topotecan profile

Topotecan is a topoisomerase I inhibitor used in the treatment of various cancers, including ovarian, small cell lung, and cervical cancer. It was first synthesized in the 1980s by scientists at the SmithKline Beecham company. Topotecan works by interfering with the activity of the enzyme topoisomerase I, which is essential for DNA replication and repair. By inhibiting topoisomerase I, topotecan prevents the proper separation of DNA strands, leading to DNA damage and cell death. Topotecan is typically administered intravenously, and its effects are targeted at rapidly dividing cancer cells. The drug has been shown to have a significant impact on tumor growth and survival rates in patients with various types of cancer. Further research is being conducted to explore the potential of topotecan in combination with other cancer therapies, as well as its use in treating other types of cancer. '

Topotecan: An antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA TOPOISOMERASES, TYPE I. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

topotecan : A pyranoindolizinoquinoline used as an antineoplastic agent. It is a derivative of camptothecin and works by binding to the topoisomerase I-DNA complex and preventing religation of these 328 single strand breaks. [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]

ID Source	ID
PubMed CID	60700
CHEMBL ID	84
CHEBI ID	63632
SCHEMBL ID	3836
MeSH ID	M0029340

Synonym
sk-s-104864-a
(s)-10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione; hydrochloride
cid_60699
bdbm50034026
10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione; hydrochloride
(s)-11-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione; hydrochloride
AB00641837-13
BSPBIO_002348
NCI60_004771
SMP2_000312
(s)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione
topotecan [inn:ban]
topotecanum [inn-latin]
1h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione, 10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-, (s)-
(s)-10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione
skf-104864-a
topotecane [inn-french]
sk&f-104864-a
SMP2_000327
NCGC00178695-01
topotecan lactone
nsc-641007
nsc641007
1h-pyrano[3',7]indolizino[1,2-b]quinoline- 3,14(4h,12h)-dione, 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-, (4s)-
hycamptamine
9-dimethylaminomethyl-10-hydroxycamptothecin
hycamtamine
skf-s 104864
hycamptin
skf 104864
1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione, 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-, (4s)-
dimethylaminomethyl-ethyl-dihydroxy-[?]dione
(s)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]-quinoline-3,14(4h,12h)-dione
123948-87-8
topotecan
(s)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]inolizino[1,2-b]-quinoline-3,14(4h,12h)-dione
DB01030
9-[(dimethylamino)methyl]-10-hydroxy-(4s)-camptothecin
HSCI1_000228
NCISTRUC2_001796
NCISTRUC1_001659
9 dimethylaminomethyl 10 hydroxycamptothecin
(4s)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione
sk&f 104864 a
HMS2090B20
AC-11592
ff-10850 (liposomal topotecan)
nogitecan
skf-104864
CHEMBL84 ,
chebi:63632 ,
D08618
topotecan (ban)
(s)-11-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione
(s)-10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione
(s)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1h-pyrano[3'''',4'''':6,7]inolizino[1,2-b]-quinoline-3,14(4h,12h)-dione
10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione (topotecan)
10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-(4s)-3,4,12,14-tetrahydro-1h-pyrano[3'''',4'''':6,7]indolizino[1,2-b]quinoline-3,14-dione
bdbm50008935
10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione
(4-ethyl-4,9-dihydroxy-3,13-dioxo-3,4,12,13-tetrahydro-1h-2-oxa-6,12a-diaza-dibenzo[b,h]fluoren-10-ylmethyl)-dimethyl-ammonium
(20s)-10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione
10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4h-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione(topotecan)
dihydroxy(oxo)silane; dioxido(dioxo)molybdenum
A805171
hsdb 8213
ccris 8163
topotecane
(s)-topotecan
topophore c
unii-7m7ykx2n15
7m7ykx2n15 ,
topoced
topotecanum
S9321
AKOS015966792
NCGC00014925-03
NCGC00014925-02
NCGC00014925-07
NCGC00014925-04
10-hydroxy-9-((dimethylamino)methyl)-(20s)-camptothecin
sk&f-104864
topotecan [vandf]
1h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione, 10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-, (4s)-
topotecan [mi]
topotecan [inn]
topotecan [who-dd]
topotecan [ema epar]
BRD-K55696337-001-03-2
gtpl7101
AB00641837-14
UCFGDBYHRUNTLO-QHCPKHFHSA-N
CCG-221171
HY-13768
AB00641837-09
SCHEMBL3836
AB00641837-11
AB00641837-12
DTXSID3042685 ,
(s)-10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1,12-dihydro-14h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h)-dione
AB00641837_15
AB00641837_16
mfcd00870670
(19s)-8-[(dimethylamino)methyl]-19-ethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.0^{2,11}.0^{4,9}.0^{15,20}]henicosa-1(21),2(11),3,5,7,9,15(20)-heptaene-14,18-dione
EX-A834
SR-01000763672-4
SR-01000763672-3
sr-01000763672
(19s)-8-[(dimethylamino)methyl]-19-ethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.0(2),(1)(1).0?,?.0(1)?,(2)?]henicosa-1(21),2,4,6,8,10,15(20)-heptaene-14,18-dione
AS-75098
topotecan hydrochloride hydrate, >=98% (hplc and enzymatic)
1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione, 10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-, (s)-
NCGC00014925-10
HMS3715L03
Q419953
BRD-K55696337-003-08-7
A16815
NCGC00014925-24
T-161
(19s)-8-[(dimethylamino)methyl]-19-ethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione
(s)-10-[(dimethylamino)methyl]-4-ethyl-4,9-dihydroxy-1h-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4h,12h)-dione monohydrochloride; nogitecan hydrochloride; hycamtin
A892572
AC-34812
EN300-117268
9-((dimethylamino)methyl)-10-hydroxy-(20s)-camptothecin
dtxcid1022685
topotecane (inn-french)
topotecanum (inn-latin)
9-((dimethylamino)methyl)-10-hydroxy-(4s)-camptothecin
topotecanum (latin)
(s)-10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1h-pyrano(3',4':6,7)indolizino(1,2-b)-quinoline-3,14(4h,12h)-dione
(4s)-10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1h-pyrano(3',4':6,7)indolizino(1,2-b)quinoline-3,14(4h,12h)-dione
Z1501485359
BP-29353

Excerpt	Reference	Relevance
"Topotecan is a camptothecin analogue with potential advantages over irinotecan for transarterial chemoembolization (TACE) of hepatic colorectal metastases including greater anti-neoplastic activity without enzymatic activation. "	( Safety and Tolerability of Topotecan-Eluting Radiopaque Microspheres for Hepatic Chemoembolization in a Rabbit Preclinical Model. Bakhutashvili, I; Banovac, F; Esparza-Trujillo, JA; Henman, A; Karanian, JW; Krishnasamy, VP; Levy, EB; Lewis, AL; Mikhail, AS; Negussie, AH; Pritchard, WF; Tang, Y; Wakim, PG; Willis, SL; Wood, BJ; Woods, DL, 2020)	2.3
"Topotecan is an anti-cancer chemotherapy drug with common side effects, including hepatotoxicity. "	( Topotecan induces hepatocellular injury via ASCT2 mediated oxidative stress. Qin, M; Yang, J; Yu, H; Zhang, X; Zhou, G, 2021)	3.51
"Topotecan is a cytostatic drug from the camptothecin group, it acts by inhibiting topoisomerase 1 (TOP1). "	( [Antitumor Activity of the Combination of Topotecan and Tyrosyl-DNA-Phosphodiesterase 1 Inhibitor on Model Krebs-2 Mouse Ascite Carcinoma]. Chepanova, AA; Dyrkheeva, NS; Lavrik, OI; Luzina, OA; Nikolin, VP; Novoselova, ES; Popova, NA; Ryabchikova, EI; Salakhutdinov, NF; Zakharenko, AL, )	1.84
"Topotecan is a useful agent for treating a variety of cancers."	( Oral delivery of topotecan in polymeric nanoparticles: Lymphatic distribution and pharmacokinetics. Jang, JH; Jeong, SH; Lee, YB, 2021)	1.68
"Topotecan is a drug used as second-line chemotherapy for this cancer type."	( New and Old Genes Associated with Topotecan Resistance Development in Ovarian Cancer Cell Lines. Brązert, M; Januchowski, R; Klejewski, A; Nowicki, M; Świerczewska, M; Zabel, M; Zaorska, K, 2017)	1.46
"Topotecan is a drug that is under investigation for the treatment of neuroblastoma and has been encapsulated into liposomes to improve its therapeutic efficacy. "	( In vitro assay for measuring real time topotecan release from liposomes: release kinetics and cellular internalization. Anantha, M; Bally, MB; Chernov, L; Dragowska, WH; Gilabert-Oriol, R, 2017)	2.17
"Topotecan (TPT) is a water-soluble derivate of camptothecin, which undergoes ring-opening hydrolysis in neutral solutions, leading to stability loss and poor cellular uptake. "	( A Novel Polymer-Lipid Hybrid Nanoparticle for the Improvement of Topotecan Hydrochloride Physicochemical Properties. Guilger, RC; Liao, LM; Marreto, RN; Queiroz Junior, LHK; Santana, MJ; Silva, EJ; Silva, LAD; Souza, LG; Taveira, SF, 2018)	2.16
"Topotecan (TPT) is a nontoxic anticancer drug characterized by a pH-dependent lactone/carboxyl equilibrium. "	( Activity of Topotecan toward the DNA/Topoisomerase I Complex: A Theoretical Rationalization. Aviyente, V; Bali, SK; Catak, S; Dikmenli, AK; Marion, A; Ugur, I, 2018)	2.3
"Topotecan is a topoisomerase-1 inhibitor that has previously been shown to enhance the clinical response and overall patient survival when combined with CDDP by a yet unclear mechanism."	( Identification of cisplatin sensitizers through high-throughput combinatorial screening. Chang, A; Chen, P; Chiao, PJ; Hu, Y; Huang, P; Jiang, W; Ling, J; Liu, K; Lu, W; Song, M; Sun, Y, 2018)	1.2
"Topotecan is a relatively large, planar, asymmetric and polar molecule with a lactone moiety. "	( Topotecan effect on the structure of normal and cancer plasma membrane lipid models: A multi-model approach. Lopes-de-Araújo, J; Nunes, C; Reis, S, 2018)	3.37
"Topotecan is a chemotherapeutic agent that is active against many pediatric tumors. "	( Determining success rates of the current pharmacokinetically guided dosing approach of topotecan in pediatric oncology patients. Gajjar, A; Mitchell, AB; Santana, VM; Stewart, CF; Vasilyeva, A, 2019)	2.18
"Topotecan (TPT) is a Topo I inhibitor and shows obvious anti-cancer effects on gastric cancer. "	( Topotecan induces apoptosis via ASCT2 mediated oxidative stress in gastric cancer. Du, HZ; He, JY; Jiang, JW; Li, ZZ; Liu, Y; Sun, L; Wang, L; Yuan, ST; Zhang, BJ; Zhao, TL, 2019)	3.4
"Topotecan (TPT) is an important anti-cancer drug that inhibits topoisomerase I. "	( Development and validation of a liquid chromatography-tandem mass spectrometry method for topotecan determination in beagle dog plasma and its application in a bioequivalence study. Liu, Z; Shi, J; Wan, S; Wang, Y; Yang, X; Ye, L; Zhang, J; Zheng, D, 2013)	2.05
"Topotecan (TPT) is a topoisomerase I inhibitor that undergoes reversible, pH-sensitive ring-opening hydrolysis."	( The role of pH and ring-opening hydrolysis kinetics on liposomal release of topotecan. Anderson, BD; Fugit, KD, 2014)	1.35
"Topotecan (TpT) is a major inhibitory compound of topoisomerase (topo) I that plays important roles in gene transcription and cell division. "	( Heparin and liver heparan sulfate can rescue hepatoma cells from topotecan action. Baghy, K; Bocsi, J; Dudás, J; Füle, T; Fullár, A; Kovalszky, I; Kudaibergenova, S, 2014)	2.08
"Topotecan is a topoisomerase 1 (TOP1) inhibitor that is used to treat various forms of cancer. "	( Topoisomerase 1 inhibition reversibly impairs synaptic function. Kullmann, PH; Mabb, AM; Miriyala, J; Philpot, BD; Twomey, MA; Zylka, MJ, 2014)	1.85
"Topotecan (TPT) is a semisynthetic, water soluble analog of the plant alkaloid camptothecin which has been widely used for the treatment of ovarian and cervical cancers. "	( Electrochemical investigation of the interaction between topotecan and DNA at disposable graphite electrodes. Congur, G; Erdem, A; Mese, F, 2015)	2.1
"Topotecan (TPT) is a therapeutic option for women with platinum-resistant or -refractory ovarian cancer. "	( Topotecan synergizes with CHEK1 (CHK1) inhibitor to induce apoptosis in ovarian cancer cells. Annunziata, CM; James, J; Kim, MK, 2015)	3.3
"Topotecan (TPT) is an anticancer drug widely used in cancer therapy. "	( Binding of topotecan to chromatin: Insights into cooperative binding and comparison with DNA. Babaei, M; Ghadam, P; Rabbani-Chadegani, A, 2015)	2.25
"Topotecan is an approved second-line chemotherapy for small cell lung cancer (SCLC)."	( Efficacy of topotecan in pretreated metastatic poorly differentiated extrapulmonary neuroendocrine carcinoma. Apostolidis, L; Bergmann, F; Jäger, D; Winkler, EC, 2016)	1.53
"topotecan is a feasible option for women withadvanced ovarian and primary peritoneal cancers."	( Phase 2 study of intraperitoneal topotecan as consolidation chemotherapy in ovarian and primary peritoneal carcinoma. Malpass, TW; McGonigle, KF; Muntz, HG; Robertson, MD; Weiden, PL, 2008)	1.35
"Topotecan is an attractive option as it exhibits growth inhibition of human glioma as well as brain penetration."	( Topotecan in combination with radiotherapy in unresectable glioblastoma: a phase 2 study. Bay, JO; Ben Hassel, M; Carsin, B; Fabbro, M; Frappaz, D; Gédouin, D; Guégan, Y; Hamlat, A; Lesimple, T; Linassier, C; Piot, G; Riffaud, L; Saïkali, S, 2009)	2.52
"Topotecan is an established second-line therapy for advanced and relapsed ovarian cancer; a regimen of 1.5 mg/m(2)/day 1-5 has been approved in the USA and many other western countries. "	( Current role and future aspects of topotecan in relapsed ovarian cancer. Oskay-Ozcelik, G; Sehouli, J, 2009)	2.07
"Topotecan is a topoisomerase I inhibitor currently approved for relapsed SCLC."	( Topotecan in second-line treatment of small-cell lung cancer--how it works in our daily clinical practice? Araújo, AM; Bravo, EM; Coelho, AL; Faria, AL; Rocha, IM; Rocha, MA, 2010)	2.52
"Topotecan is a substrate of the ATP-binding cassette transporters P-glycoprotein (P-gp/MDR1) and breast cancer resistance protein (BCRP). "	( Compartment-specific roles of ATP-binding cassette transporters define differential topotecan distribution in brain parenchyma and cerebrospinal fluid. Carcaboso, AM; Elmeliegy, MA; Hubbard, KE; Panetta, JC; Shen, J; Stewart, CF; Tagen, M; Waters, CM; Wynn, HG, 2009)	2.02
"Topotecan is a small molecule DNA topoisomerase I poison, that has been successful in clinical trials against pediatric solid tumors and leukemias. "	( Initial testing of topotecan by the pediatric preclinical testing program. Carol, H; Gorlick, R; Houghton, PJ; Kang, MH; Keir, ST; Kolb, EA; Lock, RB; Maris, JM; Morton, CL; Reynolds, CP; Smith, MA; Watkins, A, 2010)	2.13
"Topotecan is a promising drug with activity against retinoblastoma, however, attaining therapeutic concentrations in the vitreous humor is still a challenge for the treatment of vitreous seeds in retinoblastoma. "	( Pharmacokinetic analysis of topotecan after intra-vitreal injection. Implications for retinoblastoma treatment. Abramson, DH; Bramuglia, GF; Buitrago, E; Chantada, G; Fandiño, A; Höcht, C; Navo, E; Schaiquevich, P, 2010)	2.1
"Topotecan is a relatively new drug for use as a second-line treatment in patients with relapsed small cell lung cancer (SCLC). "	( Topotecan for relapsed small cell lung cancer: a systematic review and economic evaluation. Bird, A; Clegg, A; Harris, P; Hartwell, D; Jones, J; Loveman, E, 2011)	3.25
"Topotecan is a chemotherapeutic agent of choice for the second-line treatment of recurrent ovarian cancer. "	( Physiologically based pharmacokinetic model for topotecan in mice. Balthasar, JP; Shah, DK, 2011)	2.07
"Topotecan is a topoisomerase I inhibitor with good central nervous system (CNS) penetration following oral administration."	( A phase II study of metronomic oral topotecan for recurrent childhood brain tumors. Allen, JC; Belasco, JB; Fisher, PG; Janss, AJ; Minturn, JE; Patti, R; Phillips, PC, 2011)	1.37
"Topotecan is an active drug in relapsed neuroblastoma. "	( Short topotecan-based induction regimen in newly diagnosed high-risk neuroblastoma. Castellano, A; De Ioris, MA; De Pasquale, MD; De Vito, R; Donfrancesco, A; Garganese, MC; Ilari, I; Inserra, A; Jenkner, A; Locatelli, F; Natali, G; Ravà, L, 2011)	2.29
"Topotecan is an important cytotoxic drug that has gained broad acceptance in clinical use for the treatment of refractory ovarian and small-cell lung cancer. "	( Development of topotecan loaded lipid nanoparticles for chemical stabilization and prolonged release. Braga, RC; Lima, EM; Marreto, RN; Martins, AL; Mota, MF; Silva, EJ; Souza, LG; Taveira, SF; Valadares, MC, 2011)	2.16
"Topotecan (TPT) is a camptothecin derivative and is an anticancer drug working as a topoisomerase-I-specific inhibitor. "	( Evaluation of the P-glycoprotein- and breast cancer resistance protein-mediated brain penetration of 11C-labeled topotecan using small-animal positron emission tomography. Fujinaga, M; Fukumura, T; Hatori, A; Kawamura, K; Nengaki, N; Ogawa, M; Wakizaka, H; Yamasaki, T; Yanamoto, K; Yoshida, Y; Yui, J; Zhang, MR, 2011)	2.02
"Topotecan is an attractive building block for improving therapy against advanced disease."	( A pharmacokinetic evaluation of topotecan as a cervical cancer therapy. Blank, S; Muggia, F; Musa, F, 2013)	1.39
"Topotecan proved to be a promising agent for retinoblastoma treatment due to its pharmacological activity and limited toxicity."	( Ocular and systemic toxicity of intravitreal topotecan in rabbits for potential treatment of retinoblastoma. Asprea, M; Bramuglia, GF; Buitrago, E; Chantada, GL; Croxatto, JO; Del Sole, MJ; Fandino, A; Schaiquevich, P; Torbidoni, A, 2013)	1.37
"Topotecan is a topoisomerase-I inhibitor, a drug that stabilizes a covalent complex of enzymes and causes strand cleavage of DNA. "	( Phase I study of sequential administration of topotecan and 5-fluorouracil in patients with advanced malignancies. Devereux, L; Goldberg, J; Grana, G; Hageboutros, A; Khatri, J; Rodman, WD; Sbar, EI; Tritschler, L, 2002)	2.02
"Topotecan is a new topoisomerase-1 inhibitor whose early investigation suggested possible activity in hormone-refractory prostate cancer."	( SWOG-9510: evaluation of topotecan in hormone refractory prostate cancer: a Southwest Oncology Group study. Braun, TJ; Crawford, ED; Dakhil, SR; Hussain, MH; Klein, CE; Nichols, CR; Peereboom, DM; Rivkin, SE; Tangen, CM, 2002)	1.34
"Topotecan is an effective regimen with acceptable toxicity for recurrent ovarian cancer when administered for 3 consecutive days (2 mg/m(2)) every 21 days. "	( Three-consecutive-day topotecan is an active regimen for recurrent epithelial ovarian cancer. Brown, JV; Drescher, CW; Graham, CL; Micha, JP; Peters, WA; Rettenmaier, MA; Smith, MR, 2003)	2.08
"Topotecan is an active agent for the treatment of advanced endometrial carcinoma. "	( Topotecan is an active agent in the first-line treatment of metastatic or recurrent endometrial carcinoma: Eastern Cooperative Oncology Group Study E3E93. Goldberg, G; Levy, DE; Lincoln, ST; Schink, JC; Soori, GS; Wadler, S, 2003)	3.2
"Topotecan is a novel topoisomerase I inhibitor with established antitumor activity in recurrent SCLC and has a predictable, noncumulative toxicity profile."	( Treatment of relapsed small-cell lung cancer--a focus on the evolving role of topotecan. Chiappori, A; Rocha Lima, CM, 2003)	1.27
"Topotecan is a cytotoxic drug isolated from the Camptotheca acuminata tree (from China). "	( [Topotecan for pediatric patients with resistant and recurrent solid tumors]. Contra, T; Díaz Pérez, MA; Madero López, L; Pérez Martínez, A; Scaglione, C, 2003)	2.67
"Topotecan is an established therapy for the treatment of recurrent ovarian cancer and has demonstrated significant antitumor activity in both platinum-sensitive and platinum-resistant patient populations. "	( Clinical experience with topotecan in relapsed ovarian cancer. Herzog, TJ, 2003)	2.07
"Topotecan is an established treatment for patients with relapsed ovarian cancer, with good antitumor activity in both platinum-sensitive and -resistant disease. "	( Weekly topotecan in the management of ovarian cancer. Morris, RT, 2003)	2.22
"Topotecan (TPT) is a topoisomerase I inhibitor, and like the other drugs of this family, it is believed to act in a specific way on cells in S phase at the time of treatment. "	( Cytostatic and cytotoxic effects of topotecan decoded by a novel mathematical simulation approach. Branduardi, D; D'Incalci, M; Lupi, M; Matera, G; Ubezio, P, 2004)	2.04
"Topotecan is an active second-line treatment for advanced ovarian cancer. "	( Topotecan compared with no therapy after response to surgery and carboplatin/paclitaxel in patients with ovarian cancer: Multicenter Italian Trials in Ovarian Cancer (MITO-1) randomized study. Biamonte, R; Cartenì, G; Danese, S; De Laurentiis, M; De Matteis, A; De Placido, S; Di Vagno, G; Febbraro, A; Gallo, C; Gasparini, G; Greggi, S; Lauria, R; Lombardi, AV; Manzione, L; Marinaccio, M; Naglieri, E; Perrone, F; Pignata, S; Scambia, G; Valerio, MR, 2004)	3.21
"Topotecan HCl is an antitumor drug exhibiting topoisomerase 1-inhibitory activity. "	( Topotecan-induced bronchiolitis. Edgerton, CC; Gilman, M; Roth, BJ, 2004)	3.21
"Topotecan is an effective agent against pediatric medulloblastoma in patients who have received no therapy other than surgery. "	( Results of a phase II upfront window of pharmacokinetically guided topotecan in high-risk medulloblastoma and supratentorial primitive neuroectodermal tumor. Ashley, D; Chintagumpala, M; Fouladi, M; Gajjar, A; Houghton, PJ; Iacono, LC; Kellie, SJ; Kirstein, MN; Seele, LG; Stewart, CF; Wallace, D; Zamboni, WC, 2004)	2
"Topotecan, which is a Camptothecin derivative, shows a large spectrum in anti-tumor activity. "	( The effect of quercetin on topotecan cytotoxicity in MCF-7 and MDA-MB 231 human breast cancer cells. Akbas, SH; Ozben, T; Timur, M, 2005)	2.07
"Topotecan (T) is an active drug in SCLC. "	( Randomized phase II study comparing topotecan/cisplatin administration for 5 days versus 3 days in the treatment of extensive stage small cell lung cancer (SCLC). Fuhr, HG; Jensen, K; Keppler, U; Mueller, C; Neubauer, A; Schröder, M; Seifart, U; Staab, HJ; Ukena, J; Wolf, M, 2005)	2.05
"Topotecan (TPT) is a semisynthetic water-soluble derivative of camptothecin (CPT) used as second-line therapy in patients with metastatic ovarian carcinoma, small cell lung cancer, and other malignancies. "	( Topotecan is a substrate for multidrug resistance associated protein 4. Bian, JS; Chan, E; Chan, SY; Duan, W; Ho, PC; Huang, M; Li, Q; Ng, KY; Nie, YQ; Tan, TM; Tian, Q; Wei, H; Yang, HY; Yu, Q; Zhang, J; Zhou, SF; Zhu, YZ, 2006)	3.22
"Topotecan is an active drug in small-cell lung cancer (SCLC). "	( Randomised phase II study comparing topotecan/carboplatin administration for 5 versus 3 days in the treatment of extensive-stage small-cell lung cancer. Dethling, J; Fink, T; Hans, K; Koschel, G; Lorenz, R; Mueller, C; Schade-Brittinger, C; Schroeder, H; Seifart, U; Wolf, M, 2007)	2.06
"Topotecan is an active agent for the management of untreated and recurrent extensive-disease small cell lung cancer (ED-SCLC). "	( Addition of topotecan to standard cisplatin/etoposide combination in patients with extended stage small cell lung carcinoma. Aydiner, A; Camlica, H; Derin, D; Guney, N; Tas, F; Topuz, E, 2007)	2.16
"Topotecan is an active agent in ovarian cancer."	( UCN-01 in combination with topotecan in patients with advanced recurrent ovarian cancer: a study of the Princess Margaret Hospital Phase II consortium. Brown, S; Carey, MS; Dancey, JE; Hirte, HW; Hotte, SJ; Oza, AM; Pond, GR; Tsao, MS; Welch, S, 2007)	1.36
"Topotecan is an intravenous topoisomerase I inhibitor with good CSF penetration and documented efficacy in patients with relapsed systemic non-Hodgkin's lymphoma."	( Topotecan as salvage therapy for relapsed or refractory primary central nervous system lymphoma. Batchelor, T; Betensky, R; Hochberg, F; Voloschin, AD; Wen, PY, 2008)	2.51
"Topotecan is a semisynthetic derivative of camptothecin that specifically targets topoisomerase I. "	( Recent advances with topotecan in the treatment of lung cancer. Eckardt, J; O'Brien, M; Ramlau, R, 2007)	2.1
"Topotecan is a topoisomerase I inhibitor that exerts its cytotoxic effect through stabilization of the topoisomerase I-DNA complex."	( Phase I dose escalation study of vinorelbine and topotecan combination chemotherapy in patients with recurrent lung cancer. Beldner, MA; Chaudhary, U; Garrett-Mayer, E; Green, MR; Kraft, AS; Meyer, ML; Montero, AJ; Sherman, CA, 2007)	1.32
"Topotecan is a novel semisynthetic derivative of the anticancer agent camptothecin and inhibits the intranuclear enzyme topoisomerase I."	( Phase I clinical and pharmacokinetic study of topotecan administered by a 24-hour continuous infusion. Beijnen, JH; Davies, BE; Koier, I; Maes, RA; Rodenhuis, S; Rosing, H; ten Bokkel Huinink, WW; van Warmerdam, LJ, 1995)	1.27
"Topotecan is a novel semisynthetic derivative of the anticancer agent camptothecin and inhibits the intranuclear enzyme topoisomerase I. "	( Pharmacokinetics and pharmacodynamics of topotecan administered daily for 5 days every 3 weeks. Beijnen, JH; Davies, BE; de Boer-Dennert, M; Maes, RA; Rosing, H; Schellens, JH; van Warmerdam, LJ; Verweij, J, 1995)	2
"Topotecan is a promising anticancer agent presently undergoing clinical evaluation worldwide. "	( Stabilization of topotecan in low pH liposomes composed of distearoylphosphatidylcholine. Burke, TG; Gao, X, 1994)	2.07
"Topotecan is an inhibitor of topoisomerase I that has shown preclinical activity against non-small-cell lung cancer (NSCLC). "	( Phase II study of topotecan in metastatic non-small-cell lung cancer. Elias, A; Frei, E; Kalish, L; Lynch, TJ; Posner, M; Shulman, LN; Skarin, A; Strauss, G, 1994)	2.07
"Topotecan is a promising anticancer agent that deserves phase II testing in pediatric solid tumors. "	( Phase I study of topotecan for pediatric patients with malignant solid tumors. Bowman, L; Furman, W; Heideman, R; Kuttesch, JF; Marina, N; Ochs, J; Pratt, CB; Sandlund, JT; Santana, VM; Stewart, C, 1994)	2.07
"Topotecan is an interesting new topoisomerase I inhibitor exerting antitumor activity in this phase I trial. "	( Phase I and pharmacokinetics study of topotecan, a new topoisomerase I inhibitor. Beijnen, J; de Boer-Dennert, M; Hansen, H; Koier, I; Lund, B; Planting, A; Rosing, H; Verweij, J, 1993)	2
"Topotecan is an another semisynthetic derivative of camtothecin and is also topoisomerase I inhibitor."	( [Topoisomerase inhibitors developing in Japan]. Furue, H, 1993)	1.01
"Topotecan (TPT) is a topoisomerase I poison that exhibits antineoplastic activity. "	( Cytotoxic effects of topotecan combined with various anticancer agents in human cancer cell lines. Buckwalter, CA; Donehower, RC; Grochow, LB; Kaufmann, SH; Peereboom, D; Rowinsky, EK; Svingen, PA, 1996)	2.06
"Topotecan is a novel semisynthetic derivative of the anticancer agent camptothecin and inhibits the intranuclear enzyme topoisomerase I. "	( Pharmacokinetics and pharmacodynamics of topotecan given on a daily-times-five schedule in phase II clinical trials using a limited-sampling procedure. Beijnen, JH; Creemers, GJ; Davies, BE; de Boer-Dennert, M; Maes, RA; Rodenhuis, S; Rosing, H; Schellens, JH; ten Bokkel Huinink, WW; van Warmerdam, LJ; Verweij, J, 1996)	2
"Topotecan is a topoisomerase I inhibitor that has good penetration across the blood-brain barrier and significant antitumor activity against human brain tumor xenografts. "	( Phase II evaluation of topotecan for pediatric central nervous system tumors. Adamson, PC; Allen, JC; Balis, FM; Berg, SL; Blaney, SM; Heideman, RL; Horowitz, ME; Jakacki, RI; Lange, BJ; Packer, RJ; Phillips, PC; Poplack, DG; Reaman, GH; Sallan, SE, 1996)	2.05
"Topotecan is a specific inhibitor of topoisomerase I with broad antitumor activity in preclinical studies."	( Phase II study of topotecan in metastatic hormone-refractory prostate cancer. Fox, SC; Giantonio, BJ; Greenberg, R; Hudes, GR; Kosierowski, R; McAleer, CA; Ozols, RF; Ramsey, HE, 1995)	1.35
"Topotecan is a specific inhibitor of topoisomerase I. "	( Phase II and pharmacologic study of topotecan administered as a 21-day continuous infusion to patients with colorectal cancer. Creemers, GJ; de Boer-Dennert, M; Gerrits, CJ; Harteveld, M; Hudson, I; Loos, W; Planting, AS; Schellens, JH; Stoter, G; van Beurden, VM; van der Burg, ME; Verweij, J, 1996)	2.01
"Topotecan (TPT) is a water-soluble Topoisomerase I (Topo I) inhibitor with reported antineoplastic activity against a variety of solid tumors (including nonsmall cell lung, small cell lung, ovarian, breast, esophageal, and head and neck primaries) and leukemias. "	( Concentration and timing dependence of lethality enhancement between topotecan, a topoisomerase I inhibitor, and ionizing radiation. Boothman, DA; Kinsella, TJ; Lamond, JP; Wang, M, 1996)	1.97
"Topotecan is a topoisomerase I inhibitor with preclinical activity against various tumor types. "	( Topotecan, an active drug in the second-line treatment of epithelial ovarian cancer: results of a large European phase II study. Bolis, G; Creemers, GJ; Despax, R; Favalli, G; Gore, M; Guastalla, JP; Hudson, I; Kreinberg, R; Lacave, AJ; Scarfone, G; Ten Bokkel Huinink, WW; Van Belle, S; Verweij, J, 1996)	3.18
"Topotecan (TPT) is a topoisomerase I (topo I) poison that has shown promising antineoplastic activity in solid tumors and acute leukemia. "	( Altered formation of topotecan-stabilized topoisomerase I-DNA adducts in human leukemia cells. Armstrong, DK; Cheng, YC; Gore, SD; Kaufmann, SH; Rowinsky, EK; Svingen, PA, 1997)	2.06
"Topotecan is a specific inhibitor of topoisomerase I. "	( Phase I and pharmacologic study of oral topotecan administered twice daily for 21 days to adult patients with solid tumors. Broom, C; Burris, HA; Creemers, GJ; Eckardt, JR; Gerrits, CJ; Hudson, I; Loos, WJ; Planting, AS; Rodriguez, GI; Schellens, JH; Verweij, J; Von Hoff, DD, 1997)	2.01
"Topotecan is a well-tolerated new agent with similar single-agent activity to that of cisplatin, 5-fluorouracil, and methotrexate in advanced head and neck cancer."	( A phase II study of topotecan in patients with recurrent head and neck cancer. Identification of an active new agent. Robert, F; Soong, SJ; Wheeler, RH, 1997)	1.34
"Topotecan (NSC 609099) is a camptothecin analogue that demonstrated activity against a variety of human tumors in preclinical studies. "	( Phase II trial of topotecan in advanced gastric cancer: a Southwest Oncology Group study. Balcerzak, SP; Benedetti, JK; Burris, HA; Macdonald, JS, 1997)	2.07
"Topotecan (Hycamtin) is a promising new topoisomerase I-targeting anticancer agent that first entered clinical trials in 1989 under National Cancer Institute sponsorship in collaboration with SmithKline Beecham. "	( Clinical status and optimal use of topotecan. Arbuck, SG; Takimoto, CH, 1997)	2.02
"Topotecan is a topoisomerase I inhibitor with antitumor activity against hematologic and solid tumor malignancies. "	( Evaluation of topotecan in resistant and relapsing multiple myeloma: a Southwest Oncology Group study. Alsina, M; Crowley, JJ; Kraut, EH; Laufman, LR; Salmon, SE; Taylor, SA; Wade, JL, 1998)	2.1
"Topotecan is a topoisomerase I inhibitor with activity against xenografts of childhood solid tumors and established clinical activity against neuroblastoma and rhabdomyosarcoma. "	( Relationship between topotecan systemic exposure and tumor response in human neuroblastoma xenografts. Cheshire, PJ; Houghton, JA; Houghton, PJ; Luo, X; Poquette, C; Richmond, LB; Santana, VM; Stewart, CF; Thompson, J; Zamboni, WC, 1998)	2.06
"Topotecan is a novel topoisomerase I inhibitor that may have a role in the adjuvant chemotherapy of several solid tumors, including malignant glioma. "	( Potentiation of CD95L-induced apoptosis of human malignant glioma cells by topotecan involves inhibition of RNA synthesis but not changes in CD95 or CD95L protein expression. Weller, M; Winter, S, 1998)	1.97
"Topotecan is a topoisomerase I inhibitor with activity against acute leukemia. "	( Induction of apoptosis by topotecan: implications for the treatment of leukemia. Seiter, K, 1998)	2.04
"Topotecan is a topoisomerase (topo) I inhibitor with promising activity in preclinical studies. "	( Intratumoral infusion of topotecan prolongs survival in the nude rat intracranial U87 human glioma model. Barone, TA; Ciesielski, MJ; Fenstermaker, RA; Greenberg, SJ; Lis, A; Plunkett, RJ; Pollina, J, 1998)	2.05
"Topotecan is an agent as yet unstudied in bladder cancer."	( Topotecan in previously treated advanced urothelial carcinoma: an ECOG phase II trial. Burch, PA; Kuzel, T; Loehrer, PJ; Manola, J; Weinshel, EL; Witte, RS, 1998)	2.46
"Topotecan is a specific inhibitor to topoisomerase I. "	( Five days of oral topotecan (Hycamtin), a phase I and pharmacological study in adult patients with solid tumours. Burris, H; Fields, S; Gerrits, CJ; Hudson, I; Loos, WJ; Planting, AS; Rodriguez, GI; Schellens, JH; van Beurden, V; van den Burg, ME; Verweij, J; von Hoff, DD, 1998)	2.08
"Topotecan is an effective second- or third-line therapy for patients with advanced ovarian cancer and is comparable to ifosfamide, liposomal doxorubicin, and paclitaxel. "	( Topotecan: a new topoisomerase I inhibiting antineoplastic agent. Cersosimo, RJ, 1998)	3.19
"Topotecan is an effective second-line agent for patients with unresponsive or relapsed cancer of the ovary. "	( Topotecan: a new topoisomerase I inhibiting antineoplastic agent. Cersosimo, RJ, 1998)	3.19
"Topotecan is a semisynthetic product derived from camptothecin, which was discovered during a National Cancer Institute cytotoxic drug screening program almost 30 years ago."	( Topotecan - A novel topoisomerase I inhibitor: pharmacology and clinical experience. Bokemeyer, C; Jakob, A; Kanz, L; Kollmannsberger, C; Mross, K, 1999)	2.47
"Topotecan is a myelosuppressive drug that interacts with topoisomerase I and that has been used in the treatment of refractory AML."	( Incorporating new modalities into guidelines. Topotecan for myelodysplastic syndromes. Estey, EH, 1998)	1.28
"Topotecan is a new antineoplastic agent with a broad spectrum of activity. "	( Phase I trial of paclitaxel, carboplatin, and topotecan with or without filgrastim (granulocyte-colony stimulating factor) in the treatment of patients with advanced, refractory cancer. Burris, HA; Greco, FA; Hainsworth, JD; Morrissey, LH, 1999)	2
"Topotecan is an antitumor agent with activity against a variety of cancers. "	( Fluorescence spectral properties of the anticancer drug topotecan by steady-state and frequency domain fluorometry with one-photon and multi-photon excitation. Burke, TG; Gryczynski, I; Gryczynski, Z; Lakowicz, JR; Yang, D, 1999)	1.99
"Topotecan is a new antineoplastic agent active in ovarian cancer, with promising activity in small cell lung cancer and predictable toxicity. "	( Circulating progenitor cell release and functional characterization after topotecan plus G-CSF and erythropoietin in small cell lung cancer patients. Ascari, E; Brugnatelli, S; Comolli, G; Danova, M; Ferrari, S; Porta, C; Pugliese, P; Riccardi, A, 1999)	1.98
"Topotecan-cytarabine is an active induction regimen in MDS and CMML patients, is well tolerated, and is associated with a low mortality rate."	( Topotecan and cytarabine is an active combination regimen in myelodysplastic syndromes and chronic myelomonocytic leukemia. Andreeff, M; Beran, M; Cortes, J; Estey, E; Giles, FJ; Hayes, K; Kantarjian, H; Keating, M; Koller, CA; Kornblau, S; O'Brien, S; Pierce, SR; Vey, N; Wong, GC, 1999)	2.47
"Topotecan is an active drug in platinum-sensitive ovarian cancer, with significant but manageable hematologic toxicity. "	( Topotecan has substantial antitumor activity as first-line salvage therapy in platinum-sensitive epithelial ovarian carcinoma: A Gynecologic Oncology Group Study. Blessing, JA; Bookman, MA; Dunton, CJ; Lentz, SS; McGuire, WP, 2000)	3.19
"Topotecan is a topoisomerase I inhibitor with significant activity in patients with myelodysplastic syndrome and chronic myelomonocytic leukemia. "	( Cyclophosphamide, ara-C and topotecan (CAT) for patients with refractory or relapsed acute leukemia. Beran, M; Cortes, J; Estey, E; Giles, F; Kantarjian, H; Keating, M; Koller, C; O'Brien, S, 2000)	2.04
"Topotecan is a new active drug in the treatment of lung cancer. "	( [Topotecan, a recent discovery and prospects for treating tumors of the lung]. Gridelli, C, )	2.48
"Topotecan is a semi-synthetic, water soluble topoisomerase I inhibitor which has recently been approved for the treatment of ovarian cancers after failure of first-line therapy. "	( [Topotecan: prospects for using it in combination therapy for ovarian carcinoma]. Scarfone, G, )	2.48
"Topotecan (TPT) is a DNA-Topoisomerase I poison that exhibits antitumor activity. "	( Cytotoxic effects of topotecan combined with various active G2/M-phase anticancer drugs in human tumor-derived cell lines. Abad, A; Guillot, M; Martin, C; Plasencia, C; Taron, M, 2000)	2.07
"Topotecan is a topoisomerase I inhibitor which is currently evaluated as an adjuvant agent for malignant glioma. "	( Glioma cell sensitivity to topotecan: the role of p53 and topotecan-induced DNA damage. Naumann, U; Rieger, J; Schmidt, F; Weller, M; Wischhusen, J, 2001)	2.05
"Topotecan is a topoisomerase inhibitor that demonstrated initial promising activity in squamous carcinoma of the head and neck."	( Lack of efficacy of topotecan in the treatment of metastatic or recurrent squamous carcinoma of the head and neck: an Eastern Cooperative Oncology Group Trial (E3393). Burkey, B; Forastiere, A; Langer, C; Leong, T; Murphy, BA, 2001)	1.36
"Topotecan is a derivative of camptothecin which has been structurally modified to increase water solubility."	( Topoisomerase I inhibition with topotecan: pharmacologic and clinical issues. Arun, B; Frenkel, EP, 2001)	1.32
"Oral topotecan is an active, tolerable, and convenient formulation of an established agent for the second-line treatment of advanced epithelial ovarian cancer and may also facilitate exploring prolonged treatment schedules."	( Oral topotecan as single-agent second-line chemotherapy in patients with advanced ovarian cancer. Beckman, RA; Clarke-Pearson, DL; DeWitte, MH; Fields, SZ; Hanjani, P; Iveson, T; Kristensen, G; Lane, SR; Malfetano, JH; Ross, GA; Van Le, L; Whitney, CW, 2001)	1.28
"Topotecan is a topoisomerase I inhibitor with demonstrated anticancer activity in preclinical and clinical studies. "	( Synergistic interaction between topotecan and microtubule-interfering agents. Bahadori, HR; Catapano, CV; Green, MR, 2001)	2.04
"Topotecan is a topoisomerase (Topo) I inhibitor used in ovarian carcinoma chemotherapy. "	( Schedule-dependent activity of topotecan in OVCAR-3 ovarian carcinoma xenograft: pharmacokinetic and pharmacodynamic evaluation. Bugat, R; Canal, P; Chatelut, E; Guichard, S; Hennebelle, I; Montazeri, A, 2001)	2.04
"Topotecan is a topoisomerase I inhibitor and an analogue of camptothecin with demonstrated activity in small-cell lung cancer. "	( Preliminary results of combined therapy with topotecan and carboplatin in advanced non-small-cell lung cancer. Fields, SZ; Hearn, S; Martoni, A; Pujol, JL; Ross, G; Tumolo, S; von Pawel, J, 2001)	2.01
"Topotecan is an established topoisomerase I inhibitor for the treatment of relapsed ovarian cancer. "	( A dose-escalating study of weekly bolus topotecan in previously treated ovarian cancer patients. Hall, DJ; Homesley, HD; Lewandowski, GS; Martin, DA; Nahhas, WA; Penley, RG; Suggs, CL; Vaccarello, L, 2001)	2.02
"Topotecan-filgrastim is an efficacious, minimally toxic, and cost-saving combination for PBSC mobilization."	( Topotecan-filgrastim combination is an effective regimen for mobilizing peripheral blood stem cells. Bowman, LC; Cunningham, JM; Gajjar, AJ; Houghton, PJ; Houston, JA; Hunt, D; Richardson, SL; Stewart, CF; Yee, GC; Yeoh, EJ, 2001)	2.47
"Topotecan is an effective drug for the treatment of SCLC and recurrent OV. "	( [Clinical study of topotecan in the treatment of small cell lung cancer and recurrent ovarian cancer]. Feng, F; He, X; Shi, Y, 2001)	2.08
"Topotecan (SK&F 104864) is a novel antitumor agent whose mechanism of action is inhibition of the DNA unwinding protein topoisomerase I. "	( A phase I clinical and pharmacokinetic study of the topoisomerase I inhibitor topotecan (SK&F 104864) given as an intravenous bolus every 21 days. Brown, T; Burris, HA; Clark, G; Kneuper-Hall, R; O'Rourke, T; Rodriguez, G; Shaffer, D; Von Hoff, DD; Wall, JG; Weiss, G, 1992)	1.95

