Swann, J; Tuohy, K; Wang, Y; Wilson, ID, 2009
)
0.81
" There was no notable difference in adverse event frequency across eltrombopag doses."( Clinical pharmacokinetics, platelet response, and safety of eltrombopag at supratherapeutic doses of up to 200 mg once daily in healthy volunteers.
Bowen, C; Jenkins, J; Matthys, G; McGuire, S; Park, JW; Peng, B; Williams, D; Wire, MB, 2011
)
0.37
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
0.36
" The most commonly reported adverse events across all study arms (including placebo) were nausea and alopecia and eltrombopag was generally well tolerated."( A randomized, double-blind, placebo-controlled, dose ranging study to assess the efficacy and safety of eltrombopag in patients receiving carboplatin/paclitaxel for advanced solid tumors.
Bondarenko, IN; Jagiello-Gruszfeld, A; Kellum, A; Messam, C; Mostafa Kamel, Y; Patwardhan, R, 2010
)
0.36
"The new analytical method using Quick, Easy, Cheap, Effective, Rugged, and Safe (QuEChERS) procedure for simultaneous determination of diacylhydrazine insecticide residues in fruits and vegetables was developed using ultra-performance liquid chromatography coupled with tandem mass spectrometry (UPLC-MS/MS)."( Residue analysis of four diacylhydrazine insecticides in fruits and vegetables by Quick, Easy, Cheap, Effective, Rugged, and Safe (QuEChERS) method using ultra-performance liquid chromatography coupled to tandem mass spectrometry.
Dong, F; Li, Y; Liu, X; Song, W; Xu, J; Zheng, Y, 2011
)
0.86
", fungi that produce toxic aflatoxins."( Effects of a naturally occurring and a synthetic synergist on toxicity of three insecticides and a phytochemical to navel orangeworm (Lepidoptera: Pyralidae).
Berenbaum, MR; Lawrance, A; Niu, G; Pollock, HS; Siegel, JP, 2012
)
0.38
" Most adverse events reported were grade 1 or 2; 2 patients in the 37."( Efficacy and safety of eltrombopag in Japanese patients with chronic liver disease and thrombocytopenia: a randomized, open-label, phase II study.
Fujiyama, S; Hattori, T; Katsura, K; Kawaguchi, T; Komori, A; Nakamuta, M; Oketani, M; Sakisaka, S; Sasaki, Y; Sata, M; Seike, M; Tanaka, M; Watanabe, H, 2012
)
0.38
" Thirty-eight patients (13%) experienced ≥ 1 adverse events leading to study withdrawal, including patients meeting protocol-defined withdrawal criteria (11 [4%] thromboembolic events, 5 [2%] exceeding liver enzyme thresholds)."( Safety and efficacy of eltrombopag for treatment of chronic immune thrombocytopenia: results of the long-term, open-label EXTEND study.
Arning, M; Bailey, CK; Brainsky, A; Bussel, JB; Cheng, G; Meyer, O; Saleh, MN, 2013
)
0.39
" The aim of this study was to establish the protective effects of taurine against cytotoxicity induced by isoniazid and its suspected toxic metabolite hydrazine in isolated rat hepatocytes by measuring reactive oxygen species (ROS) formation, lipid peroxidation, mitochondrial depolarisation, reduced glutathione (GSH), and oxidised glutathione (GSSG)."( Cytoprotective effects of taurine against toxicity induced by isoniazid and hydrazine in isolated rat hepatocytes.
Babaei, H; Eghbal, MA; Heidari, R, 2013
)
0.82
" Adverse events were similar to those reported with short-term use of eltrombopag, and none led to treatment discontinuation."( Oral eltrombopag for up to three years is safe and well-tolerated in Japanese patients with previously treated chronic immune thrombocytopenia: an open-label, extension study.
Hattori, T; Ikeda, Y; Ishii, K; Kanakura, Y; Katsura, K; Katsutani, S; Kimura, A; Kosugi, H; Miyakawa, Y; Ninomiya, H; Okamoto, S; Okoshi, Y; Tomiyama, Y, 2013
)
0.39
"Thrombocytopenia is an independent adverse prognostic factor in patients with Myelodysplastic syndromes (MDS)."( A pilot phase I dose finding safety study of the thrombopoietin-receptor agonist, eltrombopag, in patients with myelodysplastic syndrome treated with azacitidine.
Cherif, H; Chowdhury, O; Garelius, H; Hellström-Lindberg, E; Jacobsen, SE; Lorenz, F; Saft, L; Svensson, T, 2014
)
0.4
" Severe adverse events included infectious complications, deep vein thrombosis and transient ischaemic attack."( A pilot phase I dose finding safety study of the thrombopoietin-receptor agonist, eltrombopag, in patients with myelodysplastic syndrome treated with azacitidine.
Cherif, H; Chowdhury, O; Garelius, H; Hellström-Lindberg, E; Jacobsen, SE; Lorenz, F; Saft, L; Svensson, T, 2014
)
0.4
"The use of surfactants in the development of a suitable formulation for insecticides should improve the solubility behavior, the permeability and the efficiency against pests meanwhile decrease the toxic risks of insecticides on human health."( Synergistic effect of non-ionic surfactants Tween 80 and PEG6000 on cytotoxicity of insecticides.
Huang, Q; Li, D; Tao, L; Wu, X; Yu, X, 2015
)
0.42
" Hepatotoxicity and all other adverse events were mild and manageable."( Efficacy and safety of eltrombopag in treatment-refractory primary immune thrombocytopenia: a retrospective study.
Eser, A; Firatli-Tuglular, T; Kara, O; Kaygusuz-Atagunduz, I; Noyan-Atalay, F; Ozgumus, T; Pepedil-Tanrikulu, F; Sezgin, A; Toptas, T; Yilmaz, G, 2016
)
0.43
" The primary endpoint was safety and tolerability, including adverse events, non-haematological laboratory grade 3-4 toxic effects, and changes in bone-marrow blast counts from baseline."( Safety and tolerability of eltrombopag versus placebo for treatment of thrombocytopenia in patients with advanced myelodysplastic syndromes or acute myeloid leukaemia: a multicentre, randomised, placebo-controlled, double-blind, phase 1/2 trial.
Abboud, C; Araujo, S; Bennett, J; Chan, G; Chen, CY; Cheng, G; Chiou, TJ; Dougherty, S; Feigert, J; Giagounidis, A; Gorin, NC; Götze, K; Greenberg, P; Jang, JH; Johnson, B; Kambhampati, S; Kamel, YM; Kim, YJ; Lee, JH; Lyons, R; Mannino, F; Platzbecker, U; Ruggeri, M; Santini, V; Stone, N; Verma, A; Wong, RS; Yeh, SP, 2015
)
0.42
" 63 (98%) patients in the eltrombopag group and 32 (94%) patients in the placebo group had adverse events."( Safety and tolerability of eltrombopag versus placebo for treatment of thrombocytopenia in patients with advanced myelodysplastic syndromes or acute myeloid leukaemia: a multicentre, randomised, placebo-controlled, double-blind, phase 1/2 trial.
Abboud, C; Araujo, S; Bennett, J; Chan, G; Chen, CY; Cheng, G; Chiou, TJ; Dougherty, S; Feigert, J; Giagounidis, A; Gorin, NC; Götze, K; Greenberg, P; Jang, JH; Johnson, B; Kambhampati, S; Kamel, YM; Kim, YJ; Lee, JH; Lyons, R; Mannino, F; Platzbecker, U; Ruggeri, M; Santini, V; Stone, N; Verma, A; Wong, RS; Yeh, SP, 2015
)
0.42
"Eltrombopag is effective and safe in chronic immune thrombocytopenia (ITP)."( Eltrombopag safety and efficacy for primary chronic immune thrombocytopenia in clinical practice.
Aguilar, C; Alvarez-Román, MT; Andrade, MM; Bárez, A; Bernat, S; Cortés, M; de Cabo, E; Fernández-Fuentes, F; Fernández-Miñano, C; Fernández-Rodríguez, A; Fisac, R; Fuertes-Palacio, MA; García-Frade, LJ; Gómez-Nuñez, M; González-López, TJ; González-Porras, JR; Hernández-Rivas, JA; Jarque, I; Martínez-Robles, V; Olivera, P; Pascual, C; Peñarrubia, MJ; Pérez-Crespo, S; Pérez-Rus, G; Sánchez-González, B, 2016
)
0.43
"4%) experienced adverse events, mainly grades 1-2."( Eltrombopag safety and efficacy for primary chronic immune thrombocytopenia in clinical practice.
Aguilar, C; Alvarez-Román, MT; Andrade, MM; Bárez, A; Bernat, S; Cortés, M; de Cabo, E; Fernández-Fuentes, F; Fernández-Miñano, C; Fernández-Rodríguez, A; Fisac, R; Fuertes-Palacio, MA; García-Frade, LJ; Gómez-Nuñez, M; González-López, TJ; González-Porras, JR; Hernández-Rivas, JA; Jarque, I; Martínez-Robles, V; Olivera, P; Pascual, C; Peñarrubia, MJ; Pérez-Crespo, S; Pérez-Rus, G; Sánchez-González, B, 2016
)
0.43
" Chlorfenapyr was the most toxic adulticide among all the tested insecticides."( Toxicity of 25 synthetic insecticides to the field population of Culex quinquefasciatus Say.
Ahmad, D; Alam, M; Ali, Q; Binyamin, M; Shad, SA; Shah, RM; Waqas, M, 2016
)
0.43
" This report reviews the mechanism and use of eltrombopag along with a summary of associated adverse cutaneous reactions."( Morbilliform eruption related to eltrombopag: emerging data on the cutaneous toxicity of thrombopoietin receptor agonists.
Kazemi, T; Martin, S; Worswick, S, 2016
)
0.43
" During ROMANA 3, anamorelin and placebo groups had similar incidences of treatment-emergent adverse events (TEAEs; 52."( ROMANA 3: a phase 3 safety extension study of anamorelin in advanced non-small-cell lung cancer (NSCLC) patients with cachexia.
Abernethy, A; Currow, D; Fearon, KC; Friend, J; Milanowski, J; Temel, JS, 2017
)
0.46
"Eltrombopag is safe and effective in primary chronic ITP."( Efficacy and safety of eltrombopag in persistent and newly diagnosed ITP in clinical practice.
Aguilar, C; Alvarez-Román, MT; Arrieta-Cerdán, E; Bárez, A; Bernat, S; de Cabo, E; Fernández-Fuertes, F; Fernández-Rodríguez, A; García-Frade, LJ; González-López, TJ; González-Porras, JR; Hernández-Rivas, JA; Martínez-Robles, V; Olivera, P; Pascual, C; Peñarrubia, MJ; Pérez-Rus, G; Sánchez-González, B, 2017
)
0.46
" The evaluation of the chorion of the eggshell in this study has clarified the toxic effect of methomyl and cartap hydrochloride on eggs."( Insecticide toxicity to the borer Neoleucinodes elegantalis (Guenée) (Lepidoptera: Crambidae): developmental and egg-laying effects.
Arcanjo, LP; Costa, ÁH; Ferreira, DO; Martins, JC; Picanço, MC; Serrão, JE; Silva, RS; Soares, JRS, 2018
)
0.48
" This study quantifies and compares adverse event (AE) crude rates and costs associated with ITP treatments as found in claims data."( Comparative treatment-related adverse event cost burden in immune thrombocytopenic purpura.
Babinchak, T; Bilir, SP; Donga, PZ; Little, G; Munakata, J, 2017
)
0.46
" The anti-TB drugs of first choice were developed more than 4 decades ago and present several adverse effects, making the treatment of TB even more complicated and the development of new chemotherapeutics for this disease imperative."( New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity.
Aiub, CAF; Araujo-Lima, CF; Boechat, N; Castelo-Branco, FS; Costa, TEMM; Costa-Lima, MM; de Lima, EC; Domingos, JLO; Felzenszwalb, I; Gomes, KM; Henriques, MG; Lourenço, MCS; Penido, C; Pinto, AC, 2018
)
0.48
" Conclusions This case series suggests that TPO mimetics are safe and moderately effective in patients with ITP in the setting of SLE or APS and do not contribute to increased disease activity."( Safety and efficacy of thrombopoeitin mimetics for refractory immune thrombocytopenia purpura in patients with systemic lupus erythematosus or antiphospholipid syndrome: a case series.
Carlson, A; Lusa, A, 2018
)
0.48
" However, clone evolution and adverse events were associated with treatment."( Efficacy and Safety of Eltrombopag for Aplastic Anemia: A Systematic Review and Meta-analysis.
Chen, Y; Hong, Y; Li, N; Li, X; Wan, B, 2019
)
0.51
" Most patients demonstrated a long-term stable effect in the form of an increase in blood platelet count to a safe level during months and years of ATR treatment."( Thrombopoietin Receptor Agonists in the Treatment of Chronic Resistant Primary Immune Thrombocytopenia: Efficacy and Safety Data in Real Clinical Practice.
Arshanskaya, EG; Chernikov, MV; Pankrashkina, MM; Ptushkin, VV; Tkachenko, NE; Vinogradova, OY, 2018
)
0.48
"Long-term ATR-therapy using in patients with resistant chronic ITP is an effective and largely safe treatment option."( Thrombopoietin Receptor Agonists in the Treatment of Chronic Resistant Primary Immune Thrombocytopenia: Efficacy and Safety Data in Real Clinical Practice.
Arshanskaya, EG; Chernikov, MV; Pankrashkina, MM; Ptushkin, VV; Tkachenko, NE; Vinogradova, OY, 2018
)
0.48
" Time taken for response to therapy (defined as platelets >1 lakh), dose, duration of treatment, and adverse effects of the drug were noted."( Eltrombopag: Efficacy and Safety in Steroid Refractory Lupus-Associated Immune Thrombocytopenia.
Roongta, R; Sanil, S; Shobha, V, 2020
)
0.56
" No adverse events including thrombotic complication were noted."( Eltrombopag: Efficacy and Safety in Steroid Refractory Lupus-Associated Immune Thrombocytopenia.
Roongta, R; Sanil, S; Shobha, V, 2020
)
0.56
" It indirectly contributes to reduction in the dose of steroids and immunosuppressants, thereby minimizing their cumulative adverse effects."( Eltrombopag: Efficacy and Safety in Steroid Refractory Lupus-Associated Immune Thrombocytopenia.
Roongta, R; Sanil, S; Shobha, V, 2020
)
0.56
" Treatment response rates, durable response rates, bleeding events, and adverse events were assessed during eltrombopag therapy for at least 12 weeks."( Efficacy and safety of eltrombopag in the treatment of severe chronic immune thrombocytopenia in children of China: A single-center observational study.
Chen, Z; Cheng, X; Ma, J; Wang, X; Wu, R; Yan, K; Zhao, L,
)
0.13
" We retrieved evidence on treatment-related grade III/IV adverse events, progression-free survival (PFS) and overall survival (OS)."( A systematic literature review and network meta-analysis of effectiveness and safety outcomes in advanced melanoma.
Franken, MG; Gheorghe, M; Haanen, JBAG; Leeneman, B; Uyl-de Groot, CA; van Baal, PHM, 2019
)
0.51
" We reviewed 437 patients with multiple myeloma treated with selinexor and assessed the kinetics of adverse events and impact of supportive care measures."( Integrated safety profile of selinexor in multiple myeloma: experience from 437 patients enrolled in clinical trials.
Abonour, R; Bahlis, N; Baz, R; Berdeja, JG; Chai, Y; Chari, A; Chen, C; Choquet, S; Cornell, RF; Dimopoulos, MA; Dingli, D; Gasparetto, C; Gavriatopoulou, M; Hofmeister, CC; Huff, CA; Jagannath, S; Jakubowiak, A; Kauffman, MG; Lentzsch, S; Li, K; Li, L; Lonial, S; Mohty, M; Moreau, P; Nooka, AK; Parker, TL; Reece, D; Richter, J; Shacham, S; Shah, J; Siegel, D; Tuchman, S; Unger, TJ; Vogl, DT; Weisel, KC; White, D; Yee, AJ, 2020
)
0.56
" The most common grade 3 or 4 adverse events were thrombocytopenia (eight [32%] of 25 patients) and hyponatraemia (five [20%])."( Safety and activity of selinexor in patients with myelodysplastic syndromes or oligoblastic acute myeloid leukaemia refractory to hypomethylating agents: a single-centre, single-arm, phase 2 trial.
Abdel-Wahab, O; Alvarez, K; Chung, SS; Gönen, M; Klimek, VM; Mi, X; Paffenholz, SV; Park, JH; Penson, AV; Rampal, RK; Sen, F; Sigler, A; Stein, EM; Tallman, MS; Taylor, J, 2020
)
0.56
" Adverse events were manageable with supportive care implementation."( Safety and activity of selinexor in patients with myelodysplastic syndromes or oligoblastic acute myeloid leukaemia refractory to hypomethylating agents: a single-centre, single-arm, phase 2 trial.
Abdel-Wahab, O; Alvarez, K; Chung, SS; Gönen, M; Klimek, VM; Mi, X; Paffenholz, SV; Park, JH; Penson, AV; Rampal, RK; Sen, F; Sigler, A; Stein, EM; Tallman, MS; Taylor, J, 2020
)
0.56
"Acute toxic exposures to hydrazine and its derivatives are rare."( The Toxicity, Pathophysiology, and Treatment of Acute Hydrazine Propellant Exposure: A Systematic Review.
Albertson, TE; Bebarta, VS; Chenoweth, JA; Nguyen, HN; Nowadly, CD, 2021
)
1.17
" Despite recent research efforts to generate less toxic alternatives to hydrazine fuel, it will likely continue to have a role in military and aviation industries."( The Toxicity, Pathophysiology, and Treatment of Acute Hydrazine Propellant Exposure: A Systematic Review.
Albertson, TE; Bebarta, VS; Chenoweth, JA; Nguyen, HN; Nowadly, CD, 2021
)
1.1
" Biochemical analysis of the liver function's parameters showed that the LD50 values in all animals were higher than the reference values."( Study of acute oral toxicity of the thiazole derivative N-(1-methyl-2-methyl-pyridine)-N-(p-bromophenylthiazol-2-yl)-hydrazine in a Syrian hamster.
Amaro da Silva Junior, V; Angela Aranda de Souza, M; Câmara Alves, L; de Figueiredo, RCBQ; Lima Leite, AC; Ramos Mororó Cavalcanti, R; Rogério de Freitas Silva, S; Vasconcelos Gomes de Oliveira, V; Veríssimo de Oliveira Cardoso, M, 2021
)
0.83
" Initial response rate, durable response rate, bleeding events, and adverse events were assessed during the follow-up period."( Efficacy and safety of eltrombopag in the treatment of Chinese children with chronic immune thrombocytopenia.
Chen, M; Fang, JP; Li, XY; Lin, SF; Xu, LH; Zhou, CX, 2021
)
0.62
" No serious bleeding events or serious adverse events occurred during the study period."( Efficacy and safety of eltrombopag in the treatment of Chinese children with chronic immune thrombocytopenia.
Chen, M; Fang, JP; Li, XY; Lin, SF; Xu, LH; Zhou, CX, 2021
)
0.62
"The aim of this review is to elucidate the type and frequency of ocular adverse events associated with selinexor with a goal to quantify the occurrence of these events in our investigator-initiated trial."( Overview of Ocular Side Effects of Selinexor.
Ahnert, JR; Al-Zubidi, N; Bernstam, FM; Fu, S; Gombos, DS; Hong, DS; Karp, DD; Naing, A; Piha-Paul, SA; Subbiah, V; Tsimberidou, AM, 2021
)
0.62
" All reported ocular adverse events were assessed."( Overview of Ocular Side Effects of Selinexor.
Ahnert, JR; Al-Zubidi, N; Bernstam, FM; Fu, S; Gombos, DS; Hong, DS; Karp, DD; Naing, A; Piha-Paul, SA; Subbiah, V; Tsimberidou, AM, 2021
)
0.62
"54%) patients experienced 37 ocular adverse events."( Overview of Ocular Side Effects of Selinexor.
Ahnert, JR; Al-Zubidi, N; Bernstam, FM; Fu, S; Gombos, DS; Hong, DS; Karp, DD; Naing, A; Piha-Paul, SA; Subbiah, V; Tsimberidou, AM, 2021
)
0.62
"Our findings highlight that ocular adverse events associated with oral selinexor were mild."( Overview of Ocular Side Effects of Selinexor.
Ahnert, JR; Al-Zubidi, N; Bernstam, FM; Fu, S; Gombos, DS; Hong, DS; Karp, DD; Naing, A; Piha-Paul, SA; Subbiah, V; Tsimberidou, AM, 2021
)
0.62
"Patients receiving selinexor in combination with multiple standard chemotherapy or immunotherapy agents were reviewed, with a total of 34 patients experiencing 37 ocular adverse events."( Overview of Ocular Side Effects of Selinexor.
Ahnert, JR; Al-Zubidi, N; Bernstam, FM; Fu, S; Gombos, DS; Hong, DS; Karp, DD; Naing, A; Piha-Paul, SA; Subbiah, V; Tsimberidou, AM, 2021
)
0.62
" Eltrombopag was well-tolerated; however, the most common adverse events included indirect bilirubin elevation, jaundice, and transient liver-enzyme elevation."( Efficacy and safety of eltrombopag in the first-line therapy of severe aplastic anemia in children.
Cheng, X; Fu, L; He, Y; Jie, M; Li, S; Wu, R; Yao, J; Zhang, L; Zhang, R; Zheng, J, 2021
)
0.62
"Data from 134 patients in SADAL were analyzed by DLBCL subtypes for overall response rate (ORR), overall survival (OS), duration of treatment response, progression-free survival, and adverse events rate."( Comparison of the Effectiveness and Safety of the Oral Selective Inhibitor of Nuclear Export, Selinexor, in Diffuse Large B Cell Lymphoma Subtypes.
Bakhshi, S; Caimi, PF; Canales, M; Casasnovas, RO; Cavallo, F; Chamoun, K; Choquet, S; Egyed, M; Follows, G; Goy, A; Gurion, R; Hamad, N; Hill, B; Jaeger, U; Kalakonda, N; Kauffman, MG; Ku, M; Kuruvilla, J; la Cruz, F; Ma, X; Maerevoet, M; Neste, EVD; Offner, F; Samal, P; Sancho, JM; Schuster, M; Shacham, S; Shah, J; Thieblemont, C; Vassilakopoulos, TP; Vermaat, JSP; Warzocha, K; Zijlstra, JM, 2022
)
0.72
" Similar rates of adverse events were noted in all subgroups."( Comparison of the Effectiveness and Safety of the Oral Selective Inhibitor of Nuclear Export, Selinexor, in Diffuse Large B Cell Lymphoma Subtypes.
Bakhshi, S; Caimi, PF; Canales, M; Casasnovas, RO; Cavallo, F; Chamoun, K; Choquet, S; Egyed, M; Follows, G; Goy, A; Gurion, R; Hamad, N; Hill, B; Jaeger, U; Kalakonda, N; Kauffman, MG; Ku, M; Kuruvilla, J; la Cruz, F; Ma, X; Maerevoet, M; Neste, EVD; Offner, F; Samal, P; Sancho, JM; Schuster, M; Shacham, S; Shah, J; Thieblemont, C; Vassilakopoulos, TP; Vermaat, JSP; Warzocha, K; Zijlstra, JM, 2022
)
0.72
" Adverse events between subgroups were similar to the overall study population, the most common being thrombocytopenia (29."( Effect of Prior Therapy and Disease Refractoriness on the Efficacy and Safety of Oral Selinexor in Patients with Diffuse Large B-cell Lymphoma (DLBCL): A Post-hoc Analysis of the SADAL Study.
Bakhshi, S; Caimi, P; Canales, M; Casasnovas, RO; Cavallo, F; Chamoun, K; Choquet, S; Corona, K; De la Cruz, F; Egyed, M; Follows, G; Goy, A; Gurion, R; Hamad, N; Hill, B; Jaeger, U; Kalakonda, N; Kauffman, MG; Ku, M; Kuruvilla, J; Ma, X; Maerevoet, M; Neste, EVD; Offner, F; Samal, P; Sancho, JM; Schuster, M; Shacham, S; Shah, J; Thieblemont, C; Vassilakopoulos, T; Vermaat, JSP; Warzocha, K; Zijlstra, J, 2022
)
0.72
" This study provides data for setting maximum residue limits and PHIs for the safe use of spiromesifen and chromafenozide in lettuce and perilla."( Residual characteristics and safety assessment of the insecticides spiromesifen and chromafenozide in lettuce and perilla.
Byeon, GD; Choi, JY; Ham, HJ; Hur, JH; Ishag, AESA; Sardar, SW, 2022
)
0.72
" littoralis larvae, and the same concentrations were used to assess the toxic impact of their combination on susceptible (SUS) and M-selected (MS) strains."( Toxicity and biochemical impact of methoxyfenozide/spinetoram mixture on susceptible and methoxyfenozide-selected strains of Spodoptera littoralis (Lepidoptera: Noctuidae).
Ahmed, FS; Helmy, WS; Helmy, YS, 2022
)
0.72
" Common nonhematologic adverse events were fatigue (56%), nausea (53%), anorexia (41%), and diarrhea (41%) and were mostly low grade."( Selinexor Combined with Ibrutinib Demonstrates Tolerability and Safety in Advanced B-Cell Malignancies: A Phase I Study.
Baker, S; Bhat, S; Byrd, JC; Canfield, D; Cempre, CB; Fu, Q; Hu, B; Huang, Y; Jaglowski, SM; Lapalombella, R; Lockman, H; Rogers, KA; Ruppert, AS; Shah, H; Stephens, DM; Vadeboncoeur, R; Walker, JS; Woyach, JA, 2022
)
0.72
" This study aimed to assess the relationship between eltrombopag and thrombotic events in a large population extracted from the Food and Drug Administration Adverse Event Reporting System (FAERS) database."( Does eltrombopag lead to thrombotic events? A pharmacovigilance study of the FDA adverse event reporting system.
Jiang, JJ; Li, J; Zhao, B, 2022
)
0.72
" There were no significant associations between genotypes and adverse drug reactions (ADRs) or ELT concentrations and ADRs."( Relationship between CYP2C8, UGT1A1, and ABCG2 gene polymorphisms and the exposure, efficacy, and toxicity of eltrombopag in the treatment of refractory aplastic anemia.
Chen, M; Han, B; Liu, B; Zhang, B; Zuo, W, 2022
)
0.72
"The aim of the study was to conduct a network meta-analysis to assess the efficacy and incidence of treatment-related adverse events (TRAEs) of eltrombopag, romiplostim, avatrombopag, recombinant human thrombopoietin (rhTPO), and hetrombopag for adult immune thrombocytopenia (ITP)."( Efficacy and Incidence of Treatment-Related Adverse Events of Thrombopoietin Receptor Agonists in Adults with Immune Thrombocytopenia: A Systematic Review and Network Meta-Analysis of Randomized Controlled Study.
Feng, CX; Geng, QC; Lin, X; Liu, Y; Su, J; Zhang, HX, 2023
)
0.91
" The results of meta-analysis showed that in adult patients, patients treated with TPO-RAs had longer duration of platelet response, higher platelet response rate, lower use of rescue therapy, and lower incidence of bleeding events, and similar incidence of adverse events compared with placebo."( Efficacy and safety of thrombopoietin receptor agonists in children and adults with persistent and chronic immune thrombocytopenia: a meta-analysis.
Li, T; Liu, J; Liu, Q; Pu, T; Zhang, A, 2023
)
0.91

Pharmacokinetics

The apparent plasma half-life of acetylhydrazine is about five times longer than that of isoniazid. The slowest acetylators should have a 20-plus hr plasma half-life.

ExcerptReferenceRelevance
" Thus, decarboxylase inhibition failed to alter the plasma half-life of levodopa."( Levodopa pharmacokinetics. Alterations after benserazide, a decarboxylase inhibitor.
Connor, JD; Doller, HJ; Dvorchik, BH; Lock, DR; Sloviter, RS; Vesell, ES,
)
0.13
" The results suggested that the pharmacokinetic behavior of Iso in rats belonged to a 2-compartment model."( Effects of rifampicin on pharmacokinetics of isoniazid and its metabolite acetylhydrazine in rats.
Cheng, WB; Li, D; Wang, ZY; Zhang, RL, 1992
)
0.51
" This pharmacokinetic analysis, however, also shows that the apparent plasma half-life of acetylhydrazine is about five times longer than the plasma half-life of isoniazid, and thus repeated doses of isoniazid should lead to an accumulation of acetylhydrazine in the slowest acetylators in which the plasma half-life of acetylhydrazine is 20-plus hr."( Pharmacokinetics of the toxic hydrazino metabolites formed from isoniazid in humans.
Lauterburg, BH; Mitchell, JR; Smith, CV; Todd, EL, 1985
)
0.49
" Analysis of the pharmacokinetic data with the use of a 4-compartmental model showed appreciable differences in some of the pharmacokinetic parameters of hydrazine sulfate as regards intact and tumor-bearing animals."( [Pharmacokinetics of hydrazine sulfate in intact and tumor-bearing rats].
Bezel', VS; Filov, VA; Popov, BV,
)
0.65
" Tacrolimus demonstrates considerable interindividual variation in its pharmacokinetic profile."( Measurement of tacrolimus (FK506) and its metabolites: a review of assay development and application in therapeutic drug monitoring and pharmacokinetic studies.
Alak, AM, 1997
)
0.3
" Due to its simplicity and sensitivity this method can be used on a routine basis for pharmacokinetic analysis of neuroactive steroids."( High-performance liquid chromatography of the neuroactive steroids alphaxalone and pregnanolone in plasma using dansyl hydrazine as fluorescent label: application to a pharmacokinetic-pharmacodynamic study in rats.
Danhof, M; Gladdines, WW; Irth, H; Smulders, CJ; van der Graaf, PH; Visser, SA, 2000
)
0.52
" The elimination half-life of VNP40101M was approximately 20 minutes, the peak plasma concentration (Cmax) averaged 11."( Pharmacokinetics, mass balance, and tissue distribution of a novel DNA alkylating agent, VNP40101M, in rat.
Almassain, B; Mao, J; Wu, D; Xu, Y, 2002
)
0.31
" As alkylating agents are important antileukemia drugs, a Phase I and pharmacokinetic study of VNP40101M was conducted in patients with refractory or relapsed leukemias or poor-risk myelodysplastic syndromes (MDS)."( A Phase I and pharmacokinetic study of VNP40101M, a novel sulfonylhydrazine alkylating agent, in patients with refractory leukemia.
Andreeff, M; Beran, M; Cahill, A; Clairmont, C; Cortes, J; Faderl, S; Ferrajoli, A; Garcia-Manero, G; Giles, F; Jeha, S; Kantarjian, H; Koller, C; Sznol, M; Thomas, D; Verstovsek, S, 2004
)
0.56
" Pharmacokinetic parameters were assessed in the first cycle and any cycle with a change in dose."( A phase I and pharmacokinetic study of VNP40101M, a new alkylating agent, in patients with advanced or metastatic cancer.
Chu, E; Clairmont, C; Egorin, M; Kummar, S; Modiano, M; Murren, J; Sznol, M, 2005
)
0.33
" The elimination half-life was short and estimated to be approximately 15 minutes."( A phase I and pharmacokinetic study of VNP40101M, a new alkylating agent, in patients with advanced or metastatic cancer.
Chu, E; Clairmont, C; Egorin, M; Kummar, S; Modiano, M; Murren, J; Sznol, M, 2005
)
0.33
" In a second part, pharmacokinetic studies using a (14)C isotope of each IGR showed similar patterns of penetration through the cuticle, but different absorption and distribution rates inside the insect body."( The ecological impact of four IGR insecticides in adults of Hyposoter didymator (Hym., Ichneumonidae): pharmacokinetics approach.
Pineda, S; Schneider, M; Smagghe, G; Viñuela, E, 2008
)
0.35
"The aim of these studies was to assess the effect of food and antacids on the pharmacokinetic and safety profiles of eltrombopag."( Effects of food and antacids on the pharmacokinetics of eltrombopag in healthy adult subjects: two single-dose, open-label, randomized-sequence, crossover studies.
Bailey, CK; Collins, DA; Deng, Y; Jenkins, JM; Kapsi, SG; Park, JW; Peng, B; Williams, DD; Wire, MB, 2009
)
0.35
" There was high pharmacokinetic variability and significant overlap in exposures between participants with hepatic or renal impairment and healthy participants."( Effect of hepatic or renal impairment on eltrombopag pharmacokinetics.
Bauman, JW; Park, JW; Peng, B; Vincent, CT; Williams, DD; Wire, MB, 2011
)
0.37
" Previous reports indicate that ELT is mainly eliminated in the liver, although its pharmacokinetic profile has not yet been clarified in detail."( Pharmacokinetics and hepatic uptake of eltrombopag, a novel platelet-increasing agent.
Horikawa, M; Ishiwata, N; Kato, Y; Matsubara, K; Nakamichi, N; Silver, DL; Sugiura, T; Takeuchi, K; Umeda, S, 2011
)
0.37
" Noncompartmental pharmacokinetic parameters were estimated from plasma concentration-time data collected over 72 hours post-dose."( A randomized, open-label, 5-period, balanced crossover study to evaluate the relative bioavailability of eltrombopag powder for oral suspension (PfOS) and tablet formulations and the effect of a high-calcium meal on eltrombopag pharmacokinetics when admin
Brainsky, A; Bruce, J; Gauvin, J; McGuire, S; Pendry, CJ; Qian, Y; Wire, MB, 2012
)
0.38
" Compounds inhibiting growth of both Chlamydia trachomatis and Chlamydophila pneumoniae were tested for cell toxicity and seven compounds were selected for preliminary pharmacokinetic analysis in mice using cassette dosing."( Pre-clinical pharmacokinetics and anti-chlamydial activity of salicylidene acylhydrazide inhibitors of bacterial type III secretion.
Blomgren, A; Chu, H; Dahlgren, MK; Elofsson, M; Gylfe, A; Peterson, EM; Slepenkin, A; Ur-Rehman, T; Zetterström, CE, 2012
)
0.38
" Pathogen-specific metabolism makes positron-emitting INH analogs attractive candidates for development into imaging probes with the potential to both detect bacteria and yield pharmacokinetic data in situ."( Noninvasive determination of 2-[18F]-fluoroisonicotinic acid hydrazide pharmacokinetics by positron emission tomography in Mycobacterium tuberculosis-infected mice.
Hooker, JM; Jain, SK; Liu, L; Ordonez, AA; Tonge, PJ; Wang, H; Weinstein, EA, 2012
)
0.38
" These results suggest that choice of chelator is an important pharmacokinetic consideration in the development of (99m)Tc-labeled radiopharmaceuticals targeting PSMA."( Effect of chelators on the pharmacokinetics of (99m)Tc-labeled imaging agents for the prostate-specific membrane antigen (PSMA).
Byun, Y; Falk, A; Foss, CA; Mease, RC; Nimmagadda, S; Pomper, MG; Pullambhatla, M; Ray Banerjee, S, 2013
)
0.39
" The proposed method was found to be applicable to pharmacokinetic studies."( Liquid chromatography-tandem mass spectrometric assay for eltrombopag in 50μL of human plasma: a pharmacokinetic study.
Gajula, R; Maddela, R; Maddela, S; Makula, A; Pilli, NR; Siddiraju, S, 2014
)
0.4
"This study characterized the population pharmacokinetic (pop-PK) and PK/pharmacodynamic (pop-PK/PD) properties of eltrombopag and evaluated platelet count (PLTC) response to different eltrombopag dosages through simulations in Chinese adult patients with chronic primary immune thrombocytopenia (cITP)."( Population Pharmacokinetic and Pharmacodynamic Modeling and Effects on Platelet Counts of Different Dosages of Eltrombopag in Chinese Patients With Chronic Primary Immune Thrombocytopenia.
Farrell, C; Guo, H; Hayes, S; Hou, M; Thapar, M; Wu, K; Zhang, J, 2015
)
0.42
" Pharmacodynamic effects for XPO1 inhibition were noted."( Pharmacodynamic and genomic markers associated with response to the XPO1/CRM1 inhibitor selinexor (KPT-330): A report from the pediatric preclinical testing program.
Attiyeh, EF; Carol, H; Gorlick, R; Houghton, PJ; Kang, MH; Keir, ST; Kolb, EA; Kurmasheva, RT; Landesman, Y; Lock, R; Lyalin, D; Maris, JM; Reynolds, CP; Shacham, S; Smith, MA; Wu, J, 2016
)
0.43
" The method showed the sensitivity, linearity, precision, accuracy and selectivity required to quantify LASSBio-1736 in preclinical pharmacokinetic studies according to the criteria established by the US Food and Drug Administration and European Medicines Agency."( Simple HPLC-UV for the quantification of a new leishmanicidal candidate (E)-1-4(trifluoromethyl) benzylidene)-5-(2-4-dichlorozoyl) carbonylhydrazine (LASSBio-1736) in rat plasma for pharmacokinetics assessment.
Alves, MA; Bajerski, L; Barreiro, EJ; Dalla Costa, T; Freddo, RJ; Haas, SE; Lima, LM; Moraes, BKS; Parisotto, A; Silva, CEDR, 2016
)
0.64
" The compounds were designed with the objective of improving pharmacokinetic properties."( Second-Generation Phenylthiazole Antibiotics with Enhanced Pharmacokinetic Properties.
Abdelghany, TM; Bayoumi, SA; Disouky, AM; El-Morsy, A; Elshafeey, A; Mancy, AS; Mayhoub, AS; Mohammad, H; Seleem, MA; Seleem, MN, 2016
)
0.43
" The drug-drug interactions between the anti-retroviral and anti-tubercular drugs are not clearly defined and hence, this study was conducted to evaluate the pharmacokinetic drug-drug interactions of Zidovudine (AZT) with Isoniazid (INH) and its hepatotoxic metabolites."( Investigations on the Influence of Zidovudine in the Pharmacokinetics of Isoniazid and Its Hepatotoxic Metabolites in Rats.
Ramanathan, R; Sivanesan, K, 2019
)
0.51
" Bayesian statistical approach will be applied to screen for patients' characteristics associated with eltrombopag pharmacokinetic parameters."( Bayesian Population Pharmacokinetic Modeling of Eltrombopag in Chronic Hepatitis C Patients.
Al-Ramadhani, HM; Alzubiedi, S; Melhim, SB; Saleh, MI, 2019
)
0.51
"A two-compartment pharmacokinetic model with first-order absorption with exponential error model best fit the data."( Bayesian Population Pharmacokinetic Modeling of Eltrombopag in Chronic Hepatitis C Patients.
Al-Ramadhani, HM; Alzubiedi, S; Melhim, SB; Saleh, MI, 2019
)
0.51
"Eltrombopag pharmacokinetic behavior was described using population bayesian approach."( Bayesian Population Pharmacokinetic Modeling of Eltrombopag in Chronic Hepatitis C Patients.
Al-Ramadhani, HM; Alzubiedi, S; Melhim, SB; Saleh, MI, 2019
)
0.51
"Sex and CYP1A2 rs762551 C>A were associated with the pharmacokinetic variability of eltrombopag in healthy Chinese subjects."( Pharmacokinetics of Eltrombopag in Healthy Chinese Subjects and Effect of Sex and Genetic Polymorphism on its Pharmacokinetic and Pharmacodynamic Variability.
Chen, J; Hu, Y; Jiang, B; Lou, H; Ruan, Z; Shao, R; Xu, Y; Yang, D, 2021
)
0.62
" The present study aimed to evaluate the unexplored pharmacokinetic profile of this agent in experimental rats."( Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats.
Choudhury, H; Dhanawat, M; Gupta, S; Jacob, S; Munjal, K; Nair, AB, 2021
)
0.62
" Blood samples were collected at different pre-determined time intervals to determine the pharmacokinetic parameters."( Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats.
Choudhury, H; Dhanawat, M; Gupta, S; Jacob, S; Munjal, K; Nair, AB, 2021
)
0.62
" The obtained data from the pharmacokinetic study indicated that HZC was instantaneously distributed and moderately eliminated from body fluids."( Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats.
Choudhury, H; Dhanawat, M; Gupta, S; Jacob, S; Munjal, K; Nair, AB, 2021
)
0.62
" Besides radical-scavenging activity, the pharmacokinetic and drug-likeness of the coumarin hybrids were investigated."( Radical Scavenging Activity and Pharmacokinetic Properties of Coumarin-Hydroxybenzohydrazide Hybrids.
Amić, AD; Antonijević, MR; Avdović, EH; Marković, ZS; Milanović, ŽB; Simijonović, DM, 2022
)
0.72