Excerpt	Reference	Relevance
"Topotecan has a positive influence on quality of life of patients with advanced colorectal cancer. "	( [Evaluation of quality of life in patients with advanced colorectal cancer treated with topotecan]. Brodziak, A; Bucior, J; Danikiewicz, A; Foltyn, W; Jastrzebska-Okoń, K; Knopik, J; Nowakowska-Zajdel, E; Ziółko, E, 2001)	1.98
"Topotecan has recently been used in the treatment of pediatric cancer. "	( A modified protocol with vincristine, topotecan, and cyclophosphamide for recurrent/progressive ewing sarcoma family tumors. Agaoglu, FY; Cakir, FB; Darendeliler, E; Gorgun, O; Kebudi, R, 2013)	2.1
"Oral topotecan (Hycamtin(®)) has been recently approved for the treatment of relapsed small cell lung cancer (SCLC) in 2007, however, the bioavailability and pharmacokinetic data of topotecan for Chinese patients is still limited. "	( Oral topotecan: Bioavailability, pharmacokinetics and impact of ABCG2 genotyping in Chinese patients with advanced cancers. Du, P; Gui, L; Han, X; Li, N; Shen, Y; Shi, Y; Song, Y; Sun, Y; Wang, J; Wang, S; Yang, J, 2013)	1.42
"Topotecan has shown promising antineoplastic activity in solid tumors and acute leukemia. "	( Antiproliferative and proapoptotic effects of topotecan in combination with thymoquinone on acute myelogenous leukemia. El-Hayek, S; Hodroj, MH; Khalife, R; Rizk, S; Stephany, el-H; Tarras, O, 2014)	2.1
"Topotecan has been variably incorporated in the treatment of patients with relapsed Wilms tumour (WT) who failed initial treatment with three or more effective drugs. "	( Treatment of relapsed Wilms tumour (WT) patients: experience with topotecan. A report from the SIOP Renal Tumour Study Group (RTSG). Acha, T; Bergeron, C; Catania, S; Graf, N; Howell, L; Mavinkurve-Groothuis, AM; Pritchard-Jones, KL; Spreafico, F; Tytgat, GA; van den Heuvel-Eibrink, MM; van Tinteren, H; Vujanic, G, 2015)	2.1
"Oral topotecan has been recently brought into clinical practice at a dose of 2.3 mg/m(2) for 5 days, every 3 weeks. "	( Myelotoxicity of oral topotecan in relation to treatment duration and dosage: a phase I study. Anagnostopoulos, A; Antoniou, D; Ardavanis, A; Athanasiadis, A; Koutantos, J; Papadopoulos, G; Papakotoulas, P; Pectasides, D; Stathopoulos, GP; Trafalis, D; Vaslamatzis, M, 2010)	1.19
"Oral topotecan plus BSC has advantages over BSC alone in terms of survival (hazard ratio = 0.61; 95% CI, 0.43 to 0.87) and quality of life (EQ-5 D difference: 0.15; 95% CI, 0.05 to 0.25)."	( Systematic Review of topotecan (Hycamtin) in relapsed small cell lung cancer. Bashir, Z; Gooch, CL; Kleijnen, J; Riemsma, R; Simons, JP, 2010)	1.13
"Topotecan has single-agent activity in recurrent ovarian cancer. "	( Advanced ovarian cancer: phase III randomized study of sequential cisplatin-topotecan and carboplatin-paclitaxel vs carboplatin-paclitaxel. Brotto, L; Casado, A; Cervantes, A; Chen, D; D'Hondt, V; Eisenhauer, EA; Elit, L; Germa, JR; Ghatage, P; Grimshaw, R; Hoskins, P; Katsaros, D; Mendiola, C; Ojeda, B; Oza, A; Poveda, A; Provencher, D; Roy, M; Stuart, G; Sugimoto, A; Tu, D; Vergote, I; Zola, P, 2010)	2.03
"Topotecan has recently been used as a second-line agent in treatment of advanced ovarian disease."	( The role of topotecan as second-line therapy in patients with recurrent ovarian cancer. Beshara, N; Faught, W; Fung Kee Fung, M, 2002)	1.41
"Topotecan has demonstrated efficacy in the treatment of both platinum-sensitive and platinum-resistant recurrent ovarian cancer. "	( Alternate dosing schedules for topotecan in the treatment of recurrent ovarian cancer. Morris, R; Munkarah, A, 2002)	2.04
"Topotecan has demonstrated exceptional central nervous system penetration as well as radiosensitizing properties in glioblastoma xenografts [Chastagner et al., Int J Radiat Oncol Biol Phy 50: 777-782, 2001]. "	( Prolonged infusional topotecan and accelerated hyperfractionated 3d-conformal radiation in patients with newly diagnosed glioblastoma--a phase I study. Anders, K; Feldmann, HJ; Fietkau, RJ; Grabenbauer, GG; Klautke, G; Krauseneck, P; Sauer, R; Staab, HJ; Weiser, S, 2002)	2.08
"Oral topotecan therapy has antitumor activity in a small percentage of patients with relapsed or refractory neuroblastoma. "	( Oral topotecan for refractory and relapsed neuroblastoma: a retrospective analysis. Cheung, NK; Kramer, K; Kushner, BH, 2003)	1.35
"Topotecan has also been studied in combinations: a combination of topotecan, administered using the standard 5-day schedule, with cisplatin was effective but was associated with myelosuppression."	( Combination chemotherapy with topotecan for non-small cell lung cancer. Dowlati, A; Levitan, N, 2003)	1.33
"Topotecan has demonstrable activity in high-risk MDS and CMMoL. "	( Phase II study of low-dose topotecan in myelodysplastic syndromes: a Hoosier Oncology Group (HOG) study. Cripe, LD; Pennington, K; Stender, MJ; Stephens, A; Stoner, C; Vaena, DA; Walker, P; Yiannoutsos, CT; Young, C, 2004)	2.06
"Topotecan has shown fewer side effects and higher efficacy when given as a continuous i.v."	( Phase I/II trial of topotecan given as continuous infusion in combination with oxaliplatin in 5-FU-pretreated patients with colorectal cancer. Deckert, PM; Hütter, G; Keilholz, U; Szélenyi, H; Thiel, E, 2004)	1.37
"Topotecan has demonstrated antitumor activity in heavily pretreated patients with ovarian carcinoma. "	( Topotecan in heavily pretreated patients with recurrent ovarian, peritoneal, and fallopian tube carcinoma. Piura, B; Rabinovich, A, )	3.02
"Topotecan has been emerged as a new promising anticancer drug for patients with ovarian cancer."	( Topotecan in platinum-resistant epithelial ovarian cancer. Akman, L; Dikmen, Y; Goker, E; Karabulut, B; Ozsaran, A; Sanli, UA; Sezgin, C; Terek, MC; Uslu, R, 2005)	3.21
"Topotecan has demonstrated activity in ovarian carcinomas. "	( Phase I study of high-dose topotecan with haematopoietic stem cell support in the treatment of ovarian carcinomas: the ITOV 01 protocol. Cailliot, C; Dosquet, C; Fabbro, M; Genève, J; Gligorov, J; Goetschel, A; Gosse, B; Lefèvre, G; Lhommé, C; Lokiec, F; Lotz, JP; Micléa, JM; Pautier, P; Provent, S; Ribrag, V; Selle, F; Viens, P; Viret, F, 2006)	2.07
"Topotecan has provided an efficacious and tolerable therapeutic option for patients with recurrent small-cell lung cancer, and the oral formulation has also been shown to be beneficial, even in elderly patients of poor performance status."	( Topotecan for the treatment of small-cell lung cancer. Nicum, SJ; O'Brien, ME, 2007)	2.5
"Oral topotecan has been studied in the first- and second-line settings for both SCLC and non-small cell lung cancer (NSCLC)."	( Recent advances with topotecan in the treatment of lung cancer. Eckardt, J; O'Brien, M; Ramlau, R, 2007)	1.11
"Topotecan has been shown in previous studies to be a specific inhibitor of topoisomerase I, a nuclear enzyme required for DNA replication and transcription."	( Phase I clinical and pharmacology study of topotecan given daily for 5 consecutive days to patients with advanced solid tumors, with attempt at dose intensification using recombinant granulocyte colony-stimulating factor. Barbosa, K; Niedzwiecki, D; Saltz, L; Sirott, M; Tao, Y; Tong, W; Trochanowski, B; Tzy-Jyun, Y; Wright, P; Young, C, 1993)	1.99
"Topotecan has undergone phase I clinical evaluations in USA, europe, and recently in Japan."	( [Topoisomerase inhibitors developing in Japan]. Furue, H, 1993)	1.01
"Topotecan has shown significant preclinical activity in refractory murine tumors and in human tumor xenograft models."	( Plasma and cerebrospinal fluid pharmacokinetic study of topotecan in nonhuman primates. Balis, FM; Blaney, SM; Cole, DE; Godwin, K; Poplack, DG, 1993)	1.25
"Topotecan has been administered in phase I trials in several infusion schedules ranging from 30 minutes to 21 days."	( Clinical pharmacokinetics of topotecan. Beijnen, JH; Herben, VM; ten Bokkel Huinink, WW, 1996)	1.31
"Topotecan has limited activity in advanced head and neck cancer with this dose and schedule."	( Evaluation of topotecan in patients with recurrent for metastatic squamous cell carcinoma of the head and neck. A phase II Southwest Oncology Group study. Ensley, JF; Lew, D; Rodriguez, GI; Schuller, D; Smith, RE; Taylor, SA, 1996)	1.38
"Topotecan has significant activity in SCLC, particularly in patients sensitive to prior chemotherapy, with predictable and manageable toxicity. "	( Topotecan, a new active drug in the second-line treatment of small-cell lung cancer: a phase II study in patients with refractory and sensitive disease. The European Organization for Research and Treatment of Cancer Early Clinical Studies Group and New Dr Ardizzoni, A; Dombernowsky, P; Gamucci, T; Giaccone, G; Hansen, H; Kaplan, S; Postmus, P; Schaefer, B; Verweij, J; Wanders, J, 1997)	3.18
"Topotecan has efficacy at least equivalent to paclitaxel manifested by the higher response rate and significantly longer time to progression."	( Topotecan versus paclitaxel for the treatment of recurrent epithelial ovarian cancer. Bolis, G; Broom, C; Carmichael, J; Coleman, R; Davidson, N; Fields, SC; Gordon, A; Gore, M; Heron, JF; Hudson, I; Malfetano, J; Malmström, H; Scarabelli, C; Spanczynski, M; ten Bokkel Huinink, W, 1997)	3.18
"Topotecan also has activity in other tumor types, including small-cell lung cancer, hematologic malignancies and pediatric neuroblastoma and rhabdomyosarcoma."	( Clinical status and optimal use of topotecan. Arbuck, SG; Takimoto, CH, 1997)	1.3
"Topotecan has activity in refractory and relapsing multiple myeloma. "	( Evaluation of topotecan in resistant and relapsing multiple myeloma: a Southwest Oncology Group study. Alsina, M; Crowley, JJ; Kraut, EH; Laufman, LR; Salmon, SE; Taylor, SA; Wade, JL, 1998)	2.1
"Topotecan has demonstrated significant single-agent activity in MDS and CMML with generally manageable side effects."	( Topotecan in the treatment of hematologic malignancies. Beran, M; Kantarjian, H, 1998)	2.46
"Topotecan has been considered a promising agent for the adjuvant chemotherapy of human malignant glioma because of its novel mode of action, its activity against other solid tumors, and its good penetration across the blood-brain barrier. "	( Topotecan-based combination chemotherapy for human malignant glioma. Schabet, M; Schmidt, F; Schuster, M; Streffer, J; Weller, M, )	3.02
"Topotecan has limited, single agent activity in advanced NSCLC when given as 1."	( A randomized phase II trial of two schedules of topotecan for the treatment of advanced stage non-small cell lung cancer. Bate, WW; Grill, JP; Hatfield, AK; Jett, JR; Knost, JA; Marschke, RF; Schaefer, PL; Sloan, JA; Weitz, JJ; Zenk, DW, 2000)	1.28
"Topotecan has shown a strong anti-HIV effect, however, SmithKline Beecham is not interested in developing it for AIDS because of its toxicity. "	( Topotecan now available for HIV, PML research. , 1995)	3.18
"Topotecan treatment has resulted in minimum success fighting ovarian cancer, however, its toxic effects are dangerous and powerful."	( Topotecan and PML: the limits of pharmaceutical industry research. Learned, J, 1996)	2.46
"Topotecan has a positive influence on quality of life of patients with advanced colorectal cancer. "	( [Evaluation of quality of life in patients with advanced colorectal cancer treated with topotecan]. Brodziak, A; Bucior, J; Danikiewicz, A; Foltyn, W; Jastrzebska-Okoń, K; Knopik, J; Nowakowska-Zajdel, E; Ziółko, E, 2001)	1.98
"Topotecan has shown some clinical activity in UHCC using the 5 days every 3 weeks schedule but is limited by severe hematotoxicity."	( Combination of topotecan and oxaliplatin in inoperable hepatocellular cancer patients. Alexandre, J; Azoulay, D; Goldwasser, F; Gornet, JM; Gross-Goupil, M; Misset, JL; Romain, D; Tigaud, JM, 2002)	1.39

Excerpt	Reference	Relevance
"Topotecan may cause myelosuppression, which is noncumulative but tends to increase in direct correlation with the number of prior chemotherapy courses."	( Optimal sequencing in the treatment of recurrent ovarian cancer. Spriggs, D, 2003)	1.04

Excerpt	Reference	Relevance
"Topotecan treatment induced different patterns of the DNA response network in SCLC cells: DNA damage response (DDR) was more prominently activated in SLFN11-deficient SCLC cell line H82 than in SLFN11-plentiful SCLC cell line DMS273, whereas topotecan induced significant accumulation of p-Chk1, p-RPA2 and Rad51 in H82 cells, but not in DMS273 cells."	( FK228 potentiates topotecan activity against small cell lung cancer cells via induction of SLFN11. Cao, GZ; Hua, JH; Lin, WC; Lv, XT; Ma, LY; Yin, YP, 2022)	1.78
"Topotecan and OL9-119 treatment elicited significantly fewer DEGs in WT cells and negligible DEGs in PARP1-KO cells."	( Transcriptomic Analysis of CRISPR/Cas9-Mediated PARP1-Knockout Cells under the Influence of Topotecan and TDP1 Inhibitor. Dyrkheeva, NS; Kabilov, MR; Khodyreva, SN; Lavrik, OI; Luzina, OA; Malakhova, AA; Medvedev, SP; Nushtaeva, AA; Okorokova, LS; Pavlova, SV; Salakhutdinov, NF; Shtokalo, DN; Tupikin, AE; Zakharenko, AL; Zakian, SM, 2023)	1.85
"Topotecan, an approved treatment for refractory or recurrent ovarian cancer, has clinical limitations such as rapid clearance and hematologic toxicity. "	( FF-10850, a Novel Liposomal Topotecan Achieves Superior Antitumor Activity via Macrophage- and Ammonia-Mediated Payload Release in the Tumor Microenvironment. Kemmochi, S; Kimura, T; Makita-Suzuki, K; Matulonis, UA; Mori, M; Morohashi, Y; Nakayama, S; Okada, K; Shimoyama, S, 2023)	2.65
"Topotecan-treated murine ovarian (MOSEC), colorectal (CT26), and lung (LLC) cancer cell lines displayed upregulated CDKN1A encoding p21 and downregulated Ezh2."	( Identification of key genes and pathways associated with topotecan treatment using multiple bioinformatics tools. Chao, Y; Hsu, KM; Huang, YH; Kang, YM; Lan, A; Lan, KL, 2020)	1.52
"Topotecan-treated cells showed an impaired mammosphere formation capacity in vitro and reduced tumorigenicity in immunodeficient mice."	( Topotecan-induced ABCG2 expression in MCF-7 cells is associated with decreased CD24 and EpCAM expression and a loss of tumorigenicity. Bernhardt, G; Brockhoff, G; Buschauer, A; Huber, S; Wege, AK, 2015)	2.58
"Two topotecan treatment schedules in patients with recurrent epithelial ovarian cancer were evaluated. "	( Analysis of two topotecan treatment schedules in patients with recurrent ovarian cancer. Ben-Harim, Z; Bruchim, I; Fishman, A; Haran, G; Piura, E, 2016)	1.34
"Upon topotecan treatment WRN deficient cells showed enhanced DNA replication inhibition and S-phase arrest, whereas after treatment with etoposide they showed the same cell cycle response as the wild-type."	( WRN protects against topo I but not topo II inhibitors by preventing DNA break formation. Bohr, VA; Christmann, M; Gestrich, C; Kaina, B; Roos, WP; Tomicic, MT, 2008)	0.8
"Topotecan treatment was given (i) before, (ii) after or (iii) simultaneously with [(131)I]MIBG."	( Experimental treatment of neuroblastoma using [131I]meta-iodobenzylguanidine and topotecan in combination. Babich, JW; Boyd, M; Gaze, MN; Mairs, RJ; McCluskey, AG; Pimlott, SL, 2008)	1.29
"topotecan. Non-drug treatment costs accounted for an additional 1097 pounds for oral topotecan and 4289 pounds for i.v."	( The clinical effectiveness and cost-effectiveness of topotecan for small cell lung cancer: a systematic review and economic evaluation. Bird, A; Clegg, A; Harris, P; Hartwell, D; Jones, J; Loveman, E; Welch, K, 2010)	1.33
"Topotecan treatment reduced GFP(+) cells about 10-fold and recruited progenitors by about 80-fold while providing a significant survival advantage that improved with greater treatment duration."	( Convection-enhanced delivery of topotecan into a PDGF-driven model of glioblastoma prolongs survival and ablates both tumor-initiating cells and recruited glial progenitors. Assanah, MC; Bruce, JN; Canoll, P; Gil, OD; Kangarlu, A; Linskey, K; Lopez, KA; Tannenbaum, AM; Yun, J, 2011)	1.37
"Upon topotecan treatment, topo I was degraded in wild-type but not in p53-deficient cells."	( Topotecan-triggered degradation of topoisomerase I is p53-dependent and impacts cell survival. Christmann, M; Kaina, B; Tomicic, MT, 2005)	2.23
"Topotecan treatment resulted in the formation of some ulcerative lesions in the lingual mucosa especially on the lower surface of the tongue."	( Effects of topotecan treatment on nasal, buccal, and lingual mucosa in the rabbit: light and transmission electron microscopic evaluation. Bayar Muluk, N; Cakar, AN; Kaymaz, FF, 2007)	1.45
"Topotecan or 90Y-BrE3 treatment alone delayed overall tumor growth rate transiently but did not affect survival."	( Radiosensitization of tumor-targeted radioimmunotherapy with prolonged topotecan infusion in human breast cancer xenografts. Blank, E; Ceriani, R; Furmanski, P; Hochster, H; Kramer, E; Liebes, L; Ng, B; Wasserheit, C, 2001)	1.27
"Topotecan treatment has resulted in minimum success fighting ovarian cancer, however, its toxic effects are dangerous and powerful."	( Topotecan and PML: the limits of pharmaceutical industry research. Learned, J, 1996)	2.46
"Treatment with topotecan, etoposide and cisplatin caused significant changes in the expression patterns of OATP4A1, OATP5A1, OATP6A1, chromogranin and synaptophysin."	( Specific expression of OATPs in primary small cell lung cancer (SCLC) cells as novel biomarkers for diagnosis and therapy. Ausch, C; Bajna, E; Brenner, S; Buxhofer-Ausch, V; Hamilton, G; Jäger, W; Klameth, L; Reiner, A; Riha, J; Schölm, M; Thalhammer, T, 2015)	0.76
"The treatment of Topotecan (TPT) on gastric cancer (GC) is limited by its toxicity and the potential drug resistance."	( Synergistic combination of DT-13 and topotecan inhibits human gastric cancer via myosin IIA-induced endocytosis of EGF receptor in vitro and in vivo. Du, HZ; Feng, SY; Li, RM; Lin, S; Luo, XJ; Qian, CM; Sun, L; Yu, BY; Yu, XW; Yuan, ST; Zhang, LY; Zhao, RP, 2016)	1.04
"The treatment was topotecan (oral or intravenous, i.v.) compared with one another, best supportive care (BSC) or other chemotherapy regimens."	( The clinical effectiveness and cost-effectiveness of topotecan for small cell lung cancer: a systematic review and economic evaluation. Bird, A; Clegg, A; Harris, P; Hartwell, D; Jones, J; Loveman, E; Welch, K, 2010)	0.93
"Treatment with topotecan was initiated when the tumors reached a volume between 50 and 80 mm(3)."	( Successful therapy of subcutaneously growing human hepatoblastoma xenografts with topotecan. Fuchs, J; Gratz, KF; Mildenberger, H; von Schweinitz, D; Warmann, SW; Wilkens, L, 2001)	0.88

Excerpt	Reference	Relevance
" Potentiation of cytotoxicity was obtained at concentrations of NU1025 and NU1085 that were not toxic per se; however, NU1085 alone was 3-fold more cytotoxic (LC50 values ranged from 83 to 94 microM) than NU1025 alone (LC50 > 900 microM)."	( Potentiation of temozolomide and topotecan growth inhibition and cytotoxicity by novel poly(adenosine diphosphoribose) polymerase inhibitors in a panel of human tumor cell lines. Calvert, AH; Curtin, NJ; Delaney, CA; Durkacz, BW; Hostomsky, Z; Kyle, S; Newell, DR; Wang, LZ; White, AW, 2000)	0.59
" Hematologic toxicity has been the predominant side effect associated with its use."	( Nursing considerations for managing topotecan-related hematologic side effects. Anastasia, PJ, )	0.41
" 9-aminocamptothecin glucuronide was 25-60 times less toxic than 9-aminocamptothecin to five human cancer cell lines."	( Anti-tumour activity and toxicity of the new prodrug 9-aminocamptothecin glucuronide (9ACG) in mice. Chen, BM; Chern, JW; Leu, YL; Prijovich, ZM; Roffler, SR, 2002)	0.31
" Moreover, toxicity is observed earlier than the therapeutic effect, so, toxic effects represent a major endpoint for pharmacodynamic studies of cytotoxic drugs."	( Toxicity patterns of cytotoxic drugs. Canal, P; Chatelut, E; Delord, JP, 2003)	0.32
" Hematologic adverse events were significant, with 16 of 22 patients developing grade IV neutropenia; however, there were no septic deaths."	( Topotecan in patients with advanced neuroendocrine tumors: a phase II study with significant hematologic toxicity. Ansell, SM; Green, EM; Mahoney, MR; Rubin, J, 2004)	1.77
" The most frequent non-haematological adverse experiences of all grades per patient were nausea (T/C: 43."	( A randomised phase II study of the efficacy and safety of intravenous topotecan in combination with either cisplatin or etoposide in patients with untreated extensive disease small-cell lung cancer. Breton, JL; Cardenal, F; Gervais, R; Lymboura, M; Mattson, K; Preston, A; Quoix, E; Ross, G; Schramel, F; Wilson, J, 2005)	0.56
"To compare the therapeutic and toxic profile of topotecan given intraperitoneally with intravenously in human ovarian cancer xenografted into athymic nude mice."	( Comparison of efficacy and toxicity profile between intraperitoneal and intravenous topotecan in human ovarian cancer xenografts. Fan, SM; Feng, YJ; Yao, M; Yi, XF, 2006)	0.81
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."	( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling. Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004)	0.32
" Many patients with recurrent cancer may be predisposed to treatment-related adverse events because of advanced age, renal impairment or extensive prior therapy."	( Safety of topotecan in the treatment of recurrent small-cell lung cancer and ovarian cancer. Garst, J, 2007)	0.74
"To evaluate the therapeutic and adverse effects of topotecan combined with cisplatin in the treatment of advanced squamous cell lung cancer and head and neck cancer."	( [Therapeutic and adverse effects of topotecan combined with cisplatin for treatment of advanced squamous cell lung cancer and head and neck cancer]. Li, QY; Shao, JH; Xiang, Y; Yang, JZ, 2008)	0.87
" The major adverse effects were bone marrow suppression and alopecia."	( [Therapeutic and adverse effects of topotecan combined with cisplatin for treatment of advanced squamous cell lung cancer and head and neck cancer]. Li, QY; Shao, JH; Xiang, Y; Yang, JZ, 2008)	0.62
"Topotecan combined with cisplatin may achieve a favorable response in patients with advanced squamous cell lung cancer and head and neck cancer, and causes tolerable adverse effect without accumulative toxicity."	( [Therapeutic and adverse effects of topotecan combined with cisplatin for treatment of advanced squamous cell lung cancer and head and neck cancer]. Li, QY; Shao, JH; Xiang, Y; Yang, JZ, 2008)	2.06
" Nine significant adverse events (all hematologic) were topotecan related."	( A phase I study to characterize the safety, tolerability, and pharmacokinetics of topotecan at 4 mg/m2 administered weekly as a 30-minute intravenous infusion in patients with cancer. Borad, MJ; Curtis, KK; Fitch, TR; Griffin, PP; Hartney, JT; Jewell, RC; Lebowitz, PF; Northfelt, DW; Park, JW, 2010)	0.83
" The aim of this trial was to define the daily dose and treatment duration, which permits safe toxicity."	( Myelotoxicity of oral topotecan in relation to treatment duration and dosage: a phase I study. Anagnostopoulos, A; Antoniou, D; Ardavanis, A; Athanasiadis, A; Koutantos, J; Papadopoulos, G; Papakotoulas, P; Pectasides, D; Stathopoulos, GP; Trafalis, D; Vaslamatzis, M, 2010)	0.68
" The most common adverse events (AEs) included fatigue and gastrointestinal events."	( Safety and tolerability of the poly(ADP-ribose) polymerase (PARP) inhibitor, olaparib (AZD2281) in combination with topotecan for the treatment of patients with advanced solid tumors: a phase I study. Carmichael, J; Cassidy, J; Macpherson, E; Ranson, M; Samol, J; Scott, E; Thomas, A, 2012)	0.59
"The aim of this study was to determine the dose of weekly oral topotecan that allows safe administration and to evaluate the pharmacokinetics of this dose in patients with recurrent gynecologic malignancies."	( Toxicity of weekly oral topotecan in relation to dosage for gynecologic malignancies: a phase I study. DeBernardo, RL; Eaton, SM; Frasure, HE; Fusco, NL; Heugel, AM; Smith, DA; von Gruenigen, VE; Waggoner, SE, 2012)	0.93
" The worst reported adverse events (AEs) were grade 1/2 in 11 (22%) patients and grade 3/4/5 in 39 (78%) patients."	( Efficacy and safety of oral topotecan and bevacizumab combination as second-line treatment for relapsed small-cell lung cancer: an open-label multicenter single-arm phase II study. Bhatt, K; Lane, S; Legenne, P; Spigel, DR; Waterhouse, DM, 2013)	0.68
" The two-year event-free survival after complete remission was recorded and the chemotherapy-related toxicities were evaluated according to the Common Terminology Criteria for Adverse Events of the National Cancer Institute."	( Topotecan plus cyclophosphamide as maintenance chemotherapy for children with high-risk neuroblastoma in complete remission: short-term curative effects and toxicity. Feng, C; Liu, Y; Tang, S; Wang, J; Yang, G, 2013)	1.83
"Topotecan plus cyclophosphamide for maintenance chemotherapy can be effective and relative safe for stage IV neuroblastoma in complete remission, thus giving a chance to those patients who choose not to have stem cell transplantation."	( Topotecan plus cyclophosphamide as maintenance chemotherapy for children with high-risk neuroblastoma in complete remission: short-term curative effects and toxicity. Feng, C; Liu, Y; Tang, S; Wang, J; Yang, G, 2013)	3.28
" The most common adverse events with grade 3 or 4 were neutropenia in 13 patients (56."	( Safety of topotecan monotherapy for relapsed small cell lung cancer patients with pre-existing interstitial lung disease. Enomoto, Y; Hasegawa, H; Imokawa, S; Inui, N; Karayama, M; Matsui, T; Ozawa, Y; Suda, T; Yokomura, K, 2015)	0.82
" We, therefore, investigated the cellular toxic effects of melphalan, topotecan and carboplatin on the RPE in a cell culture model."	( Toxic effects of melphalan, topotecan and carboplatin on retinal pigment epithelial cells. Aisenbrey, S; Hagemann, U; Januschowski, K; Schnichels, S; Schrader, M; Süsskind, D, 2016)	0.96
"Morphological monitoring and toxicity assays indicate a direct toxic effect of melphalan and the other two cytostatic drugs on ARPE19 cells."	( Toxic effects of melphalan, topotecan and carboplatin on retinal pigment epithelial cells. Aisenbrey, S; Hagemann, U; Januschowski, K; Schnichels, S; Schrader, M; Süsskind, D, 2016)	0.73
" In both cohorts, disease progression was the most common primary reason for discontinuing pertuzumab, and the most common all-grade adverse events (AEs) were fatigue/asthenia, anemia, and diarrhea."	( Pertuzumab Plus Chemotherapy for Platinum-Resistant Ovarian Cancer: Safety Run-in Results of the PENELOPE Trial. Bastiere-Truchot, L; Berton-Rigaud, D; Colombo, N; Del Campo, JM; du Bois, A; Gadducci, A; García, Y; González-Martín, A; Kiermaier, A; Kurzeder, C; Mahner, S; Marmé, F; Martin, N; Ortega, E; Ottevanger, P; Pautier, P; Rau, J; Selle, F, 2016)	0.43
" However, there was no excess of other adverse events of specific interest for bevacizumab, including venous thromboembolic events, in older patients."	( Safety and efficacy of single-agent bevacizumab-containing therapy in elderly patients with platinum-resistant recurrent ovarian cancer: Subgroup analysis of the randomised phase III AURELIA trial. Coeffic, D; García, Y; Gebski, V; Gibbs, E; González-Martín, A; Hilpert, F; Huizing, M; Kaern, J; Kristensen, G; Lee, CK; Levaché, CB; Lück, HJ; Pujade-Lauraine, E; Roemer-Becuwe, C; Sorio, R; Witteveen, P; Zagouri, F, 2017)	0.46
"A monocentric comparative before/after study was carried out in an oncology day hospital to evaluate the efficacy of Safe Infusion Devices in reducing drug exposure compared to usual infusion practices."	( Evaluation of a safe infusion device on reducing occupational exposure of nurses to antineoplastic drugs: a comparative prospective study. Contamoins-1. Blanc, E; Bouleftour, W; Forges, F; Guitton, J; Hugues, M; Macé, A; Macron, C; Menguy, S; Raymond, B; Simoëns, X; Tinquaut, F, 2021)	0.62
"3% of contaminated samples while Safe Infusion Devices to a rate of 15%: Safe Infusion Devices reduced the risk of gloves contamination by 85% in multivariate analysis (Odds ratio = 0."	( Evaluation of a safe infusion device on reducing occupational exposure of nurses to antineoplastic drugs: a comparative prospective study. Contamoins-1. Blanc, E; Bouleftour, W; Forges, F; Guitton, J; Hugues, M; Macé, A; Macron, C; Menguy, S; Raymond, B; Simoëns, X; Tinquaut, F, 2021)	0.62
"Despite the current practice of using neutral solvent-purged infusers, the occupational exposure remains high for nurses and Safe Infusion Devices significantly reduced this risk of exposure."	( Evaluation of a safe infusion device on reducing occupational exposure of nurses to antineoplastic drugs: a comparative prospective study. Contamoins-1. Blanc, E; Bouleftour, W; Forges, F; Guitton, J; Hugues, M; Macé, A; Macron, C; Menguy, S; Raymond, B; Simoëns, X; Tinquaut, F, 2021)	0.62
" Four weekly intravitreal injections of topotecan up to 50 μg in the animal model or a 100 μg human equivalent dose were not toxic for the rabbit eye."	( Ocular and systemic toxicity of high-dose intravitreal topotecan in rabbits: Implications for retinoblastoma treatment. Abramson, DH; Cancela, B; Chantada, G; Clausse, M; Del Río, M; Del Sole, MJ; Francis, JH; Lamas, G; Lubieniecki, F; Nejamkin, P; Schaiquevich, P, 2022)	1.24
"The objective of this study was to monitor and identify adverse events (AEs) associated with topotecan, a medication used for the treatment of solid tumors, in order to improve patient safety and guide medication usage."	( A real-world data analysis of topotecan in the FDA Adverse Event Reporting System (FAERS) database. Chen, M; Cui, W; Wan, Z; Yang, H; Zhang, X; Zhao, B, 2023)	1.42
" Among these reports, 1,896 were identified as primary suspected (PS) AEs related to topotecan, and 155 topotecan-related adverse drug reactions (ADRs) at the preferred terms (PTs) level were selected."	( A real-world data analysis of topotecan in the FDA Adverse Event Reporting System (FAERS) database. Chen, M; Cui, W; Wan, Z; Yang, H; Zhang, X; Zhao, B, 2023)	1.42
"This study identified new and unexpected signals of adverse drug reactions (ADRs) related to topotecan, providing valuable insights into the relationship between ADRs and topotecan usage."	( A real-world data analysis of topotecan in the FDA Adverse Event Reporting System (FAERS) database. Chen, M; Cui, W; Wan, Z; Yang, H; Zhang, X; Zhao, B, 2023)	1.42