Compound-Compound Interactions

Cloretazine (VNP40101M or Laromustine) is a novel sulfonylhydrazine alkylating agent with significant antileukaemic activity. The clinical actions of levodopa in Parkinsonism, given with and without an extracerebral decarboxylase, were compared.

ExcerptReferenceRelevance
"The effects of carbidopa combined with levodopa (carbidopa/levodopa) and levodopa alone on the cardiovascular system of patients with Parkinson's disease were evaluated."( Comparison of dopa decarboxylase inhibitor (carbidopa) combined with levodopa and levodopa alone on the cardiovascular system of patients with parkinson's disease.
Leibowitz, M; Lieberman, A, 1975
)
0.25
" With the combination medication, levodopa-carbidopa, on an average 420 mg/42 mg combined with 950 mg of levodopa in slow release form, a statistically significant improvement in parkinsonian signs could be achieved without any worsening of the side effects."( Effect of a slow release preparation of levodopa on Parkinson's disease in combination with a peripheral decarboxylase inhibitor.
Hokkanen, E; Myllylä, VV; Saarinen, A; Tokola, O, 1978
)
0.26
"Since L-dopa in combination with a decarboxylase inhibitor is currently the most effective therapy available for treatment of Parkinson's disease, the authors compare the actual causes of death in a large series of treated Parkinson patients with a normal population and with previous studies."( Mortality among Parkinson patients treated with L-dopa combined with a decarboxylase inhibitor.
Siegfried, J; Zumstein, H, 1976
)
0.26
"Eighty-one Parkinsonic patients were treated with L-dopa alone and/or combined with Ro4-4602, during 27 to 60 months."( [5 years of experience in the treatment of parkinsonism with L-dopa and its combination with Ro4-4602].
Chouza, C; Gomensoro, JB; Romero, S, 1976
)
0.26
" In view of the observations made it is doubtful whether the therapeutic effect of 5-HTP combined with a peripheral decarboxylase inhibitor in depressions and myoclonus can in fact be atributed to activation of central serotonergic systems."( An unexpected effect of L-5 hydroxytryptophan-ethyl-ester combined with a peripheral decarboxylase inhibitor on human serum prolactin.
Korf, J; Lequin, RM; van Praag, HM, 1976
)
0.26
" (1) Concentrations of dopa and dopamine in plasma and brain were measured in cats following intraperitoneal injection of L-dopa alone (100 mg/kg) or combined with MK-486 (10 mg/kg)."( L-dopa therapy combined with peripheral decarboxylase inhibitor (MK-486) in Parkinsonism.
Kishikawa, H; Ohmoto, T, 1975
)
0.25
"5 g of levodopa daily for up to six months and in 30 patients receiving levodopa (800-1,000 mg) combined with a dopa decarboxylase inhibitor, benserazide (200-250 mg)."( Urinary excretion of monoamines and their metabolites in patients with Parkinson's disease. Response to long-term treatment with levodopa alone or in combination with a dopa decarboxylase inhibitor and clinical correlations.
Rinne, UK; Siirtola, T; Sonninen, V, 1975
)
0.25
"In an open study 25 depressed patients were treated with L-5-hydroxytryptophan (L-5-HTP) either alone or in combination with a peripheral decarboxylase inhibitor."( L-5-hydroxytryptophan alone and in combination with a peripheral decarboxylase inhibitor in the treatment of depression.
Battegay, R; Gastpar, M; Zmilacher, K, 1988
)
0.27
"Thirty patients with Parkinson's disease were treated for four weeks with levodopa combined with an inhibitor of extracerebral dopa decarboxylase, L-alpha-methyldopahydrazine (MK 486)."( Treatment of Parkinson's disease with levodopa combined with L-alpha-methyldopahydrazine, an inhibitor of extracerebral DOPA decarboxylase.
Barry, PE; Marsden, CD; Parkes, JD; Zilkha, KJ, 1973
)
0.67
"The clinical actions of levodopa in Parkinsonism, given with and without an extracerebral decarboxylase in hibitor, L-alpha-methyldopahydrazine, were compared."( Idiopathic Parkinsonism treated with an extracerebral decarboxylase inhibitor in combination with levodopa.
Calne, DB; Gawler, J; Hilson, A; Pallis, CA; Petrie, A; Rao, S; Reid, JL; Thomas, PK; Vakil, SD, 1971
)
0.45
" A phase I study of cloretazine combined with cytarabine (1-beta-d-arabinofuranosylcytosine, ara-C) was conducted in patients with refractory disease."( Phase I study of cloretazine (VNP40101M), a novel sulfonylhydrazine alkylating agent, combined with cytarabine in patients with refractory leukemia.
Albitar, M; Cahill, A; Cortes, J; Faderl, S; Ferrajoli, A; Garcia-Manero, G; Gerson, S; Giles, F; Jabbour, E; Kantarjian, H; Karsten, V; Kornblau, S; O'Brien, S; Ravandi, F; Sznol, M; Thomas, D; Verstovsek, S; Yee, K, 2005
)
0.57
" Dose-limiting toxicities (gastrointestinal and myelosuppression) were seen with 500 and 600 mg/m(2) of cloretazine combined with the 4-day ara-C schedule but not seen with the 3-day schedule."( Phase I study of cloretazine (VNP40101M), a novel sulfonylhydrazine alkylating agent, combined with cytarabine in patients with refractory leukemia.
Albitar, M; Cahill, A; Cortes, J; Faderl, S; Ferrajoli, A; Garcia-Manero, G; Gerson, S; Giles, F; Jabbour, E; Kantarjian, H; Karsten, V; Kornblau, S; O'Brien, S; Ravandi, F; Sznol, M; Thomas, D; Verstovsek, S; Yee, K, 2005
)
0.57
" A phase I clinical trial was undertaken to determine the maximum tolerated dose, toxicity profile, and pharmacokinetics of STA-4783 in combination with paclitaxel."( Phase I clinical trial of STA-4783 in combination with paclitaxel in patients with refractory solid tumors.
Berkenblit, A; Dahl, TA; Dezube, BJ; Eder, JP; Ryan, DP; Seiden, MV; Sherman, ML; Supko, JG; Tatsuta, N, 2007
)
0.34
" In this study, Cloretazine was evaluated both as a monotherapy and in combination with fludarabine in murine tumor and human tumor xenograft models."( Anti-tumor efficacy of Cloretazine (VNP40101M) alone and in combination with fludarabine in murine tumor and human xenograft tumor models.
King, I; Li, Z; Liu, L; Song, BL; Zheng, LM, 2007
)
0.34
" These results indicate that the occurrence of redox cycling combined with a low background current yields an electrochemical immunosensor with a very low detection limit (100 fg/mL)."( Electrochemical immunosensor using p-aminophenol redox cycling by hydrazine combined with a low background current.
Das, J; Jo, K; Lee, JW; Yang, H, 2007
)
0.58
" Here, we report a new efficient method for identification of oxidatively modified proteins in complex biological samples which is based on the use of an aldehyde-reactive probe, N'-aminooxymethylcarbonylhydrazino-D-biotin (ARP), in combination with Western-type analyses and MS."( Detection of carbonyl-modified proteins in interfibrillar rat mitochondria using N'-aminooxymethylcarbonylhydrazino-D-biotin as an aldehyde/keto-reactive probe in combination with Western blot analysis and tandem mass spectrometry.
Chung, WG; Maier, CS; Miranda, CL, 2008
)
0.35
" After removal of excess derivatization reagent and urine matrix components, the monoterpene derivatives were separated by high-performance liquid chromatography (HPLC) in combination with fluorescence (FLD) detection and simultaneous mass spectrometric (MS) identification."( Sensitive determination of monoterpene alcohols in urine by HPLC-FLD combined with ESI-MS detection after online-solid phase extraction of the monoterpene-coumarincarbamate derivates.
Duisken, M; Hollender, J; Jähnigen, H; Meesters, RJ, 2008
)
0.35
"We have investigated the effect of cloretazine (VNP40101M or Laromustine), a novel sulfonylhydrazine alkylating agent with significant antileukaemic activity, alone, or combined with cytarabine or daunorubicin, on the proliferation, viability and apoptosis of cell lines and acute myeloid leukaemia blast cells in vitro."( Effect of cloretazine (VNP40101M) on acute myeloid leukaemia blast cells in vitro as a single agent and combined with cytarabine and daunorubicin.
Adams, JA; Liu Yin, JA; Morris, KL, 2009
)
0.57
" A broad spectrum of toxic organics in water was efficiently destroyed in the presence of dioxygen in combination with hydrazine hydrate at 150 °C."( Dioxygen in combination with hydrazine: a practical system for degradation of a broad spectrum of toxic organics in water.
Chu, C; Liang, X; Liao, N; Liu, R; Liu, Y; Lu, Q; Shen, J; Tao, J, 2011
)
0.87
"These studies explored questions related to the potential use of Laromustine in the treatment of solid tumors and in combination with radiotherapy."( Preclinical evaluation of Laromustine for use in combination with radiation therapy in the treatment of solid tumors.
Akintujoye, OM; Baumann, RP; Glazer, PM; Ishiguro, K; Liu, Y; Penketh, PG; Rockwell, S; Sartorelli, AC; Seow, HA; Shyam, K, 2012
)
0.38
" In both animal models the anti-lymphoma activity of selinexor is enhanced through combination with DEX or EVER."( Anti-tumor activity of selective inhibitor of nuclear export (SINE) compounds, is enhanced in non-Hodgkin lymphoma through combination with mTOR inhibitor and dexamethasone.
Aboukameel, A; Azmi, AS; Baloglu, E; Bhutani, D; Carlson, R; Elloul, S; Kauffman, M; Mohammad, RM; Muqbil, I; Senapedis, W; Shacham, S; Zonder, J, 2016
)
0.43
" By inhibiting the primary export protein, XPO1, selinexor localizes and activates tumor suppressor proteins in the nucleus and inhibits DNA damage repair, rationalizing combination with DNA-damaging agents."( Phase I Clinical Trial of Selinexor in Combination with Daunorubicin and Cytarabine in Previously Untreated Poor-Risk Acute Myeloid Leukemia.
Chavez, J; Cubitt, CL; Dawson, JL; Komrokji, R; Lancet, JE; List, AF; Padron, E; Sallman, DA; Shah, BD; Sullivan, DM; Sweet, K; Turner, JG; Zhou, J, 2020
)
0.56
"This was a single-arm phase I clinical trial of selinexor combined with cytarabine and daunorubicin (7+3)."( Phase I Clinical Trial of Selinexor in Combination with Daunorubicin and Cytarabine in Previously Untreated Poor-Risk Acute Myeloid Leukemia.
Chavez, J; Cubitt, CL; Dawson, JL; Komrokji, R; Lancet, JE; List, AF; Padron, E; Sallman, DA; Shah, BD; Sullivan, DM; Sweet, K; Turner, JG; Zhou, J, 2020
)
0.56
" A semimechanistic physiologically-based pharmacokinetic (PBPK) model was developed to evaluate the potential for clinical drug-drug interactions (DDIs)."( Prediction of Clinical Transporter-Mediated Drug-Drug Interactions via Comeasurement of Pitavastatin and Eltrombopag in Human Hepatocyte Models.
Carter, SJ; Chappell, MJ; Chouhan, B; Sharma, P, 2020
)
0.56
" We performed a phase I study to determine the safety and maximum tolerated dose (MTD) of selinexor when combined with high-dose dexamethasone, ifosfamide, carboplatin and etoposide (DICE) in relapsed/refractory (R/R) T-cell lymphoma (TCL) and natural-killer/T-cell lymphoma (NKTL)."( Phase I study of selinexor in combination with dexamethasone, ifosfamide, carboplatin, etoposide chemotherapy in patients with relapsed or refractory peripheral T-cell or natural-killer/T-cell lymphoma
Chan, JY; Farid, M; Lim, C; Lim, ST; Martin, P; Poon, E; Somasundaram, N; Tang, T; Tao, M; Toh, SQ; Yan, SX; Yunon, MJ, 2021
)
0.62
" This study assessed the efficacy and safety of eltrombopag in combination with rabbit-ATG/CsA in IST-naïve patients with non-severe or severe AA in Japan."( Eltrombopag in Combination with Rabbit Anti-thymocyte Globulin/Cyclosporine A in Immunosuppressive Therapy-naïve Patients with Aplastic Anemia in Japan.
Fanghong, Z; Hombo, Y; Iida, H; Imada, K; Imajo, K; Kumagai, A; Maeda, T; Matsuda, A; Nakao, S; Obara, N; Tajima, T; Usuki, K, 2021
)
0.62
" The study's aim was to determine the safety and efficacy of selinexor in combination with doxorubicin in patients with locally advanced/metastatic STS."( A phase 1b trial of selinexor, a first-in-class selective inhibitor of nuclear export (SINE), in combination with doxorubicin in patients with advanced soft tissue sarcomas (STS).
Abdul Razak, A; Accardi, S; Al-Ezzi, E; Fasih, S; Gupta, A; Lewin, J; Malone, E; Pedersen, P, 2021
)
0.62
" Therefore, when selinexor and posaconazole are combined, we should pay attention to the possible drug-drug interactions to reduce adverse reactions."( Establishment and Verification of UPLC-MS/MS Technique for Pharmacokinetic Drug-Drug Interactions of Selinexor with Posaconazole in Rats.
Li, CF; Qiu, XJ; Wang, HJ; Zhou, CJ; Zhou, CY; Zhu, MJ, 2021
)
0.62
" Conclusions Once weekly selinexor in combination with topotecan was viable and showed some preliminary tumor efficacy."( Selinexor in combination with topotecan in patients with advanced or metastatic solid tumors: Results of an open-label, single-center, multi-arm phase Ib study.
Bean, S; Carter, BW; Colen, R; Gong, J; Janku, F; Karp, DD; McQuinn, L; Meric-Bernstam, F; Milton, DR; Naing, A; Ogbonna, DC; Pant, S; Piha-Paul, SA; Shah, J; Subbiah, V; Thein, KZ; Tsimberidou, A; Zarifa, A, 2021
)
0.62
" In recent trials, eltrombopag combined with standard immunosuppressive therapy yielded superior responses than those to immunosuppressive therapy alone."( Predicting response of severe aplastic anemia to immunosuppression combined with eltrombopag.
Feng, X; Groarke, EM; Patel, BA; Shalhoub, R; Wu, CO; Young, NS; Zaimoku, Y, 2022
)
0.72
"When it comes to the treatment of aplastic anemia fever, the Guidelines for Aplastic Anemia regards Anti-thymocyte globulin (ATG) combined with eltrombopag as the standard immunosuppressive treatment plan, and ATG is the main mode to treat severe aplastic anemia."( A systematic review and meta-analysis of the safety and efficacy of anti-thymocyte globulin combined with eltrombopag in the treatment of severe aplastic anemia.
Chen, L; Han, S; Liu, J; Peng, Y; Wang, H; Wu, Y; Zhang, J, 2021
)
0.62
" Patients in the experimental group were administered ATG combined with eltrombopag and patients in the control group received ATG treatment alone."( A systematic review and meta-analysis of the safety and efficacy of anti-thymocyte globulin combined with eltrombopag in the treatment of severe aplastic anemia.
Chen, L; Han, S; Liu, J; Peng, Y; Wang, H; Wu, Y; Zhang, J, 2021
)
0.62
"The RP2D of selinexor was 60 mg QW in combination with CT."( Selinexor in combination with carboplatin and paclitaxel in patients with advanced solid tumors: Results of a single-center, multi-arm phase Ib study.
Carter, BW; Colen, R; Fu, S; Gong, J; Hong, DS; Janku, F; Karp, DD; McQuinn, L; Meric-Bernstam, F; Milton, DR; Naing, A; Piha-Paul, SA; Shah, J; Stephen, BA; Sulovic, S; Thein, KZ; Tsimberidou, A; Yap, TA, 2022
)
0.72
" The XPO1 inhibitor KPT-330 has also exhibited promising efficacy in combination with other novel drugs in treating relapsed/refractory MM (RRMM)."( Anti-tumor activity of the pan-RAF inhibitor TAK-580 in combination with KPT-330 (selinexor) in multiple myeloma.
Ando, K; Kawada, H; Kitamura, Y; Ogawa, Y; Ogiya, D; Suzuki, R, 2022
)
0.72
" In this paper, we demonstrate a highly sensitive PGR detection method by using terahertz time-domain spectroscopy combined with metamaterials."( Highly sensitive detection of plant growth regulators by using terahertz time-domain spectroscopy combined with metamaterials.
Du, X; Liu, Y; Ma, G; Mao, H; Wang, B; Wang, Y; Zhang, X, 2021
)
0.62
" Therefore, we sought to explore the synergistic effects and possible mechanisms of DFX combination with ELT in MDS cells."( Deferasirox combination with eltrombopag shows anti-myelodysplastic syndrome effects by enhancing iron deprivation-related apoptosis.
Fu, R; Huang, L; Liu, C; Liu, Z; Tian, M, 2022
)
0.72
" Therefore, we performed rituximab combined with a low dose of EPAG."( Early treatment of rituximab combined with eltrombopag for secondary thrombocytopenic purpura in rheumatoid arthritis: A case report.
Bao, X; Ji, C; Yuan, C; Zhang, N, 2022
)
0.72
"The patient received 2 cycles of rituximab combined with EPAG, and reported no new petechiae on her buccal mucosa and limbs during follow-up."( Early treatment of rituximab combined with eltrombopag for secondary thrombocytopenic purpura in rheumatoid arthritis: A case report.
Bao, X; Ji, C; Yuan, C; Zhang, N, 2022
)
0.72
"This case suggests that early treatment of rituximab combined with EPAG is beneficial to patients with refractory ITP in RA."( Early treatment of rituximab combined with eltrombopag for secondary thrombocytopenic purpura in rheumatoid arthritis: A case report.
Bao, X; Ji, C; Yuan, C; Zhang, N, 2022
)
0.72
"Oral selinexor in combination with weekly paclitaxel demonstrated promising clinical activity with manageable toxicity."( Selinexor in combination with weekly paclitaxel in patients with metastatic solid tumors: Results of an open label, single-center, multi-arm phase 1b study with expansion phase in ovarian cancer.
Akhmedzhanov, F; Brink, AL; Carter, B; Coleman, RL; Fu, S; Gershenson, D; Gong, J; Hong, DS; Jazaeri, A; Leung, CH; Lin, H; McQuinn, L; Meric-Bernstam, F; Naing, A; Pant, S; Piha-Paul, S; Shah, J; Sood, AK; Tsimberidou, A; Westin, SN; Yilmaz, B, 2023
)
0.91
" The purpose of this study was to evaluate the anti-tumor effects of selinexor, used in combination with chemotherapy drugs (i."( Anti-tumor activity of selinexor in combination with antineoplastic agents in chronic lymphocytic leukemia.
Arruga, F; Boccellato, E; Bruno, B; Coscia, M; Deaglio, S; Efremov, DG; Griggio, V; Jones, R; Landesman, Y; Perutelli, F; Riganti, C; Todaro, M; Vaisitti, T; Vitale, C, 2023
)
0.91