Excerpt	Reference	Relevance
" The plasma concentration-time curves were not compatible with standard linear pharmacokinetic models, and indications were found for the occurrence of nonlinear (saturation) kinetics at the dosages studied."	( Phase I clinical and pharmacokinetic study of topotecan administered by a 24-hour continuous infusion. Beijnen, JH; Davies, BE; Koier, I; Maes, RA; Rodenhuis, S; Rosing, H; ten Bokkel Huinink, WW; van Warmerdam, LJ, 1995)	0.55
" We performed a pharmacokinetic study as part of a phase I study in patients with various types of solid tumors, where topotecan was administered in a 30-min infusion daily on 5 consecutive days every 3 weeks."	( Pharmacokinetics and pharmacodynamics of topotecan administered daily for 5 days every 3 weeks. Beijnen, JH; Davies, BE; de Boer-Dennert, M; Maes, RA; Rosing, H; Schellens, JH; van Warmerdam, LJ; Verweij, J, 1995)	0.77
"To determine the feasibility of escalating the hydrophilic topoisomerase I (topo I)-inhibitor topotecan (TPT) above myelosuppressive doses in adults with refractory or relapsed acute leukemias and to assess pharmacodynamic determinants of TPT action."	( Phase I and pharmacodynamic study of the topoisomerase I-inhibitor topotecan in patients with refractory acute leukemia. Adjei, A; Burke, PJ; Cheng, YC; Donehower, RC; Gore, SD; Grochow, LB; Jones, RJ; Kaufmann, SH; Rowinsky, EK, 1994)	0.74
" Early human studies showed that topotecan (the active lactone) had a short half-life in plasma."	( Phase I/pharmacokinetic study of topotecan by 24-hour continuous infusion weekly. Brennan, JM; Haas, NB; Hudes, GR; LaCreta, FP; O'Dwyer, PJ; Ozols, RF; Walczak, J, 1994)	0.85
" In all cases, considerable effort has gone into detailed pharmacokinetic studies conducted before and during the clinical phase I studies."	( Pharmacokinetics and early clinical studies of selected new drugs. Cassidy, J; Graham, MA; Jodrell, D; Kaye, SB; Workman, P, 1993)	0.29
"The models were developed and validated using 34 pharmacokinetic curves in 19 patients who participated in a phase I study."	( Limited sampling models for topotecan pharmacokinetics. Beijnen, JH; Maes, RA; Rosing, H; Schellens, JH; van Warmerdam, LJ; Verweij, J, 1994)	0.58
" Half-life values could not be predicted with acceptable precision and accuracy."	( Limited sampling models for topotecan pharmacokinetics. Beijnen, JH; Maes, RA; Rosing, H; Schellens, JH; van Warmerdam, LJ; Verweij, J, 1994)	0.58
" This study was undertaken to better define the pharmacokinetic behavior of this highly unstable compound in both plasma and cerebrospinal fluid (CSF) and to measure the degree of CSF penetration of this novel antineoplastic agent."	( Plasma and cerebrospinal fluid pharmacokinetic study of topotecan in nonhuman primates. Balis, FM; Blaney, SM; Cole, DE; Godwin, K; Poplack, DG, 1993)	0.53
" A phase I and pharmacokinetic study was performed to determine the maximum tolerated dose (MTD) and dose-limiting toxicities, the incidence and severity of other toxicities, and the pharmacokinetics of topotecan in children."	( Pediatric phase I trial and pharmacokinetic study of topotecan administered as a 24-hour continuous infusion. Ames, MM; Balis, FM; Blaney, SM; Cole, DE; Craig, C; Hammond, D; Krailo, M; Poplack, DG; Reaman, G; Reid, JM, 1993)	0.72
"The purpose of this study was to describe the cerebrospinal fluid (CSF) penetration of topotecan in humans, to generate a pharmacokinetic model to simultaneously describe topotecan lactone and total concentrations in the plasma and CSF, and to characterize the CSF and plasma pharmacokinetics of topotecan administered as a continuous infusion (CI)."	( Cerebrospinal fluid pharmacokinetics and penetration of continuous infusion topotecan in children with central nervous system tumors. Baker, SD; Crom, WR; Gajjar, A; Heideman, RL; Kuttesch, JF; Stewart, CF, 1996)	0.75
" However, despite the large interpatient pharmacokinetic variability, the importance of regular drug monitoring on this schedule can be questioned, as the pharmacodynamic variability was relatively small."	( Pharmacokinetics and pharmacodynamics of topotecan given on a daily-times-five schedule in phase II clinical trials using a limited-sampling procedure. Beijnen, JH; Creemers, GJ; Davies, BE; de Boer-Dennert, M; Maes, RA; Rodenhuis, S; Rosing, H; Schellens, JH; ten Bokkel Huinink, WW; van Warmerdam, LJ; Verweij, J, 1996)	0.56
" The mean total body clearance of the lactone form is 30 L/h/m2, with a mean elimination half-life (t1/2 beta) of 3 hours; renal clearance accounts for approximately 40% of the administered dose with a large interindividual variability."	( Clinical pharmacokinetics of topotecan. Beijnen, JH; Herben, VM; ten Bokkel Huinink, WW, 1996)	0.59
" Pharmacokinetic studies were performed during the first infusion course."	( Phase I trial and pharmacokinetic (PK) and pharmacodynamics (PD) study of topotecan using a five-day course in children with refractory solid tumors: a pediatric oncology group study. Bell, B; Dryer, ZA; Grier, H; Kurtzberg, J; Pratt, CB; Santana, VM; Stewart, CF; Tubergen, DG; Vietti, TJ; Winick, N; Zamboni, WC, 1996)	0.52
" Using a limited sampling model, pharmacokinetic studies were performed in 36 of the 40 patients."	( Phase I trial and pharmacokinetic (PK) and pharmacodynamics (PD) study of topotecan using a five-day course in children with refractory solid tumors: a pediatric oncology group study. Bell, B; Dryer, ZA; Grier, H; Kurtzberg, J; Pratt, CB; Santana, VM; Stewart, CF; Tubergen, DG; Vietti, TJ; Winick, N; Zamboni, WC, 1996)	0.52
" The study also sought to identify pharmacodynamic (PD) determinants of both activity and toxicity."	( High-dose topotecan with granulocyte-colony stimulating factor in fluoropyrimidine-refractory colorectal cancer: a phase II and pharmacodynamic study. Baker, SD; Burks, K; Donehower, RC; Grochow, LB; O'Reilly, S; Rowinsky, EK, 1998)	0.7
" Plasma sampling with performed during course 1 to characterize the pharmacokinetic (PK) and PD behavior of TPT."	( High-dose topotecan with granulocyte-colony stimulating factor in fluoropyrimidine-refractory colorectal cancer: a phase II and pharmacodynamic study. Baker, SD; Burks, K; Donehower, RC; Grochow, LB; O'Reilly, S; Rowinsky, EK, 1998)	0.7
" A secondary objective was to measure the effect of prolonged topotecan infusion on topo-1 levels in peripheral blood mononuclear cells (PBMCs) as a pharmacodynamic end point."	( Effect of prolonged topotecan infusion on topoisomerase 1 levels: a phase I and pharmacodynamic study. Blum, RH; Chachoua, A; Hochster, H; Liebes, L; Oratz, R; Sorich, J; Speyer, J; Taubes, B; Wernz, J; Zeleniuch-Jacquotte, A, 1997)	0.86
" Pharmacokinetic analyses were performed at the recommended phase II dose."	( Phase I and pharmacokinetic study of intraperitoneal topotecan. Braly, PS; Christen, RD; Freddo, JL; Heath, D; Howell, SB; McClay, E; O'Quigley, J; Plaxe, SC, 1998)	0.55
" Pharmacokinetic analysis was performed in 55 patients using a validated high-performance liquid chromatographic assay and noncompartmental pharmacokinetic methods."	( A comparison of clinical pharmacodynamics of different administration schedules of oral topotecan (Hycamtin) Burris, H; Eckardt, JR; Gerrits, CJ; Hudson, I; Loos, WJ; Planting, AS; Rodriguez, GI; Schellens, JH; van Beurden, V; van der Burg, ME; Verweij, J; Von Hoff, DD, 1999)	0.53
" Weekly blood levels of topotecan and topoisomerase-1 (topo-1) levels in peripheral-blood mononuclear cells (PBMCs) were determined for pharmacodynamic correlation."	( Activity and pharmacodynamics of 21-Day topotecan infusion in patients with ovarian cancer previously treated with platinum-based chemotherapy. New York Gynecologic Oncology Group. Cohen, H; Hochster, H; Liebes, L; Runowicz, C; Sorich, J; Speyer, J; Taubes, B; Wadler, S; Wallach, R, 1999)	0.88
" Pharmacodynamic analysis demonstrated a statistically significant decrease in free PBMC topo-1 level at weeks 2 and 3 of drug administration."	( Activity and pharmacodynamics of 21-Day topotecan infusion in patients with ovarian cancer previously treated with platinum-based chemotherapy. New York Gynecologic Oncology Group. Cohen, H; Hochster, H; Liebes, L; Runowicz, C; Sorich, J; Speyer, J; Taubes, B; Wadler, S; Wallach, R, 1999)	0.57
" Pharmacodynamic studies demonstrate correlations between (1) the week of infusion and the PBMC topo-1 level, (2) the AUC of topotecan and the decrease in topo-1 levels, and (3) the change in topo-1 level and the neutrophil nadir."	( Activity and pharmacodynamics of 21-Day topotecan infusion in patients with ovarian cancer previously treated with platinum-based chemotherapy. New York Gynecologic Oncology Group. Cohen, H; Hochster, H; Liebes, L; Runowicz, C; Sorich, J; Speyer, J; Taubes, B; Wadler, S; Wallach, R, 1999)	0.78
" The population pharmacokinetic model was built in sequential manner, starting with a covariate-free model and progressing to a covariate model with the aid of generalized additive modeling."	( Population pharmacokinetic model for topotecan derived from phase I clinical trials. Baker, SD; Gallo, JM; Grochow, LB; Laub, PB; Rowinsky, EK, 2000)	0.58
" Four primary pharmacokinetic parameters (total clearance, volume of the central compartment, distributional clearance, and volume of the peripheral compartment) were related to various combinations of covariates."	( Population pharmacokinetic model for topotecan derived from phase I clinical trials. Baker, SD; Gallo, JM; Grochow, LB; Laub, PB; Rowinsky, EK, 2000)	0.58
"A population pharmacokinetic model for total topotecan has been developed that incorporates measures of body size and renal function to predict total clearance."	( Population pharmacokinetic model for topotecan derived from phase I clinical trials. Baker, SD; Gallo, JM; Grochow, LB; Laub, PB; Rowinsky, EK, 2000)	0.84
"The current practice for the dose calculation of most anticancer agents is based on body surface area in m2, although lower interpatient variation in pharmacokinetic parameters has been reported with pharmacokinetically guided administration."	( Pharmacokinetically guided administration of chemotherapeutic agents. Beijnen, JH; Mathôt, RA; Schellens, JH; van den Bongard, HJ, 2000)	0.31
"The inter- and intraindividual variabilities in topotecan clearance (CL) were explored using a population pharmacokinetic approach."	( Population pharmacokinetics of topotecan: intraindividual variability in total drug. Albin, N; Boucaud, M; Bugat, R; Canal, P; Chatelut, E; Culine, S; Déporte-Féty, R; Goupil, A; Laguerre, B; Lokiec, F; Montazeri, A; Pinguet, F, 2000)	0.85
"Gender-dependent differences in the clinical pharmacokinetic behavior of various drugs have been documented previously."	( Gender-dependent pharmacokinetics of topotecan in adult patients. Brouwer, E; de Jonge, MJ; Gelderblom, HJ; Loos, WJ; Sparreboom, A; Verweij, J, 2000)	0.58
"4 is an appropriate drug carrier for T-0128 regarding plasma half-life and passive tumor targeting."	( Carrier and dose effects on the pharmacokinetics of T-0128, a camptothecin analogue-carboxymethyl dextran conjugate, in non-tumor- and tumor-bearing rats. Harada, M; Murata, J; Okuno, S; Sakakibara, H; Sakamura, Y; Suzuki, T, 2001)	0.31
" A pharmacokinetic study was conducted to identify parameters related to the efficacy and toxicity of topotecan in our model."	( Schedule-dependent activity of topotecan in OVCAR-3 ovarian carcinoma xenograft: pharmacokinetic and pharmacodynamic evaluation. Bugat, R; Canal, P; Chatelut, E; Guichard, S; Hennebelle, I; Montazeri, A, 2001)	0.81
" During the first and the second courses of treatment, each patient underwent pharmacokinetic evaluation."	( Salivary and plasma pharmacokinetics of topotecan in patients with metastatic epithelial ovarian cancer. Astre, C; Boucaud, M; Bressolle, F; Culine, S; Cupissol, D; Pinguet, F; Poujol, S; Romieu, G, 2001)	0.58
"Fifteen patients with recurrent ovarian cancer in a phase I trial were treated with escalating IP topotecan doses (5-30 mg/m(2)) for pharmacokinetic analysis."	( A phase I and pharmacokinetic study of intraperitoneal topotecan. Aalders, JG; Beijnen, JH; Bos, AM; de Vries, EG; Hofstra, LS; Mulder, NH; Rosing, H; van der Zee, AG; Willemse, PH, 2001)	0.78
" A large intra-individual pharmacokinetic of topotecan between cycles 1 and 2 was also observed."	( No evidence that amifostine influences the plasma pharmacokinetics of topotecan in ovarian cancer patients. Malmström, H; Peterson, C; Zackrisson, AL, 2002)	0.81
"We designed a pharmacokinetic and pharmacodynamic phase I study of sequential topotecan (2."	( A phase I and pharmacodynamic study of sequential topotecan and etoposide in patients with relapsed or refractory acute myelogenous and lymphoblastic leukemia. Berger, SJ; Cooper, BW; Donaher, E; Gerson, SL; Gosky, DM; Green, SB; Hoppel, CL; Ingalls, ST; Lazarus, HM; Li, X; Rosenthal, NS, 2003)	0.8
" With the pharmacokinetic targeting approach, we observed that 78% (46 of 59) of the measured AUC values were within the target range."	( A pilot study of protracted topotecan dosing using a pharmacokinetically guided dosing approach in children with solid tumors. Gajjar, A; Houghton, PJ; Kirstein, MN; Liu, T; Santana, VM; Stewart, CF; Tan, M; Zamboni, WC, 2003)	0.61
"Protracted topotecan dosing using a pharmacokinetic strategy was possible in this heavily pretreated group of children."	( A pilot study of protracted topotecan dosing using a pharmacokinetically guided dosing approach in children with solid tumors. Gajjar, A; Houghton, PJ; Kirstein, MN; Liu, T; Santana, VM; Stewart, CF; Tan, M; Zamboni, WC, 2003)	1
" Topotecan pharmacokinetic analysis was performed in whole blood, plasma and RBCs."	( Red blood cells: a neglected compartment in topotecan pharmacokinetic analysis. Gelderblom, H; Loos, WJ; Nooter, K; Sparreboom, A; Stoter, G; van Boven-van Zomeren, DM; Verweij, J, 2003)	1.49
" The timing of the drug sequence was based on the prior Phase I pharmacokinetic and pharmacodynamic studies of camptothecin and etoposide, and the level of the TOP targets in peripheral blood monocytes."	( Sequencing topotecan and etoposide plus cisplatin to overcome topoisomerase I and II resistance: a pharmacodynamically based Phase I trial. Aisner, J; Beers, S; Locsin, S; Musanti, R; Rubin, EH; Smith, S, 2003)	0.71
" In conclusion, a population pharmacokinetic model for topotecan has been developed that incorporates measures of renal function and PS to predict CL."	( Factors affecting pharmacokinetic variability of oral topotecan: a population analysis. Bugat, R; Chatelut, E; Fourcade, J; Goffinet, M; Léger, F; Loos, WJ; Mathijssen, RH; Sparreboom, A; Verweij, J, 2004)	0.82
" Pharmacokinetic studies were conducted on day 1 to attain a topotecan lactone area under the plasma concentration-time curve (AUC) of 120 to 160 ng/mL."	( Results of a phase II upfront window of pharmacokinetically guided topotecan in high-risk medulloblastoma and supratentorial primitive neuroectodermal tumor. Ashley, D; Chintagumpala, M; Fouladi, M; Gajjar, A; Houghton, PJ; Iacono, LC; Kellie, SJ; Kirstein, MN; Seele, LG; Stewart, CF; Wallace, D; Zamboni, WC, 2004)	0.8
" The desired CSF topotecan exposure was achieved in seven of eight pharmacokinetic studies when the topotecan plasma AUC was within target range."	( Results of a phase II upfront window of pharmacokinetically guided topotecan in high-risk medulloblastoma and supratentorial primitive neuroectodermal tumor. Ashley, D; Chintagumpala, M; Fouladi, M; Gajjar, A; Houghton, PJ; Iacono, LC; Kellie, SJ; Kirstein, MN; Seele, LG; Stewart, CF; Wallace, D; Zamboni, WC, 2004)	0.9
"Fludarabine, carboplatin, topotecan regimen is a promising treatment based on potential pharmacodynamic interactions, which merits additional study in poor prognosis, acute leukemia patients."	( A phase I and pharmacodynamic study of fludarabine, carboplatin, and topotecan in patients with relapsed, refractory, or high-risk acute leukemia. Cooper, BW; Creger, RJ; Gerson, SL; Gosky, D; Hoppel, CL; Ingalls, ST; Koc, ON; Lazarus, HM; Meyerson, HJ; Nowell, GM; Pearson, G; Radivoyevitch, T; Tilby, MJ; Veal, GJ, 2004)	0.86
" To that end, a novel method, based on physiologically based hybrid pharmacokinetic models, is presented to predict human tumor drug concentrations."	( Pharmacokinetic model-predicted anticancer drug concentrations in human tumors. Bookman, MA; Gallo, JM; Guo, P; Li, S; Ma, J; Orlansky, A; Pulfer, S; Vicini, P; Zhou, F, 2004)	0.32
" The objective of the present study was to evaluate the potential for in vivo pharmacokinetic interactions by comparing the pharmacokinetics of topotecan (a model BCRP substrate) after oral administration of 2 mg/kg topotecan with and without different doses of the flavonoids chrysin or 7,8-benzoflavone (BF) in rats and mdr1a/1b (-/-) mice."	( Flavonoids chrysin and benzoflavone, potent breast cancer resistance protein inhibitors, have no significant effect on topotecan pharmacokinetics in rats or mdr1a/1b (-/-) mice. Morris, ME; Sagawa, K; Wang, X; Zhang, S, 2005)	0.74
" Topotecan plasma concentrations versus time were analyzed using a nonlinear mixed effect model according to a two-compartment pharmacokinetic model and a first-order conditional estimation method."	( Serum cystatin C is a better marker of topotecan clearance than serum creatinine. Canal, P; Chatelut, E; Delord, JP; Hoppe, A; Malard, L; Séronie-Vivien, S; Thomas, F, 2005)	1.51
"To develop and validate a pharmacokinetic limited sampling model (LSM) for intravenous and oral topotecan pharmacokinetic studies in children."	( Development and validation of limited sampling models for topotecan lactone pharmacokinetic studies in children. Daw, NC; Gajjar, A; Iacono, LC; Panetta, JC; Santana, VM; Stewart, CF; Turner, PK, 2006)	0.8
" Pharmacokinetic parameter estimates did not differ between the once a day and twice a day dosing groups."	( Pharmacokinetics, pharmacodynamics and adherence to oral topotecan in myelodysplastic syndromes: a Cancer and Leukemia Group B study. Grinblatt, DL; Hollis, D; Kastrissios, H; Klein, CE; Larson, RA; Miller, AA; Ratain, MJ; Rosner, GL; Yu, D, 2006)	0.58
" The optimal schedule cannot be determined from this study, as there was no evident relationship between any pharmacokinetic parameter and clinical response."	( Pharmacokinetics, pharmacodynamics and adherence to oral topotecan in myelodysplastic syndromes: a Cancer and Leukemia Group B study. Grinblatt, DL; Hollis, D; Kastrissios, H; Klein, CE; Larson, RA; Miller, AA; Ratain, MJ; Rosner, GL; Yu, D, 2006)	0.58
"The purpose of this study was to estimate ventricular cerebrospinal fluid (vCSF) topotecan lactone (TPT) exposures in pediatric medulloblastoma patients from plasma concentration-time data by using a pharmacokinetic (PK) model."	( Using plasma topotecan pharmacokinetics to estimate topotecan exposure in cerebrospinal fluid of children with medulloblastoma. Freeman, BB; Gajjar, A; Iacono, LC; Panetta, JC; Stewart, CF, 2006)	0.93
" The aim of this study was to evaluate qualitatively and quantitatively the influence of patient-specific characteristics on the neutrophil concentration-time course, to identify patient subgroups, and to compare covariates on system-related pharmacodynamic variable between drugs."	( Population pharmacokinetic-pharmacodynamic model for neutropenia with patient subgroup identification: comparison across anticancer drugs. Chatelut, E; Henningsson, A; Karlsson, MO; Kloft, C; Wallin, J, 2006)	0.33
", age) had minor (clinically irrelevant) influences but consistently shifted the pharmacodynamic variable in the same direction."	( Population pharmacokinetic-pharmacodynamic model for neutropenia with patient subgroup identification: comparison across anticancer drugs. Chatelut, E; Henningsson, A; Karlsson, MO; Kloft, C; Wallin, J, 2006)	0.33
" The disposition of TPT did not normalize in UN-ARF rats when treated with caffeine, a non-selective adenosine A1 receptor antagonist, whereas the selective adenosine A1 receptor antagonist (1,3-dipropyl-8-phenylxanthine, DPPX) normalized TPT pharmacokinetic disposition by improving renal function."	( Altered intravenous pharmacokinetics of topotecan in rats with acute renal failure (ARF) induced by uranyl nitrate: do adenosine A1 antagonists (selective/non-selective) normalize the altered topotecan kinetics in ARF? Mullangi, R; Mustafa, S; Pasha, K; Srinivas, NR; Venkatesh, P, 2006)	0.6
"A two-compartment model was fit to topotecan lactone plasma concentrations (n = 1874), and large pharmacokinetic variability was observed among studies, among individuals, and within individuals."	( Population pharmacokinetic analysis of topotecan in pediatric cancer patients. Freeman, BB; Gajjar, A; Iacono, LC; Panetta, JC; Santana, VM; Schaiquevich, P; Stewart, CF, 2007)	0.89
"We developed a descriptive and robust population pharmacokinetic model which identified patient covariates that account for topotecan disposition in pediatric patients."	( Population pharmacokinetic analysis of topotecan in pediatric cancer patients. Freeman, BB; Gajjar, A; Iacono, LC; Panetta, JC; Santana, VM; Schaiquevich, P; Stewart, CF, 2007)	0.82
"Pharmacokinetic and pharmacodynamic data were obtained from a phase II study for pediatric patients with high-risk neuroblastoma."	( Using pharmacokinetic and pharmacodynamic modeling and simulation to evaluate importance of schedule in topotecan therapy for pediatric neuroblastoma. Panetta, JC; Santana, VM; Schaiquevich, P; Stewart, CF, 2008)	0.56
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."	( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Lombardo, F; Obach, RS; Waters, NJ, 2008)	0.35
" Based on pharmacokinetic theory that suggests that penetration depth is primarily determined by the rate of drug removal via tumor capillaries, we have hypothesized that co-administration of antiangiogenic therapy will allow for decreased drug removal, increased drug concentrations in tumor, and increased efficacy of intraperitoneal chemotherapy."	( Use of an anti-vascular endothelial growth factor antibody in a pharmacokinetic strategy to increase the efficacy of intraperitoneal chemotherapy. Balthasar, JP; Bernacki, RJ; Shah, DK; Shin, BS; Tóth, K; Veith, J, 2009)	0.35
" Other pharmacodynamic factors than the ones investigated must explain the schedule-dependent differences in toxicities."	( Phase I pharmacokinetic and pharmacodynamic study of Carboplatin and topotecan administered intravenously every 28 days to patients with malignant solid tumors. Beijnen, JH; Boss, DS; Pluim, D; Rosing, H; Schellens, JH; Siegel-Lakhai, WS; Ten Bokkel Huinink, WW; van Egmond-Schoemaker, NE, 2009)	0.59
" Pharmacokinetic studies, together with the expression analysis of mRNA for enzymes involved in delimotecan metabolism, showed that T-2513 and other cytotoxic metabolites of delimotecan (SN 38 and T-0055) are generated in greater quantities in the tumor tissue than in toxicity target tissues, such as liver, thus accounting for the antitumoral activity."	( Antitumor activity of delimotecan against human metastatic melanoma: pharmacokinetics and molecular determinants. Animati, F; Bellarosa, D; Bigioni, M; Binaschi, M; Bressan, A; Bugianesi, R; Crea, A; Maggi, CA; Manzini, S; Parlani, M; Rivoltini, L, 2009)	0.35
" Topotecan pharmacokinetic parameters were determined in vitreous, aqueous and plasma using a compartmental analysis."	( Pharmacokinetic analysis of topotecan after intra-vitreal injection. Implications for retinoblastoma treatment. Abramson, DH; Bramuglia, GF; Buitrago, E; Chantada, G; Fandiño, A; Höcht, C; Navo, E; Schaiquevich, P, 2010)	1.56
" In this article, we have developed a physiologically based pharmacokinetic model to characterize and predict topotecan concentrations in mouse plasma and tissues."	( Physiologically based pharmacokinetic model for topotecan in mice. Balthasar, JP; Shah, DK, 2011)	0.84
" Topotecan pharmacokinetic analyses were carried out, and topoisomerase I levels and activity were measured."	( Phase I Study of Topotecan, Ifosfamide, and Etoposide (TIME) with autologous stem cell transplant in refractory cancer: pharmacokinetic and pharmacodynamic correlates. Dawson, JL; Field, TL; Fields, KK; Goldstein, SC; Kim, J; Lush, RM; Maddox, BL; Neuger, AM; Partyka, JS; Perkins, JB; Simonelli, CE; Sullivan, DM, 2011)	1.62
" Pharmacokinetic monitoring may be a valuable tool for optimizing the use of topotecan and to avoid toxicity seen with high-systemic exposures."	( Phase I Study of Topotecan, Ifosfamide, and Etoposide (TIME) with autologous stem cell transplant in refractory cancer: pharmacokinetic and pharmacodynamic correlates. Dawson, JL; Field, TL; Fields, KK; Goldstein, SC; Kim, J; Lush, RM; Maddox, BL; Neuger, AM; Partyka, JS; Perkins, JB; Simonelli, CE; Sullivan, DM, 2011)	0.94
" Topotecan dosing based on simultaneous drug monitoring and pharmacokinetic analysis can yield more accurate and precise estimation of the topotecan systemic exposure than that attainable with the fixed dosing approach."	( Topotecan exposure estimation in pediatric acute myeloid leukemia supported by LC-MS-based drug monitoring and pharmacokinetic analysis. Adamkiewicz-Drożyńska, E; Bączek, T; Balcerska, A; Belka, M; Konieczna, L; Maciejka-Kapuścińska, L; Niedźwiecki, M; Wachowiak, J; Wiśniewski, J, 2012)	2.73
"We performed a phase-1 pharmacokinetic optimal dosing study of intraventricular topotecan (IT), administered daily 5×, to determine whether, the maximum tolerated dose of IT topotecan was also the pharmacokinetic optimal dose."	( A phase-1 pharmacokinetic optimal dosing study of intraventricular topotecan for children with neoplastic meningitis: a Pediatric Brain Tumor Consortium study. Berg, SL; Blaney, SM; Boyett, J; Goldman, S; Gururangan, S; Kieran, MW; Kun, L; Onar-Thomas, A; Scorsone, K; Stewart, C; Su, J; Tagen, M, 2013)	0.85
" Pharmacokinetic evaluation after accrual of the first seven patients revealed that a topotecan lactone concentration >1 ng/ml for 8 hours was attained in all patients and thus, further dose escalation was not pursued."	( A phase-1 pharmacokinetic optimal dosing study of intraventricular topotecan for children with neoplastic meningitis: a Pediatric Brain Tumor Consortium study. Berg, SL; Blaney, SM; Boyett, J; Goldman, S; Gururangan, S; Kieran, MW; Kun, L; Onar-Thomas, A; Scorsone, K; Stewart, C; Su, J; Tagen, M, 2013)	0.85
"2 mg, administered daily for 5 days with concomitant dexamethasone is well tolerated and was defined to be the pharmacokinetic optimal dose in this trial."	( A phase-1 pharmacokinetic optimal dosing study of intraventricular topotecan for children with neoplastic meningitis: a Pediatric Brain Tumor Consortium study. Berg, SL; Blaney, SM; Boyett, J; Goldman, S; Gururangan, S; Kieran, MW; Kun, L; Onar-Thomas, A; Scorsone, K; Stewart, C; Su, J; Tagen, M, 2013)	0.63
" By comparing the pharmacokinetic profiles of lipid vesicles and entrapped topotecan, it was found that "empty pegylated vesicles" be formed in circulation, which might be responsible for the occurrence of ABC phenomenon."	( Prolongation of time interval between doses could eliminate accelerated blood clearance phenomenon induced by pegylated liposomal topotecan. Cui, J; Li, C; Li, H; Tian, W; Wang, Y; Yang, H; Yang, J; Zhao, X, 2013)	0.82
" Both agents are substrates for ATP-binding cassette family transporters so there is an increased likelihood for pharmacokinetic (PK) drug-drug interactions."	( Combination metronomic oral topotecan and pazopanib: a pharmacokinetic study in patients with gynecological cancer. Harstead, KE; Stewart, CF; Throm, SL; Tillmanns, TD; Turner, DC, 2013)	0.68
"Oral topotecan (Hycamtin(®)) has been recently approved for the treatment of relapsed small cell lung cancer (SCLC) in 2007, however, the bioavailability and pharmacokinetic data of topotecan for Chinese patients is still limited."	( Oral topotecan: Bioavailability, pharmacokinetics and impact of ABCG2 genotyping in Chinese patients with advanced cancers. Du, P; Gui, L; Han, X; Li, N; Shen, Y; Shi, Y; Song, Y; Sun, Y; Wang, J; Wang, S; Yang, J, 2013)	1.42
"Single-center, prospective, clinical pharmacokinetic study."	( Clinical pharmacokinetics of intra-arterial melphalan and topotecan combination in patients with retinoblastoma. Buitrago, E; Ceciliano, A; Chantada, GL; Fandino, A; Lucena, E; Romero, L; Sampor, C; Schaiquevich, P; Taich, P; Villasante, F, 2014)	0.65
" Plasma samples were obtained for pharmacokinetic studies, and a population approach via nonlinear mixed effects modeling was used."	( Clinical pharmacokinetics of intra-arterial melphalan and topotecan combination in patients with retinoblastoma. Buitrago, E; Ceciliano, A; Chantada, GL; Fandino, A; Lucena, E; Romero, L; Sampor, C; Schaiquevich, P; Taich, P; Villasante, F, 2014)	0.65
"Melphalan and topotecan pharmacokinetic parameters and efficacy and safety parameters."	( Clinical pharmacokinetics of intra-arterial melphalan and topotecan combination in patients with retinoblastoma. Buitrago, E; Ceciliano, A; Chantada, GL; Fandino, A; Lucena, E; Romero, L; Sampor, C; Schaiquevich, P; Taich, P; Villasante, F, 2014)	1.01
" Concomitant topotecan administration did not influence melphalan pharmacokinetic parameters."	( Clinical pharmacokinetics of intra-arterial melphalan and topotecan combination in patients with retinoblastoma. Buitrago, E; Ceciliano, A; Chantada, GL; Fandino, A; Lucena, E; Romero, L; Sampor, C; Schaiquevich, P; Taich, P; Villasante, F, 2014)	1.02
" To this end, we analyze previously published mathematical models of neutropenia to identify a pharmacokinetic (PK) predictor of the neutrophil nadir, and confirm this PK predictor in an in vivo experimental system."	( Dose schedule optimization and the pharmacokinetic driver of neutropenia. Chakravarty, A; Mettetal, JT; Palani, S; Patel, M; Shyu, WC; Yang, J, 2014)	0.4
"A multicentre phase I toxicity and pharmacokinetic study of oral topotecan was conducted in patients with advanced solid tumours."	( Pharmacodynamics and pharmacokinetics of oral topotecan in patients with advanced solid tumours and impaired renal function. Bang, YJ; Beijnen, JH; Chung, HC; Dar, MM; Devriese, LA; Huitema, AD; Lewis, LD; Mendelson, DS; Mergui-Roelvink, M; Schellens, JH; Smith, DA; Voest, EE; Witteveen, PE, 2015)	0.91
" Therefore, this study aimed to determine the population pharmacokinetics of oral topotecan in infants and very young children, specifically evaluating the effects of age and ABCG2 and ABCB1 on the absorption rate constant (Ka), as well as other covariate effects on all pharmacokinetic parameters."	( Population Pharmacokinetics of Oral Topotecan in Infants and Very Young Children with Brain Tumors Demonstrates a Role of ABCG2 rs4148157 on the Absorption Rate Constant. Birg, AV; Broniscer, A; Daryani, VM; Gajjar, AJ; Lin, T; Panetta, JC; Roberts, JK; Robinson, GW; Stewart, CF, 2016)	0.93
"05 fold) conferred by TOPO NPs from the in vivo pharmacokinetic study."	( Formulation and optimization of topotecan nanoparticles: In vitro characterization, cytotoxicity, cellular uptake and pharmacokinetic outcomes. Iqbal, Z; Kapoor, R; Padhi, S; Panda, AK; Verma, D, 2018)	0.76
"We sought to examine the pharmacodynamic activation of the DNA damage response (DDR) pathway in tumors following anticancer treatment for confirmation of target engagement."	( Evaluation of Pharmacodynamic Responses to Cancer Therapeutic Agents Using DNA Damage Markers. Barrett, AM; Chen, A; Doroshow, JH; Dull, AB; Hollingshead, MG; Kinders, RJ; Kummar, S; Lawrence, SM; Parchment, RE; Wilsker, DF, 2019)	0.51
"Because of inherent biological variability, baseline DDR biomarker levels were evaluated in a colorectal cancer microarray to establish clinically relevant thresholds for pharmacodynamic activation."	( Evaluation of Pharmacodynamic Responses to Cancer Therapeutic Agents Using DNA Damage Markers. Barrett, AM; Chen, A; Doroshow, JH; Dull, AB; Hollingshead, MG; Kinders, RJ; Kummar, S; Lawrence, SM; Parchment, RE; Wilsker, DF, 2019)	0.51
" Based on in vivo results, pharmacokinetic properties, distribution in the body, and delivery efficiency of these formulated nanoparticles were confirmed."	( Oral delivery of topotecan in polymeric nanoparticles: Lymphatic distribution and pharmacokinetics. Jang, JH; Jeong, SH; Lee, YB, 2021)	0.96
" Here, we investigate the pharmacokinetic drug-drug interaction potential of trilaciclib."	( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer. Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022)	0.93
" Population pharmacokinetic modeling showed no significant effect of trilaciclib on topotecan clearance."	( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer. Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022)	1.15
" Samples were quantified by high-performance liquid chromatography, and population pharmacokinetic analysis was conducted using MonolixSuite."	( Pharmacokinetics of Orbital Topotecan After Ophthalmic Artery Chemosurgery and Intravenous Infusion in the Swine Model. Abramson, DH; Asprea, M; Chantada, G; Fandiño, A; Francis, JH; Lagomarsino, E; Opezzo, J; Requejo, F; Sampor, C; Schaiquevich, P; Vater, A, 2023)	1.2
"Topotecan, an antitumor drug with systemic exposure (SE)-dependent activity against many pediatric tumors has wide interpatient pharmacokinetic variability, making it challenging to attain the desired topotecan SE."	( Topotecan clearance based on a single sample and a population pharmacokinetic model: Application to a pediatric high-risk neuroblastoma clinical trial. Campagne, O; Daryani, VM; Gajjar, AJ; Naranjo, A; Park, JR; Stewart, CF; Wu, H; Wu, J, 2023)	3.8
"Our previous population pharmacokinetic and covariate model was updated using data from 13 clinical pediatric studies."	( Topotecan clearance based on a single sample and a population pharmacokinetic model: Application to a pediatric high-risk neuroblastoma clinical trial. Campagne, O; Daryani, VM; Gajjar, AJ; Naranjo, A; Park, JR; Stewart, CF; Wu, H; Wu, J, 2023)	2.35