Bioavailability

ExcerptReferenceRelevance
"The bioavailability of levodopa-benserazide in a standard capsule and a new dispersible tablet was compared in Parkinsonian patients, with (n = 8) and without (n = 8) swallowing difficulties."( Bioavailability and acceptability of a dispersible formulation of levodopa-benserazide in parkinsonian patients with and without dysphagia.
Bayer, AJ; Day, JJ; Finucane, P; Pathy, MS, 1988
)
0.27
" The clinical response to Madopar HBS was delayed and brief; the relative bioavailability was only 50%."( Single-dose studies of a slow-release preparation of levodopa and benserazide (Madopar HBS) in Parkinson's disease.
Jenner, P; Malcolm, SL; Marion, MH; Marsden, CD; Quinn, NP; Stocchi, F, 1987
)
0.27
" In comparison with standard Madopar the rate of absorption is reduced, providing lower peak concentrations of L-dopa."( Single-dose pharmacokinetics of Madopar HBS in patients and effect of food and antacid on the absorption of Madopar HBS in volunteers.
Allen, JG; Bird, H; Malcolm, SL; Marion, MH; Marsden, CD; O'Leary, CG; Quinn, NP, 1987
)
0.27
" The mean relative bioavailability (versus standard Madopar) was 58 and 67% (value normalized to dose) for one and two HBS capsules, respectively."( Bioavailability of L-dopa after Madopar HBS administration in healthy volunteers.
Crevoisier, C; Da Prada, M; Hoevels, B; Zürcher, G, 1987
)
0.27
" Oral bioavailability of 1- and total propranolol averaged 40."( No stereoselective first-pass hepatic extraction of propranolol.
Bobik, A; Jackman, GP; Jennings, GL; McLean, AJ, 1981
)
0.26
" The four compounds showed oral bioavailability around 35% and equipotency in vitro compared to NN703."( Growth hormone secretagogues derived from NN703 with hydrazidesas c-terminal.
Ankersen, M; Kramer Nielsen, K; Kruse Hansen, T; Raun, K; Sehested Hansen, B, 2000
)
0.31
" 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
" In the present study we examined the antioxidant activity and bioavailability of these epimers compared with their corresponding precursors."( Comparison of antioxidant activity and bioavailability of tea epicatechins with their epimers.
Chang, Q; Chen, ZY; Huang, Y; Xu, JZ; Yeung, SY, 2004
)
0.32
" Peptidomimetics have been developed to circumvent problems inherent in peptides such as poor bioavailability and protease-mediated degradation, while retaining biological activity."( Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.
Arlot-Bonnemains, Y; Aubin, S; Baudy-Floc'h, M; Delcros, JG; Martin, B, 2005
)
0.33
" These data have clearly illustrated the low bioavailability of AF-2364 in rats and that this compound is not specifically taken up by any organs including the testis or the epididymis."( AF-2364 [1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide] is a potential male contraceptive: a review of recent data.
Bonanomi, M; Cheng, CY; Lee, NP; Lui, WY; Mo, MY; Mruk, D; Silvestrini, B; Siu, MK; Wong, CH, 2005
)
0.33
"The effects of acetaldehyde due to consumption of ethanol on the uptake and bioavailability of therapeutic drug compounds transported by the PEPT1 oligopeptide transporter have not been documented."( Evaluation of the effect of ethanol's toxic metabolite acetaldehyde on the gastrointestinal oligopeptide transporter, PEPT1: in vitro and in vivo studies.
Eddington, ND; Fisher, SJ; Lee, IJ; Swaan, PW, 2008
)
0.35
" Since nitric oxide bioavailability is decreased in sickle cell disease and nitric oxide may inhibit leukocyte adhesion, we investigated whether stimulation of NO-signaling pathways can reduce the adhesive properties of neutrophils from sickle cell disease individuals (sickle cell diseaseneu)."( Increased adhesive properties of neutrophils in sickle cell disease may be reversed by pharmacological nitric oxide donation.
Canalli, AA; Conran, N; Costa, FF; Franco-Penteado, CF; Saad, ST, 2008
)
0.35
" Intravenous treatment showed a more severe disturbance of spermatogenesis compared with gavage treatment, which was correlated with bioavailability of the drug."( Adjudin targeting rabbit germ cell adhesion as a male contraceptive: a pharmacokinetics study.
Bonanomi, M; Chen, BB; Chen, GR; Cheng, CY; Ge, RS; Hu, GX; Hu, LF; Li, JW; Mruk, DD; Silvestrini, B; Yang, DZ,
)
0.13
" We hypothesized that the relaxation to BAY 41-2272 is decreased in spontaneously hypertensive rats (SHR) because of the reduced NO bioavailability in this strain and that relaxation would be improved by inhibiting the oxidative stress."( Oxidative stress impairs vasorelaxation induced by the soluble guanylyl cyclase activator BAY 41-2272 in spontaneously hypertensive rats.
Priviero, FB; Teixeira, CE; Webb, RC; Zemse, SM, 2009
)
0.35
"Augmented oxidative stress in SHR impaired cGMP-dependent and -independent relaxation induced by BAY 41-2272, by decreasing NO bioavailability and sGC expression and by increasing contractile activity."( Oxidative stress impairs vasorelaxation induced by the soluble guanylyl cyclase activator BAY 41-2272 in spontaneously hypertensive rats.
Priviero, FB; Teixeira, CE; Webb, RC; Zemse, SM, 2009
)
0.35
" Preclinical testing on healthy volunteers shows high drug bioavailability and efficacy in raising platelet counts."( Eltrombopag (Promacta), a thrombopoietin receptor agonist for the treatment of thrombocytopenia: current and future considerations.
Eisert, C; Makarov, L; Sabaeva, E; Serebruany, VL,
)
0.13
" Thus, to the extent that somatodendritic DA release affects behavior, TH regulation in the midbrain may be critical for DA bioavailability to influence behavior."( Dichotomy of tyrosine hydroxylase and dopamine regulation between somatodendritic and terminal field areas of nigrostriatal and mesoaccumbens pathways.
Pruett, BS; Salvatore, MF, 2012
)
0.38
"We aimed to assess the bioavailability of eltrombopag PfOS relative to the tablet formulation and the effect of a high-calcium meal on PfOS bioavailability."( A randomized, open-label, 5-period, balanced crossover study to evaluate the relative bioavailability of eltrombopag powder for oral suspension (PfOS) and tablet formulations and the effect of a high-calcium meal on eltrombopag pharmacokinetics when admin
Brainsky, A; Bruce, J; Gauvin, J; McGuire, S; Pendry, CJ; Qian, Y; Wire, MB, 2012
)
0.38
"In a healthy adult volunteer population, bioavailability of eltrombopag PfOS was greater than the tablet and was reduced when administered with or 2 hours before or after a high-calcium meal; this effect was attenuated with PfOS dosing 2 hours before the meal."( A randomized, open-label, 5-period, balanced crossover study to evaluate the relative bioavailability of eltrombopag powder for oral suspension (PfOS) and tablet formulations and the effect of a high-calcium meal on eltrombopag pharmacokinetics when admin
Brainsky, A; Bruce, J; Gauvin, J; McGuire, S; Pendry, CJ; Qian, Y; Wire, MB, 2012
)
0.38
"Eltrombopag is an orally bioavailable thrombopoietin receptor agonist that is approved for the treatment of chronic idiopathic thrombocytopenic purpura."( Assessment of the pharmacokinetic interaction between eltrombopag and lopinavir-ritonavir in healthy adult subjects.
McLean, HB; Park, JW; Pendry, C; Peng, B; Theodore, D; Wire, MB, 2012
)
0.38
" While romiplostim was the first second generation thrombopoietin agonist to become available, eltrombopag is particularly attractive as it is an orally bioavailable agent."( Eltrombopag--an oral thrombopoietin agonist.
Aggarwal, S; Randhawa, H; Sharma, A; Sharma, V, 2012
)
0.38
" For instance, adjudin, 1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide, a potential nonhormonal male contraceptive that exerts its effects on germ cell adhesion, most notably at the Sertoli cell-spermatid interface, to induce "premature" germ cell loss from the seminiferous epithelium mimicking spermiation, has a relatively poor bioavailability largely because of the BTB."( Role of P-glycoprotein at the blood-testis barrier on adjudin distribution in the testis: a revisit of recent data.
Bonanomi, M; Cheng, CY; Cheng, YH; Jenardhanan, P; Mathur, PP; Mok, KW; Mruk, DD; Silvestrini, B; Su, L, 2012
)
0.38
"Drug transporters determine the bioavailability of drugs in the testis behind the blood-testis barrier (BTB)."( Breast cancer resistance protein regulates apical ectoplasmic specialization dynamics stage specifically in the rat testis.
Cheng, CY; Mruk, DD; Qian, X; Wong, EW, 2013
)
0.39
" These results suggest that BAY 60-2770 would be effective in the treatment of erectile dysfunction when NO bioavailability is reduced, after pelvic nerve injury, and when sGC is oxidized."( The sGC activator BAY 60-2770 has potent erectile activity in the rat.
Frink, TJ; Kadowitz, PJ; Lasker, GF; Pankey, EA; Walter, KA; Zeitzer, JR, 2013
)
0.39
"This study provides evidence that the novel orally bioavailable XPO1 inhibitor KPT-335 is safe and exhibits activity in a relevant, spontaneous large animal model of cancer."( Preclinical evaluation of the novel, orally bioavailable Selective Inhibitor of Nuclear Export (SINE) KPT-335 in spontaneous canine cancer: results of a phase I study.
Barnard, S; Bear, MD; Bernabe, LF; Borgatti, A; Henson, M; Ito, D; Jensen, K; Kauffman, M; Kisseberth, WC; London, CA; McCauley, D; Modiano, JF; Pennell, ML; Saint-Martin, JR; Shacham, S; Wilson, H, 2014
)
0.4
" The present study sought to characterize the biologic activity of an orally bioavailable selective inhibitor of nuclear export (SINE), KPT-335, against canine melanoma cell lines as a prelude to future clinical trials in dogs with melanoma."( Biologic activity of the novel orally bioavailable selective inhibitor of nuclear export (SINE) KPT-335 against canine melanoma cell lines.
Bear, MD; Breit, MN; Kashyap, T; Kauffman, MG; Kisseberth, WC; Landesman, Y; London, CA; McCauley, D; Shacham, S, 2014
)
0.4
" Orally bioavailable selective inhibitors of nuclear export (SINE) that irreversibly bind to and inhibit the function of XPO1 have been recently developed."( KPT-330 inhibitor of XPO1-mediated nuclear export has anti-proliferative activity in hepatocellular carcinoma.
Gery, S; Kauffman, M; Koeffler, HP; Shacham, S; Sun, H; Zheng, Y, 2014
)
0.4
" Our efforts have led to the discovery of compound 7l as a potent glucagon receptor antagonist with good bioavailability and satisfactory long half-life."( Discovery of furan-2-carbohydrazides as orally active glucagon receptor antagonists.
Fujii, A; Hasegawa, F; Kato, K; Matsumoto, T; Migihashi, C; Murata, M; Negoro, T; Niidome, K, 2014
)
0.4
"Eltrombopag is an orally bioavailable thrombopoietin receptor agonist approved for the treatment of thrombocytopenia associated with chronic immune (idiopathic) thrombocytopenic purpura and chronic hepatitis C virus (HCV) infection."( Lack of clinically significant pharmacokinetic interaction between the thrombopoietin receptor agonist eltrombopag and hepatitis C virus protease inhibitors boceprevir and telaprevir.
Fang, L; Hussaini, A; Kleha, JF; Theodore, D; Wire, MB, 2014
)
0.4
" Selinexor is an orally bioavailable inhibitor of exportin-1 (CRM1/XPO1) with potent anticancer activity and is currently under evaluation in human clinical trials."( Identifying drug-target selectivity of small-molecule CRM1/XPO1 inhibitors by CRISPR/Cas9 genome editing.
Baloglu, E; Crochiere, M; Daelemans, D; Jacquemyn, M; Landesman, Y; Neggers, JE; Shacham, S; Vanstreels, E; Vercruysse, T, 2015
)
0.42
" Herein, we summarize recent findings pertinent to adjudin, a non-hormonal male contraceptive, and molecular interactions of adjudin with BCRP so that this information can be helpful to devise delivery strategies to evade BCRP in the tunica propria to improve its bioavailability in the testis."( Interaction of oligomeric breast cancer resistant protein (BCRP) with adjudin: a male contraceptive with anti-cancer activity.
Cheng, CY; Cheng, YH; Jenardhanan, P; Mathur, PP; Qian, X; Silvestrini, B; Xia, W, 2014
)
0.4
"Hemolysis and consequent release of cell-free hemoglobin (CFHb) impair vascular nitric oxide (NO) bioavailability and cause oxidative and inflammatory processes."( Acute hemolytic vascular inflammatory processes are prevented by nitric oxide replacement or a single dose of hydroxyurea.
Almeida, CB; Conran, N; Costa, FF; Costa, FT; Covas, DT; Leonardo, FC; Souza, LE; Werneck, CC, 2015
)
0.42
" However, factors such as changes of pharmacokinetics might modulate the effects of eltrombopag in older patients in Japan because East Asians show higher bioavailability of eltrombopag by as-yet-unknown mechanisms."( Age and Bone Marrow Cellularity are Associated with Response to Eltrombopag in Japanese Adult Immune Thrombocytopenia Patients: A Retrospective Single-Center Study.
Arai, N; Ariizumi, H; Fujiwara, S; Harada, H; Hattori, N; Kabasawa, N; Kawaguchi, Y; Mori, H; Nakamaki, T; Saito, B; Shiozawa, E; Tsukamoto, H; Uto, Y; Yanagisawa, K, 2015
)
0.42
" Recent advances in drug formulations, such as drug particle micronization (<50 μm) and co-grinding of drug particles with ß-cyclodextrin have improved bioavailability of contraceptives via considerable increase in solubility."( Effective Delivery of Male Contraceptives Behind the Blood-Testis Barrier (BTB) - Lesson from Adjudin.
Bonanomi, M; Chen, H; Cheng, CY; Mruk, DD; Silvestrini, B; Xia, W, 2016
)
0.43
" Selective inhibitors of nuclear export (SINE) are small orally bioavailable molecules that serve as drug-like inhibitors of XPO1, with potent anti-cancer properties."( A Nuclear Attack on Traumatic Brain Injury: Sequestration of Cell Death in the Nucleus.
Acosta, SA; Borlongan, CV; Carlson, R; De La Peña, I; Kaneko, Y; Landesman, Y; Shacham, S; Tajiri, N; Tamir, S, 2016
)
0.43
"Selinexor is an orally bioavailable selective inhibitor of nuclear export that has been demonstrated to have preclinical activity in various cancer types and that is currently in Phase I and II clinical trials for advanced cancers."( Preclinical activity of selinexor, an inhibitor of XPO1, in sarcoma.
Anatone, AJ; Czaplinski, JT; Demetri, GD; Fletcher, JA; Nakayama, R; Sicinska, ET; Wagner, AJ; Zhang, YX, 2016
)
0.43
" We quantified inflammation, fibrosis, oxidative stress, nitric oxide (NO) bioavailability and thromboxane B2 levels."( Contribution of Cyclooxygenase End Products and Oxidative Stress to Intrahepatic Endothelial Dysfunction in Early Non-Alcoholic Fatty Liver Disease.
Abrante, B; Diaz-Flores, F; Gonzalez-Paredes, FJ; Hernández Mesa, G; Hernández-Guerra, M; Marcelino Reyes, R; Morales Arraez, D; Quintero, E; Salido, E, 2016
)
0.43
"Our study provides evidence that endothelial dysfunction at an early stage of NAFLD is associated with reduced NO bioavailability together with increased cyclooxygenase end products and oxidative stress, which suggests that both pathways are involved in the pathophysiology and may be worth exploring as therapeutic targets to prevent progression of the disease."( Contribution of Cyclooxygenase End Products and Oxidative Stress to Intrahepatic Endothelial Dysfunction in Early Non-Alcoholic Fatty Liver Disease.
Abrante, B; Diaz-Flores, F; Gonzalez-Paredes, FJ; Hernández Mesa, G; Hernández-Guerra, M; Marcelino Reyes, R; Morales Arraez, D; Quintero, E; Salido, E, 2016
)
0.43
"There is increasing evidence that the permeability of the glomerular filtration barrier (GFB) is partly regulated by a balance between the bioavailability of nitric oxide (NO) and that of reactive oxygen species (ROS)."( Nitric oxide synthase inhibition causes acute increases in glomerular permeability in vivo, dependent upon reactive oxygen species.
Dolinina, J; Öberg, CM; Rippe, A; Rippe, B; Sverrisson, K, 2016
)
0.43
" In this review, we examine the use of Verdinexor (KPT-335, a novel orally bioavailable drug that functions as a selective inhibitor of nuclear export, SINE), as an antiviral with multifaceted therapeutic potential."( Verdinexor Targeting of CRM1 is a Promising Therapeutic Approach against RSV and Influenza Viruses.
Pickens, JA; Tripp, RA, 2018
)
0.48
" Selective inhibitor of nuclear export (SINE) compounds are novel, orally bioavailable class of agents that specifically inhibit XPO1."( Clinical Implications of Targeting XPO1-mediated Nuclear Export in Multiple Myeloma.
Baloglu, E; Chari, A; Cornell, RF; Gandhi, UH; Senapedis, W; Unger, TJ; Vogl, D, 2018
)
0.48
" KPT-335 (verdinexor) is a novel orally bioavailable selective inhibitor of nuclear export (SINE) that exhibited anti-tumor activity against non-Hodgkin lymphoma in a prior phase I study."( Phase II study of the oral selective inhibitor of nuclear export (SINE) KPT-335 (verdinexor) in dogs with lymphoma.
Borgatti, A; Gardner, HL; Klein, MK; Lachowicz, J; London, CA; Manley, C; Sadowski, AR; Sahora, A; Turner, A; Vail, DM; Waite, A; Wilson, H, 2018
)
0.48
"The bioavailability of the non-hormonal male contraceptive adjudin is low in rats due to the blood-testis barrier (BTB)."( F5-peptide enhances the efficacy of the non-hormonal male contraceptive adjudin.
Chen, H; Cheng, CY; Mruk, D; Silvestrini, B; Wong, CKC, 2019
)
0.51
" In this study, we show that the orally bioavailable XPO1 inhibitor KPT-330 reduced Mcl-1 protein level, by which it synergized with Bcl-xL inhibitor A-1331852 to induce apoptosis in cancer cells."( XPO1 inhibitor KPT-330 synergizes with Bcl-xL inhibitor to induce cancer cell apoptosis by perturbing rRNA processing and Mcl-1 protein synthesis.
Liu, JW; Xiong, ZQ; Yang, C; Zhao, M; Zhu, ZC, 2019
)
0.51
"Verdinexor (KPT-335) is a novel orally bioavailable selective inhibitor of nuclear export (SINE) compound that inhibits the function of the nuclear export protein Exportin 1 (XPO1/CRM1)."( The selective inhibitor of nuclear export (SINE) verdinexor exhibits biologic activity against canine osteosarcoma cell lines.
Breitbach, JT; Davies, AE; Fenger, JM; Louke, DS; Tobin, SJ; Watts, MR, 2021
)
0.62
"Curcumin, a natural polyphenol from Curcuma longa, is known to possess diversified pharmacological roles including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic properties; however, its bioavailability is severely limited due to its poor solubility, poor absorption, rapid metabolism, and significant elimination."( Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats.
Choudhury, H; Dhanawat, M; Gupta, S; Jacob, S; Munjal, K; Nair, AB, 2021
)
0.62
" These results revealed a faster rate and longer duration of absorption with intraperitoneal administration, which further resulted in enhanced absolute bioavailability of HZC (29."( Pharmacokinetics and tissue distribution of hydrazinocurcumin in rats.
Choudhury, H; Dhanawat, M; Gupta, S; Jacob, S; Munjal, K; Nair, AB, 2021
)
0.62
" Compound 5k also showed considerable bioavailability in SD mice."( Novel 1,3,5-triazine-nicotinohydrazide derivatives induce cell arrest and apoptosis in osteosarcoma cancer cells and inhibit osteosarcoma in a patient-derived orthotopic xenograft mouse model.
Gong, Z; Su, Q; Tian, Z; Xu, B, 2022
)
0.72
"Eltrombopag is an orally bioavailable drug developed as a second-line treatment for immune thrombocytopenia."( Does eltrombopag lead to thrombotic events? A pharmacovigilance study of the FDA adverse event reporting system.
Jiang, JJ; Li, J; Zhao, B, 2022
)
0.72
" The additional studies like pharmacokinetics, bioavailability scores and drug-likeness properties were also evaluated."( Synthesis and Biological Evaluation of Some Hydrazide-Hydrazone Derivatives as Anticancer Agents.
Akdağ, K; Çevik, Ö; Erdoğan, Ö; Karakuş, S; Koçyiğit-Kaymakçıoğlu, B; Tok, F, 2022
)
0.72