Excerpt	Reference	Relevance
"The cytotoxic effects of various antimetabolites (fluorouracil, methotrexate, or cytarabine), antimicrotubule agents (vincristine or paclitaxel [Taxol]), DNA alkylating agents (melphalan, bis[chloroethyl]nitrosourea [BCNU], or 4-hydroperoxycyclophosphamide [4HC]), and a DNA-platinating agent (cisplatin), alone and in combination with TPT, were measured in clonogenic (i."	( Cytotoxic effects of topotecan combined with various anticancer agents in human cancer cell lines. Buckwalter, CA; Donehower, RC; Grochow, LB; Kaufmann, SH; Peereboom, D; Rowinsky, EK; Svingen, PA, 1996)	0.61
"TPT cytotoxicity appears to be enhanced more by combination with certain DNA-damaging agents than by combination with antimetabolites or antimicrotubule agents."	( Cytotoxic effects of topotecan combined with various anticancer agents in human cancer cell lines. Buckwalter, CA; Donehower, RC; Grochow, LB; Kaufmann, SH; Peereboom, D; Rowinsky, EK; Svingen, PA, 1996)	0.61
"Based on preclinical data that demonstrated synergy between alkylating agents and topoisomerase (topo) I poisons, we determined the maximum-tolerated dose (MTD) of topotecan, using a 5 day bolus schedule, that could be given in combination with a single, fixed dose of cyclophosphamide."	( Dose-escalation and pharmacodynamic study of topotecan in combination with cyclophosphamide in patients with refractory cancer. Anderson, S; Beidler, D; Belliveau, D; Burtness, BA; Cheng, YC; Fedele, J; Flynn, SD; Murren, JR; Pizzorno, G; Tocino, I; Zelterman, D, 1997)	0.75
"0 mg/ m2/d if it is administered with G-CSF."	( Dose-escalation and pharmacodynamic study of topotecan in combination with cyclophosphamide in patients with refractory cancer. Anderson, S; Beidler, D; Belliveau, D; Burtness, BA; Cheng, YC; Fedele, J; Flynn, SD; Murren, JR; Pizzorno, G; Tocino, I; Zelterman, D, 1997)	0.56
"To determine the maximum-tolerated dose (MTD) and dose-limiting toxicity of topotecan when combined with cyclophosphamide in pediatric patients with recurrent or refractory malignant solid tumors."	( Phase I study of topotecan in combination with cyclophosphamide in pediatric patients with malignant solid tumors: a Pediatric Oncology Group Study. Bell, B; Saylors, RL; Stewart, CF; Stine, KC; Vietti, TJ; Wall, DA; Zamboni, WC, 1998)	0.87
"The combination of topotecan and cyclophosphamide shows activity in a wide variety of pediatric solid tumors and can be given with acceptable hematopoietic toxicity with the use of filgrastim support."	( Phase I study of topotecan in combination with cyclophosphamide in pediatric patients with malignant solid tumors: a Pediatric Oncology Group Study. Bell, B; Saylors, RL; Stewart, CF; Stine, KC; Vietti, TJ; Wall, DA; Zamboni, WC, 1998)	0.97
" A previous Cancer and Leukemia Group B (CALGB) trial of topotecan, given on a daily bolus schedule in combination with cisplatin, produced more hematologic toxicity than expected with either drug alone."	( Phase I and pharmacologic study of continuous infusion topotecan in combination with cisplatin in patients with advanced cancer: a Cancer and LeukemiaGroup B study. Batist, G; Bernard, S; Egorin, MJ; Hollis, DR; Lilenbaum, RC; Miller, AA; Ratain, MJ; Rosner, GL; Schilsky, RL, 1998)	0.79
"Cisplatin can be given safely in combination with CIVI topotecan."	( Phase I and pharmacologic study of continuous infusion topotecan in combination with cisplatin in patients with advanced cancer: a Cancer and LeukemiaGroup B study. Batist, G; Bernard, S; Egorin, MJ; Hollis, DR; Lilenbaum, RC; Miller, AA; Ratain, MJ; Rosner, GL; Schilsky, RL, 1998)	0.79
" In conclusion, our findings further support the potential cytotoxic role of TPT in combination with other active drugs when the correct schedule of administration is applied."	( Cytotoxic effects of topotecan combined with various active G2/M-phase anticancer drugs in human tumor-derived cell lines. Abad, A; Guillot, M; Martin, C; Plasencia, C; Taron, M, 2000)	0.63
" The studies were conducted to evaluate the antitumor activity of MGI 114 as a single agent and in combination with topotecan against pediatric solid tumor cell lines and xenograft models."	( MGI 114: augmentation of antitumor activity when combined with topotecan. Barrera, H; Gonzalez, C; Hilsenbeck, S; MacDonald, JR; Marty, J; Moore, R; Von Hoff, D; Waters, SJ; Weitman, S, )	0.58
" In this study, the potential application of MGI 114 in the treatment of lung cancer was explored by evaluating the activity of MGI 114 in combination with either topotecan (TPT) or paclitaxel."	( Enhanced antitumour activity of 6-hydroxymethylacylfulvene in combination with topotecan or paclitaxel in the MV522 lung carcinoma xenograft model. Eckhardt, SG; Hammond, LA; Hilsenbeck, SG; MacDonald, JR; Mangold, G; Marty, J; Rowinsky, EK; Von Hoff, DD; Weitman, S, 2000)	0.73
" A phase I trial was initiated to identify the optimal sequence and maximum-tolerated dose of topotecan in combination with paclitaxel and carboplatin."	( Phase I dose escalation study of topotecan combined with alternating schedules of paclitaxel and carboplatin in advanced solid tumors. Cantrell, CL; Dunleavy, TL; Dunphy, FR; Harrison, BR; Petruska, PJ; Pincus, SM; Richart, JM; Visconti, JL, 2001)	0.81
"To define the dose-limiting toxicities (DLTs) and the maximum tolerated doses (MTDs) of topotecan in combination with epirubicin in pretreated patients with small-cell lung cancer (SCLC)."	( A dose escalation study of topotecan in combination with epirubicin in pretreated patients with small-cell lung cancer. Agelaki, S; Georgoulias, V; Kakolyris, S; Kalbakis, K; Kouroussis, C; Mavroudis, D; Palamidas, P; Raptis, A, 2001)	0.83
"This daily-times-3-day schedule of topotecan in combination with carboplatin is safe."	( A phase I/II study of topotecan in combination with carboplatin in recurrent epithelial ovarian cancer. Bolis, G; Guarnerio, P; Parazzini, F; Polverino, GP; Rosa, C; Scarfone, G; Sciatta, C, 2001)	0.9
" Survival was comparable to that of patients of other studies with secondary cytoreductive surgery in combination with chemotherapy."	( Adenovirus-mediated thymidine kinase gene therapy in combination with topotecan for patients with recurrent ovarian cancer: 2.5-year follow-up. Aguilar-Cordova, E; Fischer, DC; Hasenburg, A; Kaplan, AL; Kaufman, RH; Kieback, DG; Nyberg-Hoffman, C; Ramzy, I; Rojas-Martinez, A; Tong, XW, 2001)	0.54
"This study was designed to evaluate the efficacy and toxicity of topotecan hydrochloride, used singly or combined with other drugs in patients with recurrent advanced ovarian cancer."	( [Single topotecan or in combination with other chemotherapeutic agents for 18 recurrent advanced ovarian cancer patients]. Li, H; Liu, L; Zhang, W, 2001)	0.98
" Topotecan combined with cisplatin and taxol would be effective even if single topotecan has failed."	( [Single topotecan or in combination with other chemotherapeutic agents for 18 recurrent advanced ovarian cancer patients]. Li, H; Liu, L; Zhang, W, 2001)	1.66
"A mouse model of human ovarian cancer was used to investigate the effect of adenovirus-mediated thymidine kinase gene therapy (gt) in combination with chemotherapy."	( Intraperitoneal adenovirus-mediated suicide gene therapy in combination with either topotecan or paclitaxel in nude mice with human ovarian cancer. Aguilar-Cordova, E; Engehausen, DG; Fischer, DC; Kieback, DG; Oehler, MK; Sauerbrei, W; Tong, XW, 2002)	0.54
" As carboplatin is less nephrotoxic and increasingly replacing cisplatin in clinical practice, the aim of this study was to define the optimal sequence and dose for topotecan in combination with carboplatin."	( Topotecan in combination with carboplatin: phase I trial evaluation of two treatment schedules. Boddy, AV; Calvert, AH; Calvert, PM; Fishwick, K; Griffin, MJ; Ross, GA; Schätzlein, A; Simpson, AB; Sludden, JA; Twelves, CJ; Wheatley, A; Wilson, P, 2002)	1.95
" A pilot study of Mylotarg combined with topotecan and ara-C (MTA) was conducted in patients with refractory AML."	( Mylotarg combined with topotecan and cytarabine in patients with refractory acute myelogenous leukemia. Alvarez, R; Beran, M; Cortes, J; Estey, E; Giles, FJ; Kantarjian, H; Thomas, D; Tsimberidou, AM, 2002)	0.89
" This study was conducted to define the dose-limiting toxicities (DLTs) of its combination with cytarabine (ara-C), idarubicin, or topotecan."	( Randomized phase I/II study of troxacitabine combined with cytarabine, idarubicin, or topotecan in patients with refractory myeloid leukemias. Cortes, JE; Douer, D; Estey, EH; Faderl, S; Garcia-Manero, G; Giles, FJ; Jeha, SS; Kantarjian, HM; Koller, CA; Levine, AM; O'Brien, SM; Thomas, DA, 2003)	0.75
" Preclinical in vitro studies have shown synergism with ZD0473 in combination with several agents, including vinorelbine and topotecan."	( ZD0473 combined with other chemotherapeutic agents for the treatment of solid malignancies. Douillard, JY; Schiller, J, 2002)	0.52
" We report results from two open-label, multicentre, phase I and phase II trials, investigating the pharmacokinetics, tolerability and efficacy of ZD9331, when used in combination with topotecan in patients with relapsed or refractory tumours."	( ZD9331 in combination with topotecan: phase I and II experience. Benson, A; Poplin, E; Vergote, I, 2003)	0.81
"ZD9331, in combination with topotecan, showed manageable toxicity and some evidence of activity in patients with ovarian cancer."	( ZD9331 in combination with topotecan: phase I and II experience. Benson, A; Poplin, E; Vergote, I, 2003)	0.91
"A phase I study was performed to determine the maximum tolerated dose and the recommended dose of continuous intravenous infusion of topotecan in combination with radiotherapy (RT) in patients with previously untreated glioblastoma multiforme (GBM)."	( Phase I study of topotecan in combination with concurrent radiotherapy in adults with glioblastoma. Carsin, B; Gédouin, D; Guégan, Y; Hamlat, A; Hassel, MB; Lesimple, T; Malhaire, JP; Riffaud, L; Seigneuret, E; Simon, H, 2003)	0.86
" infusion compared to single doses, but this regimen has not yet been combined with oxaliplatin."	( Phase I/II trial of topotecan given as continuous infusion in combination with oxaliplatin in 5-FU-pretreated patients with colorectal cancer. Deckert, PM; Hütter, G; Keilholz, U; Szélenyi, H; Thiel, E, 2004)	0.65
"Topotecan and pegylated liposomal doxorubicin (Doxil) interact with topoisomerase I and II (topo I and II), respectively, with schedule dependent, and potentially synergistic cytotoxicity."	( Phase I trial of escalating doses of topotecan in combination with a fixed dose of pegylated liposomal doxorubicin in women with müllerian malignancies. Atkinson, T; Berkowitz, RS; Campos, SM; Fuller, AF; Goodman, A; Krasner, C; Lee, H; Matulonis, UA; Penson, RT; Seiden, MV, 2004)	2.04
"To determine maximum tolerated dose (MTD) and evidence of antitumor activity of topotecan in combination with gemcitabine in refractory cancer patients."	( Phase I trial of topotecan in combination with gemcitabine in refractory solid tumor patients. Adams, N; Cunningham, CC; MacEachern, JB; Nemunaitis, J; Paulson, AS; Rich, D; Ruxer, RL; Vukelja, S, 2004)	0.89
" We therefore investigated the therapeutic efficacy of STI571, alone or combined with chemotherapy, in human SCLC cells or tumors xenografted into nude mice."	( In vivo efficacy of STI571 in xenografted human small cell lung cancer alone or combined with chemotherapy. de Cremoux, P; Decaudin, D; Fréneaux, P; Judde, JG; Livartowski, A; Nemati, F; Pouillart, P; Poupon, MF; Sastre, X; Tran-Perennou, C, 2005)	0.33
") topotecan combined with standard doses of intravenous (i."	( A phase I study of intraperitoneal topotecan in combination with intravenous carboplatin and paclitaxel in advanced ovarian cancer. Beijnen, JH; Bos, AM; De Vos, FY; de Vries, EG; Gietema, JA; Mourits, MJ; Rosing, H; van der Zee, AG; Willemse, PH, 2005)	1.33
"05 microM), and was modified differentially in fibroblasts and in glioblastoma cells in combination with irradiation."	( Cell cycle effects of topotecan alone and in combination with irradiation. Kehlbach, R; Ohneseit, PA; Prager, D; Rodemann, HP, 2005)	0.64
" This phase II study investigated the efficacy and safety of topotecan in combination with either cisplatin or etoposide in untreated extensive disease SCLC (ED SCLC)."	( A randomised phase II study of the efficacy and safety of intravenous topotecan in combination with either cisplatin or etoposide in patients with untreated extensive disease small-cell lung cancer. Breton, JL; Cardenal, F; Gervais, R; Lymboura, M; Mattson, K; Preston, A; Quoix, E; Ross, G; Schramel, F; Wilson, J, 2005)	0.8
" Due to the difference of concentration between batches containing irinotecan or topotecan, HPLC and HPTLC both combined with fluorescence detection were investigated."	( Fluorescence detection combined with either HPLC or HPTLC for pharmaceutical quality control in a hospital chemotherapy production unit: application to camptothecin derivatives. Bourget, P; Gravel, E; Mercier, L; Paci, A, 2005)	0.55
"75 mg/m2 was combined with paclitaxel 70 mg/m2; these cytotoxic agents were administered once every week (day 1) for 3 consecutive weeks (one cycle), and repeated every 28 days (three infusions per cycle) for a minimum of three cycles."	( Second-line chemotherapy in small cell lung cancer in a modified administration of topotecan combined with paclitaxel: a phase II study. Antoniou, D; Armenaki, O; Athanasiadis, A; Christodoulou, Ch; Dimitroulis, J; Georgatou, N; Giamboudakis, P; Giannakakis, T; Katis, K; Rigatos, SK; Skarlos, D; Stathopoulos, GP; Stathopoulos, J, 2006)	0.56
"Topotecan combined with paclitaxel, given on day 1 on a weekly basis, produced a response rate of 26."	( Second-line chemotherapy in small cell lung cancer in a modified administration of topotecan combined with paclitaxel: a phase II study. Antoniou, D; Armenaki, O; Athanasiadis, A; Christodoulou, Ch; Dimitroulis, J; Georgatou, N; Giamboudakis, P; Giannakakis, T; Katis, K; Rigatos, SK; Skarlos, D; Stathopoulos, GP; Stathopoulos, J, 2006)	2
" The purpose of this Phase I trial was to determine the maximally tolerated systemic exposure (MTSE) of topotecan in combination with carboplatin and etoposide."	( A phase I trial defining the maximum tolerated systemic exposure of topotecan in combination with Carboplatin and Etoposide in extensive stage small cell lung cancer. Donahue, A; Faucette, S; Gillenwater, HH; Kirstein, MN; Lindley, C; McCune, JS; Moore, D; Shord, S; Socinski, MA; Stewart, CF; Zamboni, WC, 2005)	0.78
"Thirty-four chemotherapy-naïve ES-SCLC patients received topotecan in combination with carboplatin AUC 5 mg/mL*min and oral etoposide 100 mg/m2/day."	( A phase I trial defining the maximum tolerated systemic exposure of topotecan in combination with Carboplatin and Etoposide in extensive stage small cell lung cancer. Donahue, A; Faucette, S; Gillenwater, HH; Kirstein, MN; Lindley, C; McCune, JS; Moore, D; Shord, S; Socinski, MA; Stewart, CF; Zamboni, WC, 2005)	0.81
" We sought to determine the therapeutic potential of TRA-8 (anti-DR5 monoclonal antibody) in combination with chemotherapy and radiation therapy in a cervical cancer model."	( Anti-tumor activity of TRA-8 anti-death receptor 5 (DR5) monoclonal antibody in combination with chemotherapy and radiation therapy in a cervical cancer model. Alvarez, RD; Buchsbaum, DJ; Grizzle, WE; Oliver, PG; Straughn, JM; Wang, W; Zhou, T, 2006)	0.33
"DR5 expression in 7 human cervical cancer cell lines was analyzed by indirect immunofluorescence using murine TRA-8 in combination with flow cytometry."	( Anti-tumor activity of TRA-8 anti-death receptor 5 (DR5) monoclonal antibody in combination with chemotherapy and radiation therapy in a cervical cancer model. Alvarez, RD; Buchsbaum, DJ; Grizzle, WE; Oliver, PG; Straughn, JM; Wang, W; Zhou, T, 2006)	0.33
"Aims of this study were to determine the toxicity profile and the recommended dose of pegylated liposomal doxorubicin (Caelyx) in combination with topotecan in patients with advanced malignancies."	( Phase I dose escalation study of pegylated liposomal doxorubicin (Caelyx) in combination with topotecan in patients with advanced malignancies. Armand, JP; Djafari, L; Djazouli, K; Faivre, S; Ghesquières, H; Lhommé, C; Lozahic, S; Pautier, P; Raymond, E, 2006)	0.75
"Topotecan, a camptothecin analog previously approved for the treatment of ovarian cancer and small-cell lung cancer, was granted regular approval by the US Food and Drug Administration (FDA) on June 14, 2006, for use in combination with cisplatin to treat women with stage IVB, recurrent, or persistent carcinoma of the cervix not amenable to curative treatment with surgery and/or radiation therapy."	( Topotecan in combination with cisplatin for the treatment of stage IVB, recurrent, or persistent cervical cancer. Abraham, S; Booth, B; Brave, M; Dagher, R; Farrell, A; Gobburu, J; Jiang, X; Justice, R; Pazdur, R; Ramchandani, R; Sridhara, R, 2006)	3.22
"A regimen comprising single-agent topotecan given with a standard 3-drug combination was effective in inducing remission in pediatric patients with relapsed ALL and was tolerated well."	( Phase II study of topotecan in combination with dexamethasone, asparaginase, and vincristine in pediatric patients with acute lymphoblastic leukemia in first relapse. Campana, D; Coustan-Smith, E; Gajjar, A; Hijiya, N; Pui, CH; Relling, MV; Rivera, GK; Stewart, CF; Zhou, Y, 2008)	0.96
"To evaluate the therapeutic and adverse effects of topotecan combined with cisplatin in the treatment of advanced squamous cell lung cancer and head and neck cancer."	( [Therapeutic and adverse effects of topotecan combined with cisplatin for treatment of advanced squamous cell lung cancer and head and neck cancer]. Li, QY; Shao, JH; Xiang, Y; Yang, JZ, 2008)	0.87
"2 mg/m2 (for 5 consecutive days) combined with intravenous infusion of cisplantin at 25-30 mg/m2 for 3 consecutive days."	( [Therapeutic and adverse effects of topotecan combined with cisplatin for treatment of advanced squamous cell lung cancer and head and neck cancer]. Li, QY; Shao, JH; Xiang, Y; Yang, JZ, 2008)	0.62
"Topotecan combined with cisplatin may achieve a favorable response in patients with advanced squamous cell lung cancer and head and neck cancer, and causes tolerable adverse effect without accumulative toxicity."	( [Therapeutic and adverse effects of topotecan combined with cisplatin for treatment of advanced squamous cell lung cancer and head and neck cancer]. Li, QY; Shao, JH; Xiang, Y; Yang, JZ, 2008)	2.06
"In vitro assessment of drug candidates' affinity for multi-drug resistance proteins is of crucial importance for the prediction of in vivo pharmacokinetics and drug-drug interactions."	( Characterization of substrates and inhibitors for the in vitro assessment of Bcrp mediated drug-drug interactions. Gnoth, MJ; Grieshop, B; Ickenroth, K; Muenster, U, 2008)	0.35
" In order to not overlook potential drug-drug interactions when testing drug candidates for inhibitory potential towards Bcrp, distinct Bcrp probe substrates should be used."	( Characterization of substrates and inhibitors for the in vitro assessment of Bcrp mediated drug-drug interactions. Gnoth, MJ; Grieshop, B; Ickenroth, K; Muenster, U, 2008)	0.35
" Topotecan in combination with radiotherapy was well tolerated."	( Topotecan in combination with radiotherapy in unresectable glioblastoma: a phase 2 study. Bay, JO; Ben Hassel, M; Carsin, B; Fabbro, M; Frappaz, D; Gédouin, D; Guégan, Y; Hamlat, A; Lesimple, T; Linassier, C; Piot, G; Riffaud, L; Saïkali, S, 2009)	2.71
"The aim of this trial was to investigate the efficacy and toxicity of a relative high-dose of topotecan combined with carboplatin in recurrent or persistent epithelial ovarian cancer (EOC)."	( Topotecan combined with carboplatin in recurrent epithelial ovarian cancer: results of a single-institutional phase II study. Bae, DS; Choi, CH; Kang, H; Kim, BG; Kim, TJ; Lee, JW; Lee, YY, 2009)	2.01
"0 mg/m(2)/day intravenously (IV) on days 1 to 5 in combination with carboplatin AUC 5 IV on day 5, every 21 days."	( Topotecan combined with carboplatin in recurrent epithelial ovarian cancer: results of a single-institutional phase II study. Bae, DS; Choi, CH; Kang, H; Kim, BG; Kim, TJ; Lee, JW; Lee, YY, 2009)	1.8
"The relative high-dose of topotecan combined with carboplatin was feasible and produced modest activity in recurrent or persistent EOC."	( Topotecan combined with carboplatin in recurrent epithelial ovarian cancer: results of a single-institutional phase II study. Bae, DS; Choi, CH; Kang, H; Kim, BG; Kim, TJ; Lee, JW; Lee, YY, 2009)	2.1
" The activity of bevacizumab, either alone or in combination with the HIF-1alpha inhibitor topotecan, was evaluated in U251-HRE xenografts."	( Increased antitumor activity of bevacizumab in combination with hypoxia inducible factor-1 inhibition. Anver, MR; Bonomi, CA; Borgel, SD; Carter, JP; Gehrs, B; Hollingshead, M; Kinders, RJ; Melillo, G; Parchment, R; Raffeld, M; Rapisarda, A; Shoemaker, RH; Uranchimeg, B, 2009)	0.57
"We designed a phase I clinical trial of escalating doses of topotecan with CY and carboplatin in combination with autologous hematopoietic SCT (AHSCT) for the treatment of relapsed or persistent platinum sensitive ovarian or primary peritoneal carcinoma."	( Phase I trial of autologous hematopoietic SCT with escalating doses of topotecan combined with CY and carboplatin in patients with relapsed or persistent ovarian or primary peritoneal carcinoma. Ames, MM; Ansell, SM; Barrette, BA; Dispenzieri, A; Elliott, MA; Frost, MH; Gastineau, DA; Gertz, MA; Hartmann, LC; Inwards, DJ; Kaufmann, SH; Keeney, GL; Lacy, MQ; Lingle, WL; Litzow, MR; Long, HJ; Micallef, IN; Peethambaram, PP; Porrata, LF; Reid, JM; Safgren, SL; Suman, VJ, 2010)	0.84
"Activity and toxiciy of gefitinib in combination with topotecan and cyclophosphamide (CPA) were evaluated in a case-series of relapsed neuroblastoma (NB) patients."	( Gefitinib in combination with oral topotecan and cyclophosphamide in relapsed neuroblastoma: pharmacological rationale and clinical response. Castellano, A; Cialfi, S; De Ioris, MA; De Laurentis, C; De Pasquale, MD; Dominici, C; Donfrancesco, A; Ilari, I; Jenkner, A; McDowell, HP, 2010)	0.89
" Antitumor activity of gefitinib as single agent and in combination with either topotecan or CPA was assessed in a panel of NB cell lines."	( Gefitinib in combination with oral topotecan and cyclophosphamide in relapsed neuroblastoma: pharmacological rationale and clinical response. Castellano, A; Cialfi, S; De Ioris, MA; De Laurentis, C; De Pasquale, MD; Dominici, C; Donfrancesco, A; Ilari, I; Jenkner, A; McDowell, HP, 2010)	0.86
" To evaluate further the potential therapeutic impact of metronomic chemotherapy for ovarian cancer, we developed a preclinical model of advanced human ovarian cancer and tested various low-dose metronomic chemotherapy regimens alone or in concurrent combination with an antiangiogenic drug, pazopanib."	( Potent preclinical impact of metronomic low-dose oral topotecan combined with the antiangiogenic drug pazopanib for the treatment of ovarian cancer. Cruz-Munoz, W; Hashimoto, K; Kerbel, RS; Kumar, R; Man, S; Tang, T; Xu, P, 2010)	0.61
"To evaluate maximum tolerated dose and recommended dose (RD) for phase II studies of topotecan (TPT) combined with temozolomide (TMZ) (TOTEM) in children and adolescents with relapsed or refractory solid malignancies."	( Phase I study of topotecan in combination with temozolomide (TOTEM) in relapsed or refractory paediatric solid tumours. Aerts, I; Chastagner, P; Chatelut, E; Corradini, N; Dias, N; Djafari, L; Frappaz, D; Gentet, JC; Geoerger, B; Landman-Parker, J; Le Deley, MC; Leblond, P; Ndiaye, A; Paci, A; Pasquet, M; Rubie, H; Schmitt, A; Vassal, G, 2010)	0.92
"This phase I study evaluated the safety, tolerability, preliminary antitumor activity, and pharmacokinetic interaction of weekly topotecan (days 1 and 8) in combination with pemetrexed (day 1 only) in patients with advanced solid tumors."	( A phase I study of weekly topotecan in combination with pemetrexed in patients with advanced malignancies. Burris, HA; Greco, FA; Infante, JR; Jewell, RC; Jones, SF; Spigel, DR; Thompson, DS, 2010)	0.87
"Patients with ROC after first- or second-line treatment including a platinum and taxane and progression within 6 months were randomized to weekly paclitaxel (wP, 80 mg/m(2)/week) alone or in combination with carboplatin (C, area under the curve of 5 mg/ml/min every 4 weeks) or weekly topotecan (wT, 3 mg/m(2)/week)."	( Weekly paclitaxel as a single agent or in combination with carboplatin or weekly topotecan in patients with resistant ovarian cancer: the CARTAXHY randomized phase II trial from Groupe d'Investigateurs Nationaux pour l'Etude des Cancers Ovariens (GINECO). Alexandre, J; Dauba, J; Durando, X; Gladieff, L; Largillier, R; Lortholary, A; Paraiso, D; Pujade-Lauraine, E; Slama, B; Weber, B, 2012)	0.78
"The aim of this phase I study was to determine the safety and tolerability and to establish the maximum tolerated dose (MTD) of orally administered olaparib (AZD2281) in combination with topotecan in patients with advanced solid tumors."	( Safety and tolerability of the poly(ADP-ribose) polymerase (PARP) inhibitor, olaparib (AZD2281) in combination with topotecan for the treatment of patients with advanced solid tumors: a phase I study. Carmichael, J; Cassidy, J; Macpherson, E; Ranson, M; Samol, J; Scott, E; Thomas, A, 2012)	0.78
"0 mg/m(2)/day × 3 days) intravenously in combination with oral olaparib 50, 100 or 200 mg bid for six cycles."	( Safety and tolerability of the poly(ADP-ribose) polymerase (PARP) inhibitor, olaparib (AZD2281) in combination with topotecan for the treatment of patients with advanced solid tumors: a phase I study. Carmichael, J; Cassidy, J; Macpherson, E; Ranson, M; Samol, J; Scott, E; Thomas, A, 2012)	0.59
"A phase I trial of ABT-888 (veliparib), a PARP inhibitor, in combination with topotecan, a topoisomerase I-targeted agent, was carried out to determine maximum tolerated dose (MTD), safety, pharmacokinetics, and pharmacodynamics of the combination in patients with refractory solid tumors and lymphomas."	( Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults with refractory solid tumors and lymphomas. Ames, M; Bonner, W; Carter, J; Chen, A; Doroshow, JH; Hollingshead, M; Ji, J; Jia, L; Kinders, R; Kummar, S; Melillo, G; Murgo, AJ; Parchment, RE; Pommier, Y; Reid, JM; Rubinstein, L; Speranza, G; Stotler, H; Tomaszewski, JE; Wang, L; Weil, M; Zhang, Y, 2011)	0.84
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."	( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions. Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012)	0.38
" This study evaluates the toxicity of escalating doses of topotecan alone or in combination with thiotepa or treosulfan."	( Escalating topotecan in combination with treosulfan has acceptable toxicity in advanced pediatric sarcomas. Bauer, F; Burdach, S; Filipiak-Pittroff, B; von Luettichau, I; Wawer, A, 2013)	1.02
"To assess objective response rate (ORR) after two cycles of temozolomide in combination with topotecan (TOTEM) in children with refractory or relapsed neuroblastoma."	( Phase II study of temozolomide in combination with topotecan (TOTEM) in relapsed or refractory neuroblastoma: a European Innovative Therapies for Children with Cancer-SIOP-European Neuroblastoma study. Aerts, I; Amoroso, L; Boubaker, A; Casanova, M; Chastagner, P; Courbon, F; Devos, A; Di Giannatale, A; Dias-Gastellier, N; Ducassoul, S; Geoerger, B; Landman-Parker, J; Le Deley, MC; Malekzadeh, K; Mc Hugh, K; Munzer, C; Riccardi, R; Rubie, H; Verschuur, A; Zwaan, CM, 2014)	0.87
" We evaluated the optimal schedule of oral topotecan in combination with everolimus in patients with endometrial cancer."	( Phase I clinical trial of the mammalian target of rapamycin inhibitor everolimus in combination with oral topotecan for recurrent and advanced endometrial cancer. Abu-Khalaf, MM; Acevedo-Gadea, C; Azodi, M; Higgins, SA; Ratner, E; Rutherford, T; Santin, AD; Schwartz, PE; Silasi, DA; Urva, S, 2014)	0.88
"9 mg/m on days 1 to 5 in combination with oral everolimus 5 mg every other day."	( Phase I clinical trial of the mammalian target of rapamycin inhibitor everolimus in combination with oral topotecan for recurrent and advanced endometrial cancer. Abu-Khalaf, MM; Acevedo-Gadea, C; Azodi, M; Higgins, SA; Ratner, E; Rutherford, T; Santin, AD; Schwartz, PE; Silasi, DA; Urva, S, 2014)	0.62
" No drug-drug interactions were apparent."	( A phase 1b study of trebananib in combination with pegylated liposomal doxorubicin or topotecan in women with recurrent platinum-resistant or partially platinum-sensitive ovarian cancer. Adewoye, H; Ananda, S; Bass, MB; Dirix, L; Gordon, AN; Kridelka, F; Leach, JW; Litten, J; Melara, R; Nanayakkara, N; Pippitt, CH; Schilder, RJ; Scudder, S; Vergote, I; Wenham, RM; Wong, S, 2014)	0.63
" Inhibition of PARP-1 is tested in combination with DNA damaging agents such as topoisomerase I inhibitors or ionizing radiations (RT) for the treatment of glioblastoma (GBM)."	( Effect of p53 activity on the sensitivity of human glioblastoma cells to PARP-1 inhibitor in combination with topoisomerase I inhibitor or radiation. Carlomagno, C; Della Vittoria Scarpati, G; Ferrone, S; Fusciello, C; Leonardi, A; Pacelli, R; Pepe, S; Pepin, D; Poudel, R; Sabbatino, F; Somma, D, 2014)	0.4
"Thymoquinone, when combined with topotecan in noncytotoxic doses, produced synergistic antiproliferative and proapoptotic effects in AML cells."	( Antiproliferative and proapoptotic effects of topotecan in combination with thymoquinone on acute myelogenous leukemia. El-Hayek, S; Hodroj, MH; Khalife, R; Rizk, S; Stephany, el-H; Tarras, O, 2014)	0.94
"This retrospective study aimed to observe the cura-tive effect and adverse reactions of three-dimensional conformal radiotherapy combined with topotecan chemotherapy in patients with platinum-resistant recurrent epithelial ovarian carcinoma."	( Clinical observational study of conformal radiotherapy combined with topotecan chemotherapy in patients with platinum-resistant recurrent ovarian cancer. Du, XL; Li, L; Shan, CP; Sheng, XG; Wei, P; Zhang, ZH, 2015)	0.85
"This phase I study evaluated the safety, tolerability, maximum tolerated dose (MTD) and pharmacokinetics of two dosing schedules of oral topotecan in combination with pazopanib in patients with advanced solid tumours."	( Phase I and pharmacological study of pazopanib in combination with oral topotecan in patients with advanced solid tumours. Devriese, LA; Giantonio, BJ; Kerklaan, BM; Lane, S; Langenberg, M; Legenne, P; Lolkema, MP; Mergui-Roelvink, M; Mykulowycz, K; Nol-Boekel, A; Schellens, JH; Smith, DA; Stoebenau, J; Voest, EE; Wissel, P; Witteveen, PO, 2015)	0.85
" In stage II, the MTD and safety profile of oral topotecan given weekly on days 1, 8 and 15 in a 28-day cycle; or daily-times-five on days 1-5 in a 21-day cycle, both in combination with daily pazopanib, were explored."	( Phase I and pharmacological study of pazopanib in combination with oral topotecan in patients with advanced solid tumours. Devriese, LA; Giantonio, BJ; Kerklaan, BM; Lane, S; Langenberg, M; Legenne, P; Lolkema, MP; Mergui-Roelvink, M; Mykulowycz, K; Nol-Boekel, A; Schellens, JH; Smith, DA; Stoebenau, J; Voest, EE; Wissel, P; Witteveen, PO, 2015)	0.9
"Various cytotoxic agents were evaluated in combination with (131) I-MIP-1095 for their capacity to delay the growth of LNCaP cells cultured as multicellular tumour spheroids."	( Preliminary evaluation of prostate-targeted radiotherapy using (131) I-MIP-1095 in combination with radiosensitising chemotherapeutic drugs. Babich, JW; Mairs, RJ; Nixon, C; Rae, C; Tesson, M, 2016)	0.43
"To determine the maximum tolerated dose (MTD), toxicities, and pharmacodynamics effects of sirolimus combined with oral metronomic topotecan and cyclophosphamide in a pediatric population."	( Phase 1 study of sirolimus in combination with oral cyclophosphamide and topotecan in children and young adults with relapsed and refractory solid tumors. Allen, S; DuBois, SG; Gustafson, WC; Hollinger, F; Karski, EE; Long-Boyle, JR; Matthay, KK; Nasholm, NM; Shiboski, S; Vo, KT, 2017)	0.89
"The aim of this study was to evaluate the outcomes of patients with advanced or recurrent ovarian cancer treated with cisplatin combined with topotecan as second- or higher-line palliative chemotherapy."	( Efficacy of cisplatin combined with topotecan in patients with advanced or recurrent ovarian cancer as second- or higher-line palliative chemotherapy. Jo, DY; Ko, YB; Lee, HJ; Lee, MW; Ryu, H; Song, IC; Yun, HJ, 2020)	1.03
" 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)	1.16
" In the present research, the impact of beta-particles of iodine-131 in combination with Topotecan (TPT), as the inhibitor of topoisomerase I, and A-966492, as the inhibitor of the PARP enzyme on the possible increase of radio-sensitivity of glioblastoma cells was assessed."	( The effect of iodine-131 beta-particles in combination with A-966492 and Topotecan on radio-sensitization of glioblastoma: An in-vitro study. Eynali, S; Eyvazzadeh, N; Kamalabadi, MA; Koosha, F, 2021)	1.07
" Here, we investigate the pharmacokinetic drug-drug interaction potential of trilaciclib."	( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer. Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022)	0.93
"Overall, the drug-drug interaction and safety profiles of trilaciclib in these studies support its continued use in patients with extensive-stage small-cell lung cancer."	( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer. Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022)	0.93

Excerpt	Reference	Relevance
"7-fold that of parenteral administration, indicative of excellent oral bioavailability in the mouse."	( Comparative activity of oral and parenteral topotecan in murine tumor models: efficacy of oral topotecan. Johnson, RK; McCabe, FL, 1994)	0.55
" The drug is well absorbed from small intestine."	( [Topoisomerase inhibitors developing in Japan]. Furue, H, 1993)	0.29
" We determined the apparent bioavailability and pharmacokinetics of topotecan administered orally to 12 patients with solid tumours in a two-part crossover study."	( Bioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitor. Beijnen, JH; Creemers, GJ; Davies, B; de Boer-Dennert, M; McDonald, M; Rosing, H; Schellens, JH; Verweij, J, 1996)	0.79
" The low bioavailability may be caused by hydrolysis of topotecan lactone in the gut, yielding substantial amounts of the open-ring form, which is poorly absorbed."	( Clinical pharmacokinetics of topotecan. Beijnen, JH; Herben, VM; ten Bokkel Huinink, WW, 1996)	0.83
" Recently bioavailability of an oral formulation of approximately 30% with limited variability was reported."	( Phase I and pharmacologic study of oral topotecan administered twice daily for 21 days to adult patients with solid tumors. Broom, C; Burris, HA; Creemers, GJ; Eckardt, JR; Gerrits, CJ; Hudson, I; Loos, WJ; Planting, AS; Rodriguez, GI; Schellens, JH; Verweij, J; Von Hoff, DD, 1997)	0.56
" After oral administration the bioavailability varied between 30 and 35%."	( [Topoisomerase I inhibitor with potential radiosensitizing effect]. Heuser, A; Sauer, R, 1997)	0.3
" Any SK&F 105,992 formed in the GI tract did not appear to be well absorbed following oral administration of topotecan to dogs."	( The pharmacokinetics of topotecan and its carboxylate form following separate intravenous administration to the dog. Beijnen, JH; Davies, BE; Dennis, MJ; Minthorn, EA; Rosing, H, 1997)	0.82
" An oral bioavailability of TPT of 32-44% enables convenient prolonged administration."	( Oral topotecan given once or twice daily for ten days: a phase I pharmacology study in adult patients with solid tumors. Burris, H; Eckardt, JR; Fields, S; Gerrits, CJ; Hudson, I; Loos, WJ; Planting, AS; Rodriguez, GI; Schellens, JH; van Beurden, V; van der Burg, ME; Verweij, J; Von Hoff, DD, 1998)	0.81
" An oral formulation of topotecan is available with a bioavailability of 32-44% in humans."	( Five days of oral topotecan (Hycamtin), a phase I and pharmacological study in adult patients with solid tumours. Burris, H; Fields, S; Gerrits, CJ; Hudson, I; Loos, WJ; Planting, AS; Rodriguez, GI; Schellens, JH; van Beurden, V; van den Burg, ME; Verweij, J; von Hoff, DD, 1998)	0.94
" An oral formulation of topotecan with a bioavailability of 32-44% in humans enables convenient prolonged administration."	( A comparison of clinical pharmacodynamics of different administration schedules of oral topotecan (Hycamtin) Burris, H; Eckardt, JR; Gerrits, CJ; Hudson, I; Loos, WJ; Planting, AS; Rodriguez, GI; Schellens, JH; van Beurden, V; van der Burg, ME; Verweij, J; Von Hoff, DD, 1999)	0.83
"Evaluation of inter- and intrapatient variability of topotecan oral bioavailability and disposition was performed in children with malignant solid tumors."	( Interpatient variability in bioavailability of the intravenous formulation of topotecan given orally to children with recurrent solid tumors. Bowman, LC; Gajjar, AJ; Heideman, RL; Houghton, PJ; Meyer, WH; Pappo, AS; Pratt, CB; Santana, VM; Stewart, CF; Tan, M; Zamboni, WC, 1999)	0.78
"The aims of the study were twofold: (1) to evaluate the effect of food on the relative oral bioavailability of topotecan gelatin capsules in patients with solid tumours, and (2) to determine the absolute bioavailability of oral topotecan with reference to the intravenous (i."	( Oral topotecan: bioavailablity and effect of food co-administration. Batchelor, D; Beijnen, JH; Beusenberg, FD; Doyle, E; Herben, VM; Rosing, H; Schellens, JH; ten Bokkel Huinink, WW; van Zomeren, DM, 1999)	1.03
"Although topoisomerase inhibitors, such as camptothecin and topotecan, have been widely used in the treatment of nonglial tumors, their application for gliomas has been limited by poor efficacy relative to toxicity that may in part reflect limited bioavailability and blood stability of these agents."	( Potent topoisomerase I inhibition by novel silatecans eliminates glioma proliferation in vitro and in vivo. Bom, D; Burke, TG; Curran, DP; Erff, M; Pollack, IF; Strode, JT, 1999)	0.55
"Temozolomide (TMZ) is a new, orally administered, second-generation imidazotetrazine prodrug with essentially 100% oral bioavailability that has demonstrated meaningful efficacy and an acceptable safety profile in the treatment of patients with recurrent glioblastoma multiforme."	( Future directions in the treatment of malignant gliomas with temozolomide. Prados, MD, 2000)	0.31
" In spite of the low bioavailability of oral topotecan (23."	( Efficacy and toxicity profile of oral topotecan in a panel of human tumour xenografts. De Cesare, M; Pace, S; Pisano, C; Pratesi, G; Zunino, F, 2000)	0.84
" A slightly faster rate of absorption of topotecan was also observed, which is unlikely to be of clinical significance."	( Pretreatment with ranitidine does not reduce the bioavailability of orally administered topotecan. Akhtar, S; Beckman, RA; Doyle, E; Fields, SZ; Mould, DR; Wright, J, 2000)	0.8
" To avoid the confounding drug transport provided by P-glycoprotein (P-gp), the roles of Bcrp1 in the bioavailability of topotecan and the effect of GF120918 were studied in both wild-type and P-gp-deficient mice and their fetuses."	( Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. Beijnen, JH; Brinkhuis, RF; Jonker, JW; Maliepaard, M; Schellens, JH; Schinkel, AH; Smit, JW, 2000)	0.74
" When both topotecan and GF120918 were administered orally, the bioavailability (i."	( Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. Beijnen, JH; Brinkhuis, RF; Jonker, JW; Maliepaard, M; Schellens, JH; Schinkel, AH; Smit, JW, 2000)	0.92
" These results may have therapeutic implications because the antitumor efficacy of ST1481 is in part related to a good bioavailability after oral administration, and the drug is currently under Phase I clinical evaluation."	( A novel 7-modified camptothecin analog overcomes breast cancer resistance protein-associated resistance in a mitoxantrone-selected colon carcinoma cell line. Beggiolin, G; Carenini, N; Carminati, P; De Cesare, M; De Isabella, P; Palumbo, M; Perego, P; Pezzoni, G; Pisano, C; Pratesi, G; Scheffer, GL; Tartaglia, L; Zunino, F, 2001)	0.31
" Presently, several strategies are explored to alter the low and variable oral bioavailability of several important anticancer agents by taking advantage of an intentional interaction between anticancer agents and drugs that modulate active intestinal drug transporters or (intestinal) enzymes."	( The use of oral cytotoxic and cytostatic drugs in cancer treatment. de Jonge, MJ; Sparreboom, A; Verweij, J, 2002)	0.31
"We discovered that breast cancer resistance protein (BCRP), a recently identified adenosine triphosphate-binding cassette drug transporter, substantially limits the oral bioavailability of topotecan in mdr1a/1b(-/-) P-glycoprotein (P-gp) knockout and wild-type mice."	( Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. Beijnen, JH; Jewell, RC; Kruijtzer, CM; Paul, EM; Rosing, H; Schellens, JH; Schot, M; ten Bokkel Huinink, WW, 2002)	0.78
" The apparent bioavailability in this cohort increased significantly from 40."	( Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. Beijnen, JH; Jewell, RC; Kruijtzer, CM; Paul, EM; Rosing, H; Schellens, JH; Schot, M; ten Bokkel Huinink, WW, 2002)	0.59
" The apparent oral bioavailability increased from 40."	( Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. Beijnen, JH; Jewell, RC; Kruijtzer, CM; Paul, EM; Rosing, H; Schellens, JH; Schot, M; ten Bokkel Huinink, WW, 2002)	0.59
"The novel camptothecin derivative BNP1350 (7-[2-trimethylsilyl)ethyl]-20(S)-camptothecin), also known as Karenitecin, has been developed for superior oral bioavailability and increased lactone stability."	( Novel camptothecin derivative BNP1350 in experimental human ovarian cancer: determination of efficacy and possible mechanisms of resistance. Boven, E; Hausheer, FH; Pinedo, HM; Schlüper, HM; Van Hattum, AH, 2002)	0.31
" Pharmacokinetic and pharmacodynamic biomodulation, to enhance the bioavailability of the active anticancer agent or to reduce drug related toxicities have currently reached clinical application."	( Pharmacology of topoisomerase I inhibitors irinotecan (CPT-11) and topotecan. Loos, WJ; Mathijssen, RH; Sparreboom, A; Verweij, J, 2002)	0.55
" In this work we investigated the effect of association of temozolomide (TMZ), an orally bioavailable alkylating agent, with three chemotherapeutic drugs, liposomal doxorubicin (DOXO), cis-platinum (CDDP)."	( Effect of association of temozolomide with other chemotherapic agents on cell growth inhibition in glioma cell lines. Balzarotti, M; Boiardi, A; Calatozzolo, C; Ciusani, E; Croci, D; Salmaggi, A, 2004)	0.32
" Coadministration of 50 mg/kg GF120918 [N-(4-[2-(1,2,3,4-tetrahydro-6,7-dimethoxy-2-isoquinolinyl)ethyl]-phenyl)-9, 10-dihydro-5-methoxy-9-oxo-4-acridine carboxamide] with 2 mg/kg topotecan significantly increased the area under the plasma concentration-time curve and bioavailability of topotecan by more than 4-fold in these animals, indicating the importance of BCRP in the bioavailability and disposition of topotecan in rats."	( Flavonoids chrysin and benzoflavone, potent breast cancer resistance protein inhibitors, have no significant effect on topotecan pharmacokinetics in rats or mdr1a/1b (-/-) mice. Morris, ME; Sagawa, K; Wang, X; Zhang, S, 2005)	0.73
"34-fold increased oral bioavailability of topotecan compared to the bioavailability in ten patients with the wild-type allele (42."	( Effect of ABCG2 genotype on the oral bioavailability of topotecan. Burger, H; Figg, WD; Gelderblom, H; Loos, WJ; Nooter, K; Sissung, TM; Sparreboom, A; Verweij, J, 2005)	0.84
", irinotecan), resulting in increased bioavailability and reduced clearance of these agents."	( Cyclosporin A, tacrolimus and sirolimus are potent inhibitors of the human breast cancer resistance protein (ABCG2) and reverse resistance to mitoxantrone and topotecan. Dai, Y; Gupta, A; Hebert, MF; Mao, Q; Ross, DD; Thummel, KE; Unadkat, JD; Vethanayagam, RR, 2006)	0.53
" Oral administration of 4-AQ molecules, such as gefitinib, inhibits ATP-binding cassette (ABC) transporter-mediated drug efflux and strongly increases the apparent bioavailability of coadministered drug molecules that are transporter substrates."	( Gefitinib modulates the function of multiple ATP-binding cassette transporters in vivo. Bai, F; Houghton, PJ; Johnston, B; Leggas, M; Panetta, JC; Schuetz, JD; Sorrentino, B; Stewart, CF; Zhou, S; Zhuang, Y, 2006)	0.33
" ABCG2 also appears influential in the inter-patient variation and generally poor oral bioavailability of certain chemotherapeutic drugs such as topotecan."	( The emerging pharmacotherapeutic significance of the breast cancer resistance protein (ABCG2). Hardwick, LJ; van Veen, HW; Velamakanni, S, 2007)	0.54
"Breast cancer resistance protein (ABCG2) substantially limits the oral bioavailability of topotecan."	( A phase I, randomized, open-label, parallel-cohort, dose-finding study of elacridar (GF120918) and oral topotecan in cancer patients. Beijnen, JH; Jewell, RC; Kuppens, IE; Mangum, SG; Paul, EM; Radema, SA; Schellens, JH; Voest, EE; Witteveen, EO, 2007)	0.78
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."	( Hologram QSAR model for the prediction of human oral bioavailability. Andricopulo, AD; Moda, TL; Montanari, CA, 2007)	0.34
" Topotecan, an anti-cancer drug widely used in metastatic carcinoma, is a P-glycoprotein substrate having oral bioavailability of 30% with large inter-patient variability."	( Concurrent determination of topotecan and model permeability markers (atenolol, antipyrine, propranolol and furosemide) by reversed phase liquid chromatography: utility in Caco-2 intestinal absorption studies. Bansal, T; Jaggi, M; Khar, RK; Mishra, G; Mukherjee, R; Singh, M; Talegaonkar, S, 2007)	1.54
"The bioavailability of belotecan and topotecan in rats was determined following oral administration of each drug at a dose of 5 mg/kg body weight."	( Involvement of P-glycoprotein, multidrug resistance protein 2 and breast cancer resistance protein in the transport of belotecan and topotecan in Caco-2 and MDCKII cells. Chung, SJ; Han, YH; Jin, HE; Kim, DD; Kim, W; Li, H; Shim, CK, 2008)	0.82
"The bioavailability of belotecan (11."	( Involvement of P-glycoprotein, multidrug resistance protein 2 and breast cancer resistance protein in the transport of belotecan and topotecan in Caco-2 and MDCKII cells. Chung, SJ; Han, YH; Jin, HE; Kim, DD; Kim, W; Li, H; Shim, CK, 2008)	0.55
"The involvement of secretory transporters P-gp, MRP2 and BCRP, particularly for belotecan, as well as a low passive permeability, appears to be responsible for the low bioavailability of belotecan and topotecan."	( Involvement of P-glycoprotein, multidrug resistance protein 2 and breast cancer resistance protein in the transport of belotecan and topotecan in Caco-2 and MDCKII cells. Chung, SJ; Han, YH; Jin, HE; Kim, DD; Kim, W; Li, H; Shim, CK, 2008)	0.74
" They determine the pharmacokinetics of the formulation and the bioavailability of the drugs."	( Characterization of PEGylated nanoliposomes co-remotely loaded with topotecan and vincristine: relating structure and pharmacokinetics to therapeutic efficacy. Andriyanov, AV; Barenholz, Y; Raviv, U; Steiner, A; Zucker, D, 2012)	0.61
" Intravitreal drug injection is a promissing route for maximum bioavailability to the vitreous but it requires a well defined dose for achieving tumor control while limited toxicity to the retina."	( Ocular and systemic toxicity of intravitreal topotecan in rabbits for potential treatment of retinoblastoma. Asprea, M; Bramuglia, GF; Buitrago, E; Chantada, GL; Croxatto, JO; Del Sole, MJ; Fandino, A; Schaiquevich, P; Torbidoni, A, 2013)	0.65
" As topotecan bioavailability and pharmacokinetic data for Chinese patients is limited, the aim of the study was to assess the absolute bioavailability and pharmacokinetics of Xinze(®) in Chinese patients with SCLC treated intravenously (i."	( Absolute bioavailability studies of a new oral topotecan formulation in Chinese patients using UHPLC-MS/MS. Du, P; Gui, L; Han, X; Li, N; Shi, Y; Song, Y; Yang, J, 2013)	1.2
" This experimental system is useful for clarifying the cause of low bioavailability of various drugs."	( In vivo assessment of the impact of efflux transporter on oral drug absorption using portal vein-cannulated rats. Hashimoto, T; Konno, Y; Matsuda, Y; Nagai, M; Satsukawa, M; Taguchi, T; Yamashita, S, 2013)	0.39
" However, in the periphery, venlafaxine treatment significantly reduced the topotecan oral bioavailability by nearly 40%, whereas the impact of desvenlafaxine on topotecan plasma levels was more modest (23%)."	( Effect of venlafaxine and desvenlafaxine on drug efflux protein expression and biodistribution in vivo. Bachmeier, C; Beaulieu-Abdelahad, D; Levin, GM; Mullan, M; Reed, J, 2013)	0.62
"Oral topotecan (Hycamtin(®)) has been recently approved for the treatment of relapsed small cell lung cancer (SCLC) in 2007, however, the bioavailability and pharmacokinetic data of topotecan for Chinese patients is still limited."	( Oral topotecan: Bioavailability, pharmacokinetics and impact of ABCG2 genotyping in Chinese patients with advanced cancers. Du, P; Gui, L; Han, X; Li, N; Shen, Y; Shi, Y; Song, Y; Sun, Y; Wang, J; Wang, S; Yang, J, 2013)	1.42
" It also showed a moderate oral bioavailability and good safety in vivo."	( Novel N-substituted sophoridinol derivatives as anticancer agents. Bi, CW; Deng, HB; Li, YH; Shao, RG; Song, DQ; Tang, S; Wang, Z; Zhang, CX; Zhao, WL, 2014)	0.4
" Current treatment involves the administration of systemic chemotherapy combined with radiation, but there is a clear need for improvement of chemotherapy bioavailability in the optic nerve."	( Topotecan Delivery to the Optic Nerve after Ophthalmic Artery Chemosurgery. Abramson, DH; Asprea, M; Chantada, G; Gobin, P; Requejo, F; Schaiquevich, P; Sgroi, M; Taich, P, 2016)	1.88
" However, high interpatient variability in oral drug bioavailability is common in children less than 3 years old."	( Population Pharmacokinetics of Oral Topotecan in Infants and Very Young Children with Brain Tumors Demonstrates a Role of ABCG2 rs4148157 on the Absorption Rate Constant. Birg, AV; Broniscer, A; Daryani, VM; Gajjar, AJ; Lin, T; Panetta, JC; Roberts, JK; Robinson, GW; Stewart, CF, 2016)	0.71
"Fluorination is a well-known strategy for improving the bioavailability of bioactive molecules in the lead optimization phase of drug discovery projects."	( Design, semisynthesis and potent cytotoxic activity of novel 10-fluorocamptothecin derivatives. Goto, M; Hsu, PL; Lee, KH; Liu, YQ; Morris-Natschke, SL; Shang, XF; Song, ZL; Wang, MJ; Yang, CJ; Yang, QR; Zhang, XS, 2017)	0.46
" These findings were further supported by the enhancement of bioavailability (13."	( Formulation and optimization of topotecan nanoparticles: In vitro characterization, cytotoxicity, cellular uptake and pharmacokinetic outcomes. Iqbal, Z; Kapoor, R; Padhi, S; Panda, AK; Verma, D, 2018)	0.76
" The SD formulation was effective in improving the bioavailability of topotecan, a BCRP substrate in rats."	( Improved In vivo Effect of Chrysin as an Absorption Enhancer Via the Preparation of Ternary Solid Dispersion with Brij®L4 and Aminoclay. Han, HK; Lee, SH; Lee, YS; Song, JG, 2019)	0.75
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."	( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019)	0.51
" However, oral bioavailability of topotecan was not satisfactory in previous studies."	( Oral delivery of topotecan in polymeric nanoparticles: Lymphatic distribution and pharmacokinetics. Jang, JH; Jeong, SH; Lee, YB, 2021)	1.24
" Pharmacokinetic studies showed enhanced bioavailability of the TPT with improved plasma concentration and AUC."	( Development, Characterization, and Evaluation of SLN-Loaded Thermoresponsive Hydrogel System of Topotecan as Biological Macromolecule for Colorectal Delivery. Ali, T; Ali, Z; Baseer, A; Batool, S; Din, F; Malik, M; Mukhtiar, M; Mustapha, O; Rehman, M; Shafique, S; Shah, F; Sohail, S; Xing, R; Yousaf, A; Zahid, F; Zaidi, SS; Zeb, A, 2021)	0.84
" Future studies should focus not only on developing other active molecules but also on improving the bioavailability and pharmacokinetics of potent synthetic derivatives."	( The design and discovery of topoisomerase I inhibitors as anticancer therapies. Alonso, C; Martín-Encinas, E; Palacios, F; Selas, A, 2022)	0.72
" For lead optimization in new drug discovery stages, fluorination is an effective and robust approach to increase the bioavailability and optimize the pharmacokinetics of candidate compounds, thereby improving their efficacy."	( Improved anti-tumor activity of fluorinated camptothecin derivatives 9-fluorocamptothecin and 7-ethyl-9-fluorocamptothecin on hepatocellular carcinoma by targeting topoisomerase I. Bai, YP; Li, L; Liu, YQ; Luo, HB; Peng, LZ; Wang, ZP; Xu, CR; Yan, JX; Yang, CJ; Zhang, M; Zhang, ZJ; Zhu, LZ, 2023)	0.91
"P-glycoprotein (Pgp) plays a pivotal role in drug bioavailability and multi-drug resistance development."	( Drug-Induced Conformational Dynamics of P-Glycoprotein Underlies the Transport of Camptothecin Analogs. Bartlett, MG; King, GM; Mensah, GAK; Roberts, AG; Schaefer, KG, 2023)	0.91