Dosage Studied

Male rats and rabbits were singly dosed with either 1-[14C]acetyl isoniazid (acetylisonicotinoylhydrazine, acetyl-INH, 200 mg/kg po) or 1 [14C ]acetylHydrazine (50 or 100mg/kg ip) In all these bioassays on Drosophila larvae, the two purely synthetic hydrazines exhibited similar dose-response relationships as did the natural steroid hormone, 20-hydroxyecdysone.

ExcerptRelevanceReference
"2 mg/kg) of apomorphine reduced locomotion in a dose-dependent manner, while the reduction after higher doses was less pronounced, indicating a biphasic dose-response relationship."( Catecholamine receptor agonists: effects on motor activity and rate of tyrosine hydroxylation in mouse brain.
Strömbom, U, 1976
)
0.26
" By the use of the combination preparation, the daily dosage of levodopa could be reduced by 77%."( A comparative clinical investigation of the therapeutic effect of levodopa alone and in combination with a decarboxylase inhibitor (carbidopa) in cases of Parkinson's disease.
Dorner, A; Wajsbort, E; Wajsbort, J, 1978
)
0.26
" Mean daily maintenance dosage was 612."( Levodopa/benserazide ('Madopar') combination therapy in elderly patients with parkinsonism.
Carlyle, D; Williams, BO, 1979
)
0.26
" With both drugs, Madopar or Sinemet, an optimum therapeutic result was obtained with relatively small doses of L-dopa (the reduction in L-dopa dosage amounting to about 80%)."( [The combined treatment of Parkinson's disease with L-dopa plus decarboxylase inhibitors (carbidopa, benserazide) (author's transl)].
Birkmayer, W; Mentasti, M; Podiwinsky, F; Riederer, P, 1979
)
0.26
"It was found that under the influence of hydrazine sulfate, which in the dosage of 60 mg/kg would induce a 50% suppression of Walker carcinosarcoma in rats, there is the decreased activity of mitochondrial monoamine oxidase and a sharp reduction in the activity of some microsomal phosphatases."( [Experimental data to substantiate the antitumor action of hydrazine sulfate].
Filov, VA; Riazanov, EM; Tarkov, AS; Tret'iakov, AV, 1979
)
0.77
" The treatment periods were 12 weeks; similar dosage schedules were used, with doses that induced equal levels of plasma levodopa in both combinations."( Levodopa with benserazide or carbidopa in Parkinson disease.
Mölsä, P; Rinne, UK, 1979
)
0.26
" The study was designed as paired series of growth hormone stimulation tests in which the effect of L-dopa alone, in different dosage schedules, was compared with the same dose level of L-dopa plus carbidopa, When L-dopa was given in full dose (125-500 mg), there was no significant difference in the serum GH concentrations at any time of sampling."( The effect of L-dopa with and without decarboxylase inhibitor on growth hormone secretion in children with short stature.
Aarskog, D; Fevang, FO; Stoa, RF; Thorsen, T, 1977
)
0.26
" Generally the dosage range was up to a maximum of one tablet three times daily."( [Treatment of Parkinson's disease with the combination drug L-carbidopa/L-dopa. Report on a 2 years study].
Hayek, J, 1977
)
0.26
" A reduced mean L-Dopa dosage was ruled out as the cause of this deterioration."( Study of deterioration in long-term treatment of parkinsonism with L-dopa plus decarboxylase inhibitor.
Bass-Verrey, F; Ludin, HP, 1976
)
0.26
" Combination therapy resulted in a reduction in L-dopa dosage to 1/3 of the amount required during the baseline."( Alpha methyldopahydrazine as an adjunct to levodopa therapy in Parkinson's disease.
Jaatoul, N; Kertesz, A; McInnis, W; Paty, DW, 1975
)
0.6
" Clinical pharmacological studies disclosed that a 1 : 10 ratio of MK-486 to L-dopa in dosage was preferable."( L-dopa therapy combined with peripheral decarboxylase inhibitor (MK-486) in Parkinsonism.
Kishikawa, H; Ohmoto, T, 1975
)
0.25
" Patients were allocated at random to treatment with either levodopa + benserazide ratio 4:1 (Madopar) or levodopa + carbidopa ratio 10:1 (Sinemet) using dosage schedules recommended by the manufacturers which they had to adhere to for 6 months."( Parkinson's disease treated with Sinemet or Madopar. A controlled multicenter trial.
Birket-Smith, E; Dupont, E; Hansen, E; Mikkelsen, B; Pakkenberg, H; Presthus, J; Rautakorpi, I; Riman, E; Rinne, UK, 1976
)
0.26
" Dose-response analyses indicated that the DNDH/HRP chemiluminescence system could give linear standard curves with hydrogen peroxide concentrations into the nmol l-1 range."( Enhanced detection of reactive oxygen species produced by human spermatozoa with 7-dimethyl amino-naphthalin-1, 2-dicarbonic acid hydrazide.
Aitken, RJ; Buckingham, D, 1992
)
0.28
"1 mg/kg iv, responses to U-46619 and U-44069 were reduced significantly, and the dose-response curves for these TxA2 mimics were shifted to the right in a parallel manner at a time when responses to PGF2 alpha and PGD2 were not altered."( Characterization of thromboxane receptor blocking effects of SQ 29548 in the feline pulmonary vascular bed.
Hood, JS; Hyman, AL; Kadowitz, PJ; McMahon, TJ; Nossaman, BD, 1992
)
0.28
" The relationship held over an extensive range of experimental conditions including different drugs, different dosage levels of the same drug, different time intervals after administration of the same drug, and both single and multiple injections of drugs."( Regulation of the GABAA receptor/ion channel complex by intracellular GABA levels.
Davies, M; Wood, JD, 1991
)
0.28
" Following the administration of SQ 29,548, pressor responses to both U44069 and U46619 were reduced significantly, and the dose-response curves for both TXA2 mimics were shifted to the right in a parallel fashion."( Influence of SQ 29,548 on vasoconstrictor responses in the hindquarters vascular bed of the cat.
Bellan, JA; Kadowitz, PJ; McMahon, TJ; McNamara, DB; Minkes, RK, 1991
)
0.28
" SQ 30741 had no significant effect on mean vascular pressures in the cat, and the dose-response curve for U-46619 was shifted to the right in a parallel manner with a similar apparent maximal response."( Influence of SQ 30741 on thromboxane receptor-mediated responses in the feline pulmonary vascular bed.
Feng, CJ; Hood, JS; Ibrahim, IN; Kadowitz, PJ; McMahon, TJ; Nossaman, BD, 1991
)
0.28
"The non-steroidal ecdysone agonist RH 5849 (1,2-dibenzoyl-1-tert-butylhydrazine) was found to inhibit in a dose-response and apparently competitive fashion the cytochrome P-450 dependent ecdysone 20-monooxygenase activity in the midgut of wandering stage last instar larvae of the tobacco hornworn, Manduca sexta."( Regulation of cytochrome P-450 dependent steroid hydroxylase activity in Manduca sexta: effects of the ecdysone agonist RH 5849 on ecdysone 20-monooxygenase activity.
Keogh, DP; Smith, SL, 1991
)
0.52
" Preincubation of rat aorta with 10 microM SQ 29,548, a "selective" antagonist of thromboxane A2/prostaglandin H2 (TP) receptors, caused a rightward shift in the dose-response curve and a reduction in the maximal response to endothelin-1."( Role of thromboxane A2/prostaglandin H2 receptor in the vasoconstrictor response of rat aorta to endothelin.
Mok, LL; Reynolds, EE, 1990
)
0.28
"The urinary excretion of taurine by rats after dosing with various hepatotoxins has been investigated by 1H NMR spectroscopy."( Hepatotoxin-induced hypertaurinuria: a proton NMR study.
Elcombe, C; Nicholson, JK; Sanins, SM; Timbrell, JA, 1990
)
0.28
" The equivalent L-dopa dosage had to be increased by 56% (29-100%) with Madopar HBS while mean dopamine levels increased in four patients (by 47-257%) without the occurrence of peripheral side-effects."( Controlled-release levodopa/benserazide (Madopar HBS): clinical observations and levodopa and dopamine plasma concentrations in fluctuating parkinsonian patients.
Ceballos-Baumann, AO; Eckert, W; von Kummer, R; Weicker, H, 1990
)
0.28
" Topical application of exogenous PGF2 alpha and U46619 resulted in dose-dependent cerebral vasoconstriction, and the dose-response curve for each agonist was shifted to the right by the increasing concentrations of SQ29548 (10(-6)-10(-8) M)."( Effect of thromboxane A2/endoperoxide antagonist SQ29548 on the contractile response to acetylcholine in newborn piglet cerebral arteries.
Busija, DW; Wagerle, LC, 1990
)
0.28
" In separate groups of rats, the log dose-response curve for bolus intravenous injection of AII was shifted to the right by SQ-29,548 while that for PE was unaffected."( Thromboxane mediation of the pressor response to infused angiotensin II.
Welch, WJ; Wilcox, CS, 1990
)
0.28
" The optimal therapeutic dosage of Sinemet CR was equal to that of Madopar HBS but 12% higher than that of standard Madopar."( Treatment of early Parkinson's disease with controlled-release levodopa preparations.
Rinne, JO; Rinne, UK, 1989
)
0.28
" Fetal weight and crown-rump length were reduced in the highest dosage group."( Effects of paternal subacute exposure to Tordon 202c on fetal growth and development in CD-1 mice.
Blakley, PM; Firneisz, GD; Kim, JS, 1989
)
0.28
" The model is then used to optimize the dosage regimen for each patient individually (according to the clinical particularities and needs of each patient) with respect to an objective function which includes the symptoms dynamically and the total amount of levodopa which is to be administered."( Optimization of symptomatic therapy in Parkinson's disease.
Albani, C; Hacisalihzade, SS; Mansour, M, 1989
)
0.28
" Even better results could be accomplished in an extended trial attempting to establish the best dosage ratio of the combination, possibly admitting increased dosage."( A combined regimen of subcutaneous lisuride and oral Madopar HBS in Parkinson's disease.
Aljanati, R; Caamaño, JL; Chouza, C; de Medina, O; Romero, S; Scaramelli, A, 1988
)
0.27
" During the first month the dosage titration was aimed at finding the optimal therapeutic effect."( Clinical trial of Madopar HBS in parkinsonian patients with fluctuating drug response after long-term levodopa therapy.
Aymard, N; Holzer, J; Rondot, P; Ziegler, M, 1987
)
0.27
"Madopar HBS (125 mg) is a controlled-release dosage form with 100 mg L-dopa and 25 mg benserazide."( The hydrodynamically balanced system: a novel principle of controlled drug release.
Erni, W; Held, K, 1987
)
0.27
" At the beginning the patients were switched from standard Madopar to Madopar HBS, initially keeping constant L-dopa dosage and the number of daily doses."( Open clinical study of Madopar HBS.
Ludin, HP, 1987
)
0.27
" However, with the new formulation the dosage had to be increased by 86% on average as compared with standard Madopar."( Treatment of parkinsonian conditions with a controlled-release form of levodopa--preliminary study.
D'Andrea, G; Durisotti, C; Ferro-Milone, F; Lion, P; Lorizio, A; Nordera, GP, 1987
)
0.27
" For the first few days (up to 1 week) dosage and number of daily intakes of HBS were the same as those of the standard formulation."( Preliminary experience with Madopar HBS: clinical observations and plasma levodopa concentrations.
Baas, H; Fischer, PA, 1987
)
0.27
" The overall increase in dosage of levodopa with Madopar HBS was 54% in comparison with the initial standard Madopar dosage."( Open multicenter trial with Madopar HBS in parkinsonian patients. Preliminary assessment after short-term treatment.
Heersema, T; Jansen, EN; Meerwaldt, JD; Speelman, JD; van Manen, J, 1987
)
0.27
" The frequency of drug intake was unaltered but daily dosage could be increased by 30% without increasing severity of abnormal movements to a similar degree."( [Controlled release levodopa-benserazide and changes in efficacy during treatment of Parkinson's disease].
Aymard, N; Holzer, J; Rondot, P; Ziegler, M, 1987
)
0.27
" In 13 patients a considerable diminution in nocturnal akinesia and in the frequency of waking up was reached with a mean dosage of 308 mg of Madopar HBS."( Madopar HBS in Parkinson patients with nocturnal akinesia.
Jansen, EN; Meerwaldt, JD, 1988
)
0.27
" Although the bioavailability after oral dosing is reduced as compared with standard Madopar (60-70%), this difference seems to be due to incomplete absorption rather than altered disposition of the drug."( Single-dose pharmacokinetics of Madopar HBS in patients and effect of food and antacid on the absorption of Madopar HBS in volunteers.
Allen, JG; Bird, H; Malcolm, SL; Marion, MH; Marsden, CD; O'Leary, CG; Quinn, NP, 1987
)
0.27
" At the end of the dosage adaptation phase (9 weeks) most patients improved; in patients with 'on-off' phenomenon, parkinsonism became less severe, on periods were longer, and fluctuations decrease; end-of-dose impairment resolved in 4 patients."( Substitution of standard Madopar by Madopar HBS in parkinsonians with fluctuations.
Aljanati, R; Caamano, JL; Chouza, C; de Medina, O; Gonzales Panizza, V; Romero, S; Scarmelli, A, 1987
)
0.27
" The dosage was adjusted until optimal response was obtained."( Madopar HBS: slow-release levodopa and benserazide in parkinsonian patients presenting marked fluctuations in symptoms on standard L-dopa treatment.
Dupont, E; Hansen, E; Jensen, NO; Mikkelsen, B; Mikkelsen, BO, 1987
)
0.27
" In all patients of the first group, after 3 months on stable 'optimal' dosage schedule, the previous L-dopa treatment was abruptly replaced, dose for dose, from one day to another by Madopar HBS, a new controlled-release form of Madopar."( Therapeutic value of Madopar HBS: judgment after 2 years experience.
Siegfried, J, 1987
)
0.27
" In an experiment similar to the dose-response study, 20 mg hydrazine/kg body wt was given to the two strains of mice, and animals were killed at 24 hr intervals to determine the persistence of these aberrant purines in DNA."( Comparative study on the indirect methylation of liver DNA guanine by the 1-carbon pool in hepatotoxicity.
Shank, RC, 1987
)
0.52
"The blood pressure and pulse rate have been compared in a 'double blind, cross over' study involving twenty patients with idiopathic Parkinsonism receiving maximum tolerated dosage of levodopa with and without an extracerebral decarboxylase inhibitor, L-alpha-methyldopahydrazine."( Action of L- -methyldopa-hydrazine on the blood pressure of patients receiving levodopa.
Calne, DB; Petrie, A; Rao, S; Reid, JL; Vakil, SD, 1972
)
0.73
" The effects of SK & F 92657 on resting flow and on the dose-response relationship for intra-arterial isoprenaline were studied."( Investigation of a combined arteriolar dilator and beta-adrenoceptor antagonist (SK & F 92657) in the peripheral vessels of man.
Collier, JG; Pitcher, DW, 1980
)
0.26
" Following effective stereotaxic surgery, drug therapy should be continued with reduced dosage of the drugs."( [Combined (surgical and drug) therapy of parkinsonism].
Iadgarov, IS; Kandel', EI, 1984
)
0.27
" Dose-response relationships for water flow (Jv) and capacitance increases (delta C) were similar from 1 to 20 mU/ml ADH."( Modulation of antidiuretic hormone-dependent capacitance and water flow in toad urinary bladder.
Palmer, LG; Speez, N, 1984
)
0.27
" The treatment with hydrazine sulfate (60 mg/kg) plus thiophosphamide (1 mg/kg) resulted in suppression of tumor growth up to 90%, the dosage of thiophosphamide being therapeutically ineffective."( [Selective action of hydrazine sulfate in combination with thiophosphamide on tumor cell mitochondria].
Filov, VA; Golovatova, VA; Tret'iakov, AV, 1982
)
0.91
"Male rats and rabbits were singly dosed with either 1-[14C]acetyl isoniazid (acetylisonicotinoylhydrazine, acetyl-INH, 200 mg/kg po) or 1-[14C]acetylhydrazine (50 or 100 mg/kg ip)."( Metabolism of [14C]acetylisoniazid and [14C]acetylhydrazine by the rat and rabbit.
Thomas, BH; Whitehouse, LW; Zeitz, W, 1984
)
0.74
"L-Tryptophan at moderately low dosage (20 mg/kg) reduced the activity of rats taken during a dark period (red light) and put into an open field illuminated by bright white light."( The effect of L-tryptophan on motor activity and its prevention by an extracerebral decarboxylase inhibitor and by 5-HT receptor blockers.
Curzon, G; Drewitt, PN; Tricklebank, MD, 1980
)
0.26
" PRL increase after benserazide was compared with PRL response after carbidopa at the same dosage in untreated parkinsonian patients."( Prolactin response to acute administration of different L-dopa plus decarboxylase inhibitors in Parkinson's disease.
Agnoli, A; Baldassarre, M; D'Urso, R; De Giorgio, G; Falaschi, P; Rocco, A; Ruggieri, S, 1982
)
0.26
" At equivalent germ-cell stages and dosage the mouse UDS assay is more sensitive, by a factor of 2 to 3, than the rabbit assay for the induction of UDS by procarbazine and MMS."( Induction of unscheduled DNA synthesis in the germ cells of male mice after treatment with hydrazine or procarbazine.
Chauhan, PS; Ehling, UH; Sotomayor, RE, 1982
)
0.48
" These changes were detectable by light or electron microscopy 24 h after dosing with hydrazine."( Studies on hydrazine hepatotoxicity. 1. Pathological findings.
Scales, MD; Timbrell, JA, 1982
)
0.88
" Pyd action is modified only by the most active purine 2-Cl-adenosine, which displaces the dose-response curves to the right."( Interactions between hydralazine, propildazine and purines on arterial smooth muscle.
Chevillard, C; Saiag, B; Worcel, M, 1981
)
0.26
" Dose-response curves were produced for these compounds."( Comparative mutagenicity of hydrazine and 3 methylated derivatives in L5178Y mouse lymphoma cells.
Back, KC; Rogers, AM, 1981
)
0.56
" infused over 2 min; n = 4-8 per group) produced a bell-shaped dose-response curve for MPAP and haematocrit, and evoked maximal increases of 12."( Intrinsic activity of the non-prostanoid thromboxane A2 receptor antagonist, daltroban (BM 13,505), in human platelets in vitro and in the rat vasculature in vivo.