Excerpt	Relevance	Reference
" The steady-state concentrations of total drug will be measured in several of these trials to establish its potential role in adaptive dosing using this schedule."	( Clinical, pharmacokinetic and biological studies of topotecan. Frucht, H; Goosenberg, E; Haas, NB; Halbherr, T; LaCreta, FP; O'Dwyer, PJ; Yao, KS, 1994)	0.54
" Total drug steady-state plasma concentration provided a good estimate of neutropenia, suggesting a simple, easily monitored, pharmacokinetic parameter for adaptive dosing using this schedule."	( Phase I/pharmacokinetic study of topotecan by 24-hour continuous infusion weekly. Brennan, JM; Haas, NB; Hudes, GR; LaCreta, FP; O'Dwyer, PJ; Ozols, RF; Walczak, J, 1994)	0.57
"0-mg/m2 dosage level; thus, additional patients were treated with this dosage, followed by human recombinant granulocyte-colony stimulating factor (G-CSF)."	( Phase I study of topotecan for pediatric patients with malignant solid tumors. Bowman, L; Furman, W; Heideman, R; Kuttesch, JF; Marina, N; Ochs, J; Pratt, CB; Sandlund, JT; Santana, VM; Stewart, C, 1994)	0.63
" Css was calculated for each patient; if it differed by more than 20% of target, a new dosage was begun within 6 hours."	( Escalating systemic exposure of continuous infusion topotecan in children with recurrent acute leukemia. Baker, SD; Evans, WE; Furman, WL; Pratt, CB; Rivera, GK; Stewart, CF, 1996)	0.54
" However, dosing guidelines for the administration of topotecan to patients with impaired hepatic function have not yet been established."	( Phase I and pharmacologic studies of topotecan in patients with impaired hepatic function. Bowling, K; Brubaker, A; Chen, TL; Donehower, RC; Ettinger, D; Forastiere, A; Grochow, LB; Ignacio, V; Lubejko, B; O'Reilly, S; Rowinsky, E; Sartorius, S; Slichenmyer, W; Smith, J, 1996)	0.82
" Because the concurrent administration of TPT and G-CSF resulted in severe myelosuppression at the lowest TPT dose level, an alternate posttreatment G-CSF schedule in which G-CSF dosing began after TPT (starting on day 6) was subsequently evaluated."	( Phase I and pharmacologic study of high doses of the topoisomerase I inhibitor topotecan with granulocyte colony-stimulating factor in patients with solid tumors. Bowling, MK; Donehower, RC; Grochow, LB; Kaufmann, SH; Peereboom, D; Rowinsky, EK; Sartorius, SE, 1996)	0.52
" Further exploration of topotecan in pancreatic carcinoma using different dosing schedules is warranted."	( Phase II trial of topotecan in advanced or metastatic adenocarcinoma of the pancreas. Alexander, R; Amfoh, K; Engstrom, PF; Fox, S; Green, F; Kosierowski, R; Lusch, C; O'Dwyer, PJ; Raskay, B; Redei, I; Scher, RM, 1996)	0.93
" Neutropenia was the principal toxicity of topotecan on this dosing schedule."	( A phase II trial of topotecan in patients with previously untreated pancreatic cancer. Donehower, RC; Grochow, LB; O'Reilly, S; Ord, S; Rowinsky, EK, 1996)	0.88
" Phase I trials found antitumor activity in many topotecan dosing schedules, one of which involved the administration of topotecan daily as a 30-minute infusion for 5 consecutive days, with the cycle repeated every 21 days."	( Efficacy and safety of topotecan in the treatment of advanced ovarian carcinoma. Armstrong, D; Carmichael, J; Gordon, A; Malfetano, J; ten Bokkel Huinink, W, 1997)	0.86
" Proliferation does not seem to be necessary for the effect of Topo, and no superiority for protracted dosing schedules was observed."	( Cytotoxic activity of topotecan in human tumour cell lines and primary cultures of human tumour cells from patients. Csóka, K; Dhar, S; Fridborg, H; Jonsson, E; Larsson, R; Nygren, P; Sundström, C, 1997)	0.61
" Reduction of the treatment interval to 3 weeks and prolonging etoposide dosing to 10 days did not permit further dose intensification, as a time delay to retreatment owing to unrecovered bone marrow rapidly emerged as the DLT."	( Phase I and pharmacological study of sequential intravenous topotecan and oral etoposide. Beijnen, JH; Dubbelman, AC; Groot, Y; Herben, VM; Mandjes, IA; ten Bokkel Huinink, WW; van Gortel-van Zomeren, DM, 1997)	0.54
" A large number of phase I studies with topotecan have been conducted since 1992 in both adults and children with a broad range of refractory malignancies and as many as 14 different dosing schedules."	( Review of phase I clinical studies with topotecan. Rowinsky, EK; Verweij, J, 1997)	0.83
" At this juncture, additional phase I and II trials are required to evaluate the toxicity and efficacy of topotecan in combination with other agents and address critical issues related to optimal drug dosing and sequencing."	( Topotecan in combination chemotherapy. Kaufmann, SH; Rowinsky, EK, 1997)	1.95
" Clinical studies with topotecan have not yielded as promising results, with response rates of approximately 7% to 10%, but modifications in dosing schedule or combinations with other agents may enhance antitumor activity."	( Topotecan in advanced colorectal cancer. Creemers, GJ, 1997)	2.05
" However, the degree of myelotoxicity that already occurs will preclude any substantially higher dosing with the weekly regimen."	( Randomized phase II study of two schedules of topotecan in previously treated patients with ovarian cancer: a National Cancer Institute of Canada Clinical Trials Group study. Beare, S; Bryson, P; Capstick, V; Drouin, P; Eisenhauer, E; Grimshaw, R; Hoskins, P; Roy, M; Stuart, G; Zee, B, 1998)	0.56
" Dosage and administration, status of clinical application, pharmacokinetics, pharmacodynamics and drug interactions are discussed."	( Clinical pharmacokinetics of camptothecin topoisomerase I inhibitors. Beijnen, JH; Herben, VM; Schellens, JH; Ten Bokkel Huinink, WW, 1998)	0.3
" Our hypothesis is that the camptothecins require a prolonged schedule of administration given continuously at low doses or frequent intermittent dosing schedules to be most effective."	( Camptothecins: a review of their development and schedules of administration. Muggia, FM; O'Leary, J, 1998)	0.3
" Results of the study were: (a) VN coatings, in a dose-dependent manner, inhibited topoisomerase (Topo)-induced apoptosis by up to 50% (optimal coating density, 500 ng/cm2); in contrast, fibronectin (FN), an ECM protein present in abundance in the brain, demonstrated no protection; (b) in a dose-response study, VN clearly conferred a survival advantage (LD50 of Topo: on VN, 120 ng/ml; on FN, 35 ng/ml); (c) the protective effect of VN was not due to enhanced cell adhesion or alterations in the cell cycle distribution; (d) both of the classic integrin receptors that bind VN (alpha(v)beta3, alpha(v)beta5) were capable of mediating this protective effect, because ligation of either of the two classic integrins conferred chemoresistance to Topo; and (e) chemoresistance observed with VN was associated with an increase in expression of two antiapoptotic proteins, Bcl-2 and Bcl-X(L), with a consequent increase in the ratios for Bcl-2:Bax and Bcl-X(L):Bax."	( Vitronectin, a glioma-derived extracellular matrix protein, protects tumor cells from apoptotic death. Dooley, NP; Gladson, CL; Kyritsis, AP; Rao, JS; Uhm, JH, 1999)	0.3
"Our aim was to compare and evaluate apoptosis formation as detected by propidium-iodide (PI)/annexin-V or PI/fluorescein-diacetate (FDA) as dose-response parameters in a human promyelocytic leukemia cell line, HL60."	( Comparative analysis of apoptosis in HL60 detected by annexin-V and fluorescein-diacetate. Bartkowiak, D; Baust, H; Högner, S; Nothdurft, W; Röttinger, EM, 1999)	0.3
" A dose-response model with a logit link function was used to investigate whether the combination of topotecan and vincristine resulted in greater than expected responses compared with the activity of the agents when administered alone."	( Synergy of topotecan in combination with vincristine for treatment of pediatric solid tumor xenografts. Cheshire, PJ; de Graaf, SS; George, EO; Houghton, PJ; Ma, M; Poquette, CA; Richmond, LB; Stewart, CF; Thompson, J, 1999)	0.91
" The type and degree of toxicity appeared to be related to the dosing schedule (number of days of consecutive treatment), but overall, oral topotecan appeared to be associated with less hematologic toxicity than the IV formulation."	( The evolving role of oral topotecan. Burris, HA, 1999)	0.81
" Serial plasma and pleural or ascitic fluid samples were collected during each dosing and analyzed by high-performance liquid chromatography for both the intact lactone form of topotecan and its ring-opened carboxylate form."	( Topotecan lacks third space sequestration. de Jonge, MJ; Gelderblom, H; Loos, WJ; Sparreboom, A; Verweij, J, 2000)	1.94
" A number of different dosing schedules are being investigated in clinical trials including oral administration, a daily infusion on 5- or 3-consecutive days and a continuous infusion for 21 days."	( [Topotecan: prospects for using it in combination therapy for ovarian carcinoma]. Scarfone, G, )	1.04
" The model can be used prospectively to obtain a revised and validated model that can then be used to design individualized dosing regimens."	( Population pharmacokinetic model for topotecan derived from phase I clinical trials. Baker, SD; Gallo, JM; Grochow, LB; Laub, PB; Rowinsky, EK, 2000)	0.58
" This review discusses the mechanism of action of TMZ and strategies for overcoming pathways of resistance to this promising agent, including the use of TMZ in combination with other chemotherapeutic agents or radiation therapy, and exploration of alternate dosing schedules."	( Future directions in the treatment of malignant gliomas with temozolomide. Prados, MD, 2000)	0.31
"Anticancer drugs still are dosed based on the body-surface area (BSA) of the individual patient, although the BSA is not the main predictor of the clearance for the majority of drugs."	( Inter- and intrapatient variability in oral topotecan pharmacokinetics: implications for body-surface area dosage regimens. de Jonge, MJ; Gelderblom, H; Loos, WJ; Sparreboom, A; Verweij, J, 2000)	0.57
" Dosage adjustments of orally administered topotecan should not be necessary in patients who are pretreated with ranitidine, an H2 antagonist, or another agent that comparably raises gastric pH."	( Pretreatment with ranitidine does not reduce the bioavailability of orally administered topotecan. Akhtar, S; Beckman, RA; Doyle, E; Fields, SZ; Mould, DR; Wright, J, 2000)	0.79
" We tested the hypothesis that much higher dosing would meet critical goals of salvage therapy: antitumor effect and a lack of toxicity to key organs, so as not to preclude subsequent consolidative treatments needed for cure."	( Pilot study of topotecan and high-dose cyclophosphamide for resistant pediatric solid tumors. Cheung, NK; Kramer, K; Kushner, BH; Meyers, PA; Wollner, N, 2000)	0.66
" The released T-2513 levels in the liver and tumor of the tumor-bearing rats dosed with each conjugate increased with the length of Gly linker, suggesting a good in vitro to in vivo relationship."	( Determinants for the drug release from T-0128, camptothecin analogue-carboxymethyl dextran conjugate. Harada, M; Okuno, S; Sakakibara, H; Suzuki, T; Yano, T, 2000)	0.31
" Patients received an assigned topotecan dosage in combination with fixed doses of carboplatin and thiotepa, followed by autologous hematopoietic stem cells infusion."	( Phase I topotecan preparative regimen for high-risk neuroblastoma, high-grade glioma, and refractory/recurrent pediatric solid tumors. Gooley, T; Hawkins, D; Lindsley, K; Matthay, KK; Park, JR; Sanders, JE; Slattery, J; Villablanca, JG, 2000)	1.03
" Prospective studies of pharmacokinetically guided versus surface area-based administration should be performed to validate pharmacokinetic-pharmacodynamic relationships and to facilitate optimal dosage of anticancer agents in the clinic."	( Pharmacokinetically guided administration of chemotherapeutic agents. Beijnen, JH; Mathôt, RA; Schellens, JH; van den Bongard, HJ, 2000)	0.31
" Animal weights during treatment were markedly reduced by intraperitoneal dosing (n = 6) but not by low-dose intracerebral clysis (32 microg/kg/d for 5 d; n = 6)."	( Tissue distribution and antitumor activity of topotecan delivered by intracerebral clysis in a rat glioma model. Bruce, JN; Chakrabarti, I; Fine, RL; Hall, JS; Kaiser, MG; Parsa, AT, 2000)	0.57
" These studies provide compelling justification for further preclinical testing to formally evaluate toxicity and efficacy with variable dosing schedules."	( Tissue distribution and antitumor activity of topotecan delivered by intracerebral clysis in a rat glioma model. Bruce, JN; Chakrabarti, I; Fine, RL; Hall, JS; Kaiser, MG; Parsa, AT, 2000)	0.57
" Severe hematologic toxicity was more common with topotecan and was more likely to be associated with dosage modification, or growth factor or blood product utilization."	( Recurrent epithelial ovarian carcinoma: a randomized phase III study of pegylated liposomal doxorubicin versus topotecan. Fleagle, JT; Gordon, AN; Gore, ME; Guthrie, D; Lacave, AJ; Parkin, DE, 2001)	0.78
"The comparable efficacy, favorable safety profile, and convenient dosing support the role of PLD as a valuable treatment option in this patient population."	( Recurrent epithelial ovarian carcinoma: a randomized phase III study of pegylated liposomal doxorubicin versus topotecan. Fleagle, JT; Gordon, AN; Gore, ME; Guthrie, D; Lacave, AJ; Parkin, DE, 2001)	0.52
" Maximum tolerated dosage (MTD) for the topotecan and irinotecan combination was defined as that which permitted 4 weeks of topotecan and irinotecan administration with G-CSF at or near the dose intensity reported for each single agent."	( Phase I clinical trial of weekly combined topotecan and irinotecan. Lokich, J, 2001)	0.84
" The carboplatin dosage was escalated from an AUC of 4 to 5 to 6 (Calvert formula)."	( Phase I and pharmacologic study of sequential topotecan, carboplatin, and etoposide. Miller, AA; Niell, HB, )	0.39
"The purpose of this study was to define the maximum tolerated dose (MTD) of topotecan given as escalating doses combined to a fixed dosage of carboplatin in late relapsing ovarian carcinomas."	( A phase I/II study of topotecan in combination with carboplatin in recurrent epithelial ovarian cancer. Bolis, G; Guarnerio, P; Parazzini, F; Polverino, GP; Rosa, C; Scarfone, G; Sciatta, C, 2001)	0.85
" A multicentric clinical trial with individualized dosing of topotecan was performed in patients with platinum-refractory ovarian cancer."	( Individual adaptive dosing of topotecan in ovarian cancer. Albin, N; Bugat, R; Canal, P; Chatelut, E; Culine, S; Déporte-Féty, R; Goupil, A; Laguerre, B; Lokiec, F; Montazeri, A; Pinguet, F, 2002)	0.84
"Phase I studies of nogitecan hydrochloride given by single and 5-day repeat dosing were carried out in patients with various solid tumors at 15 medical institutions in Japan."	( Phase I studies of nogitecan hydrochloride for Japanese. Fukuoka, M; Furuse, K; Hasegawa, K; Hino, M; Horikoshi, N; Kanamaru, R; Kimura, I; Kinoshita, H; Kobayashi, K; Niitani, H; Noda, K; Taguchi, T; Takeuchi, K; Yoneda, S, 2002)	0.31
" The plasma concentration of nogitecan hydrochloride increased with increasing dose, and the half-life after single dosing ranged from 3 to 5h."	( Phase I studies of nogitecan hydrochloride for Japanese. Fukuoka, M; Furuse, K; Hasegawa, K; Hino, M; Horikoshi, N; Kanamaru, R; Kimura, I; Kinoshita, H; Kobayashi, K; Niitani, H; Noda, K; Taguchi, T; Takeuchi, K; Yoneda, S, 2002)	0.31
" These preliminary data suggest that weekly topotecan is active; further evaluations are planned to confirm the activity and therapeutic index and to determine optimal dosing of a weekly schedule."	( Weekly topotecan: an alternative to topotecan's standard daily x 5 schedule? Rowinsky, EK, 2002)	1.03
" 34 advanced cancer patients and 186 cycles were evaluable for toxicity over five dosing levels."	( Topotecan preceded by oxaliplatin using a 3 week schedule: a phase I study in advanced cancer patients. Goldwasser, F; Gross-Goupil, M; Hasbini, A; Lokiec, F; Lopez, G; Misset, JL; Romain, D; Tigaud, JM, 2002)	1.76
" However, the optimal dosing for topotecan has not been established."	( Alternate dosing schedules for topotecan in the treatment of recurrent ovarian cancer. Morris, R; Munkarah, A, 2002)	0.88
" Hematologic toxicity was significant and resulted in incomplete etoposide dosing in half of all cycles in 16/22 patients."	( Phase II study of sequential topotecan and etoposide in patients with intermediate grade non-Hodgkin's lymphoma: a National Cancer Institute of Canada Clinical Trials Group study. Couban, S; Crump, M; Eisenhauer, E; Gluck, S; Hoskins, P; Maksymiuk, A; Matthews, S; Meyer, R; Rudinskas, L; Zanke, B, 2002)	0.61
" Dose-limiting thrombocytopenia at week 3 necessitated less frequent gemcitabine dosing (days 1 and 15 of each cycle)."	( A dose-escalation study of weekly topotecan, cisplatin, and gemcitabine front-line therapy in patients with inoperable non-small cell lung cancer. Biggs, DD; Grubbs, SS; Guarino, MJ; Himelstein, AL; Hogaboom, K; Schneider, CJ; Tilak, S, 2002)	0.59
"Protracted topotecan dosing using a pharmacokinetic strategy was possible in this heavily pretreated group of children."	( A pilot study of protracted topotecan dosing using a pharmacokinetically guided dosing approach in children with solid tumors. Gajjar, A; Houghton, PJ; Kirstein, MN; Liu, T; Santana, VM; Stewart, CF; Tan, M; Zamboni, WC, 2003)	1
" The goal is to predict a dosage regimen with controlled toxicity."	( Population pharmacokinetics/pharmacodynamics relationships of an anticancer drug. Ané, C; Concordet, D, 2003)	0.32
" Topotecan administered by continuous infusion demonstrated response rates comparable to other dosing schedules with minimal hematologic toxicity."	( The use of continuous infusion topotecan in persistent and recurrent ovarian cancer. Berek, JS; Elkas, JC; Holschneider, CH; Katz, B; Li, AJ; Louie, R; McGonigle, KF, )	1.33
" Among the newer agents available for the experimental treatment arms, three stood out-gemcitabine, polyethylene-glycol (PEG)-liposomal doxorubicin, and topotecan-based on evidence of their activity demonstrated in previous phase I and II trials and, with appropriate dosage modifications, manageable toxicity when used in combination with platinum."	( Clinical trials of newer regimens for treating ovarian cancer: the rationale for Gynecologic Oncology Group Protocol GOG 182-ICON5. Bookman, M; Copeland, LJ; Trimble, E, 2003)	0.52
" The main toxicity associated with topotecan when used in the standard 5-day dosing schedule is myelosuppression, which is generally predictable, reversible, noncumulative, and manageable."	( Clinical experience with topotecan in relapsed ovarian cancer. Herzog, TJ, 2003)	0.9
" Alternative dosing schedules also show promise."	( Weekly topotecan in the management of ovarian cancer. Morris, RT, 2003)	0.77
" Topotecan tolerability and convenience may be improved by employing a lower dose, shorter schedule, 21-day continuous infusion or weekly dosing in relapsed/refractory disease."	( Workshop: options for therapy in ovarian cancer. Herzog, TJ; Holloway, RW; Stuart, GC, 2003)	1.23
" Alternate dosing strategies have sought to improve toxicity."	( Phase II evaluation of three-day topotecan in recurrent platinum-sensitive ovarian carcinoma: a gynecologic oncology group study. Blessing, JA; Lentz, SS; McMeekin, DS; Miller, DS, 2003)	0.6
" Preclinical data supported intermittent dosing with topotecan and clinical studies with weekly dosing in ovarian cancer have indicated reduced myelosuppression compared with the 5-day regimen."	( Weekly topotecan in the management of lung cancer. Treat, J, 2003)	1.02
" Dose-response curves were interpolated to provide 50% lethal concentrations (LC(50))."	( Ex vivo analysis of topotecan: advancing the application of laboratory-based clinical therapeutics. Evans, SS; Harper, SM; Nagourney, RA; Radecki, S; Sommers, BL, 2003)	0.64
"Topotecan dosing considerations and alternative dosing schedules to reduce and manage myelosuppression during the treatment of relapsed ovarian cancer were reviewed."	( Topotecan dosing guidelines in ovarian cancer: reduction and management of hematologic toxicity. Armstrong, DK, 2004)	3.21
" A schedule in which the daily dose is split so that dosing is performed twice daily may be superior to the current schedule."	( Oral topotecan in children with recurrent or progressive high-grade glioma: a Phase I/II study by the German Society for Pediatric Oncology and Hematology. Albani, M; Bucsky, P; Emser, A; Erdlenbruch, B; Gnekow, A; Kühl, J; Längler, A; Peters, O; Völpel, S; Wagner, S; Wolff, JE, 2004)	0.84
" Partial responses were documented in three patients with ovarian cancer dosed below the MTD."	( Phase I and pharmacokinetic study of the combination of topotecan and ifosfamide administered intravenously every 3 weeks. Ambaum, B; Beijnen, JH; Groenewegen, G; Herben, VM; Jansen, S; Kerbusch, T; Mathôt, RA; Rosing, H; Schellens, JH; Swart, M; ten Bokkel Huinink, WW; Voest, EE, 2004)	0.57
"Treatment of recurrent ovarian cancer with low-dose continuous infusion of topotecan over 14 days demonstrated response rates comparable to other dosing schedules with minimal toxicity in a preliminary series of 12 patients."	( Topotecan as a continuous infusion over 14 days in recurrent ovarian cancer patients. Denschlag, D; Gitsch, G; Hörig, K; Kissel, C; Tempfer, C; Watermann, D, )	1.8
"To assess the antitumor efficacy of pharmacokinetically guided topotecan dosing in previously untreated patients with medulloblastoma and supratentorial primitive neuroectodermal tumors, and to evaluate plasma and CSF disposition of topotecan in these patients."	( Results of a phase II upfront window of pharmacokinetically guided topotecan in high-risk medulloblastoma and supratentorial primitive neuroectodermal tumor. Ashley, D; Chintagumpala, M; Fouladi, M; Gajjar, A; Houghton, PJ; Iacono, LC; Kellie, SJ; Kirstein, MN; Seele, LG; Stewart, CF; Wallace, D; Zamboni, WC, 2004)	0.8
" After 10 patients were enrolled, the infusion was modified to 4 hours, with dosage individualization."	( Results of a phase II upfront window of pharmacokinetically guided topotecan in high-risk medulloblastoma and supratentorial primitive neuroectodermal tumor. Ashley, D; Chintagumpala, M; Fouladi, M; Gajjar, A; Houghton, PJ; Iacono, LC; Kellie, SJ; Kirstein, MN; Seele, LG; Stewart, CF; Wallace, D; Zamboni, WC, 2004)	0.56
" Pharmacokinetically guided dosing achieved the target plasma AUC in the majority of patients."	( Results of a phase II upfront window of pharmacokinetically guided topotecan in high-risk medulloblastoma and supratentorial primitive neuroectodermal tumor. Ashley, D; Chintagumpala, M; Fouladi, M; Gajjar, A; Houghton, PJ; Iacono, LC; Kellie, SJ; Kirstein, MN; Seele, LG; Stewart, CF; Wallace, D; Zamboni, WC, 2004)	0.56
" Recently, topotecan has been studied on a weekly dosing schedule for the treatment of ovarian cancer and found to have efficacy with reduced toxicity."	( Weekly topotecan for recurrent endometrial cancer: a case series and review of the literature. Aghajanian, C; Dupont, J; Sabbatini, P; Traina, TA, 2004)	1.17
" This review aims to evaluate the role of topotecan in the management of this disease by considering the properties of the compound, the clinical efficacy in Phase II and III studies, its role in first- and second-line treatment and alternative dosing strategies to overcome toxicity."	( Review of the use of topotecan in ovarian carcinoma. Ahmad, T; Gore, M, 2004)	0.91
" Alternative dosing regimens (lower dose, weekly) and the introduction of an oral formulation may expand the use of topotecan as a single agent and in combination therapy in the second- and first-line treatment of this disease."	( Topotecan in the treatment of recurrent small cell lung cancer: an update. Ardizzoni, A, 2004)	1.98
" Herein, the future role of topotecan in the first- and second-line treatment of NSCLC and the potential role of resistance mechanisms obtained from in vivo dose-response studies in designing future combination regimens are discussed."	( Update on the role of topotecan in the treatment of non-small cell lung cancer. Stewart, DJ, 2004)	0.93
"Data were obtained from 59 patients who underwent drug monitoring for individual dosing of topotecan."	( Serum cystatin C is a better marker of topotecan clearance than serum creatinine. Canal, P; Chatelut, E; Delord, JP; Hoppe, A; Malard, L; Séronie-Vivien, S; Thomas, F, 2005)	0.82
" It deserves to be further explored as a promising covariate for drug dosing as well as selection criteria for clinical studies of drugs eliminated mainly or partially by the kidney."	( Serum cystatin C is a better marker of topotecan clearance than serum creatinine. Canal, P; Chatelut, E; Delord, JP; Hoppe, A; Malard, L; Séronie-Vivien, S; Thomas, F, 2005)	0.6
"We performed a phase I study of two fixed dosing schemes of cisplatin, a DNA cross-linker, with intravenous escalating topotecan, a DNA-topoisomerase I inhibitor."	( Phase I trial of intravenous cisplatin-topotecan chemotherapy for three consecutive days in patients with advanced solid tumors: parallel topotecan escalation in two fixed platinum dosing schemes. Briasoulis, E; Karavassilis, V; Mauri, D; Pavlidis, N; Pentheroudakis, G; Rammou, D; Tzamakou, E, 2005)	0.81
"To estimate the response rate and toxicity associated with intravenous topotecan when it is administered on a protracted schedule according to a pharmacokinetically guided dosing approach to treat childhood high-risk neuroblastoma."	( Improved response in high-risk neuroblastoma with protracted topotecan administration using a pharmacokinetically guided dosing approach. Billups, CA; Davidoff, AM; Furman, WL; Hoffer, F; Houghton, PJ; Santana, VM; Stewart, CF, 2005)	0.8
" Weekly topotecan may be an appropriate treatment option for patients with recurrent ovarian cancer, especially heavily pretreated patients who might require dosing schedules with improved tolerability."	( Weekly topotecan in heavily pretreated patients with recurrent epithelial ovarian carcinoma. Azodi, M; Kelly, M; Makkenchery, A; McAlpine, J; O'Malley, DM; Rutherford, T; Schwartz, P; Tangir, J, 2005)	1.22
" We present a concise review of cancer chemotherapy dosing in the setting of liver dysfunction."	( Chemotherapy dosing in the setting of liver dysfunction. Eklund, JW; Mulcahy, MF; Trifilio, S, 2005)	0.33
" Dosing histories were collected using electronic monitoring devices fitted to medication vials."	( Pharmacokinetics, pharmacodynamics and adherence to oral topotecan in myelodysplastic syndromes: a Cancer and Leukemia Group B study. Grinblatt, DL; Hollis, D; Kastrissios, H; Klein, CE; Larson, RA; Miller, AA; Ratain, MJ; Rosner, GL; Yu, D, 2006)	0.58
" Pharmacokinetic parameter estimates did not differ between the once a day and twice a day dosing groups."	( Pharmacokinetics, pharmacodynamics and adherence to oral topotecan in myelodysplastic syndromes: a Cancer and Leukemia Group B study. Grinblatt, DL; Hollis, D; Kastrissios, H; Klein, CE; Larson, RA; Miller, AA; Ratain, MJ; Rosner, GL; Yu, D, 2006)	0.58
" Significant interpatient variability in the topotecan systemic exposure results when it is dosed based on body surface area (mg/m2)."	( A phase I trial defining the maximum tolerated systemic exposure of topotecan in combination with Carboplatin and Etoposide in extensive stage small cell lung cancer. Donahue, A; Faucette, S; Gillenwater, HH; Kirstein, MN; Lindley, C; McCune, JS; Moore, D; Shord, S; Socinski, MA; Stewart, CF; Zamboni, WC, 2005)	0.82
" Topotecan was administered as a 30-minute infusion either on Days 1-5 or Days 1-3 and the dosage was individualized to attain a topotecan lactone AUC range (ng/mL*hr) in successive patient cohorts from 7 to 23; 24 to 36; 37 to 53; 54 to 66."	( A phase I trial defining the maximum tolerated systemic exposure of topotecan in combination with Carboplatin and Etoposide in extensive stage small cell lung cancer. Donahue, A; Faucette, S; Gillenwater, HH; Kirstein, MN; Lindley, C; McCune, JS; Moore, D; Shord, S; Socinski, MA; Stewart, CF; Zamboni, WC, 2005)	1.47
" Analysis of neutrophil and platelet nadirs and dosing for each course of therapy showed no apparent evidence of cumulative neutropenia or thrombocytopenia."	( Hematologic safety and tolerability of topotecan in recurrent ovarian cancer and small cell lung cancer: an integrated analysis. Armstrong, DK; Lane, S; Levin, J; Poulin, R; Spriggs, D, 2005)	0.6
" Food and Drug Administration-approved dosage and schedule."	( Topotecan: weighing in when there are many options. Penson, RT; Seiden, MV, 2005)	1.77
"These mechanistic models, including patient characteristics that influence drug-specific parameters, form the rationale basis for more tailored dosing of individual patients or subgroups to minimize the risk of infection and thus might contribute to a more successful therapy."	( Population pharmacokinetic-pharmacodynamic model for neutropenia with patient subgroup identification: comparison across anticancer drugs. Chatelut, E; Henningsson, A; Karlsson, MO; Kloft, C; Wallin, J, 2006)	0.33
" However, this treatment requires the use of Filgrastim and attenuated dosing of topotecan in both a 5-day and 3-day topotecan infusion schedule."	( A phase I study of paclitaxel, topotecan, cisplatin and Filgrastim in patients with newly diagnosed advanced ovarian epithelial malignancies: a Gynecologic Oncology Group study. Armstrong, DK; Bookman, MA; Bristow, RE; McGuire, W; Schilder, JM, 2007)	0.85
"Topotecan combined with PE regimen with this schedule and dosage does not seem to provide any benefit in terms of response and survival in ED-SCLC patients and does not deserve further studies."	( Addition of topotecan to standard cisplatin/etoposide combination in patients with extended stage small cell lung carcinoma. Aydiner, A; Camlica, H; Derin, D; Guney, N; Tas, F; Topuz, E, 2007)	2.16
" PEG-liposomal doxorubicin was given intravenously at a dosage of 30-40 mg/m(2) over 4 h once every 4 weeks."	( Pegylated-liposomal doxorubicin and oral topotecan in eight children with relapsed high-grade malignant brain tumors. Fels, C; Hau, P; Janssen, G; Liebeskind, AK; Peters, O; Sauerbrey, A; Suttorp, M; Wagner, S; Wolff, JE, 2008)	0.61
"Different dosing regimens of S-CKD602, free CKD-602 and topotecan were compared for antitumor activity in female athymic nude mice bearing human A375 melanoma, ES-2 ovarian, H82 SCLC or HT-29 colon tumor xenografts."	( STEALTH liposomal CKD-602, a topoisomerase I inhibitor, improves the therapeutic index in human tumor xenograft models. Chen, JY; Conway, C; Pena, RL; Yu, NY, )	0.38
" In A375 tumors, once-weekly dosing of S-CKD602 was superior to once every 2 weeks or twice weekly schedules."	( STEALTH liposomal CKD-602, a topoisomerase I inhibitor, improves the therapeutic index in human tumor xenograft models. Chen, JY; Conway, C; Pena, RL; Yu, NY, )	0.13
" We found that TPT-induced toxicity increased dose-dependently for each mode of dosing investigated."	( Mathematical modeling of topotecan pharmacokinetics and toxicodynamics in mice. Balthasar, JP; Chen, J; Lu, Q, 2007)	0.64
" Additionally, dosing topotecan based on the covariate model led to a more accurate and precise estimation topotecan systemic exposure compared with a fixed dosing approach, and could be a tool to assist clinicians to individualize topotecan dosing."	( Population pharmacokinetic analysis of topotecan in pediatric cancer patients. Freeman, BB; Gajjar, A; Iacono, LC; Panetta, JC; Santana, VM; Schaiquevich, P; Stewart, CF, 2007)	0.92
" Considerable hematologic toxicities have been reported with topotecan dosed for 5 consecutive days in combination with vinorelbine."	( Phase I dose escalation study of vinorelbine and topotecan combination chemotherapy in patients with recurrent lung cancer. Beldner, MA; Chaudhary, U; Garrett-Mayer, E; Green, MR; Kraft, AS; Meyer, ML; Montero, AJ; Sherman, CA, 2007)	0.84
" The topotecan dosage was individualized to attain a topotecan lactone area under the plasma concentration-time curve between 80 and 120 ng/mL h and given over a protracted schedule (i."	( Using pharmacokinetic and pharmacodynamic modeling and simulation to evaluate importance of schedule in topotecan therapy for pediatric neuroblastoma. Panetta, JC; Santana, VM; Schaiquevich, P; Stewart, CF, 2008)	1.07
") topotecan studies, 20 mg/m(2) dosing was tolerable."	( Phase 2 study of intraperitoneal topotecan as consolidation chemotherapy in ovarian and primary peritoneal carcinoma. Malpass, TW; McGonigle, KF; Muntz, HG; Robertson, MD; Weiden, PL, 2008)	1.35
"To review the role of topotecan in the treatment of advanced and relapsed ovarian cancer, and the efficacy and safety of novel dosing regimens and formulations of topotecan."	( Current role and future aspects of topotecan in relapsed ovarian cancer. Oskay-Ozcelik, G; Sehouli, J, 2009)	0.94
" A number of alternative dosing regimens and formulations have been investigated in an attempt to improve the toxicity profile of topotecan without compromising anti-tumour activity."	( Current role and future aspects of topotecan in relapsed ovarian cancer. Oskay-Ozcelik, G; Sehouli, J, 2009)	0.83
"Individualization of topotecan dosing reduces inter-patient variability in topotecan exposure, presumably reducing toxicity and increasing efficacy."	( Application of a highly specific and sensitive fluorescent HPLC method for topotecan lactone in whole blood. Bai, F; Fraga, CH; Hubbard, KE; Miller, L; Panetta, JC; Schaiquevich, P; Stewart, CF, 2009)	0.9
"5 and 15 mg/kg; weekly) dosing regimens reduced tumor growth in dose-finding experiments, but significant morbidity and mortality was observed with higher doses."	( Anti-angiogenic properties of metronomic topotecan in ovarian carcinoma. Chandra, J; Coleman, RL; Danes, CG; Gershenson, DM; Han, LY; Jaffe, RB; Kamat, AA; Kim, HS; Lin, YG; Mangala, LS; Merritt, WM; Nick, AM; Shahzad, MM; Sood, AK; Spannuth, WA; Stone, RL, 2009)	0.62
"The MTD was not reached in Stratum 1, but a DLT occurred at the lowest cladribine dosage (9."	( Combination of cladribine plus topotecan for recurrent or refractory pediatric acute myeloid leukemia. Crews, KR; Inaba, H; Pounds, S; Pui, CH; Razzouk, BI; Ribeiro, RC; Rubnitz, JE; Stewart, CF; Yang, S, 2010)	0.65
" Further studies using alternative dose levels could help define an optimal dosing schedule for this treatment combination in patients with platinum-sensitive recurrent disease."	( An open-label, single-arm Phase II study of intravenous weekly (Days 1 and 8) topotecan in combination with carboplatin (Day 1) every 21 days as second-line therapy in patients with platinum-sensitive relapsed ovarian cancer. Hartney, J; Lane, S; Legenne, P; Monk, BJ; Provencher, D; Rose, PG, 2011)	0.6
" Grade 3/4 neutropenia rate was 93% with daily×5 dosing and 28% for weekly treatment."	( A phase II study of two topotecan regimens evaluated in recurrent platinum-sensitive ovarian, fallopian tube or primary peritoneal cancer: a Gynecologic Oncology Group Study (GOG 146Q). DeBernardo, RL; DeGeest, K; Herzog, TJ; Lentz, SS; Mutch, D; O'Malley, D; Shahin, M; Sill, MW; Walker, JL; Weiner, SA, 2011)	0.68
" Sublethal dosage of NSC 19630 and the chemotherapy drug topotecan acted synergistically to inhibit cell proliferation and induce DNA damage."	( Inhibition of helicase activity by a small molecule impairs Werner syndrome helicase (WRN) function in the cellular response to DNA damage or replication stress. Aggarwal, M; Brosh, RM; Shoemaker, RH; Sommers, JA, 2011)	0.61
" 3a and 3b demonstrated significant brain penetration when dosed orally in mice."	( 14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment. Ahluwalia, D; Bhupathi, D; Cai, X; Duan, JX; Hart, CP; Huang, H; Jiao, H; Jung, B; Jung, D; Liu, Q; Matteucci, J; Matteucci, M; Meng, F; Sun, JD, 2011)	0.37
" Subsequently Genz-644282 was tested at 4, 3, 2, and 1 mg/kg in 3 models to assess the dose-response relationship."	( Testing of the topoisomerase 1 inhibitor Genz-644282 by the pediatric preclinical testing program. Anders Kolb, E; Billups, CA; Carol, H; Gorlick, R; Houghton, PJ; Kang, MH; Keir, ST; Lock, R; Madden, SL; Maris, JM; Morton, CL; Reynolds, CP; Smith, MA; Teicher, BA; Zhang, MX, 2012)	0.38
") weekly dosing resulted in low-grade 3/4 toxicity but an overall response rate (ORR) < 10%."	( A phase II study of higher dose weekly topotecan in relapsed small-cell lung cancer. Arrowsmith, ER; Burris, HA; Clark, BL; Greco, FA; Hainsworth, JD; Shipley, DL; Spigel, DR; Whorf, RC, 2011)	0.64
"The objective of this study was to determine the antitumor effects of alternate dosing schedules of topotecan in prostate cancer."	( Enhanced antitumor activity of low-dose continuous administration schedules of topotecan in prostate cancer. Aljuffali, IA; Arnold, RD; Costyn, LJ; Cummings, BS; Mock, JN; Nagy, T; Nguyen, H, 2011)	0.81
"4-18 fold, after 72 hr) was observed following metronomic dosing compared to conventional dosing administration in both cell lines."	( Enhanced antitumor activity of low-dose continuous administration schedules of topotecan in prostate cancer. Aljuffali, IA; Arnold, RD; Costyn, LJ; Cummings, BS; Mock, JN; Nagy, T; Nguyen, H, 2011)	0.6
"The cytotoxicity of topotecan after conventional or metronomic dosing was determined by examining cellular morphology, mitochondrial enzymatic activity (MTT), total cellular protein (SRB), annexin V and propidium iodine (PI) staining, cell cycle and western blot analysis in human prostate cancer cell lines (PC-3 and LNCaP) and the effects metronomic or continuous infusion on tumor growth in an in vivo tumor xenograft model."	( Enhanced antitumor activity of low-dose continuous administration schedules of topotecan in prostate cancer. Aljuffali, IA; Arnold, RD; Costyn, LJ; Cummings, BS; Mock, JN; Nagy, T; Nguyen, H, 2011)	0.92
"These data support the hypothesis that low-dose continuous administration of topotecan increases potency compared to conventional dosing in prostate cancer."	( Enhanced antitumor activity of low-dose continuous administration schedules of topotecan in prostate cancer. Aljuffali, IA; Arnold, RD; Costyn, LJ; Cummings, BS; Mock, JN; Nagy, T; Nguyen, H, 2011)	0.83
"In vitro dose-response study of topotecan and pazopanib was conducted on several neuroblastoma, osteosarcoma, and rhabdomyosarcoma cell lines."	( Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Baruchel, S; Kerbel, RS; Kumar, S; Man, S; Mokhtari, RB; Oliveira, ID; Sheikh, R; Wu, B; Xu, P; Yeger, H; Zhang, L, 2011)	1
" Pharmacokinetically guided topotecan dosing (target systemic exposure with area under the curve of 50 to 70 ng/mL/hr) was performed."	( Pilot induction regimen incorporating pharmacokinetically guided topotecan for treatment of newly diagnosed high-risk neuroblastoma: a Children's Oncology Group study. Cohn, SL; London, WB; Matthay, KK; Naranjo, A; Park, JR; Santana, VM; Scott, JR; Shaw, PJ; Stewart, CF, 2011)	0.9
" Once MTD was defined, we expanded this dosing cohort to include patients with high-risk lymphoma due to activity seen during dose escalation."	( Phase I Study of Topotecan, Ifosfamide, and Etoposide (TIME) with autologous stem cell transplant in refractory cancer: pharmacokinetic and pharmacodynamic correlates. Dawson, JL; Field, TL; Fields, KK; Goldstein, SC; Kim, J; Lush, RM; Maddox, BL; Neuger, AM; Partyka, JS; Perkins, JB; Simonelli, CE; Sullivan, DM, 2011)	0.71
"Individualization of the topotecan dosing can reduce inter-patient variability, toxicity, and at the same time increases chemotherapy efficacy."	( Topotecan exposure estimation in pediatric acute myeloid leukemia supported by LC-MS-based drug monitoring and pharmacokinetic analysis. Adamkiewicz-Drożyńska, E; Bączek, T; Balcerska, A; Belka, M; Konieczna, L; Maciejka-Kapuścińska, L; Niedźwiecki, M; Wachowiak, J; Wiśniewski, J, 2012)	2.13
"We performed a phase-1 pharmacokinetic optimal dosing study of intraventricular topotecan (IT), administered daily 5×, to determine whether, the maximum tolerated dose of IT topotecan was also the pharmacokinetic optimal dose."	( A phase-1 pharmacokinetic optimal dosing study of intraventricular topotecan for children with neoplastic meningitis: a Pediatric Brain Tumor Consortium study. Berg, SL; Blaney, SM; Boyett, J; Goldman, S; Gururangan, S; Kieran, MW; Kun, L; Onar-Thomas, A; Scorsone, K; Stewart, C; Su, J; Tagen, M, 2013)	0.85
" The dosing schedule appears to affect the toxicity profile of the drug."	( A systematic review on topoisomerase 1 inhibition in the treatment of metastatic breast cancer. Balslev, E; Brünner, N; Kümler, I; Nielsen, DL; Stenvang, J, 2013)	0.39
" No adjustment of low dose metronomic topotecan dosing is merited when used in conjunction with pazopanib."	( Combination metronomic oral topotecan and pazopanib: a pharmacokinetic study in patients with gynecological cancer. Harstead, KE; Stewart, CF; Throm, SL; Tillmanns, TD; Turner, DC, 2013)	0.95
"Patients with brain metastasis from lung cancer received concurrent chemotherapy and radiotherapy: conventional fractionated whole-brain irradiation, 2 fields/time, 1 fraction/day, 2 Gy/fraction, 5 times/week, and DT 40 Gy/20 fractions; for the patients with ≤ 3 lesions with diameter ≥ 2 cm, a three-dimensional (3-D) conformal localised boost was given to increase the dosage to 56-60 Gy; and during radiotherapy, concurrent chemotherapy with topotecan was given (the chemoradiotherapy group, CRT)."	( Phase II clinical trial of whole-brain irradiation plus three-dimensional conformal boost with concurrent topotecan for brain metastases from lung cancer. Cao, B; Chen, XJ; Ge, XH; Li, ZG; Lin, Q; Liu, ML; Liu, YE; Ren, XC; Wang, DY; Wang, YQ, 2013)	0.77
" Dose-response curves were constructed, and the combination index (CI) for drug interaction was calculated."	( Dasatinib (BMS-35482) interacts synergistically with docetaxel, gemcitabine, topotecan, and doxorubicin in ovarian cancer cells with high SRC pathway activation and protein expression. Adams, DJ; Grace, L; Jia, J; Murphy, SK; Nixon, AB; Secord, AA; Teoh, D, 2014)	0.63
"We attempted to investigate the safety and efficacy of alternative weekly topotecan dosing in a heavily pretreated Taiwanese population with recurrent epithelial ovarian cancer (EOC) and primary peritoneal carcinoma (PPC)."	( The use of weekly topotecan in the treatment of heavily pretreated recurrent epithelial ovarian and primary peritoneal cancer: the Kaohsiung Chang Gung experience. Chang Chien, CC; Fu, HC; Hu, CF; Lin, H; Ou, YC; Tsai, CC; Wu, CH, 2015)	0.98
"Topotecan administered as a weekly dosage (2."	( The use of weekly topotecan in the treatment of heavily pretreated recurrent epithelial ovarian and primary peritoneal cancer: the Kaohsiung Chang Gung experience. Chang Chien, CC; Fu, HC; Hu, CF; Lin, H; Ou, YC; Tsai, CC; Wu, CH, 2015)	2.19
"This phase I study evaluated the safety, tolerability, maximum tolerated dose (MTD) and pharmacokinetics of two dosing schedules of oral topotecan in combination with pazopanib in patients with advanced solid tumours."	( Phase I and pharmacological study of pazopanib in combination with oral topotecan in patients with advanced solid tumours. Devriese, LA; Giantonio, BJ; Kerklaan, BM; Lane, S; Langenberg, M; Legenne, P; Lolkema, MP; Mergui-Roelvink, M; Mykulowycz, K; Nol-Boekel, A; Schellens, JH; Smith, DA; Stoebenau, J; Voest, EE; Wissel, P; Witteveen, PO, 2015)	0.85
" An in silico pharmacodynamic model using established effects of each of these agents on the cell cycle was used to validate the regimen and to guide the dosing regimen."	( Novel phase I study combining G1 phase, S phase, and G2/M phase cell cycle inhibitors in patients with advanced malignancies. Gad, Y; Helgason, T; Hong, DS; Jain, RK; Kurzrock, R; Naing, A; Shi, NY; Wheler, J, 2015)	0.42
" On the basis of their unique antiangiogenic effects, we tested the efficacy of nab-paclitaxel, which stimulates thrombospondin-1, and topotecan, which inhibits hypoxia-inducible factor 1-α, at metronomic dosing for the treatment of ovarian carcinoma."	( Dual Metronomic Chemotherapy with Nab-Paclitaxel and Topotecan Has Potent Antiangiogenic Activity in Ovarian Cancer. Armaiz-Pena, GN; Coleman, RL; Dalton, HJ; Davis, AN; Hansen, JM; Langley, RR; Lin, YG; Merritt, WM; Nick, AM; Pradeep, S; Previs, RA; Sood, AK, 2015)	0.87
" Two dosing schedules of the novel indenoisoquinoline, indotecan (LMP400), were evaluated in patients with advanced solid tumors."	( Clinical and pharmacologic evaluation of two dosing schedules of indotecan (LMP400), a novel indenoisoquinoline, in patients with advanced solid tumors. Allen, D; Beumer, JH; Bonner, WM; Chen, A; Collins, J; Covey, JM; Doroshow, JH; Eiseman, JL; Gutierrez, M; Holleran, JL; Ji, J; Kinders, RJ; Kummar, S; Parchment, R; Pfister, TD; Pommier, Y; Redon, C; Rubinstein, L; Tomaszewski, J; Wang, L; Yutzy, W; Zhang, Y, 2016)	0.43
"We established the MTD of two dosing schedules for a novel TopI inhibitor, indotecan."	( Clinical and pharmacologic evaluation of two dosing schedules of indotecan (LMP400), a novel indenoisoquinoline, in patients with advanced solid tumors. Allen, D; Beumer, JH; Bonner, WM; Chen, A; Collins, J; Covey, JM; Doroshow, JH; Eiseman, JL; Gutierrez, M; Holleran, JL; Ji, J; Kinders, RJ; Kummar, S; Parchment, R; Pfister, TD; Pommier, Y; Redon, C; Rubinstein, L; Tomaszewski, J; Wang, L; Yutzy, W; Zhang, Y, 2016)	0.43
" This review discusses these problems and the means to overcome them, including modification of TLs using zwitterionic poly(carboxybetaine), prolongation in dosing interval (long-term therapy), and modified liposomal encapsulation techniques including active loading methods."	( Topotecan Liposomes: A Visit from a Molecular to a Therapeutic Platform. Hurkat, P; Jain, A; Jain, SK; Saraf, S, 2016)	1.88
" This study aims to evaluate the success of the pharmacokinetically (PK) guided dosing process, which was used to achieve a target topotecan area under the concentration-time curve (AUC)."	( Determining success rates of the current pharmacokinetically guided dosing approach of topotecan in pediatric oncology patients. Gajjar, A; Mitchell, AB; Santana, VM; Stewart, CF; Vasilyeva, A, 2019)	0.94
"Patients received an empiric topotecan dosage on the first day; the topotecan lactone AUC was determined, and based upon these values the topotecan dosage was adjusted."	( Determining success rates of the current pharmacokinetically guided dosing approach of topotecan in pediatric oncology patients. Gajjar, A; Mitchell, AB; Santana, VM; Stewart, CF; Vasilyeva, A, 2019)	1.03
" The empiric dosing success rate was 35."	( Determining success rates of the current pharmacokinetically guided dosing approach of topotecan in pediatric oncology patients. Gajjar, A; Mitchell, AB; Santana, VM; Stewart, CF; Vasilyeva, A, 2019)	0.74
"The low empiric dosing success rate indicates that additional studies are needed to refine the initial topotecan dosage."	( Determining success rates of the current pharmacokinetically guided dosing approach of topotecan in pediatric oncology patients. Gajjar, A; Mitchell, AB; Santana, VM; Stewart, CF; Vasilyeva, A, 2019)	0.95
" 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)	0.91
"The addition of LCL161 to oral topotecan caused more myelosuppression when dosed together than what was associated with either drug alone."	( A Phase Ib Dose-Escalation Study of LCL161 Plus Oral Topotecan for Patients With Relapsed/Refractory Small Cell Lung Cancer and Select Gynecologic Malignancies. Aljumaily, R; Burris Iii, HA; Johnson, ML; Jones, SF; Patel, MR; Spigel, DR, 2023)	1.45
"Maximum tolerable dosing (MTD) of chemotherapeutics has long been the gold standard for aggressive malignancies."	( Extended Exposure Topotecan Significantly Improves Long-Term Drug Sensitivity by Decreasing Malignant Cell Heterogeneity and by Preventing Epithelial-Mesenchymal Transition. Arnold, RD; Bird, RC; Davis, JT; Ghosh, TM; Mazumder, S; Mitra, A, 2023)	1.24
"A simple single-sample approach during topotecan therapy could guide dosing for patients, resulting in more patients reaching target attainment."	( Topotecan clearance based on a single sample and a population pharmacokinetic model: Application to a pediatric high-risk neuroblastoma clinical trial. Campagne, O; Daryani, VM; Gajjar, AJ; Naranjo, A; Park, JR; Stewart, CF; Wu, H; Wu, J, 2023)	2.62

Role	Description
EC 5.99.1.2 (DNA topoisomerase) inhibitor	A topoisomerase inhibitor that inhibits the bacterial enzymes of the DNA topoisomerases, Type I class (EC 5.99.1.2) that catalyze ATP-independent breakage of one of the two strands of DNA, passage of the unbroken strand through the break, and rejoining of the broken strand. These bacterial enzymes reduce the topological stress in the DNA structure by relaxing negatively, but not positively, supercoiled DNA.
antineoplastic agent	A substance that inhibits or prevents the proliferation of neoplasms.
[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]

Class	Description
pyranoindolizinoquinoline
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Fumarate hydratase	Homo sapiens (human)	Potency	0.0418	0.0030	8.7949	48.0869	AID1347053
EWS/FLI fusion protein	Homo sapiens (human)	Potency	0.0262	0.0013	10.1577	42.8575	AID1259252; AID1259253; AID1259255; AID1259256
polyprotein	Zika virus	Potency	0.0418	0.0030	8.7949	48.0869	AID1347053
tyrosine-protein kinase Yes	Homo sapiens (human)	Potency	61.3494	0.0000	5.0182	79.2586	AID686947
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Solute carrier family 22 member 2	Homo sapiens (human)	IC50 (µMol)	61.0000	0.4000	3.1000	9.7000	AID721751
Cytochrome P450 3A4	Homo sapiens (human)	IC50 (µMol)	1.5211	0.0001	1.7536	10.0000	AID625251
DNA topoisomerase 1	Homo sapiens (human)	IC50 (µMol)	3.3000	0.0210	1.8626	10.0000	AID1544048; AID1544076; AID1740932; AID1740933; AID1811235; AID210946; AID241607; AID56567; AID56570
DNA topoisomerase 2-alpha	Homo sapiens (human)	IC50 (µMol)	0.6050	0.4800	4.3564	9.9400	AID1600550; AID1600554
DNA topoisomerase 2-beta	Homo sapiens (human)	IC50 (µMol)	0.6050	0.0300	2.7716	7.8000	AID1600550; AID1600554
DNA topoisomerase 1	Mus musculus (house mouse)	IC50 (µMol)	20.0000	4.0000	4.0000	4.0000	AID211118
Hypoxia-inducible factor 1-alpha	Homo sapiens (human)	IC50 (µMol)	1.5300	0.0007	2.4652	9.2100	AID527977; AID527978
Multidrug and toxin extrusion protein 2	Homo sapiens (human)	IC50 (µMol)	8.6000	0.1600	3.9571	8.6000	AID721752
Multidrug and toxin extrusion protein 1	Homo sapiens (human)	IC50 (µMol)	1.3000	0.0100	2.7656	10.0000	AID721754
Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)	IC50 (µMol)	0.1700	0.0040	1.9666	10.0000	AID679628
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
NPYLR7B	Aedes aegypti (yellow fever mosquito)	EC50 (µMol)	0.7690	0.0390	2.2899	18.3000	AID1259426
DNA topoisomerase 1	Homo sapiens (human)	EC50 (µMol)	0.0627	0.0500	0.3359	2.0150	AID714170; AID714171
DNA topoisomerase 1	Homo sapiens (human)	Kd	0.0265	0.0265	0.0265	0.0265	AID610760
Hypoxia-inducible factor 1-alpha	Homo sapiens (human)	EC50 (µMol)	0.0713	0.0200	1.2990	5.0100	AID333717
Endothelial PAS domain-containing protein 1	Homo sapiens (human)	EC50 (µMol)	0.0713	0.0200	0.9330	3.3000	AID333717
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
DNA topoisomerase 1	Homo sapiens (human)	CC50	3.2000	0.8000	1.2029	3.2000	AID56562
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
activation of cysteine-type endopeptidase activity involved in apoptotic process	Solute carrier family 22 member 2	Homo sapiens (human)
positive regulation of gene expression	Solute carrier family 22 member 2	Homo sapiens (human)
organic cation transport	Solute carrier family 22 member 2	Homo sapiens (human)
monoatomic cation transport	Solute carrier family 22 member 2	Homo sapiens (human)
neurotransmitter transport	Solute carrier family 22 member 2	Homo sapiens (human)
serotonin transport	Solute carrier family 22 member 2	Homo sapiens (human)
body fluid secretion	Solute carrier family 22 member 2	Homo sapiens (human)
organic cation transport	Solute carrier family 22 member 2	Homo sapiens (human)
quaternary ammonium group transport	Solute carrier family 22 member 2	Homo sapiens (human)
prostaglandin transport	Solute carrier family 22 member 2	Homo sapiens (human)
amine transport	Solute carrier family 22 member 2	Homo sapiens (human)
putrescine transport	Solute carrier family 22 member 2	Homo sapiens (human)
spermidine transport	Solute carrier family 22 member 2	Homo sapiens (human)
acetylcholine transport	Solute carrier family 22 member 2	Homo sapiens (human)
choline transport	Solute carrier family 22 member 2	Homo sapiens (human)
dopamine transport	Solute carrier family 22 member 2	Homo sapiens (human)
norepinephrine transport	Solute carrier family 22 member 2	Homo sapiens (human)
xenobiotic transport	Solute carrier family 22 member 2	Homo sapiens (human)
epinephrine transport	Solute carrier family 22 member 2	Homo sapiens (human)
histamine transport	Solute carrier family 22 member 2	Homo sapiens (human)
serotonin uptake	Solute carrier family 22 member 2	Homo sapiens (human)
histamine uptake	Solute carrier family 22 member 2	Homo sapiens (human)
norepinephrine uptake	Solute carrier family 22 member 2	Homo sapiens (human)
thiamine transmembrane transport	Solute carrier family 22 member 2	Homo sapiens (human)
purine-containing compound transmembrane transport	Solute carrier family 22 member 2	Homo sapiens (human)
amino acid import across plasma membrane	Solute carrier family 22 member 2	Homo sapiens (human)
dopamine uptake	Solute carrier family 22 member 2	Homo sapiens (human)
L-arginine import across plasma membrane	Solute carrier family 22 member 2	Homo sapiens (human)
export across plasma membrane	Solute carrier family 22 member 2	Homo sapiens (human)
transport across blood-brain barrier	Solute carrier family 22 member 2	Homo sapiens (human)
L-alpha-amino acid transmembrane transport	Solute carrier family 22 member 2	Homo sapiens (human)
spermidine transmembrane transport	Solute carrier family 22 member 2	Homo sapiens (human)
L-arginine transmembrane transport	Solute carrier family 22 member 2	Homo sapiens (human)
cellular detoxification	Solute carrier family 22 member 2	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Solute carrier family 22 member 2	Homo sapiens (human)
lipid hydroxylation	Cytochrome P450 3A4	Homo sapiens (human)
lipid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
steroid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
cholesterol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
androgen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
estrogen metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
alkaloid catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
monoterpenoid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
calcitriol biosynthetic process from calciol	Cytochrome P450 3A4	Homo sapiens (human)
xenobiotic catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D catabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinol metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
long-chain fatty acid biosynthetic process	Cytochrome P450 3A4	Homo sapiens (human)
aflatoxin metabolic process	Cytochrome P450 3A4	Homo sapiens (human)
oxidative demethylation	Cytochrome P450 3A4	Homo sapiens (human)
DNA topological change	DNA topoisomerase 1	Homo sapiens (human)
chromatin remodeling	DNA topoisomerase 1	Homo sapiens (human)
circadian rhythm	DNA topoisomerase 1	Homo sapiens (human)
response to xenobiotic stimulus	DNA topoisomerase 1	Homo sapiens (human)
programmed cell death	DNA topoisomerase 1	Homo sapiens (human)
phosphorylation	DNA topoisomerase 1	Homo sapiens (human)
peptidyl-serine phosphorylation	DNA topoisomerase 1	Homo sapiens (human)
circadian regulation of gene expression	DNA topoisomerase 1	Homo sapiens (human)
embryonic cleavage	DNA topoisomerase 1	Homo sapiens (human)
chromosome segregation	DNA topoisomerase 1	Homo sapiens (human)
DNA replication	DNA topoisomerase 1	Homo sapiens (human)
hematopoietic progenitor cell differentiation	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA topological change	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA ligation	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA damage response	DNA topoisomerase 2-alpha	Homo sapiens (human)
chromosome segregation	DNA topoisomerase 2-alpha	Homo sapiens (human)
female meiotic nuclear division	DNA topoisomerase 2-alpha	Homo sapiens (human)
apoptotic chromosome condensation	DNA topoisomerase 2-alpha	Homo sapiens (human)
embryonic cleavage	DNA topoisomerase 2-alpha	Homo sapiens (human)
regulation of circadian rhythm	DNA topoisomerase 2-alpha	Homo sapiens (human)
positive regulation of apoptotic process	DNA topoisomerase 2-alpha	Homo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediate	DNA topoisomerase 2-alpha	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	DNA topoisomerase 2-alpha	Homo sapiens (human)
rhythmic process	DNA topoisomerase 2-alpha	Homo sapiens (human)
negative regulation of DNA duplex unwinding	DNA topoisomerase 2-alpha	Homo sapiens (human)
resolution of meiotic recombination intermediates	DNA topoisomerase 2-alpha	Homo sapiens (human)
sister chromatid segregation	DNA topoisomerase 2-alpha	Homo sapiens (human)
neuron migration	DNA topoisomerase 2-beta	Homo sapiens (human)
DNA topological change	DNA topoisomerase 2-beta	Homo sapiens (human)
axonogenesis	DNA topoisomerase 2-beta	Homo sapiens (human)
B cell differentiation	DNA topoisomerase 2-beta	Homo sapiens (human)
forebrain development	DNA topoisomerase 2-beta	Homo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediate	DNA topoisomerase 2-beta	Homo sapiens (human)
cellular response to hydrogen peroxide	DNA topoisomerase 2-beta	Homo sapiens (human)
cellular response to ATP	DNA topoisomerase 2-beta	Homo sapiens (human)
cellular senescence	DNA topoisomerase 2-beta	Homo sapiens (human)
positive regulation of double-strand break repair via nonhomologous end joining	DNA topoisomerase 2-beta	Homo sapiens (human)
sister chromatid segregation	DNA topoisomerase 2-beta	Homo sapiens (human)
resolution of meiotic recombination intermediates	DNA topoisomerase 2-beta	Homo sapiens (human)
positive regulation of chemokine-mediated signaling pathway	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of signaling receptor activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
response to hypoxia	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of DNA-templated transcription	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
response to reactive oxygen species	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
angiogenesis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
response to hypoxia	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
intracellular glucose homeostasis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
neural crest cell migration	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
epithelial to mesenchymal transition	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
embryonic placenta development	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
B-1 B cell homeostasis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of endothelial cell proliferation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
heart looping	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of neuroblast proliferation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
chondrocyte differentiation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
glandular epithelial cell maturation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
connective tissue replacement involved in inflammatory response wound healing	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
outflow tract morphogenesis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cardiac ventricle morphogenesis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
lactate metabolic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of glycolytic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of DNA-templated transcription	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
intracellular iron ion homeostasis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
signal transduction	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
neuroblast proliferation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
lactation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
visual learning	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
response to iron ion	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of gene expression	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
vascular endothelial growth factor production	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of vascular endothelial growth factor production	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of gene expression	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of gene expression	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of epithelial cell migration	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
response to muscle activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
axonal transport of mitochondrion	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
neural fold elevation formation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cerebral cortex development	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
bone mineralization	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of bone mineralization	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of vascular endothelial growth factor receptor signaling pathway	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
TOR signaling	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of TOR signaling	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
intracellular oxygen homeostasis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of chemokine production	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of transforming growth factor beta2 production	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
collagen metabolic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cellular response to oxidative stress	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
embryonic hemopoiesis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
insulin secretion involved in cellular response to glucose stimulus	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of insulin secretion involved in cellular response to glucose stimulus	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
hemoglobin biosynthetic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of blood vessel endothelial cell migration	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of erythrocyte differentiation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of angiogenesis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of DNA-templated transcription	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of growth	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
muscle cell cellular homeostasis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of hormone biosynthetic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
digestive tract morphogenesis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of nitric-oxide synthase activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
neuron apoptotic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
elastin metabolic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
intestinal epithelial cell maturation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
epithelial cell differentiation involved in mammary gland alveolus development	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
iris morphogenesis	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
retina vasculature development in camera-type eye	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of thymocyte apoptotic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cellular response to interleukin-1	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cellular response to hypoxia	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
dopaminergic neuron differentiation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
mesenchymal cell apoptotic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
hypoxia-inducible factor-1alpha signaling pathway	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cellular response to virus	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of cytokine production involved in inflammatory response	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of mitophagy	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of miRNA transcription	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
positive regulation of miRNA transcription	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of oxidative stress-induced neuron intrinsic apoptotic signaling pathway	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of aerobic respiration	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of reactive oxygen species metabolic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of protein neddylation	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
negative regulation of mesenchymal cell apoptotic process	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
organic cation transport	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
transmembrane transport	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
proton transmembrane transport	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membrane	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
xenobiotic transmembrane transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
organic cation transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
putrescine transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
xenobiotic transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
transmembrane transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
thiamine transmembrane transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
amino acid import across plasma membrane	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
L-arginine import across plasma membrane	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
L-alpha-amino acid transmembrane transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
proton transmembrane transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
L-arginine transmembrane transport	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membrane	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
response to hypoxia	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
angiogenesis	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
embryonic placenta development	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
blood vessel remodeling	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
regulation of heart rate	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
epithelial cell maturation	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
response to oxidative stress	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
mitochondrion organization	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
signal transduction	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
visual perception	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
erythrocyte differentiation	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
lung development	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
norepinephrine metabolic process	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
mRNA transcription by RNA polymerase II	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
surfactant homeostasis	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
myoblast fate commitment	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
multicellular organismal-level iron ion homeostasis	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
cellular response to hypoxia	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
positive regulation of cold-induced thermogenesis	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
regulation of protein neddylation	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
regulation of transcription by RNA polymerase II	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
lipid transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid biosynthetic process	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate metabolic process	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transmembrane transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transepithelial transport	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
renal urate salt excretion	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
export across plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
transport across blood-brain barrier	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
cellular detoxification	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transport across blood-brain barrier	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
amine transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
acetylcholine transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
neurotransmitter transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
monoamine transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
organic anion transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
organic cation transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
prostaglandin transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
L-amino acid transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
pyrimidine nucleoside transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
choline transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
thiamine transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
putrescine transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
efflux transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
spermidine transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
quaternary ammonium group transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
toxin transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
L-arginine transmembrane transporter activity	Solute carrier family 22 member 2	Homo sapiens (human)
monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
steroid binding	Cytochrome P450 3A4	Homo sapiens (human)
iron ion binding	Cytochrome P450 3A4	Homo sapiens (human)
protein binding	Cytochrome P450 3A4	Homo sapiens (human)
steroid hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
retinoic acid 4-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxidoreductase activity	Cytochrome P450 3A4	Homo sapiens (human)
oxygen binding	Cytochrome P450 3A4	Homo sapiens (human)
enzyme binding	Cytochrome P450 3A4	Homo sapiens (human)
heme binding	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D3 25-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
caffeine oxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
quinine 3-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
testosterone 6-beta-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 8,9 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 11,12 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
anandamide 14,15 epoxidase activity	Cytochrome P450 3A4	Homo sapiens (human)
aromatase activity	Cytochrome P450 3A4	Homo sapiens (human)
vitamin D 24-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 16-alpha-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
estrogen 2-hydroxylase activity	Cytochrome P450 3A4	Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activity	Cytochrome P450 3A4	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	DNA topoisomerase 1	Homo sapiens (human)
DNA binding	DNA topoisomerase 1	Homo sapiens (human)
chromatin binding	DNA topoisomerase 1	Homo sapiens (human)
double-stranded DNA binding	DNA topoisomerase 1	Homo sapiens (human)
single-stranded DNA binding	DNA topoisomerase 1	Homo sapiens (human)
RNA binding	DNA topoisomerase 1	Homo sapiens (human)
DNA topoisomerase type I (single strand cut, ATP-independent) activity	DNA topoisomerase 1	Homo sapiens (human)
protein serine/threonine kinase activity	DNA topoisomerase 1	Homo sapiens (human)
protein binding	DNA topoisomerase 1	Homo sapiens (human)
ATP binding	DNA topoisomerase 1	Homo sapiens (human)
DNA binding, bending	DNA topoisomerase 1	Homo sapiens (human)
protein domain specific binding	DNA topoisomerase 1	Homo sapiens (human)
supercoiled DNA binding	DNA topoisomerase 1	Homo sapiens (human)
magnesium ion binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
chromatin binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
RNA binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activity	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein kinase C binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
ATP binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
ATP-dependent activity, acting on DNA	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA binding, bending	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein homodimerization activity	DNA topoisomerase 2-alpha	Homo sapiens (human)
ubiquitin binding	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein heterodimerization activity	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA binding	DNA topoisomerase 2-beta	Homo sapiens (human)
chromatin binding	DNA topoisomerase 2-beta	Homo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activity	DNA topoisomerase 2-beta	Homo sapiens (human)
protein binding	DNA topoisomerase 2-beta	Homo sapiens (human)
ATP binding	DNA topoisomerase 2-beta	Homo sapiens (human)
ribonucleoprotein complex binding	DNA topoisomerase 2-beta	Homo sapiens (human)
metal ion binding	DNA topoisomerase 2-beta	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
sequence-specific DNA binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cis-regulatory region sequence-specific DNA binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
DNA-binding transcription activator activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
DNA-binding transcription repressor activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
transcription coactivator binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
p53 binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
DNA-binding transcription factor activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
protein binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
nuclear receptor binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
enzyme binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
protein kinase binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
protein domain specific binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
ubiquitin protein ligase binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
histone deacetylase binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
protein heterodimerization activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
Hsp90 protein binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
E-box binding	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
transcription regulator activator activity	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
organic cation transmembrane transporter activity	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
antiporter activity	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
transmembrane transporter activity	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
polyspecific organic cation:proton antiporter activity	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
protein binding	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
organic cation transmembrane transporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
L-amino acid transmembrane transporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
thiamine transmembrane transporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
antiporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
putrescine transmembrane transporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
transmembrane transporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
L-arginine transmembrane transporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
polyspecific organic cation:proton antiporter activity	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
sequence-specific DNA binding	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA binding	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specific	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
transcription coactivator binding	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specific	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
protein binding	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
protein heterodimerization activity	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor binding	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA binding	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
organic anion transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ABC-type xenobiotic transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
urate transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
biotin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
efflux transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATP hydrolysis activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
riboflavin transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
ATPase-coupled transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
identical protein binding	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
protein homodimerization activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
xenobiotic transmembrane transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
sphingolipid transporter activity	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Solute carrier family 22 member 2	Homo sapiens (human)
basal plasma membrane	Solute carrier family 22 member 2	Homo sapiens (human)
membrane	Solute carrier family 22 member 2	Homo sapiens (human)
basolateral plasma membrane	Solute carrier family 22 member 2	Homo sapiens (human)
apical plasma membrane	Solute carrier family 22 member 2	Homo sapiens (human)
extracellular exosome	Solute carrier family 22 member 2	Homo sapiens (human)
presynapse	Solute carrier family 22 member 2	Homo sapiens (human)
cytoplasm	Cytochrome P450 3A4	Homo sapiens (human)
endoplasmic reticulum membrane	Cytochrome P450 3A4	Homo sapiens (human)
intracellular membrane-bounded organelle	Cytochrome P450 3A4	Homo sapiens (human)
nuclear chromosome	DNA topoisomerase 1	Homo sapiens (human)
P-body	DNA topoisomerase 1	Homo sapiens (human)
fibrillar center	DNA topoisomerase 1	Homo sapiens (human)
male germ cell nucleus	DNA topoisomerase 1	Homo sapiens (human)
nucleus	DNA topoisomerase 1	Homo sapiens (human)
nucleoplasm	DNA topoisomerase 1	Homo sapiens (human)
nucleolus	DNA topoisomerase 1	Homo sapiens (human)
perikaryon	DNA topoisomerase 1	Homo sapiens (human)
protein-DNA complex	DNA topoisomerase 1	Homo sapiens (human)
nucleolus	DNA topoisomerase 1	Homo sapiens (human)
nucleolus	DNA topoisomerase 2-alpha	Homo sapiens (human)
nuclear chromosome	DNA topoisomerase 2-alpha	Homo sapiens (human)
centriole	DNA topoisomerase 2-alpha	Homo sapiens (human)
chromosome, centromeric region	DNA topoisomerase 2-alpha	Homo sapiens (human)
condensed chromosome	DNA topoisomerase 2-alpha	Homo sapiens (human)
male germ cell nucleus	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleus	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleoplasm	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleolus	DNA topoisomerase 2-alpha	Homo sapiens (human)
cytoplasm	DNA topoisomerase 2-alpha	Homo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complex	DNA topoisomerase 2-alpha	Homo sapiens (human)
protein-containing complex	DNA topoisomerase 2-alpha	Homo sapiens (human)
ribonucleoprotein complex	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleus	DNA topoisomerase 2-alpha	Homo sapiens (human)
nucleolus	DNA topoisomerase 2-beta	Homo sapiens (human)
heterochromatin	DNA topoisomerase 2-beta	Homo sapiens (human)
nucleus	DNA topoisomerase 2-beta	Homo sapiens (human)
nucleoplasm	DNA topoisomerase 2-beta	Homo sapiens (human)
nucleolus	DNA topoisomerase 2-beta	Homo sapiens (human)
cytosol	DNA topoisomerase 2-beta	Homo sapiens (human)
ribonucleoprotein complex	DNA topoisomerase 2-beta	Homo sapiens (human)
nucleus	DNA topoisomerase 2-beta	Homo sapiens (human)
nucleus	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
nucleoplasm	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cytoplasm	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
cytosol	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
nuclear body	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
nuclear speck	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
motile cilium	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
axon cytoplasm	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
chromatin	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
euchromatin	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
protein-containing complex	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
RNA polymerase II transcription regulator complex	Hypoxia-inducible factor 1-alpha	Homo sapiens (human)
plasma membrane	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
apical plasma membrane	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
membrane	Multidrug and toxin extrusion protein 2	Homo sapiens (human)
plasma membrane	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
basolateral plasma membrane	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
apical plasma membrane	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
membrane	Multidrug and toxin extrusion protein 1	Homo sapiens (human)
nucleoplasm	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
cytosol	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
nuclear speck	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
chromatin	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
transcription regulator complex	Endothelial PAS domain-containing protein 1	Homo sapiens (human)
nucleoplasm	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
brush border membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
mitochondrial membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
membrane raft	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
external side of apical plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
plasma membrane	Broad substrate specificity ATP-binding cassette transporter ABCG2	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (821)