Bertolino, F; Bessac, AM; Colpaert, FC; Delhon, A; Grelac, F; Lévy-Toledano, S; Maclouf, J; Maffre, M; Patoiseau, JF; Valentin, JP, 1995
)
0.29
" Increases in perfusion pressure in response to bolus injections of U46619 were used to construct dose-response curves."( Reduced thromboxane receptor affinity and vasoconstrictor responses in placentae from diabetic pregnancies.
Hollander, AM; Mento, PF; Wilkes, BM, 1994
)
0.29
"Time- and dose-response analyses were undertaken to investigate the effects of the substituted hydrazine monoamine oxidase (MAO) inhibitors iproniazid and nialamide on the following: MAO-A and -B activity; levels of gamma-aminobutyric acid (GABA), alanine (ALA), and the neurotransmitter amines dopamine, noradrenaline, and 5-hydroxytryptamine (serotonin) and their acid metabolites; and the activity of GABA-transaminase and ALA-transaminase."( Effects of two substituted hydrazine monoamine oxidase (MAO) inhibitors on neurotransmitter amines, gamma-aminobutyric acid, and alanine in rat brain.
Baker, GB; Paetsch, PR; Takahashi, S; Todd, KG; Yamada, N, 1993
)
0.8
" The effect of pretreatment of rats with various inhibitors and inducers of cytochrome P450 on these dose-response relationships was investigated."( Influence of inducers and inhibitors of cytochrome P450 on the hepatotoxicity of hydrazine in vivo.
Jenner, AM; Timbrell, JA, 1994
)
0.51
" Of these, 1-acetyl-1,2-bis-(methylsulfonyl)-2-(2-chloroethyl)hydrazine produced "cures" of mice bearing the L1210 leukemia at dosage levels that were considerably less than those at which the tris(sulfonyl) analog produced its antineoplastic effects."( Synthesis and evaluation of 1-acyl-1,2-bis(methylsulfonyl)-2-(2- chloroethyl)hydrazines as antineoplastic agents.
Divo, AA; Loomis, RH; Penketh, PG; Rose, WC; Sartorelli, AC; Shyam, K, 1993
)
0.76
" To obtain dose-response curves, single doses (as boluses) of acetylcholine were infused and the maximal A-V delay induced by each dose was determined."( Endothelium-mediated negative dromotropic effects of intravascular acetylcholine.
Ceballos, G; Rubio, R, 1998
)
0.3
" The dose-response for SNAP increases in cyclic GMP was shifted nearly two orders of magnitude lower in the presence of glutathione."( Comparative effects of several nitric oxide donors on intracellular cyclic GMP levels in bovine chromaffin cells: correlation with nitric oxide production.
Ferrero, R; Miras-Portugal, MT; Rodríguez-Pascual, F; Torres, M, 1999
)
0.3
") elevated blood pressure to a plateau of 30-50 mm Hg above baseline level and shifted the dose-response curve for acetylcholine-induced responses to the right by about 70-fold."( Inhibitory mechanism of N(G)-nitro-L-arginine on acetylcholine-induced depressor responses in dogs.
Ishii, K; Nakahara, T; Nakayama, K; Nejishima, H, 1999
)
0.3
" In all these bioassays on Drosophila larvae, the two purely synthetic hydrazines exhibited similar dose-response relationships as did the natural steroid hormone, 20-hydroxyecdysone."( Effect of bisacylhydrazine ecdysteroid mimics (RH-5849 and RH-5992) on chromosomal puffing, imaginal disc proliferation and pupariation in larvae of Drosophila melanogaster.
Farkas, R; Sláma, K, 1999
)
0.88
" Depending on the dosing of the administered compound, rats became infertile for 4-14 wk before their fertility gradually bounced back, illustrating the reversibility and efficacy of these new compounds."( Two new male contraceptives exert their effects by depleting germ cells prematurely from the testis.
Cheng, CY; Grima, J; Johansson, E; Leone, MG; Mo , MY; Mruk, D; Palmery, M; Saso, L; Silvestrini, B; Zhu , LJ, 2001
)
0.31
" Dose-response curves to quinpirole were unchanged in D(3) knock-out tissue, but secretion-regulated release exhibited a Hill slope decreased to 1 in the wild-type animals."( Dopamine autoreceptor regulation of release and uptake in mouse brain slices in the absence of D(3) receptors.
Budygin, EA; Caron, MG; Gainetdinov, RR; Joseph, JD; Miles, PR; Picetti, R; Wang, YM; Wightman, RM, 2002
)
0.31
" Dose-response regression lines for tebufenozide were parallel across populations, suggesting that the resistance mechanism(s) were quantitatively, but not qualitatively, different."( Resistance and cross-resistance to four insecticides in populations of obliquebanded leafroller (Lepidoptera: Tortricidae).
Lowery, DT; Smirle, MJ; Zurowski, CL, 2002
)
0.31
" 4-n-nonylphenol contamination caused an inverted dose-response curve."( Environmental chemicals with known endocrine potential affect yolk protein content in the aquatic insect Chironomus riparius.
Hahn, T; Schenk, K; Schulz, R, 2002
)
0.31
" The contributions of the metabolites to the separation of control from dosed liver tissues varied depending on the type of spectral editing method used."( Spectral editing and pattern recognition methods applied to high-resolution magic-angle spinning 1H nuclear magnetic resonance spectroscopy of liver tissues.
Antti, H; Beckonert, O; Bollard, ME; Ebbels, TM; Holmes, E; Keun, H; Lindon, JC; Nicholson, JK; Tang, H; Wang, Y, 2003
)
0.32
" Several examples of the utility of this approach from toxicological studies are presented as follows: interlaboratory variation in hydrazine response, CCl(4) dose-response relationships, and interspecies comparison of bromobenzene toxicity."( Geometric trajectory analysis of metabolic responses to toxicity can define treatment specific profiles.
Antti, H; Beckonert, O; Bollard, ME; Ebbels, TM; Holmes, E; Keun, HC; Lindon, JC; Nicholson, JK, 2004
)
0.53
" Oral and intravenous dosing of GTE-epimer mixture led to increase in total plasma antioxidant capacity in rats."( Comparison of antioxidant activity and bioavailability of tea epicatechins with their epimers.
Chang, Q; Chen, ZY; Huang, Y; Xu, JZ; Yeung, SY, 2004
)
0.32
" Dose-response relationships were determined for the three agonists; RH-2485 was found to be the most effective endocrine disruptor against all three species."( Comparative larvicidal toxicities of three ecdysone agonists on the mosquitoes Aedes aegypti, Culex quinquefasciatus, and Anopheles gambiae.
Beckage, NE; Marion, KM; Tan, FF; Walton, WE; Wirth, MC, 2004
)
0.32
" The NMR spectra of the renal cortex at 24 h after dosing were dominated by a marked increase in the tissue concentration of 2-aminoadipate (2-AA) and beta-alanine, concomitant with depletions in TMAO, myo-inositol, choline, taurine, glutamate, and lysine."( Integrated metabonomic analysis of the multiorgan effects of hydrazine toxicity in the rat.
Bollard, ME; Connelly, J; Connor, SC; Garrod, S; Holmes, E; Nicholls, AW; Nicholson, JK, 2005
)
0.57
" The potential adverse effects of excessive pyridoxine dosage will also be summarized."( Pyridoxine in clinical toxicology: a review.
Gris, M; Lheureux, P; Penaloza, A, 2005
)
0.33
" Dose-response experiments revealed that RH-5992 was even more potent than 20E."( Comparative effects of a non-steroidal ecdysone agonist RH-5992 and 20-hydroxyecdysone in a lepidopteran cell line (IAL-PID2).
Auzoux-Bordenave, S; Bozzolan, F; Debernard, S; Mottier, V; Porcheron, P; Queguiner, I; Siaussat, D; Solvar, M, 2005
)
0.33
" Dose-response associations were observed for both outcomes; similar associations were found for lung cancer mortality but not for colorectal cancer mortality."( Estimated effects of hydrazine exposure on cancer incidence and mortality in aerospace workers.
Kennedy, N; Krishnadasan, A; Morgenstern, H; Ritz, B; Zhao, Y, 2006
)
0.65
" Analysis of the dose-response effect also revealed that before reaching a threshold point, there is a linear relationship between increases in antioxidative activity and increases in the concentration of the koji extract."( Enhanced antioxidative activity of soybean koji prepared with various filamentous fungi.
Chou, CC; Lin, CH; Wei, YT, 2006
)
0.33
" Dose-response trends were evaluated using Cox proportional hazards models."( Mortality among Rocketdyne workers who tested rocket engines, 1948-1999.
Blot, WJ; Boice, JD; Brill, AB; Cohen, SS; Fryzek, JP; Henderson, BE; Marano, DE; McLaughlin, JK; Mumma, MT, 2006
)
0.33
" The preliminary bioassay showed that some of the chromanone analogues exhibited good insecticidal activity against Mythima separata at the dosage of 500 mg L-1."( Synthesis and insecticidal activity of chromanone and chromone analogues of diacylhydrazines.
Li, J; Yang, GF; Zhao, PL, 2007
)
0.57
" Clinical efficacy was observed when dosing with LJP 1207 was initiated either at the peak of initial flare or during remission."( Benefit of inhibiting SSAO in relapsing experimental autoimmune encephalomyelitis.
Gao, HF; Huang, L; Jones, DS; Linnik, MD; Miller, A; O'Rourke, AM; Podar, E; Salter-Cid, L; Wang, EY, 2007
)
0.34
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
0.13
"With the advancement of high-throughput biomolecular screening techniques to the lead optimization stage, there is a critical need to quality control (QC) dose-response curves generated by robotic liquid handlers to ensure accurate affinity determinations."( Quality control procedures for dose-response curve generation using nanoliter dispense technologies.
Hughes, B; Kariv, I; Middleton, R; Quintero, C; Rosenstein, C, 2007
)
0.34
" Evidence is provided that this dose-response difference is related to whether or not an effective dose of tebufenozide is ingested by the first instar prior to the peak of moulting hormone (20-hydroxyecdysone) in first instars."( Diapause disruption with tebufenozide for early-instar control of the spruce budworm, Choristoneura fumiferana.
Arif, B; Bauce, E; Cusson, M; Doucet, D; Frisco, C; Palli, SR; Retnakaran, A; Tomkins, B, 2007
)
0.34
"A sensitive method has been developed for the identification and assessment of phosphorothioate oligonucleotide accumulation in dosed animal tissues using an in situ hybridization approach, which is both sequence specific yet adaptable to every antisense oligonucleotide (ASO), which has been tested to date."( Development of a sensitive and specific in situ hybridization technique for the cellular localization of antisense oligodeoxynucleotide drugs in tissue sections.
Berridge, B; Brown-Augsburger, PL; Goebl, N; Wroblewski, VJ, 2007
)
0.34
" Dose-response curves were described using a linear function with AOE expressed as a coefficient of the slope."( Evaluation of antioxidative activity of Croatian propolis samples using DPPH* and ABTS*+ stable free radical assays.
Besic, E; Bojic, M; Bucan, K; Jasprica, I; Medic-Saric, M; Mornar, A, 2007
)
0.34
"Two spectrophotometric methods are proposed for the assay of oxcarbazepine (OXC) in bulk and dosage forms using Folin-Ciocalteu phenol reagent (FCP) and 3-methyl-2-benzothiazolinone hydrazine hydrochloride (MBTH) as reagents."( Use of Folin-Ciocalteu phenol reagent and 3-methyl-2-benzothiazolinone hydrazine hydrochloride in the determination of oxcarbazepine in pharmaceuticals.
Gandhimathi, M; Ravi, TK, 2008
)
0.77
" The 4 high-dose NTG pulse injections produced a marked shift in the dose-response curves for arterial pressure depression induced by intravenous injection of the challenge doses of NTG, but did not alter hypotensive responses to sodium nitroprusside."( Effects of nitric oxide and noradrenergic activation in the posterior hypothalamus on arterial pressure tolerance to nitroglycerin in rats.
Guettler, DL; Ma, SX, 2008
)
0.35
" A small-molecule thrombopoietin mimetic, eltrombo-pag, has demonstrated a dose-response associated increase in platelet count in a phase 2 study, allowing initiation and completion of a 12-week course of peginterferon plus ribavirin in 36%, 53%, and 65% of patients receiving 30 mg, 50 mg, or 75 mg of eltrombopag daily, respectively, compared with 6% in the placebo arm."( Role of growth factors and thrombopoietic agents in the treatment of chronic hepatitis C.
McHutchison, JG; Patel, K; Tillmann, HL, 2009
)
0.35
" Furthermore study indicated that blocking the thromboxane A2 receptor reduced dosage sensitive sex reversal-adrenal hypoplasia congenita critical region on the X chromosome, gene 1 protein, a transcriptional repressor of StAR gene expression."( Involvement of the thromboxane A2 receptor in the regulation of steroidogenic acute regulatory gene expression in murine Leydig cells.
Grammas, P; Hutson, JC; Pandey, AK; Schiffer, RB; Stocco, DM; Wang, X; Yin, X, 2009
)
0.35
" Cytotoxicity was determined from the dose-response curve as the CC50 using a curve-fitting program."( Synthesis and antituberculosis activity of some N-pyridyl-N'-thiazolylhydrazine derivatives.
Kaplancikli, ZA; Ozdemir, A; Turan-Zitouni, G, 2010
)
0.59
" Although significant activity was seen, safety and optimal dosing in combination regimen remain to be established and are now being investigated."( Laromustine (cloretazine).
Giles, F; Vey, N, 2010
)
0.36
" Plasma eltrombopag concentrations accumulated between days 1 and 5, with average increases of 66% to 81% for area under the plasma concentration-time curve from time zero to the end of the 24-hour dosing interval (AUC(0-τ)) and 32% to 45% for maximum observed plasma concentration (C(max)) across doses."( Clinical pharmacokinetics, platelet response, and safety of eltrombopag at supratherapeutic doses of up to 200 mg once daily in healthy volunteers.
Bowen, C; Jenkins, J; Matthys, G; McGuire, S; Park, JW; Peng, B; Williams, D; Wire, MB, 2011
)
0.37
" When deciding which of these agents to prescribe, considerations include oral versus injectable dosage form, adverse-event profiles, and patient adherence with both taking the drug and keeping clinic appointments for monitoring of platelet counts."( Treatment options for chronic refractory idiopathic thrombocytopenic purpura in adults: focus on romiplostim and eltrombopag.
Chouhan, JD; Herrington, JD, 2010
)
0.36
" In the ongoing open-label extension study, Eltrombopag EXTENDed Dosing Study (EXTEND; n = 154), measures were administered at baseline, at the beginning of each stage, and at permanent discontinuation of study medication."( Validation of the FACIT-fatigue subscale, selected items from FACT-thrombocytopenia, and the SF-36v2 in patients with chronic immune thrombocytopenia.
Brainsky, A; Grotzinger, KM; Signorovitch, J, 2011
)
0.37
" There was however a significant improvement in neurobehavioral function 24 h post-SBI with both dosing regimens."( Prostaglandin E2 EP1 receptor inhibition fails to provide neuroprotection in surgically induced brain-injured mice.
Applegate, R; Fathali, N; Jadhav, V; Khatibi, NH; Martin, R; Matus, B; Tang, J; Zhang, JH, 2011
)
0.37
" Dose-response curves to both prostanoids were competitively shifted to the right by all antagonists, but to different extents."( Thromboxane and isoprostane share the same prostanoid receptors to increase human placental tone.
Hausermann, L; St-Louis, J, 2011
)
0.37
" The absorption lag time and t(½) did not differ between treatments; T(max) was delayed 1 hour when the PfOS was dosed with a high-calcium meal."( A randomized, open-label, 5-period, balanced crossover study to evaluate the relative bioavailability of eltrombopag powder for oral suspension (PfOS) and tablet formulations and the effect of a high-calcium meal on eltrombopag pharmacokinetics when admin
Brainsky, A; Bruce, J; Gauvin, J; McGuire, S; Pendry, CJ; Qian, Y; Wire, MB, 2012
)
0.38
"In a healthy adult volunteer population, bioavailability of eltrombopag PfOS was greater than the tablet and was reduced when administered with or 2 hours before or after a high-calcium meal; this effect was attenuated with PfOS dosing 2 hours before the meal."( A randomized, open-label, 5-period, balanced crossover study to evaluate the relative bioavailability of eltrombopag powder for oral suspension (PfOS) and tablet formulations and the effect of a high-calcium meal on eltrombopag pharmacokinetics when admin
Brainsky, A; Bruce, J; Gauvin, J; McGuire, S; Pendry, CJ; Qian, Y; Wire, MB, 2012
)
0.38
" Similarly, oral dosing of WIN 18,446, which inhibits testicular retinoic acid biosynthesis, effectively contracepts rabbits."( New approaches to male non-hormonal contraception.
Amory, JK; Nya-Ngatchou, JJ, 2013
)
0.39
" This open-label, single-arm study evaluated consistency of response and safety following repeated intermittent dosing of eltrombopag 50 mg daily over 3 cycles (1 cycle = up to 6 weeks on therapy followed by up to 4 weeks off therapy)."( Repeated short-term use of eltrombopag in patients with chronic immune thrombocytopenia (ITP).
Arning, M; Bussel, JB; Mayer, B; Saleh, MN; Stone, NL; Vasey, SY, 2013
)
0.39
" This can also reduce long-term toxicity and health risk if the effective dosing can be lowered in order to widen the margin between its safety and efficacy."( Role of P-glycoprotein at the blood-testis barrier on adjudin distribution in the testis: a revisit of recent data.
Bonanomi, M; Cheng, CY; Cheng, YH; Jenardhanan, P; Mathur, PP; Mok, KW; Mruk, DD; Silvestrini, B; Su, L, 2012
)
0.38
"Patients aged 18 or older with histologically confirmed, locally advanced or metastatic STS were treated with 1 cycle of AI followed by AI with eltrombopag starting at Cycle 2, using 2 different dosing schedules."( Results of a phase I dose escalation study of eltrombopag in patients with advanced soft tissue sarcoma receiving doxorubicin and ifosfamide.
Chawla, SP; Hendifar, A; Kamel, YM; Messam, CA; Patwardhan, R; Staddon, A, 2013
)
0.39
" Available data suggest a potential pre- and post-chemotherapy dosing scheme for eltrombopag when administered with AI chemotherapy, and support further investigation of eltrombopag treatment in patients with chemotherapy-induced thrombocytopenia."( Results of a phase I dose escalation study of eltrombopag in patients with advanced soft tissue sarcoma receiving doxorubicin and ifosfamide.
Chawla, SP; Hendifar, A; Kamel, YM; Messam, CA; Patwardhan, R; Staddon, A, 2013
)
0.39
" Recovery groups of five males and five non-pregnant females per group were dosed for 42 days followed by a 14-day recovery period."( Combined repeated dose and reproductive/developmental toxicity screening test of tert-butylhydrazine monohydrochloride in rats.
Ajimi, S; Aso, S; Furukawa, K; Hasegawa, R; Hoshuyama, S; Kobayashi, T; Koga, T; Kusune, Y; Miyata, K; Muroi, T; Oshima, Y; Yoshida, T, 2013
)
0.61
" Due to the delay in platelet response after the administration of eltrombopag or chemotherapy, a modeling and simulation approach was used to optimize the eltrombopag dosing regimen."( Population PK/PD modeling of eltrombopag in subjects with advanced solid tumors with chemotherapy-induced thrombocytopenia.
Gibiansky, E; Hayes, S; Johnson, BM; Mudd, PN; Ouellet, D; Williams, D, 2013
)
0.39
" Alternative eltrombopag dosing regimens were then simulated."( Population PK/PD modeling of eltrombopag in subjects with advanced solid tumors with chemotherapy-induced thrombocytopenia.
Gibiansky, E; Hayes, S; Johnson, BM; Mudd, PN; Ouellet, D; Williams, D, 2013
)
0.39
"Simulations indicated that eltrombopag administered 5 days before and 5 days after chemotherapy minimizes the decrease and fluctuations in platelet counts relative to other evaluated dosing regimens."( Population PK/PD modeling of eltrombopag in subjects with advanced solid tumors with chemotherapy-induced thrombocytopenia.
Gibiansky, E; Hayes, S; Johnson, BM; Mudd, PN; Ouellet, D; Williams, D, 2013
)
0.39
" At the studying of the bile formation and bile secretion functions in the conditions of the toxic tetrachlormethane lesion the hepatoprotective effect of the dosage form was confirmed, which was realized by the increasing of the speed of bile secretion and its volume."( [Studying of hepatoprotective properties of dry extract from apricot leaves on the model of liver lesion by tetrachloromethane].
Fira, LS; Likhatskiĭ, PG; Medvid', II; Pyla, VP; Shtroblia, AL; Vashkeba, EM, 2013
)
0.39
" Patients received eltrombopag once daily at the last dosage received in the prior study (12."( Oral eltrombopag for up to three years is safe and well-tolerated in Japanese patients with previously treated chronic immune thrombocytopenia: an open-label, extension study.
Hattori, T; Ikeda, Y; Ishii, K; Kanakura, Y; Katsura, K; Katsutani, S; Kimura, A; Kosugi, H; Miyakawa, Y; Ninomiya, H; Okamoto, S; Okoshi, Y; Tomiyama, Y, 2013
)
0.39
" Eltrombopag was examined at dosage levels of 75, 150, 225, and 300 mg given orally once daily for 27 days, starting at 24 to 48 hours post-transplantation."( A phase 1 trial of eltrombopag in patients undergoing stem cell transplantation after total body irradiation.
Andolina, JR; Becker, M; Chen, Y; Constine, LS; Dawson, KL; DeBolt, J; Erickson-Miller, CL; Friedberg, J; Hyrien, O; Johnson, BM; Liesveld, JL; Milner, LA; Phillips, GL; Smudzin, T, 2013
)
0.39
" The dosing was as follows: period 1, single 200-mg dose of eltrombopag; period 2, 800 mg boceprevir or 750 mg telaprevir every 8 hours (q8h) for 10 days; and period 3, single 200-mg dose of eltrombopag with either 800 mg boceprevir or 750 mg telaprevir q8h (3 doses)."( Lack of clinically significant pharmacokinetic interaction between the thrombopoietin receptor agonist eltrombopag and hepatitis C virus protease inhibitors boceprevir and telaprevir.
Fang, L; Hussaini, A; Kleha, JF; Theodore, D; Wire, MB, 2014
)
0.4
" Alemtuzumab and eltrombopag have been studied for treatment of AA; recruiting is ongoing in clinical trials to assess the appropriate dosing strategy and place in therapy."( Recent developments in drug therapy for aplastic anemia.
Bryan, J; Kadia, TM; Rexwinkle, A; Willis, L, 2014
)
0.4
" A drastic effect was observed on spermatozoon production, with a dose-response relationship."( Proteomic investigation of male Gammarus fossarum, a freshwater crustacean, in response to endocrine disruptors.
Abbaci, K; Armengaud, J; Chaumot, A; Gaillard, JC; Geffard, O; Habtoul, Y; Pible, O; Trapp, J, 2015
)
0.42
"The pharmacokinetics of eltrombopag and its stimulation of platelet production were characterized in patients with chronic hepatitis C virus (HCV) infection to optimize an eltrombopag dosing regimen for treatment of HCV-related thrombocytopenia before and throughout peginterferon (pegIFN)-based antiviral therapy."( Modeling and simulation support eltrombopag dosing in thrombocytopenic patients with chronic HCV infection.
Farrell, C; Thapar, M; Wire, MB; Zhang, J, 2015
)
0.42
" Simulations were conducted using various dosing scenarios in the same patient population."( Modeling and simulation support eltrombopag dosing in thrombocytopenic patients with chronic HCV infection.
Farrell, C; Thapar, M; Wire, MB; Zhang, J, 2015
)
0.42
"Modeling and simulation results support once-daily eltrombopag 25 mg as an appropriate starting dosing regimen followed by biweekly dose escalation (in 25-mg increments) up to once-daily eltrombopag 100 mg to raise platelet counts sufficiently for initiation of pegIFN-based antiviral therapy in patients with HCV."( Modeling and simulation support eltrombopag dosing in thrombocytopenic patients with chronic HCV infection.
Farrell, C; Thapar, M; Wire, MB; Zhang, J, 2015
)
0.42
" Dosing patterns were also analyzed before and after switching."( Treatment patterns and clinical outcomes in patients with chronic immune thrombocytopenia (ITP) switched to eltrombopag or romiplostim.
Dawson, KL; Grotzinger, KM; Kuter, DJ; Macahilig, C; Poston, SA; Wang, PF; Ward, M, 2015
)
0.42
" Patients with chronic immune thrombocytopenia participating in the Eltrombopag Extended Dosing (EXTEND) study underwent BM biopsies to identify clinically relevant BM fibrosis-related increases."( Evaluation of bone marrow reticulin in patients with chronic immune thrombocytopenia treated with eltrombopag: Data from the EXTEND study.
Bailey, CK; Bakshi, KK; Brynes, RK; Burgess, P; Orazi, A; Thein, MM; Theodore, D, 2015
)
0.42
" The 25-mg once-daily dosage was associated with a more balanced response than were the 12."( Population Pharmacokinetic and Pharmacodynamic Modeling and Effects on Platelet Counts of Different Dosages of Eltrombopag in Chinese Patients With Chronic Primary Immune Thrombocytopenia.
Farrell, C; Guo, H; Hayes, S; Hou, M; Thapar, M; Wu, K; Zhang, J, 2015
)
0.42
" The modeling and simulation results support the eltrombopag dose-titration regimen, with 25 mg once daily as a starting dosage and a 2-week titration interval, in Chinese patients with cITP."( Population Pharmacokinetic and Pharmacodynamic Modeling and Effects on Platelet Counts of Different Dosages of Eltrombopag in Chinese Patients With Chronic Primary Immune Thrombocytopenia.
Farrell, C; Guo, H; Hayes, S; Hou, M; Thapar, M; Wu, K; Zhang, J, 2015
)
0.42
"492) and an increase in the percentage of administrated dosage (89."( [Experience of off-label use of Eltrombopag in the treatment of thrombocytopenia associated with solid tumors].
Cerezuela Fuentes, P; García Coronel, M; García Lagunar, MH; Gutiérrez-Meca Maestre, DP; Martínez Ortiz, MJ; Martínez Penella, M, 2015
)
0.42
"This study aims to identify patient characteristics that predict effective eltrombopag dosage for the treatment of Hepatitis C virus (HCV)-related thrombocytopenia."( Eltrombopag dose predictors in thrombocytopenic subjects with hepatitis C virus infection.
Anter, HA; Khanfar, AA; Obeidat, AR; Saleh, MI, 2015
)
0.42
"To test our hypothesis, we used the selective XPO1 inhibitor, selinexor, to inhibit nuclear export in combination with radiation fractions similar to that given in clinical practice for rectal cancer: hypofractionated short-course radiation dosage of 5 Gy per fraction or the conventional long-course radiation dosage of 1 Gy fractions."( XPO1 Inhibition Enhances Radiation Response in Preclinical Models of Rectal Cancer.
Chan, CH; Cusack, JC; Ferreiro-Neira, I; Hong, TS; Landesman, Y; Liesenfeld, LF; Penson, T; Senapedis, W; Shacham, S; Torres, NE, 2016
)
0.43
" Binding to XPO1 was quantitated from SINE compound treated adherent and suspension cells in vitro, dosed ex vivo human peripheral blood mononuclear cells (PBMCs), and PBMCs from mice dosed orally with drug in vivo."( A method for quantification of exportin-1 (XPO1) occupancy by Selective Inhibitor of Nuclear Export (SINE) compounds.
Baloglu, E; Crochiere, ML; Del Alamo, D; Donovan, S; Kauffman, M; Klebanov, B; Landesman, Y; Lee, M; Shacham, S, 2016
)
0.43
" We permitted dose adjustments on the basis of platelet response up to a maximum dosage of 75 mg per day."( Eltrombopag for the treatment of children with persistent and chronic immune thrombocytopenia (PETIT): a randomised, multicentre, placebo-controlled study.
Bailey, CK; Bakshi, KK; Blanchette, VS; Boayue, KB; Bussel, JB; Chagin, KD; Chan, GW; Connor, P; David, M; de Miguel, PG; Despotovic, JM; Grainger, JD; Iyengar, M; Krishnamurti, L; Lambert, MP; Marcello, LM; Matthews, DC; Sevilla, J; Theodore, D, 2015
)
0.42
" Only 40% of patients demonstrated a stable response with consistent dosing over time."( Thrombopoietin Receptor Agonist Use in Children: Data From the Pediatric ITP Consortium of North America ICON2 Study.
Bennett, C; Brown, T; Despotovic, J; Forbes, PW; Grace, RF; Haley, K; Klaassen, R; Lambert, MP; Neunert, C; Nottage, K; Pastore, Y; Shimano, K; Stine, K; Thompson, A, 2016
)
0.43
" The improved selinexor dosing regimen described herein is crucial to help reduce thrombocytopenia in selinexor patients, allowing them to continue their course of chemotherapy and have the best chance of survival."( Selinexor-induced thrombocytopenia results from inhibition of thrombopoietin signaling in early megakaryopoiesis.
Crochiere, M; Italiano, JE; Kashyap, T; Klebanov, B; Landesman, Y; Liu, ZJ; Machlus, KR; Shacham, E; Sola-Visner, M; Soussou, TS; Unger, TJ; Vijey, P; Wu, SK, 2017
)
0.46
"Despite twice-a-week dosing and maximal symptomatic management, selinexor was associated with significant anorexia, nausea, and fatigue in mCRPC patients refractory to second-generation anti-androgen therapies, limiting further clinical development in this patient population."( A Phase II Trial of Selinexor, an Oral Selective Inhibitor of Nuclear Export Compound, in Abiraterone- and/or Enzalutamide-Refractory Metastatic Castration-Resistant Prostate Cancer.
Aggarwal, R; Chang, E; Fong, L; Friedlander, TW; Kim, W; Lin, AM; Louttit, M; Ryan, CJ; Siegel, AP; Wei, XX; Zhang, L, 2018
)
0.48
" This model can be applied to optimize eltrombopag dosing in order to reduce the incidence of thrombocytopenia in HCV-infected patient receiving interferon-based therapy."( Bayesian Population Pharmacokinetic Modeling of Eltrombopag in Chronic Hepatitis C Patients.
Al-Ramadhani, HM; Alzubiedi, S; Melhim, SB; Saleh, MI, 2019
)
0.51
"Eltrombopag, an oral thrombopoietin receptor agonist, is dosed daily to treat chronic immune thrombocytopenia (ITP)."( An alternative intermittent eltrombopag dosing protocol for the treatment of chronic immune thrombocytopenia.
Al-Samkari, H; Kuter, DJ, 2018
)
0.48
" Other dosing schedules or combinations may be evaluated."( Selinexor (KPT-330), an Oral Selective Inhibitor of Nuclear Export (SINE) Compound, in Combination with FOLFOX in Patients with Metastatic Colorectal Cancer (mCRC) - Final Results of the Phase I Trial SENTINEL.
Amberg, S; Bokemeyer, C; Kranich, AL; Mann, J; Nilsson, S; Papadimitriou, K; Rolfo, C; Stein, A; Theile, S, 2020
)
0.56
" The dosage of eltrombopag varies from 25 mg every other day (qod) to 100 mg every day (qd) (median 75 mg qd) with the duration of 13 (3~23) months."( Eltrombopag is effective in patients with relapse/refractory aplastic anemia-report from a single center in China.
Chen, M; Han, B; Ruan, J; Yang, C; Zuo, W, 2020
)
0.56
" Therapies dosed soon after peak viral load when symptoms develop may decrease shedding duration and immune response intensity but have little effect on viral area under the curve (AUC), which is driven by high early viral loads."( Potency and timing of antiviral therapy as determinants of duration of SARS-CoV-2 shedding and intensity of inflammatory response.
Cardozo-Ojeda, EF; Goyal, A; Schiffer, JT, 2020
)
0.56
" However, the analyze of the kidney injury parameters showed an increase in the urea's dosage but a decrease in the albumin's dosage in all animals when compared to the reference values."( Study of acute oral toxicity of the thiazole derivative N-(1-methyl-2-methyl-pyridine)-N-(p-bromophenylthiazol-2-yl)-hydrazine in a Syrian hamster.
Amaro da Silva Junior, V; Angela Aranda de Souza, M; Câmara Alves, L; de Figueiredo, RCBQ; Lima Leite, AC; Ramos Mororó Cavalcanti, R; Rogério de Freitas Silva, S; Vasconcelos Gomes de Oliveira, V; Veríssimo de Oliveira Cardoso, M, 2021
)
0.83
" One patient dosed at selinexor 80 mg had grade 3 nausea and vomiting and one patient dosed at selinexor 60 mg experienced grade 4 neutropenia and thrombocytopenia."( Selinexor in combination with topotecan in patients with advanced or metastatic solid tumors: Results of an open-label, single-center, multi-arm phase Ib study.
Bean, S; Carter, BW; Colen, R; Gong, J; Janku, F; Karp, DD; McQuinn, L; Meric-Bernstam, F; Milton, DR; Naing, A; Ogbonna, DC; Pant, S; Piha-Paul, SA; Shah, J; Subbiah, V; Thein, KZ; Tsimberidou, A; Zarifa, A, 2021
)
0.62
" Fourteen patients were included, and selinexor dosage was 60 mg (3 patients), 80 mg (3 patients), and 100 mg (7 patients) weekly."( A phase I trial of selinexor plus FLAG-Ida for the treatment of refractory/relapsed adult acute myeloid leukemia patients.
Acuña-Cruz, E; Barragán, E; Bergua, JM; Boluda, B; Cano-Ferri, I; Martín-Herreros, B; Martínez Sánchez, MP; Martínez-Cuadrón, D; Martínez-López, J; Megías-Vericat, JE; Montesinos, P; Rodríguez-Veiga, R; Sanz, M; Sargas, C; Sempere, A; Serrano, A; Suárez-Varela, S; Torrent, A; Torres-Miñana, L; Vives, S, 2021
)
0.62
" In 134 patients treated with the approved dosage (60 mg orally on days 1 and 3 of each week), the ORR was 29% (95% confidence interval, 22-38), with complete response in 13% and with 38% of responses lasting at least 6 months."( FDA Approval Summary: Selinexor for Relapsed or Refractory Diffuse Large B-Cell Lymphoma.
Gormley, NJ; Kasamon, YL; Li, RJ; Ma, L; Okusanya, OO; Pazdur, R; Price, LSL; Richardson, NC; Theoret, M; Wu, YT, 2021
)
0.62
"28/45 (62%) of patients dosed were evaluable at Day 43."( Anamorelin combined with physical activity, and nutritional counseling for cancer-related fatigue: a preliminary study.
Basen-Engquist, K; Bruera, E; Dev, R; Fellman, BM; Hui, D; Maddi, R; Reuben, JM; Shete, S; Williams, JL; Yennurajalingam, S, 2022
)
0.72
" Patient 2 did not respond to high dosage of steroid, IVIG, rhTPO and rituximab."( Successful treatment of acquired amegakaryocytic thrombocytopenia with eltrombopag and immunosuppressant.
Gu, C; Kong, D; Li, Y; Tian, H; Wang, Z; Wu, D; Yin, J; Yu, Z, 2022
)
0.72
" With more available safety and efficacy data supporting the increased interval between dosing of selinexor (and lesser cumulative weekly dosing) and schedule, contrary to the originally approved dose of 160 mg per week, the supportive care guidelines needed to be revisited."( Guidance for Use and dosing of Selinexor in Multiple Myeloma in 2021: Consensus From International Myeloma Foundation Expert Roundtable.
Chari, A; Costa, LJ; Gasparetto, CJ; Jagannath, S; Lentzsch, S; Mikhael, J; Nooka, AK; Richardson, PG; Siegel, DS, 2022
)
0.72
" However, EPAG dosage and combinations remain to be optimized for AA of different severities."( Eltrombopag as frontline treatment of aplastic anaemia in routine practice: implications on cost and efficacy.
Chan, FHY; Chan, KP; Chan, TSY; Hwang, YY; Kho, B; Kwong, YL; Lau, CK; Lau, CWP; Lau, GWN; Lau, JSM; Leung, KH; Lin, SY; Luk, YY; Mak, V; Sim, JPY; Yip, SF, 2022
)
0.72
"The aim of this article is to summarize the available evidence and present real-life experience on eltrombopag as second-line therapy in pediatric patients with ITP, with a focus on dosing and response to therapy as well as its tapering and discontinuation."( Pediatric immune thrombocytopenia: a focus on eltrombopag as second-line therapy.
Borchiellini, A; Dufour, C; Farruggia, P; Giona, F; Giordano, P; Ladogana, S; Palumbo, G; Perrotta, S; Pession, A; Ramenghi, U; Russo, G; Spinelli, M; Zecca, M, 2023
)
0.91
"Patients preferred therapies delivered orally, dosed less frequently and without food restrictions."( Patient preferences and experiences regarding thrombopoietin-receptor agonists for immune thrombocytopenia in The Netherlands (TRAPeze Netherlands study).
Bastiaanse, M; Daykin-Pont, O; Eriksson, D; Geldman, E; Gerard Jansen, AJ; McDonald, V; Morgan, M; Newland, A; Prince, S; Wilson, K; Zwaginga, JJ, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
EC 4.3.1.10 (serine-sulfate ammonia-lyase) inhibitorAn EC 4.3.1.* (ammonia-lyase) inhibitor that interferes with the action of serine-sulfate ammonia-lyase (EC 4.3.1.10).
[role 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]

Drug Classes (2)

ClassDescription
hydrazinesHydrazine (diazane) and its substituted derivatives.
azaneSaturated acyclic nitrogen hydrides having the general formula NnHn+2.
[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]

Pathways (18)

PathwayProteinsCompounds
u03B2-alanine biosynthesis III210
methanol and methylamine oxidation to formaldehyde1315
superpathway of C1 compounds oxidation to CO22232
superpathway of trimethylamine degradation1224
superpathway of L-lysine degradation33112
L-lysine fermentation to acetate and butanoate857
phosphatidylethanolamine biosynthesis I59
superpathway of coenzyme A biosynthesis I (bacteria)942
histamine biosynthesis421
ammonia oxidation IV (autotrophic ammonia oxidizers)724
ammonia oxidation I (aerobic)924
methylamine degradation II917
methylamine degradation I812
L-arginine degradation VIII (arginine oxidase pathway)325
trans-4-hydroxy-L-proline degradation II643
L-isoleucine biosynthesis III019
nitrifier denitrification1425
ammonia oxidation II (anaerobic)89

Bioassays (23)

Assay IDTitleYearJournalArticle
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID540235Phospholipidosis-negative literature compound
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (11,434)

TimeframeStudies, This Drug (%)All Drugs %
pre-19905040 (44.08)18.7374
1990's1014 (8.87)18.2507
2000's1960 (17.14)29.6817
2010's2515 (22.00)24.3611
2020's905 (7.91)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 85.74

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 very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index85.74 (24.57)
Research Supply Index9.42 (2.92)
Research Growth Index4.65 (4.65)
Search Engine Demand Index160.02 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (85.74)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials330 (2.74%)5.53%
Reviews470 (3.91%)6.00%
Case Studies233 (1.94%)4.05%
Observational17 (0.14%)0.25%
Other10,984 (91.27%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Phase I/II Trial of the Pharmacokinetics, Tolerability, and Safety of Once-Weekly Rifapentine and Isoniazid in HIV-1-infected and HIV-1-uninfected Pregnant and Postpartum Women With Latent Tuberculosis Infection [NCT02651259]Phase 1/Phase 250 participants (Actual)Interventional2017-03-13Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT02651259 (24) [back to overview]Absorption (ka) of INH
NCT02651259 (24) [back to overview]Absorption Rate Constant (ka) for Rifapentine (RPT)
NCT02651259 (24) [back to overview]Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT)
NCT02651259 (24) [back to overview]Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT) for Intensive and Sparse PK
NCT02651259 (24) [back to overview]Clearance Relative to Bioavailability (CLmet/F) for Desacetyl Rifapentine (Des-RPT)
NCT02651259 (24) [back to overview]Cord Blood Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants
NCT02651259 (24) [back to overview]Cord Blood Concentrations of Rifapentine (RPT) Among Infants
NCT02651259 (24) [back to overview]Incidence of Related Serious Adverse Events (SAEs) in Pregnant and Postpartum Women Taking Once-weekly RPT + INH
NCT02651259 (24) [back to overview]Number of Infants With Active TB up to 24 Weeks of Life
NCT02651259 (24) [back to overview]Number of Mothers With Active TB up to 24 Weeks Postpartum
NCT02651259 (24) [back to overview]Number of Participants With Discontinuation of Study Drug Due to Intolerance (Tolerability of Study Drug Regimen - i.e., RPT, INH, and Pyridoxine)
NCT02651259 (24) [back to overview]Percentage of Participants With All AEs Leading to Permanent Discontinuation of Study Drug Regimen (i.e., RPT, INH, and Pyridoxine)
NCT02651259 (24) [back to overview]Percentage of Participants With All Grade 3 and 4 AEs
NCT02651259 (24) [back to overview]Percentage of Participants With All Serious AEs
NCT02651259 (24) [back to overview]Percentage of Participants With Grade 2 Adverse Events (AEs) Judged to be Related to Study Drug Regimen
NCT02651259 (24) [back to overview]Percentage of Participants With Related Serious Adverse Events (AEs) in Infants Born to Women Taking Once-weekly RPT + INH
NCT02651259 (24) [back to overview]Plasma Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants
NCT02651259 (24) [back to overview]Plasma Concentrations of Rifapentine (RPT) Among Infants
NCT02651259 (24) [back to overview]Volume of Distribution of INH
NCT02651259 (24) [back to overview]Volume of Distribution Relative to Bioavailability (Vc/F) for Rifapentine (RPT)
NCT02651259 (24) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC0-24) for RPT and Area Under the Curve From 0 to 24 Hours (AUC0-24) for Des-RPT Pregnant Women in 2nd and 3rd Trimester
NCT02651259 (24) [back to overview]Clearance (CL/F) of INH
NCT02651259 (24) [back to overview]Maximum Concentration (Cmax) for RPT Maximum Concentration (Cmax) for Des-RPT Pregnant Women in 2nd and 3rd Trimester
NCT02651259 (24) [back to overview]Maximum Concentration (Cmin) for RPT and Maximum Concentration (Cmin) for Des-RPT Pregnant Women in 2nd and 3rd Trimester

Absorption (ka) of INH

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~• Estimated a single absorption rate constant (ka) for the whole population" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

Interventionhr-1 (Mean)
All Cohorts1.74

[back to top]

Absorption Rate Constant (ka) for Rifapentine (RPT)

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Estimated the transit compartment rate constant (ktr), which is synonymous with the absorption constant (ka), for the whole population Note that the mean stated below is actually the value that is obtained from a population analysis and represents a population estimate" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

Interventionhr-1 (Mean)
All Cohorts1.43

[back to top]

Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT)

"PK parameters from postpartum women were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Calculated an average CL for all post-partum individuals" (NCT02651259)
Timeframe: Data used in the population PK analysis for postpartum women included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
All Cohorts1.64

[back to top]

Clearance Relative to Bioavailability (CL/F) for Rifapentine (RPT) for Intensive and Sparse PK

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Calculated an average CL for all women in the 2nd trimester (cohort I) and all women in the 3rd trimester (cohort II)" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)1.4
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)1.50

[back to top]

Clearance Relative to Bioavailability (CLmet/F) for Desacetyl Rifapentine (Des-RPT)

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption and a separate compartment for metabolite formation~Estimated a single des-RPT CLmet/F for the whole population Note: that the mean stated below is actually the value that is obtained from a population analysis and represents a population estimate with the relative standard error" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
All Cohorts2.82

[back to top]

Cord Blood Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants

Cord blood concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery (within 3 days of life for infants).

Interventionmcg/mL (Mean)
All Cohorts3.24

[back to top]

Cord Blood Concentrations of Rifapentine (RPT) Among Infants

Cord blood concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery - (within 3 days of life for infants)

Interventionmcg/mL (Mean)
All Cohorts2.97

[back to top] [back to top]

Number of Infants With Active TB up to 24 Weeks of Life

Based on site-specified confirmatory TB test. If women and infants were diagnosed with active TB during study they would be referred to local care for TB management and treatment. (NCT02651259)
Timeframe: Measured from birth through participants' last study visit at 24 weeks after delivery

InterventionParticipants (Count of Participants)
Cohort 1(Infants Born to Women Enrolled in Second Trimester)0
Cohort 2 (Infants Born to Women Enrolled in Third Trimester)0

[back to top]

Number of Mothers With Active TB up to 24 Weeks Postpartum

Based on site-specified confirmatory TB test. If women and infants were diagnosed with active TB during study they would be referred to local care for TB management and treatment. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

InterventionParticipants (Count of Participants)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)0
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)0

[back to top]

Number of Participants With Discontinuation of Study Drug Due to Intolerance (Tolerability of Study Drug Regimen - i.e., RPT, INH, and Pyridoxine)

At entry and follow-up, all lab results, sign and symptoms, and diagnoses will be recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that result in discontinuation of study drug regimen, and that meet criteria for EAE reporting will be further evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

InterventionParticipants (Count of Participants)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)0
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)0

[back to top]

Percentage of Participants With All AEs Leading to Permanent Discontinuation of Study Drug Regimen (i.e., RPT, INH, and Pyridoxine)

At entry and follow-up, all lab results, sign and symptoms, and diagnoses were recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that resulted in discontinuation of study drug regimen, and that met criteria for EAE reporting would further be evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study treatment dispensation (approximately for 12 weeks)

Interventionpercent of participants (Number)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)0
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)0

[back to top]

Percentage of Participants With All Grade 3 and 4 AEs

At entry and follow-up, all lab results, sign and symptoms, and diagnoses were recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that resulted in discontinuation of study drug regimen, and that met criteria for EAE reporting would further be evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

Interventionpercent of participants (Number)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)20
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)16

[back to top]

Percentage of Participants With All Serious AEs

At entry and follow-up, all lab results, sign and symptoms, and diagnoses were recorded. Also, during follow-up grade 2 events related to pregnancy complications, hepatotoxicity, hemorrhage, or peripheral neuropathy, and all grade 3 or events that resulted in discontinuation of study drug regimen, and that met criteria for EAE reporting would further be evaluated and recorded. The DAIDS Table for Grading Adult and Pediatric Adverse Events (V 2.0) and Expedited AE Manual (V 2.0) were used. (NCT02651259)
Timeframe: Measured from study entry through participants' last study visit at 24 weeks after delivery

Interventionpercent of participants (Number)
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)8
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)12

[back to top] [back to top] [back to top]

Plasma Concentrations of Desacetyl Rifapentine (Des-RPT) Among Infants

Plasma blood concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery - (within 3 days of life for infants).

Interventionmcg/mL (Mean)
All Cohorts5.31

[back to top]

Plasma Concentrations of Rifapentine (RPT) Among Infants

Plasma concentrations were summarized using using R (version 3.5.1). (NCT02651259)
Timeframe: at delivery - (within 3 days of life for infants).

Interventionmcg/mL (Mean)
All Cohorts2.47

[back to top]

Volume of Distribution of INH

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~• Estimated a single INH Vc/F for the whole population" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL (Mean)
All Cohorts107

[back to top]

Volume of Distribution Relative to Bioavailability (Vc/F) for Rifapentine (RPT)

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Estimated a single RPT Vc/F for for the whole population Note: that the mean stated below is actually the value that is obtained from a population analysis and represents a population estimate with the relative standard error" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL (Mean)
All Cohorts30.1

[back to top]

Area Under the Curve From 0 to 24 Hours (AUC0-24) for RPT and Area Under the Curve From 0 to 24 Hours (AUC0-24) for Des-RPT Pregnant Women in 2nd and 3rd Trimester

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Obtained AUC by model-based integration" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

,
Interventionhour*mg/L (Mean)
AUC (0-24) for RPTAUC (0-24) for des-RPT
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)424.7158.7
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)406.8153.7

[back to top]

Clearance (CL/F) of INH

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with 2 mixtures to characterize subpopulations based on acetylation status~Estimated a separate INH CL/F based on acetylation status (fast, slow)" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

InterventionL/hr (Mean)
CL/F (slow acetylators)CL/F (fast acetylators)
All Cohorts8.9832.7

[back to top]

Maximum Concentration (Cmax) for RPT Maximum Concentration (Cmax) for Des-RPT Pregnant Women in 2nd and 3rd Trimester

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Obtained Cmax by model-based estimation" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

,
Interventionmg/L (Mean)
Cmax for RPTCmax for des-RPT
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)30.28.76
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)28.68.50

[back to top]

Maximum Concentration (Cmin) for RPT and Maximum Concentration (Cmin) for Des-RPT Pregnant Women in 2nd and 3rd Trimester

"PK parameters were determined from plasma concentration-time profiles using a nonlinear mixed effects model (version 7.4; ICON PLC, Dublin, Ireland).~Developed a 1 compartment PK model with transit compartments for oral absorption~Obtained Cmin by model-based estimation" (NCT02651259)
Timeframe: Data used in the population PK analysis included the intensive PK visit (pre-dose (t0) and 0.5, 1, 2. 4, 5, 8, 12, 24, 48, 72 hours post-dose) and sparse PK visit (1, 4, 24, 48 hours post-dose).

,
Interventionmg/L (Mean)
Cmin for RPTCmin for des-RPT
Cohort 1 (Pregnant Women Enrolled in the Second Trimester)1.451.06
Cohort 2 (Pregnant Women Enrolled in the Third Trimester)1.581.20

[back to top]