Assay ID	Title	Year	Journal	Article
AID625285	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID46485	Cytotoxicity measured using the COR-L23 parental (COR-L23/P) human non small cell lung carcinoma cell line	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Novel angular benzophenazines: dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents.
AID1462689	Cytotoxicity against human KB cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17	Design, synthesis, and cytotoxic activity of novel 7-substituted camptothecin derivatives incorporating piperazinyl-sulfonylamidine moieties.
AID143176	Complete response in CD1 mice with human Non-Small-Cell tumor xenograft at a oral dose of 9 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1127187	Antiproliferative activity against human H1299 cells after 3 days by XTT assay	2014	European journal of medicinal chemistry, May-22, Volume: 79	Synthesis, antiproliferative and anti-dengue virus evaluations of 2-aroyl-3-arylquinoline derivatives.
AID1274795	Antiproliferative activity against human MRC5 cells after 72 hrs by XTT assay	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID389685	Cytotoxicity against camptothecin-resistant human CPT-K5 cells after MTT assay	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.
AID7477	Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 2	2000	Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22	Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
AID1127190	Antiproliferative activity against human HuH7 cells after 3 days by XTT assay	2014	European journal of medicinal chemistry, May-22, Volume: 79	Synthesis, antiproliferative and anti-dengue virus evaluations of 2-aroyl-3-arylquinoline derivatives.
AID1127186	Antiproliferative activity against human A549 cells after 3 days by XTT assay	2014	European journal of medicinal chemistry, May-22, Volume: 79	Synthesis, antiproliferative and anti-dengue virus evaluations of 2-aroyl-3-arylquinoline derivatives.
AID78568	Cytotoxicity measured using the drug resistant, P-glycoprotein (Pgp) expressing human small cell lung carcinoma cell line H69/LX4	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Novel angular benzophenazines: dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents.
AID721753	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells at 20 uM after 1.5 mins by fluorescence assay	2013	Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3	Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1433676	Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 25 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 32.80%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID101466	Percentage of body weight loss in mice bearing lung carcinoma LX-1 at a oral dose of 15 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID46271	Tumor volume index was measured on colon carcinoma (COCF) cells at a dose of 15 mg/kg intravenously in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID331826	Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
AID307321	Growth inhibition of HeLa cells after 4 days	2007	Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12	Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives.
AID431819	Cytotoxicity against p53-deficient human Hep3B cells after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID414759	Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method	2009	Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7	12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents.
AID1702824	Inhibition of topoisomerase 1 in human A549 cells nuclear extract assessed as reduction in supercoiled DNA relaxation at 0.2 uM preincubated for 6 hrs followed by supercoiled DNA addition and further incubated for 30 mins by SYBR-green staining based agar	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID1239182	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16	Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents.
AID214576	Tested in vitro for cytotoxicity against human tumor cell line UACC 62 (melanoma)	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID167217	Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Nitro and amino substitution in the D-ring of 5-(2-dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones: effect on topoisomerase-I targeting activity and cytotoxicity.
AID588218	FDA HLAED, lactate dehydrogenase (LDH) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID600080	Cell cycle arrest in human PC3 cells assessed as accumulation at G1 phase at 2 uM after 48 hrs using propidium iodide staining by flow cytometry (Rvb = 54.14 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID321330	Antitumor activity against human A549 cells after 4 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3	New homocamptothecins: synthesis, antitumor activity, and molecular modeling.
AID1854773	Antiproliferative activity against human SW-620 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	2022	European journal of medicinal chemistry, Nov-05, Volume: 241	Design, synthesis, and biological evaluation of novel 7-substituted 10,11-methylenedioxy-camptothecin derivatives against drug-resistant small-cell lung cancer in vitro and in vivo.
AID10169	In vitro cytotoxicity against A2780 (human ovarian cancer)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions.
AID431817	Cytotoxicity against human AGS cells expressing wild type p53 after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID111467	The no. of deaths of mice(infected with HT-29 cells) was reported at a dose of 11 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID721725	Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay	2013	European journal of medicinal chemistry, Jan, Volume: 59	Synthesis and antiproliferative evaluation of 3-phenylquinolinylchalcone derivatives against non-small cell lung cancers and breast cancers.
AID1387399	Toxicity in Balb/C mouse administered as daily dose for 1 week measured daily for up to 28 days	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID10041	In vitro anti-cancer activity against ACHN(Renal) human tumor cell line	1999	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12	Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.
AID7476	Potentiation of growth inhibition of A2780 cells along with 10 uM NU1085 in experiment 1	2000	Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22	Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
AID586342	Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID1228611	Growth inhibition of human MCF7 cells by five-dose growth inhibition assay	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID56570	Inhibition of topoisomerase I activity was determined in vitro by using the cleavable complex assay(calf thymus)	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID111314	Compound was tested for number of deaths of the animals at a dose of 11 mg/Kg in mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1817017	Induction of DNA damage in human MCF7/TDP1 cells assessed as increase in gammaH2AX foci at 1 uM measured after 6 hrs by DAPI staining based immunofluorescence assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID56881	TOP-1 mediated DNA cleavage measured as effective concentration relative to topotecan = 1	2002	Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22	Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435.
AID98921	Inhibitory concentration against L1210 leukemia cell proliferation	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	Synthesis and pharmacological evaluation of novel non-lactone analogues of camptothecin.
AID143187	Percentage inhibition of tumor volume in treated versus control mice against human Non-Small-Cell tumor xenograft at a oral dose of 9 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID746434	Cytotoxicity against human PNT2 cells assessed as growth inhibition at 0.1 to 10 uM after 72 hrs by cell titre glo assay	2013	Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10	Structure-based design of HSPA5 inhibitors: from peptide to small molecule inhibitors.
AID1823976	Antiproliferative activity against human MGC-803 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID1600550	Inhibition of DNA topoisomerase 2 in human HeLa cells incubated for 18 to 24 hrs by kinase assay	2019	Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19	Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives.
AID1410928	Inhibition of colony formation of human A498 cells after 2 weeks by crystal violet staining-based microscopic analysis	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan.
AID1387394	Cytotoxicity in human SGC7901 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID377022	Cytotoxicity against human A549 cells after 96 hrs by MTT assay	2006	Journal of natural products, Jun, Volume: 69, Issue:6	Mono-, Bi-, and triphenanthrenes from the tubers of Cremastra appendiculata.
AID247768	Inhibitory concentration against KB/V-1 cells overexpress MDR1	2005	Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3	5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
AID684316	Toxicity in human A549 cells xenografted in BALB/c mouse assessed as mortality at 0.5 mg/kg, iv qd for 5 days measured after 14 days	2012	European journal of medicinal chemistry, Oct, Volume: 56	Synthesis and preliminary bioevaluation of novel E-ring modified acetal analog of camptothecin as cytotoxic agents.
AID586343	Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID219146	In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3)	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID269222	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 5 mg/kg, po measured as body weight loss	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID269223	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 9 mg/kg, po measured as body weight loss	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID527988	Antiproliferative activity against human MRC5 cells by [3H]thymidine incorporation assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID634951	Growth inhibition of human Hep3B cells after 72 hrs by XTT assay	2011	Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24	Synthesis and antiproliferative evaluation of 6-aryl-11-iminoindeno[1,2-c]quinoline derivatives.
AID489630	Toxicity in C57BL/6 mouse at 0.5 mg/kg, ip qd for 5 days	2010	European journal of medicinal chemistry, Jul, Volume: 45, Issue:7	Trifluoromethyl-promoted homocamptothecins: synthesis and biological activity.
AID28644	Rf is the resistance factor and is the ratio of the IC50 on the resistant cell line over the IC50 on the parental H69/P cell line	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Novel angular benzophenazines: dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents.
AID1387391	Cytotoxicity in human MGC803 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID590392	Cytotoxicity against human A549 cells after 3 days	2011	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7	Synthesis and antitumor activity of 10-arylcamptothecin derivatives.
AID1255490	Cell cycle arrest in human M21 cells assessed as accumulation at G0/G1 phase at 1.5 uM after 24 hrs by DAPI staining-based flow cytometry (Rvb = 65.1%)	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Synthesis and biological evaluation of novel N-phenyl ureidobenzenesulfonate derivatives as potential anticancer agents. Part 2. Modulation of the ring B.
AID1443373	Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.
AID343607	Cytotoxicity against human HepG2 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID599608	Cell cycle arrest in human PC3 cells assessed as accumulation at S phase at 2 uM after 72 hrs using propidium iodide staining by flow cytometry (Rvb = 37.73 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID1221964	Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID377532	Growth inhibition of RAD52/topoisomerase 1 deficient Saccharomyces cerevisiae RS321N harbouring plasmid containing human topoisomerase 1 in glucose medium after 48 hrs	2000	Journal of natural products, Sep, Volume: 63, Issue:9	Use of COMPARE analysis to discover new natural product drugs: isolation of camptothecin and 9-methoxycamptothecin from a new source.
AID586400	Antitumor activity against human H460 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 2 mg/kg, po QD for 5 days followed by 2days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID247676	In vitro cytotoxicity against human lung carcinoma A549 cells	2004	Journal of medicinal chemistry, Oct-21, Volume: 47, Issue:22	Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase.
AID78397	Toxic deaths was recorded on non-small-cell lung carcinoma H460 cells at a dose of 15 mg/kg intravenously in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1464542	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20	Design, semisynthesis and potent cytotoxic activity of novel 10-fluorocamptothecin derivatives.
AID101472	Percentage inhibition of tumor volume in treated versus control mice bearing lung carcinoma LX-1 at a oral dose of 15 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID143175	Complete response in CD1 mice with human Non-Small-Cell tumor at a oral dose of 5 mg/kg after treatment with compound	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID379519	Cytotoxicity against human BGC-823 cells after 96 hrs by MTT assay	2006	Journal of natural products, Nov, Volume: 69, Issue:11	A nitrogen-containing 3-alkyl-1,4-benzoquinone and a gomphilactone derivative from Embelia ribes.
AID113231	Efficacy against HT-29 human colon xenograft infected mice expressed as tumor growth ratio at dose 9 mg/Kg	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID527984	Antiproliferative activity against human U251 cells by [3H]thymidine incorporation assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID377530	Growth inhibition of RAD52/topoisomerase 1 deficient Saccharomyces cerevisiae RS321N harbouring plasmid containing human topoisomerase 1 in galactose medium after 48 hrs	2000	Journal of natural products, Sep, Volume: 63, Issue:9	Use of COMPARE analysis to discover new natural product drugs: isolation of camptothecin and 9-methoxycamptothecin from a new source.
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AID1600549	Inhibition of DNA topoisomerase 2 in human HeLa cells at 0.2 uM incubated for 18 to 24 hrs by kinase assay relative to control	2019	Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19	Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives.
AID56567	Average concentration of compound to cause 50% inhibition of topoisomerase-1 isolated from calf thymus	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID214578	In vitro anti-cancer activity against UACC 62(Melanoma) human tumor cell line	1999	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12	Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.
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AID586346	Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID1405132	Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 1.8 uM after 24 hrs by DAPI staining based flow cytometry relative to control	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID684300	Antiproliferative activity against human A549 cells after 3 days by MTT assay	2012	European journal of medicinal chemistry, Oct, Volume: 56	Synthesis and preliminary bioevaluation of novel E-ring modified acetal analog of camptothecin as cytotoxic agents.
AID1826597	Antiproliferative activity against human A549 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID314507	Cytotoxicity against human NCI-H460 cells after 1 hr	2008	Bioorganic & medicinal chemistry letters, Feb-15, Volume: 18, Issue:4	Synthesis and cytotoxic activity of a new series of topoisomerase I inhibitors.
AID1387392	Cytotoxicity in human SK-N-SH cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID588975	Substrates of transporters of clinical importance in the absorption and disposition of drugs, BCRP	2010	Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3	Membrane transporters in drug development.
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AID111698	Mean body weight loss for animals in all experimental conditions at dose 11 mg/Kg in HT-29 human colon xenograft infected mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1079933	Acute 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
AID426064	Antitumor activity against human NCI-H460 cells by SRB method	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation.
AID81349	In vitro anti-cancer activity against HOP 62(Lung) human tumor cell line	1999	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12	Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.
AID26144	Half-life in PBS buffer solution in the absence of human serum albumin	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
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AID680978	TP_TRANSPORTER: intracellular concentration of the drug is lower compared with IGROV1 in T8 cells	1999	Cancer research, Sep-15, Volume: 59, Issue:18	Overexpression of the BCRP/MXR/ABCP gene in a topotecan-selected ovarian tumor cell line.
AID396726	Antitumor activity against human HCT8 xenografted in BALB/c nu/nu mouse assessed as change in body weight at 10 mg/kg, ip q3d for 3 days	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Synthesis and antitumor activity of novel 20s-camptothecin analogues.
AID1079947	Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
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AID537735	Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u	2010	European journal of medicinal chemistry, Nov, Volume: 45, Issue:11	Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1817001	Synergistic cytotoxicity against human MCF7 cells at 50 nM after 96 hrs in presence of 12-(2-(Dimethylamino)ethyl)-1,2-dihydroxy-[1,3]dioxolo[4',5':4,5]benzo[1,2-c]phenanthridine-13(12H)-one by MTT assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID1339542	Antiproliferative activity against human HMLE cells assessed as reduction in cell viability by MTT assay	2017	ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2	Synthesis, Biological Evaluation, and Autophagy Mechanism of 12
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AID684301	Antiproliferative activity against human HCT116 cells after 3 days by MTT assay	2012	European journal of medicinal chemistry, Oct, Volume: 56	Synthesis and preliminary bioevaluation of novel E-ring modified acetal analog of camptothecin as cytotoxic agents.
AID489626	Antitumor activity against mouse LLC transplanted in C57BL/6 mouse assessed as tumor weight at 0.5 mg/kg, ip qd for 5 days (RVb = 1.8 +/- 0.47 g)	2010	European journal of medicinal chemistry, Jul, Volume: 45, Issue:7	Trifluoromethyl-promoted homocamptothecins: synthesis and biological activity.
AID599606	Cell cycle arrest in human PC3 cells assessed as accumulation at G1 phase at 2 uM after 72 hrs using propidium iodide staining by flow cytometry (Rvb = 42.19 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
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AID1702896	Toxicity in FVB/N mouse model of pCMV/SB/pT3-Caggs-NRasV12/myr-AKT/pT3-EF1alpha plasmids-induced primary hepatocellular carcinoma assessed as reduction in liver weight at 2 mg/kg, iv administered every other day for 2 weeks relative to control	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID136690	The compound (2.5 mg/kg) administered intravenously was tested for antitumor activity against DU-145 (prostate) xenograft model in mice	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
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AID1824013	Induction of apoptosis in human MGC-803 cells assessed as viable cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 99.9%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID586336	Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID276577	Inhibition of HIF1alpha production in c4-2 cells at 10 uM after 24 hrs relative to control	2006	Bioorganic & medicinal chemistry letters, Dec-01, Volume: 16, Issue:23	Microwave expedited synthesis of 5-aminocamptothecin analogs: Inhibitors of hypoxia inducible factor HIF-1alpha.
AID681572	TP_TRANSPORTER: drug resistance in BCRP-expressing MEF3.8 cells	2003	Cancer research, Mar-15, Volume: 63, Issue:6	Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein.
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AID1824015	Induction of apoptosis in human MGC-803 cells assessed as late apoptic cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0.05%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
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AID1188716	Antiproliferative activity against human H184B5F5/M10 cells after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Synthesis and biological evaluation of hydroxycinnamic acid hydrazide derivatives as inducer of caspase-3.
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AID431811	Cytotoxicity against human HepG2 cells expressing wild type p53 after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID113225	Efficacy against HT-29 human colon xenograft infected mice expressed as tumor growth ratio at dose 11 mg/Kg	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1433646	Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
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AID599601	Induction of apoptosis in human PC3 cells at 2 uM after 48 hrs using propidium iodide staining by flow cytometry (Rvb = 0.84 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID1410926	Inhibition of miR-21 RNA (unknown origin) transfected in human HeLa cells at 0.1 to 1000 nM after 48 hrs by Bright-Glo luciferase reporter gene assay	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan.
AID156017	Antiproliferative activity measured against PC-3 human prostate adenocarcinoma	1998	Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27	Homocamptothecins: synthesis and antitumor activity of novel E-ring-modified camptothecin analogues.
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AID86087	In vivo efficacy of tumor growth ratio(T/B) of compound was calculated by using the HT-29 Human colon Xenograft model in mice at a dose of 7 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1854772	Antiproliferative activity against human 2008 cells assessed as inhibition of cell growth incubated for 72 hrs by SRB assay	2022	European journal of medicinal chemistry, Nov-05, Volume: 241	Design, synthesis, and biological evaluation of novel 7-substituted 10,11-methylenedioxy-camptothecin derivatives against drug-resistant small-cell lung cancer in vitro and in vivo.
AID586340	Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID228735	MDR ratio as the ratio of IC50 value against SKVLB to that of SKOV3	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1299122	Cytotoxicity against human HCT116 cells at 3 uM	2016	Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12	Synthesis and biological evaluation of 1,2-dithiol-3-thiones and pyrrolo[1,2-a]pyrazines as novel hypoxia inducible factor-1 (HIF-1) inhibitor.
AID431818	Cytotoxicity against estrogen receptor-positive human MCF7 cells expressing wild type p53 after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID389689	Cytotoxicity against multidrug resistant human KBV-1 cells overexpressing MDR1 after MTT assay	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.
AID721721	Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by XTT assay	2013	European journal of medicinal chemistry, Jan, Volume: 59	Synthesis and antiproliferative evaluation of 3-phenylquinolinylchalcone derivatives against non-small cell lung cancers and breast cancers.
AID746435	Cytotoxicity against human HCT116 cells assessed as cell viability at 0.1 to 100 uM after 48 hrs by cell titre glo assay	2013	Bioorganic & medicinal chemistry letters, May-15, Volume: 23, Issue:10	Structure-based design of HSPA5 inhibitors: from peptide to small molecule inhibitors.
AID409906	Cytotoxicity against human KB3-1 cells by MTT method	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
AID1544048	Poison activity at recombinant human TOP1 expressed in baculovirus infected Sf9 insect cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis	2019	Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7	Discovery and Mechanistic Study of Tailor-Made Quinoline Derivatives as Topoisomerase 1 Poison with Potent Anticancer Activity.
AID1228603	Growth inhibition of human NCI60 cells assessed as cell growth at 10 uM	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID588217	FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1387402	Antitumor activity against human HepG2 cells xenografted in Balb/C mouse assessed as inhibition of tumor growth at 2 mg/kg, iv dosed once per week for 30 days followed by 2 weeks observation relative untreated control	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID1274796	Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for human MDA-MB-231 cells	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID248382	Concentration required to inhibit cell proliferation in P388/CPT-45 tumor cell line; camptothecin resistant	2004	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22	Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
AID586350	Resistance ratio of of IC50 for human H69AR cells overexpressing MDR1 after 72 hrs s to IC50 for human H69 cells after 72 hrs	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID600074	Cell cycle arrest in human PC3 cells assessed as accumulation at S phase at 2 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 34.84 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID1188714	Antiproliferative activity against human NL20 cells after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Synthesis and biological evaluation of hydroxycinnamic acid hydrazide derivatives as inducer of caspase-3.
AID379520	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay	2006	Journal of natural products, Nov, Volume: 69, Issue:11	A nitrogen-containing 3-alkyl-1,4-benzoquinone and a gomphilactone derivative from Embelia ribes.
AID269224	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 15 mg/kg, po measured as body weight loss	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID221332	In Vitro cytotoxicity against human lung cancer cell line (A549)	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
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AID1254847	Selectivity index, ratio of IC50 for normal human astrocytes to IC50 for human GBM3 cells	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID1387389	Cytotoxicity in human Bel7402 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID1075765	Cytotoxicity against human mitoxantrone-resistant H460 cells after 72 hrs by MTT assay	2014	Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4	Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID527977	Inhibition of HIF1alpha in human U251 cells under hypoxic condition by luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID1182907	Cytotoxicity against human MDA-MB-231 cells after 72 hrs sulforhodamine B colorimetric assay	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Design and synthesis of new 7-(N-substituted-methyl)-camptothecin derivatives as potent cytotoxic agents.
AID241607	Inhibition of topoisomerase I-DNA complex in trapping assay	2005	Journal of medicinal chemistry, Apr-07, Volume: 48, Issue:7	Structures of three classes of anticancer agents bound to the human topoisomerase I-DNA covalent complex.
AID1826596	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1405120	Antiproliferative activity against human M21 cells after 48 hrs by SRB assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID612418	Antiproliferative activity against human NCI-H460 cells after 72 hrs by coulter counter analysis	2011	Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16	Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D.
AID269215	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 15 mg/kg, po measured as log10 of cell kill to reach 1000 mm3 tumor volume	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID1221966	Ratio of plasma AUC in po dosed mdr1 knock out mouse to plasma AUC in po dosed wild type mouse	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID432403	Induction of covalent human topoisomerase 1-plasmid O6#7 DNA adduct stabilization assessed as appearance of nicked plasmid at 1.6 uM by agarose gel electrophoresis	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	On the role of topoisomerase I in mediating the cytotoxicity of 9-aminoacridine-based anticancer agents.
AID1816999	Synergistic cytotoxicity against human MCF7/TDP1 cells at 100 nM after 96 hrs in presence of 12-(2-(Dimethylamino)ethyl)-1,2-dihydroxy-[1,3]dioxolo[4',5':4,5]benzo[1,2-c]phenanthridine-13(12H)-one by MTT assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID1387390	Cytotoxicity in human SMMC7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID745328	Cytotoxicity against human HT-29 cells	2013	European journal of medicinal chemistry, May, Volume: 63	Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID421978	Reduction in VEGF mRNA expression in wild type human U251 cells under hypoxic condition after 8 hrs	2009	Journal of natural products, May-22, Volume: 72, Issue:5	Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii.
AID1228607	Growth inhibition of human UACC62 cells by five-dose growth inhibition assay	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID1433714	Antitumor activity against human Bel7402 cells xenografted in BALB/c nude mouse assessed as tumor volume at 5 mg/kg, ip administered once in a week for two weeks starting from 6 days post tumor transplantation measured 27 to 30 days post tumor transplanta	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
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AID401946	Cytotoxicity against human A549 cells after 96 hrs by MTT assay	2004	Journal of natural products, May, Volume: 67, Issue:5	Phelligridins C-F: cytotoxic pyrano[4,3-c][2]benzopyran-1,6-dione and furo[3,2-c]pyran-4-one derivatives from the fungus Phellinus igniarius.
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AID1824003	Induction of apoptosis in human SGC-7901 cells assessed as late apoptic cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0.03%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
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AID1648758	Toxicity in nude mouse xenografted with human HCT116 cells assessed as change in body weight at 0.5 mg/kg, ip qd measured every two days for 21 days	2020	ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4	Natural Product Evodiamine with Borate Trigger Unit: Discovery of Potent Antitumor Agents against Colon Cancer.
AID586349	Resistance ratio of of IC50 for human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs to IC50 for human MESSA cells after 72 hrs	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID343612	Cytotoxicity against human KB cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID333717	Inhibition of hypoxia-induced HIF1 activation in human U251 cells	2004	Journal of natural products, Dec, Volume: 67, Issue:12	Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells.
AID601072	Cytotoxicity against human HCT116 cells after 3 days by MTT assay	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors.
AID93500	Concentration causing 50% decrease of ovarian carcinoma (IGROV-1)cell growth over that of untreated control	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID600072	Cell cycle arrest in human PC3 cells assessed as accumulation at G1 phase at 2 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 46.97 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID1079932	Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID99195	No. of dead mice/ total No. of mice bearing lung carcinoma LX-1 at a oral dose of 15 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1227812	Antitumor activity against human MCF7 cells xenografted in BALB/c nude mouse assessed as decrease in tumor volume at 0.023 mmol/kg, ip administered every 2 days for 3 times measured after day 6	2015	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1	The biological characteristics of a novel camptothecin-artesunate conjugate.
AID136695	The compound (5 mg/kg) administered intravenously was tested for antitumor activity against DU-145 (prostate) xenograft model in mice	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID1079931	Moderate 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]
AID1079935	Cytolytic 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]
AID269213	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 5 mg/kg, po measured as log10 of cell kill to reach 1000 mm3 tumor volume	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID625280	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID401949	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay	2004	Journal of natural products, May, Volume: 67, Issue:5	Phelligridins C-F: cytotoxic pyrano[4,3-c][2]benzopyran-1,6-dione and furo[3,2-c]pyran-4-one derivatives from the fungus Phellinus igniarius.
AID396729	Antitumor activity against human HCT8 xenografted in BALB/c nu/nu mouse assessed as tumor inhibition rate at 10 mg/kg, ip q3d for 3 days	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Synthesis and antitumor activity of novel 20s-camptothecin analogues.
AID537733	Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u	2010	European journal of medicinal chemistry, Nov, Volume: 45, Issue:11	Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1143388	Antiproliferative activity against human NCI-H1299 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81	Novel N-substituted sophoridinol derivatives as anticancer agents.
AID136685	The compound (10 mg/kg) administered intravenously was tested for antitumor activity against DU-145 (prostate) xenograft model in mice	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID1474167	Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status	2016	Drug discovery today, Apr, Volume: 21, Issue:4	DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID537734	Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay	2010	European journal of medicinal chemistry, Nov, Volume: 45, Issue:11	Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID343610	Cytotoxicity against human BEL-7402 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID343608	Cytotoxicity against human A549 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID46871	Cytotoxic activity against human lymphoblast tumor cell line CPT-K5 after 4 days of treatment	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Nitro and amino substitution in the D-ring of 5-(2-dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones: effect on topoisomerase-I targeting activity and cytotoxicity.
AID1462687	Cytotoxicity against human A549 cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17	Design, synthesis, and cytotoxic activity of novel 7-substituted camptothecin derivatives incorporating piperazinyl-sulfonylamidine moieties.
AID1826598	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID775809	Toxicity in BALB/C nude mouse xenografted with human A549 cells assessed as weight loss at 2 mg/kg, ip after 5 days relative to vehicle-treated control	2013	Journal of medicinal chemistry, Oct-24, Volume: 56, Issue:20	A new strategy to improve the metabolic stability of lactone: discovery of (20S,21S)-21-fluorocamptothecins as novel, hydrolytically stable topoisomerase I inhibitors.
AID143171	Percentage of body weight loss in CD1 mice with human Non-Small-Cell tumor xenograft at a oral dose of 5 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1221957	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID111437	Compound was tested for number of deaths of the animals at a dose of 7 mg/Kg in mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID247785	Inhibitory concentration against KBH5.0 cells overexpress BCRP	2005	Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3	5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
AID1702827	Systemic toxicity in FVB/N x BALB/c mouse assessed as body weight loss at 50 mg/kg, ip measured every 3 days for 15 days	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID690587	Cytotoxicity against human PC3 cells expressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20	Camptothecins in tumor homing via an RGD sequence mimetic.
AID1702823	Inhibition of topoisomerase 1 in human A549 cells nuclear extract assessed as reduction in supercoiled DNA relaxation at 0.2 uM incubated for 6 hrs by SYBR-green staining based agarose gel electrophoresis	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID527986	Antiproliferative activity against human DU145 cells by [3H]thymidine incorporation assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID625291	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID760272	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID1172294	Cytotoxicity against human KBVIN cells after 72 hrs by SRB assay	2014	Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22	Design and synthesis of novel spin-labeled camptothecin derivatives as potent cytotoxic agents.
AID78398	Toxic deaths was recorded on non-small-cell lung carcinoma H460 cells at a dose of 15 mg/kg perorally in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID610759	Cytotoxicity against human H460 cells assessed as stimulation of topoisomerase 1-mediated DNA cleavage	2011	Journal of natural products, Jun-24, Volume: 74, Issue:6	Inverse virtual screening of antitumor targets: pilot study on a small database of natural bioactive compounds.
AID1656654	Cytotoxicity against human LNCAP cells assessed as reduction in cell viability at 10 uM after 24 hrs by trypan blue dye exclusion assay	2020	Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3	Molecular mechanism of C-phycocyanin induced apoptosis in LNCaP cells.
AID333718	Inhibition of iron chelator DFO-induced HIF1 activation in human U251 cells	2004	Journal of natural products, Dec, Volume: 67, Issue:12	Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells.
AID1702780	Cytotoxicity against human MCF7 cells assessed as growth inhibition measured after 72 hrs by MTT assay	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID1824002	Induction of apoptosis in human SGC-7901 cells assessed as early apoptic cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0.01%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID625283	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID46486	Cytotoxicity measured with the drug resistant human non small cell lung carcinoma cell line COR-L23 (COR-L23/R) which over expresses multidrug resistance associated with protein(MRP)	2002	Journal of medicinal chemistry, Jan-31, Volume: 45, Issue:3	Novel angular benzophenazines: dual topoisomerase I and topoisomerase II inhibitors as potential anticancer agents.
AID331823	Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
AID56864	DNA topoisomerase I cleavage at 1 uM relative to SN38	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	Synthesis and pharmacological evaluation of novel non-lactone analogues of camptothecin.
AID679781	TP_TRANSPORTER: transepithelial transport in Bcrp-expressing MDCKII cells	2004	Cancer research, Aug-15, Volume: 64, Issue:16	Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions.
AID143198	Percentage of body weight loss of CD1 mice after treatment with compound	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1079939	Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID1075785	Inhibition of human recombinant topoisomerase 1 in human HCT116 cells assessed as stabilization of topoisomerase 1-DNA cleavage complex at 1 uM after 1 hr by DNA immunoblotting analysis	2014	Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4	Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID56562	Cytotoxicity against DNA topoisomerase I purified from calf thymus	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID1433678	Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 75 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 58.84%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID681273	TP_TRANSPORTER: transepithelial transport (basal to apical) in Bcrp1-expressing LLC-PK1 cells	2000	Journal of the National Cancer Institute, Oct-18, Volume: 92, Issue:20	Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan.
AID227412	Dose modifying factor expressed as the ratio of IC50 for the chemotherapy drug to IC50 for drug + GG918; Range = 1.0-23	2004	Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4	Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID343611	Cytotoxicity against human HT29 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID431815	Cytotoxicity against p53-deficient human HeLa cells after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID230378	Resistance index expressed as the ratio of IC50 value in resistant cells to that of sensitive line	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1433673	Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 8 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 32.80%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID1221978	Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1079942	Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID527985	Antiproliferative activity against human OVCAR-3 cells by [3H]thymidine incorporation assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID27126	Equilibrium association constant interacting with unilamellar vesicles of negatively charged DMPG in PBS buffer at pH of 7.4 and 37 degrees celsius.	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID1191162	Cytotoxicity against human PC3 cells assessed as inhibition of cell growth	2015	European journal of medicinal chemistry, Jan-27, Volume: 90	Synthetic approaches, functionalization and therapeutic potential of quinazoline and quinazolinone skeletons: the advances continue.
AID477295	Octanol-water partition coefficient, log P of the compound	2010	European journal of medicinal chemistry, Apr, Volume: 45, Issue:4	QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations.
AID1339541	Antiproliferative activity against human K562 cells assessed as reduction in cell viability by MTT assay	2017	ACS medicinal chemistry letters, Feb-09, Volume: 8, Issue:2	Synthesis, Biological Evaluation, and Autophagy Mechanism of 12
AID247637	Inhibitory concentration against human Bel-7402 liver cancer cell line	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID1817002	Synergistic cytotoxicity against human MCF7 cells at 50 nM after 96 hrs by MTT assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID1255492	Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 1.5 uM after 24 hrs by DAPI staining-based flow cytometry (Rvb = 16%)	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Synthesis and biological evaluation of novel N-phenyl ureidobenzenesulfonate derivatives as potential anticancer agents. Part 2. Modulation of the ring B.
AID489625	Antitumor activity against mouse LLC transplanted in C57BL/6 mouse assessed as tumor growth inhibition at 0.5 mg/kg, ip qd for 5 days	2010	European journal of medicinal chemistry, Jul, Volume: 45, Issue:7	Trifluoromethyl-promoted homocamptothecins: synthesis and biological activity.
AID156208	Tumor volume index was measured on small--cell lung carcinoma (POVD) cells at a dose of 15 mg/kg intravenously in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID103786	Tested in vitro for cytotoxicity against human tumor cell line MCF-7/ADR (breast)	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID1433675	Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 25 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 58.84%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID527979	Specificity index, ratio of IC50 for HIF1alpha in human U251 cells under normoxic condition to IC50 for HIF1alpha in human U251 cells under hypoxic condition	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID402279	Cytotoxicity against human Ketr3 cells after 96 hrs by MTT assay	2004	Journal of natural products, May, Volume: 67, Issue:5	Phelligridins C-F: cytotoxic pyrano[4,3-c][2]benzopyran-1,6-dione and furo[3,2-c]pyran-4-one derivatives from the fungus Phellinus igniarius.
AID1656704	Induction of apoptosis in human LNCAP cells assessed as decrease in uncleaved PARP expression at 10 uM measured after 24 hrs by Western blot analysis	2020	Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3	Molecular mechanism of C-phycocyanin induced apoptosis in LNCaP cells.
AID1824016	Induction of apoptosis in human MGC-803 cells assessed as necrotic cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0.05%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID56880	Effective concentration required to cleave DNA, mediated by human DNA topoisomerase I (TOP1) reported as REC i.e. concentration relative to topotecan (assumed as 1)	2003	Journal of medicinal chemistry, May-22, Volume: 46, Issue:11	Nitro and amino substitution in the D-ring of 5-(2-dimethylaminoethyl)- 2,3-methylenedioxy-5H-dibenzo[c,h][1,6]naphthyridin-6-ones: effect on topoisomerase-I targeting activity and cytotoxicity.
AID721723	Antiproliferative activity against human A549 cells after 72 hrs by XTT assay	2013	European journal of medicinal chemistry, Jan, Volume: 59	Synthesis and antiproliferative evaluation of 3-phenylquinolinylchalcone derivatives against non-small cell lung cancers and breast cancers.
AID721722	Antiproliferative activity against human MCF7 cells after 72 hrs by XTT assay	2013	European journal of medicinal chemistry, Jan, Volume: 59	Synthesis and antiproliferative evaluation of 3-phenylquinolinylchalcone derivatives against non-small cell lung cancers and breast cancers.
AID200293	Cytotoxicity was determined in vitro in SKVLB cells(ovarian with upregulated MDRp-glycoprotein) of human tumor cell lines by using MTT assay	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1143386	Antiproliferative activity against human HepG2 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81	Novel N-substituted sophoridinol derivatives as anticancer agents.
AID111702	Mean body weight loss for animals in all experimental conditions at dose 7 mg/Kg in HT-29 human colon xenograft infected mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1211545	Total clearance in rat	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID421975	Inhibition of HIF1 activation in human U251 cells transiently transfected in pGL2-TK-HRE plasmid under hypoxic condition at 0.05 uM after 16 hrs by luciferase reporter gene assay	2009	Journal of natural products, May-22, Volume: 72, Issue:5	Cytotoxic and HIF-1alpha inhibitory compounds from Crossosoma bigelovii.
AID721724	Antiproliferative activity against human H460 cells after 72 hrs by XTT assay	2013	European journal of medicinal chemistry, Jan, Volume: 59	Synthesis and antiproliferative evaluation of 3-phenylquinolinylchalcone derivatives against non-small cell lung cancers and breast cancers.
AID1462691	Cytotoxicity against human KBVIN cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17	Design, synthesis, and cytotoxic activity of novel 7-substituted camptothecin derivatives incorporating piperazinyl-sulfonylamidine moieties.
AID1221977	Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID94333	In vitro cytotoxicity against KB/VCR (Vincristine-resistant cancer cell line)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions.
AID1824037	Induction of cell cycle arrest in human MGC-803 cells assessed as accumulation at S phase at 0.9 uM after 24 hrs by propidium iodide staining based flow cytometry	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID699539	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1255491	Cell cycle arrest in human M21 cells assessed as accumulation at S phase at 1.5 uM after 24 hrs by DAPI staining-based flow cytometry (Rvb = 17.4%)	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Synthesis and biological evaluation of novel N-phenyl ureidobenzenesulfonate derivatives as potential anticancer agents. Part 2. Modulation of the ring B.
AID588214	FDA HLAED, liver enzyme composite activity	2004	Current drug discovery technologies, Dec, Volume: 1, Issue:4	Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID145078	The compound (2.5 mg/kg) administered intravenously was tested for antitumor activity against NCI-H23 (lung) xenograft model in mice	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID1443372	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.
AID1075783	Inhibition of human recombinant topoisomerase 1 in human HCT116 cells assessed as reversal of topoisomerase 1-DNA cleavage complex stabilization at 1 uM incubated for 1 hr followed by compound washout measured after 24 hrs by DNA immunoblotting analysis	2014	Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4	Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID1075764	Resistance ratio of GI50 for human mitoxantrone-resistant H460 cells to GI50 for human H460 cells	2014	Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4	Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID1817014	Cytotoxicity against human MCF-7/TDP1 cells assessed as cell growth inhibition after 72 hrs by MTT assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID1211553	Drug uptake in iv dosed Sprague-Dawley rat liver after 5 hrs by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID26145	Half-life in PBS buffer solution in the presence of human serum albumin	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID396723	Cytotoxicity against human HCT8 cells by MTT assay	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Synthesis and antitumor activity of novel 20s-camptothecin analogues.
AID431839	Cell cycle distribution in human HT-29 cells assessed as accumulation at S phase at 0.1 uM after 48 hrs by flow cytometry	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID1079937	Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1600555	Inhibition of DNA topoisomerase 2 in human MCF7 cells at 5 uM incubated for 18 to 24 hrs by kinase assay relative to control	2019	Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19	Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives.
AID389690	Cytotoxicity against multidrug resistant human KBH5.0 cells overexpressing BCRP after MTT assay	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.
AID590485	Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 25 uM after 24 hrs by flow cytometry (Rvb = 10.34%)	2011	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7	Synthesis and antitumor activity of 10-arylcamptothecin derivatives.
AID1824004	Induction of apoptosis in human SGC-7901 cells assessed as necrotic cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0.01%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID22190	Excited-state lifetime value for carboxylate form of compound bound to human serum albumin	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID1433677	Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 25 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 8.36%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID16882	Equilibrium association (binding) constant interacting with Unilamellar Vesicles of negatively charged DMPG in PBS buffer at pH 7.4 and 37 C	1999	Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16	Novel A,B,E-ring-modified camptothecins displaying high lipophilicity and markedly improved human blood stabilities.
AID425653	Renal clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID1433695	Toxicity in BALB/c nude mouse xenografted with human Bel7402 cells assessed as body weight at 5 mg/kg, ip administered once in a week for two weeks starting from 6 days post tumor transplantation measured every 3 days for 21 days (Rvb = 14.5 g)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID431820	Cytotoxicity against p53-deficient human PC3 cells after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID373528	Cytotoxicity against human RPMI8226 cells by MTT method	2009	European journal of medicinal chemistry, Apr, Volume: 44, Issue:4	Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones.
AID321331	Antitumor activity against human LOVO cells after 4 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3	New homocamptothecins: synthesis, antitumor activity, and molecular modeling.
AID103947	Antiproliferative activity measured against MCF-7-mdr cells.	1998	Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27	Homocamptothecins: synthesis and antitumor activity of novel E-ring-modified camptothecin analogues.
AID227859	In Vitro cytotoxicity against human stomach cancer cell line (MKN45)	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1387410	Inhibition of human recombinant topoisomerase-1-mediated DNA cleavage in at 50 uM using supercoiled pHOT-1 DNA incubated for 30 mins by ethidium bromide staining based agarose gel elctrophoresis method	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID481180	Cytotoxicity against human A549 cells after 72 hrs by MTT assay	2010	Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9	Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities.
AID586352	Cytotoxicity against mouse bone marrow cell by CFU-GM assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID1811234	Inhibition of human recombinant COX-2 using arachidonic acid as substrate preincubated 10 mins followed by substrate addition and measured after 2 mins by ELISA	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation.
AID625289	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID200937	Tested in vitro for cytotoxicity against human tumor cell line SF-268 (CNS).	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID219883	In Vitro cytotoxicity against human colon cancer cell line (WiDr)	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID586335	Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID625287	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID389686	Cytotoxicity against mouse P388 cells after MTT assay	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.
AID490171	Cytotoxicity against human KB cells after 3 days by MTT assay	2010	European journal of medicinal chemistry, Jul, Volume: 45, Issue:7	Cytotoxicity and topo I targeting activity of substituted 10--nitrogenous heterocyclic aromatic group derivatives of SN-38.
AID1188713	Antiproliferative activity against human H1299 cells after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Synthesis and biological evaluation of hydroxycinnamic acid hydrazide derivatives as inducer of caspase-3.
AID599609	Induction of apoptosis in human PC3 cells at 2 uM after 72 hrs using propidium iodide staining by flow cytometry (Rvb = 1.79 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID1702828	Systemic toxicity in FVB/N x BALB/c mouse assessed as mouse death at 50 mg/kg, ip measured within 14 days	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID16881	Equilibrium association (binding) constant interacting with Unilamellar Vesicles of electroneutral DMPC in PBSbuffer at pH 7.4 and 37 C	1999	Journal of medicinal chemistry, Aug-12, Volume: 42, Issue:16	Novel A,B,E-ring-modified camptothecins displaying high lipophilicity and markedly improved human blood stabilities.
AID702840	Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations.
AID1221972	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID702842	Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations.
AID1823978	Antiproliferative activity against human GES1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID1221980	Transporter substrate index of efflux ratio in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1172291	Cytotoxicity against human A549 cells after 72 hrs by SRB assay	2014	Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22	Design and synthesis of novel spin-labeled camptothecin derivatives as potent cytotoxic agents.
AID223634	In Vitro cytotoxicity against human ovarian cancer cell line (SK-OV-3)	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID115141	Maximally tolerated dose that caused <=30% body weight loss in mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1648756	Antitumour activity against human HCT116 cells xenografted in nude mouse assessed as tumour growth inhibition at 0.5 mg/kg, ip qd measured every two days for 21 days by caliper method relative to control	2020	ACS medicinal chemistry letters, Apr-09, Volume: 11, Issue:4	Natural Product Evodiamine with Borate Trigger Unit: Discovery of Potent Antitumor Agents against Colon Cancer.
AID527978	Inhibition of HIF1alpha in human U251 cells under normoxic condition by luciferase reporter gene assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID1254844	Selectivity index, ratio of IC50 for normal human astrocytes to IC50 for human GBM2 cells	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID681208	TP_TRANSPORTER: increase in intracellular accumulation by GF120918 in T8 cell	2001	Clinical cancer research : an official journal of the American Association for Cancer Research, Apr, Volume: 7, Issue:4	Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918.
AID143196	No. of dead mice/ total No. of mice with human Non-Small-Cell tumor xenograft at a oral dose of 9 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1668358	Induction of apoptosis in human S1 cells assessed as viable cells at 5 uM incubated for 48 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 94.1%)	2020	Journal of natural products, 05-22, Volume: 83, Issue:5	Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.
AID1079945	Animal toxicity known. [column 'TOXIC' in source]
AID540210	Clearance in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID78394	Tumor volume index was measured on non-small-cell lung carcinoma H460 cells at a dose of 15 mg/kg intravenously in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID714171	Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of hypoxia-induced HIF-1alpha accumulation in nuclear extract after 6 to 24 hrs by immunoblot analysis	2012	European journal of medicinal chemistry, Mar, Volume: 49	Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
AID600063	Inhibition of serotonin-induced AKT phosphorylation in human PC3 cells at 2 uM after 48 hrs by Western blotting	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID681334	TP_TRANSPORTER: transepithelial transport in Caco 2 cell	2004	Pharmaceutical research, May, Volume: 21, Issue:5	Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo.
AID1443375	Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.
AID332046	Cytotoxicity against human H460 cells	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	Synthesis and cytotoxic activity of new 9-substituted camptothecins.
AID586338	Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID1433712	Inhibition of Escherichia coli topoisomerase 1-mediated relaxation of supercoiled Pcmv-6 plasmid DNA at 1 to 50 uM after 30 mins by ethidium bromide staining based agarose gel electrophoretic analysis	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID1221958	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1228604	Growth inhibition of human HOP62 cells by five-dose growth inhibition assay	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID586390	Ratio of IC90 for mouse bone marrow cell to IC90 for human bone marrow cell	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID211118	Average concentration to cause 50% inhibition of topo 1 using the cleavable complex assay	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID247815	Concentration required to inhibit cell proliferation in RPM18402 tumor cell line	2004	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22	Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
AID721752	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	2013	Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3	Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID625284	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID760276	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID699541	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID210946	Inhibition of Topoisomerase I by cleavage complex formation in human HL-60 cells	1993	Journal of medicinal chemistry, Sep-03, Volume: 36, Issue:18	Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs.
AID1387411	Inhibition of human recombinant topoisomerase-1-mediated DNA cleavage in at 100 uM using supercoiled pHOT-1 DNA incubated for 30 mins by ethidium bromide staining based agarose gel elctrophoresis method	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID1443374	Cytotoxicity against human KBVIN cells after 72 hrs by sulforhodamine B assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.
AID9868	Tested in vitro for cytotoxicity against human tumor cell line ACHN (renal).	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID426062	Antitumor activity against human A549/ATCC cells by SRB method	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation.
AID1532298	Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as liver index at 1.5 mg/kg, ip administered on day 4, 5, 7 and 9 post-transplantation measured 17 days post-transplantation (Rvb = 5.8 +/- 0.38%)	2019	European journal of medicinal chemistry, Jan-01, Volume: 161	Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
AID586417	Toxicity in nu/nu mouse assessed as body weight loss at 2 mg/kg, po QD for 5 days followed by 4 days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID1221982	Fraction absorbed in human	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID431823	Cytotoxicity against p53-deficient human K562 cells after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID17281	Equilibrium association constant interacting with unilamellar vesicles of electroneutral in PBS buffer at pH 7.4	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	The novel silatecan 7-tert-butyldimethylsilyl-10-hydroxycamptothecin displays high lipophilicity, improved human blood stability, and potent anticancer activity.
AID537736	Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay	2010	European journal of medicinal chemistry, Nov, Volume: 45, Issue:11	Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID586414	Toxicity in nu/nu mouse assessed as body weight loss at 2 mg/kg, po QD for 5 days followed by 2 days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID248252	Concentration required to inhibit cell proliferation in CPT-K5 tumor cell line; camptothecin resistant	2004	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22	Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
AID145080	The compound (5 mg/kg) administered intravenously was tested for antitumor activity against NCI-H23 (lung) xenograft model in mice	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID377270	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay	2006	Journal of natural products, Jun, Volume: 69, Issue:6	Mono-, Bi-, and triphenanthrenes from the tubers of Cremastra appendiculata.
AID95164	Antiproliferative activity measured against K562adr leukemia cells.	1998	Journal of medicinal chemistry, Dec-31, Volume: 41, Issue:27	Homocamptothecins: synthesis and antitumor activity of novel E-ring-modified camptothecin analogues.
AID247744	Concentration required to inhibit cell proliferation in P388 tumor cell line	2004	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22	Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
AID57904	In vitro anti-cancer activity against DU-145 (Prostate) human tumor cell line	1999	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12	Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.
AID373531	Cytotoxicity against multidrug resistant human KBV1 cells overexpressing MDR1 by MTT method	2009	European journal of medicinal chemistry, Apr, Volume: 44, Issue:4	Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones.
AID590483	Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 25 uM after 24 hrs by flow cytometry (Rvb = 62.14%)	2011	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7	Synthesis and antitumor activity of 10-arylcamptothecin derivatives.
AID1433647	Antiproliferative activity against human BGC823 cells after 96 hrs by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID1143391	Antiproliferative activity against human KB cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81	Novel N-substituted sophoridinol derivatives as anticancer agents.
AID1387384	Cytotoxicity in human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID146690	Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460)	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID95849	In vitro cytotoxicity against KB (human epidermoid carcinoma of the nasopharynx)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions.
AID600081	Cell cycle arrest in human PC3 cells assessed as accumulation at G2 phase at 2 uM after 48 hrs using propidium iodide staining by flow cytometry (Rvb = 13.36 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID156205	log10 cell kill was measured on small--cell lung carcinoma (POVD) cells at a dose of 15 mg/kg intravenously in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1079944	Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1702784	Cytotoxicity against human KB-VIN cells assessed as growth inhibition measured after 72 hrs by MTT assay	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID46269	log10 cell kill was measured on colon carcinoma (COCF) cells at a dose of 15 mg/kg perorally in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1228610	Growth inhibition of human DU145 cells by five-dose growth inhibition assay	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID1668356	Induction of apoptosis in human S1 cells assessed as late apoptotic cells at 5 uM incubated for 48 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 3.6%)	2020	Journal of natural products, 05-22, Volume: 83, Issue:5	Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.
AID239852	Relative effective concentration to cleave plasmid DNA with human topoisomerase I; compared to camptothecin=1	2004	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22	Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
AID1269400	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3	Design, synthesis and biological evaluation of 3-substituted indenoisoquinoline derivatives as topoisomerase I inhibitors.
AID269231	Toxicity in nude athymic mouse at 5 mg/kg, po	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID200271	Human tumor cell cytotoxicity assay was performed using MTT (SK-OV3 cell line )	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1443371	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay	2017	Bioorganic & medicinal chemistry letters, 04-15, Volume: 27, Issue:8	Design, synthesis and potent cytotoxic activity of novel 7-(N-[(substituted-sulfonyl)piperazinyl]-methyl)-camptothecin derivatives.
AID7483	Potentiation factor at 50% growth inhibition (IC50 of compound to that of compound along with PARP inhibitor) in experiment 2	2000	Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22	Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
AID1433648	Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID431816	Cytotoxicity against human HT-29 cells expressing p53 mutant after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID269204	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 5 mg/kg, po measured as tumor volume inhibition relative to control	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID1600548	Inhibition of DNA topoisomerase 2 in human HeLa cells at 1 uM incubated for 18 to 24 hrs by kinase assay relative to control	2019	Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19	Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives.
AID1075767	Cytotoxicity against human H460 cells after 72 hrs by MTT assay	2014	Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4	Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID1274797	Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for human H1299 cells	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID1387400	Antitumor activity against human HepG2 cells xenografted in Balb/C mouse assessed as inhibition of tumor growth at 2 mg/kg, iv dosed once per week for 30 days followed by 2 weeks observation	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID230835	MDR ratio is defined as the quotient of SKVLB IC50/SKOV3 IC50	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1433649	Antiproliferative activity against human A2780 cells after 96 hrs by MTT assay	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID527982	Antiproliferative activity against human PC3 cells by [3H]thymidine incorporation assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID625290	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1211550	In vivo intrinsic biliary clearance in iv dosed Sprague-Dawley rat by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID121158	Delay in tumor growth in drug treated animals compared to controls at a dose of 54(mg/kg)	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID202366	Cytotoxic potentiation of Topotecan (TP) by the compound in human colon carcinoma SW620 cell line	2002	Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23	Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.
AID1274793	Antiproliferative activity against human PC3 cells after 72 hrs by XTT assay	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID411093	Cytotoxicity against human HT-29 cells by SRB method	2008	Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24	Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin.
AID248502	Inhibitory concentration against camptothecin-resistant variant of P388 cell line was determined	2005	Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3	5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
AID1211551	Drug uptake in sandwich cultured Sprague-Dawley rat hepatocytes by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID1387385	Cytotoxicity in human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID721720	Antiproliferative activity against human SKBR3 cells after 72 hrs by XTT assay	2013	European journal of medicinal chemistry, Jan, Volume: 59	Synthesis and antiproliferative evaluation of 3-phenylquinolinylchalcone derivatives against non-small cell lung cancers and breast cancers.
AID540213	Half life in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID277799	Cytotoxicity against human A2708 cells	2007	Journal of natural products, Feb, Volume: 70, Issue:2	Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius.
AID612417	Antiproliferative activity against human NCI-H460 cells after 1 hr by coulter counter analysis	2011	Bioorganic & medicinal chemistry, Aug-15, Volume: 19, Issue:16	Synthesis and topoisomerase I inhibitory activity of a novel diazaindeno[2,1-b]phenanthrene analogue of Lamellarin D.
AID1274794	Antiproliferative activity against human HuH7 cells after 72 hrs by XTT assay	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID78416	In vitro cytotoxicity against H460 a human non-small lung carcinoma cell line after 1 hour drug exposure	2001	Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3	Novel cytotoxic 7-iminomethyl and 7-aminomethyl derivatives of camptothecin.
AID89761	Percentage inhibition of tumor volume in treated versus control mice against human Non-Small-Cell tumor xenograft at a oral dose of 5 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID486938	Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay	2010	European journal of medicinal chemistry, Jun, Volume: 45, Issue:6	Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I.
AID745331	Cytotoxicity against mouse L1210 cells	2013	European journal of medicinal chemistry, May, Volume: 63	Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID377023	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	2006	Journal of natural products, Jun, Volume: 69, Issue:6	Mono-, Bi-, and triphenanthrenes from the tubers of Cremastra appendiculata.
AID1227811	Toxicity in BALB/c nude mouse assessed as animal death at 0.023 mmol/kg, ip administered every 2 days for 3 times measured on day 6	2015	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1	The biological characteristics of a novel camptothecin-artesunate conjugate.
AID57214	TOP-2 mediated DNA cleavage measured as effective concentration relative to VM26	2002	Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22	Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435.
AID78391	log10 cell kill was measured on non-small-cell lung carcinoma H460 cells at a dose of 15 mg/kg intravenously in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1462690	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17	Design, synthesis, and cytotoxic activity of novel 7-substituted camptothecin derivatives incorporating piperazinyl-sulfonylamidine moieties.
AID111436	Compound was tested for number of deaths of the animals at a dose of 5 mg/Kg in mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1299119	Reduction of insulin-induced HIF-1 alpha expression in human HCT116 cells at 3 uM by western blot analysis	2016	Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12	Synthesis and biological evaluation of 1,2-dithiol-3-thiones and pyrrolo[1,2-a]pyrazines as novel hypoxia inducible factor-1 (HIF-1) inhibitor.
AID1221960	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID379516	Cytotoxicity against human A549 cells after 96 hrs by MTT assay	2006	Journal of natural products, Nov, Volume: 69, Issue:11	A nitrogen-containing 3-alkyl-1,4-benzoquinone and a gomphilactone derivative from Embelia ribes.
AID156212	Toxic deaths was recorded on small--cell lung carcinoma (POVD) cells at a dose of 15 mg/kg perorally in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID426063	Antitumor activity against human HT-29 cells by SRB method	2009	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15	7-Cycloalkylcamptothecin derivatives: Preparation and biological evaluation.
AID453828	Antiproliferative activity against human H1299 cells after 72 hrs by XTT assay	2009	Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21	Synthesis and antiproliferative evaluation of 6-arylindeno[1,2-c]quinoline derivatives.
AID31609	Percent inhibition of acetylcholinesterase using ATCh1 as a substrate	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID1702782	Cytotoxicity against human KB cells assessed as growth inhibition measured after 72 hrs by MTT assay	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID7218	Tested in vitro for cytotoxicity against 56 human tumor cell lines	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID1405118	Antiproliferative activity against human HT1080 cells after 48 hrs by SRB assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID1075784	Inhibition of human recombinant topoisomerase 1 in human HCT116 cells assessed as reversal of topoisomerase 1-DNA cleavage complex stabilization at 1 uM incubated for 1 hr followed by compound washout measured up to 6 hrs by DNA immunoblotting analysis	2014	Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4	Optimization of the lactam side chain of 7-azaindenoisoquinoline topoisomerase I inhibitors and mechanism of action studies in cancer cells.
AID1228598	Inhibition of recombinant topoisomerase 1 (unknown origin) assessed as DNA cleavage using 3'-[32P]-labeled 117-bp DNA oligonucleotide at 1 uM by PAGE assay	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID490172	Cytotoxicity against human MCF7 cells after 3 days by MTT assay	2010	European journal of medicinal chemistry, Jul, Volume: 45, Issue:7	Cytotoxicity and topo I targeting activity of substituted 10--nitrogenous heterocyclic aromatic group derivatives of SN-38.
AID1254839	Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID1826599	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID600075	Induction of apoptosis in human PC3 cells at 2 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 1.27 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID111477	The no. of deaths of mice(infected with HT-29 cells) was reported at a dose of 9 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1221971	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID414760	Cytotoxicity against BCRP overexpressing human KBH5.0 cells after 4 days by MTT method	2009	Bioorganic & medicinal chemistry, Apr-01, Volume: 17, Issue:7	12-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridines as novel topoisomerase I-targeting antitumor agents.
AID401947	Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay	2004	Journal of natural products, May, Volume: 67, Issue:5	Phelligridins C-F: cytotoxic pyrano[4,3-c][2]benzopyran-1,6-dione and furo[3,2-c]pyran-4-one derivatives from the fungus Phellinus igniarius.
AID146563	In vivo antitumor activity in NSCLC H460 xenografted sc in athymic nude mice expressed as lethal toxicity at a dose of 15 mg/kg orally for q4dx4;0/4	2001	Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3	Novel cytotoxic 7-iminomethyl and 7-aminomethyl derivatives of camptothecin.
AID111439	Compound was tested for number of deaths of the animals at a dose of 9 mg/Kg in mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID307320	Growth inhibition of adriamycin-resistant MCF7 cells after 4 days	2007	Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12	Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives.
AID269202	Inhibition of human H460 cell growth	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID1462688	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17	Design, synthesis, and cytotoxic activity of novel 7-substituted camptothecin derivatives incorporating piperazinyl-sulfonylamidine moieties.
AID1239181	Cytotoxicity against human A549 cells after 72 hrs by MTT assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16	Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents.
AID1405130	Cell cycle arrest in human M21 cells assessed as accumulation at sub-G1 phase at 1.8 uM after 24 hrs by DAPI staining based flow cytometry relative to control	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID760279	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID8660	Cytotoxic potentiation of Topotecan (TP) by the compound in human lung carcinoma A549 cell line	2002	Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23	Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.
AID610760	Binding affinity to topoisomerase 1	2011	Journal of natural products, Jun-24, Volume: 74, Issue:6	Inverse virtual screening of antitumor targets: pilot study on a small database of natural bioactive compounds.
AID1239183	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16	Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents.
AID486939	Cytotoxicity against human LoVo cells after 3 days by MTT assay	2010	European journal of medicinal chemistry, Jun, Volume: 45, Issue:6	Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I.
AID46272	Tumor volume index was measured on colon carcinoma (COCF) cells at a dose of 15 mg/kg perorally in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1274798	Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for human PC3 cells	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID1817007	Induction of TDP1-DNA complex formation in human MCF7 cells at 10 uM by ICE assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID396725	Antitumor activity against human HCT8 xenografted in BALB/c nu/nu mouse assessed as change in body weight at 5 mg/kg, ip q3d for 3 days	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Synthesis and antitumor activity of novel 20s-camptothecin analogues.
AID1582321	Toxicity in mouse xenografted with human HCT116 cells assessed as reduction in body weight at 0.5 mg/kg, ip qd for 21 days administration starting from 10 days after tumor cell implantation measured every 2 or 4 days till the end of the treatment period	2020	Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2	Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer.
AID1221973	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1143387	Antiproliferative activity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81	Novel N-substituted sophoridinol derivatives as anticancer agents.
AID343605	Cytotoxicity against human NCI446 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID1532287	Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as state and behavioral changes at 1.5 mg/kg, ip administered on day 4, 5, 7 and 9 post-transplantation	2019	European journal of medicinal chemistry, Jan-01, Volume: 161	Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
AID200779	In vitro anti-cancer activity against SF 268(CNS) human tumor cell line	1999	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12	Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.
AID684312	Toxicity in human A549 cells xenografted in BALB/c mouse assessed as reduction in body weight at 0.5 mg/kg, iv qd for 5 days measured after 14 days	2012	European journal of medicinal chemistry, Oct, Volume: 56	Synthesis and preliminary bioevaluation of novel E-ring modified acetal analog of camptothecin as cytotoxic agents.
AID431837	Cell cycle distribution in human HT-29 cells assessed as accumulation at S phase at 0.1 uM after 12 hrs by flow cytometry	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID527987	Antiproliferative activity against human PANC1 cells by [3H]thymidine incorporation assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID702841	Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTT assay	2012	Journal of medicinal chemistry, Sep-13, Volume: 55, Issue:17	New tricks for an old natural product: discovery of highly potent evodiamine derivatives as novel antitumor agents by systemic structure-activity relationship analysis and biological evaluations.
AID100463	Inhibitory activity in mice bearing L1210 leukemia	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID1464540	Cytotoxicity against human KB cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20	Design, semisynthesis and potent cytotoxic activity of novel 10-fluorocamptothecin derivatives.
AID111714	The body weight loss was measured in mice in vivo by using the HT-29 Human colon Xenograft model at a dose of 7 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1702781	Cytotoxicity against human A549 cells assessed as growth inhibition measured after 72 hrs by MTT assay	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID721751	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay	2013	Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3	Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID1228605	Growth inhibition of human HCT116 cells by five-dose growth inhibition assay	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID745329	Inhibition of topoisomerase 1 (unknown origin)-mediated DNA cleavage at 1 uM relative to SN-38	2013	European journal of medicinal chemistry, May, Volume: 63	Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID379517	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay	2006	Journal of natural products, Nov, Volume: 69, Issue:11	A nitrogen-containing 3-alkyl-1,4-benzoquinone and a gomphilactone derivative from Embelia ribes.
AID1221981	Efflux ratio of permeability from apical to basolateral over basolateral to apical side of MDCK cells expressing BCRP	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID586345	Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID111475	The no. of deaths of mice(infected with HT-29 cells) was reported at a dose of 7 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1254845	Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID307322	Growth inhibition of MCF7 cells after 4 days	2007	Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12	Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives.
AID321333	Antitumor activity against mouse C26 cells implanted in C57BL/6 mouse at 1 mg/kg, sc QD for 5 days	2008	Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3	New homocamptothecins: synthesis, antitumor activity, and molecular modeling.
AID453825	Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay	2009	Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21	Synthesis and antiproliferative evaluation of 6-arylindeno[1,2-c]quinoline derivatives.
AID343609	Cytotoxicity against human A2780 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID634883	Growth inhibition of human HepG2 cells after 72 hrs by XTT assay	2011	Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24	Synthesis and antiproliferative evaluation of 6-aryl-11-iminoindeno[1,2-c]quinoline derivatives.
AID377274	Cytotoxicity against human WISH cells after 96 hrs by MTT assay	2006	Journal of natural products, Jun, Volume: 69, Issue:6	Mono-, Bi-, and triphenanthrenes from the tubers of Cremastra appendiculata.
AID625292	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID113229	Efficacy against HT-29 human colon xenograft infected mice expressed as tumor growth ratio at dose 7 mg/Kg	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1532301	Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as spleen weight at 1.5 mg/kg, ip administered on day 4, 5, 7 and 9 post-transplantation measured 17 days post-transplantation (Rvb = 252 +/- 12 mg)	2019	European journal of medicinal chemistry, Jan-01, Volume: 161	Novel tyrosyl-DNA phosphodiesterase 1 inhibitors enhance the therapeutic impact of topoteсan on in vivo tumor models.
AID373530	Cytotoxicity against human KB3-1 cells by MTT method	2009	European journal of medicinal chemistry, Apr, Volume: 44, Issue:4	Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones.
AID396724	Cytotoxicity against human PC3 cells by MTT assay	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Synthesis and antitumor activity of novel 20s-camptothecin analogues.
AID396728	Antitumor activity against human HCT8 xenografted in BALB/c nu/nu mouse assessed as tumor inhibition rate at 5 mg/kg, ip q3d for 3 days	2009	Bioorganic & medicinal chemistry letters, Jan-15, Volume: 19, Issue:2	Synthesis and antitumor activity of novel 20s-camptothecin analogues.
AID1079940	Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID248143	Inhibitory concentration against P388 cell line in mouse leukemia was determine	2005	Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3	5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
AID111473	The no. of deaths of mice(infected with HT-29 cells) was reported at a dose of 5 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID540209	Volume of distribution at steady state in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID113381	In vivo efficacy of tumor growth ratio(T/B) of compound was calculated by using the HT-29 Human colon Xenograft model in mice at a dose of 9 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1817003	Synergistic cytotoxicity against human MCF7 cells after 96 hrs in presence of 12-(2-(Dimethylamino)ethyl)-1,2-dihydroxy-[1,3]dioxolo[4',5':4,5]benzo[1,2-c]phenanthridine-13(12H)-one by MTT assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID1702783	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition measured after 72 hrs by MTT assay	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID1188715	Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay	2014	European journal of medicinal chemistry, Oct-06, Volume: 85	Synthesis and biological evaluation of hydroxycinnamic acid hydrazide derivatives as inducer of caspase-3.
AID343606	Cytotoxicity against human MCF7 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID1387397	Aqueous solubility of the compound	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID131159	Effect in increasing life span of mice bearing L1210 leukemia	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID1826600	Antiproliferative activity against human K562 cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID409902	Inhibition of human topoisomerase 1 expressed in Escherichia coli assessed as drug level causing 10% mediated DNA cleavage relative to topotecan	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
AID113379	In vivo efficacy of tumor growth ratio(T/B) of compound was calculated by using the HT-29 Human colon Xenograft model in mice at a dose of 5 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID377272	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay	2006	Journal of natural products, Jun, Volume: 69, Issue:6	Mono-, Bi-, and triphenanthrenes from the tubers of Cremastra appendiculata.
AID93640	Concentration causing 50% decrease of ovarian carcinoma cisplatin resistant variant (IGROV-1/pt1) cell growth over that of untreated control.	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1255450	Antiproliferative activity against human HT1080 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Synthesis and biological evaluation of novel N-phenyl ureidobenzenesulfonate derivatives as potential anticancer agents. Part 2. Modulation of the ring B.
AID453829	Cytotoxicity against human MRC5 cells after 72 hrs by XTT assay	2009	Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21	Synthesis and antiproliferative evaluation of 6-arylindeno[1,2-c]quinoline derivatives.
AID634881	Growth inhibition of human A549 cells after 72 hrs by XTT assay	2011	Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24	Synthesis and antiproliferative evaluation of 6-aryl-11-iminoindeno[1,2-c]quinoline derivatives.
AID1582355	Antitumor activity against human HCT116 cells xenografted in mouse assessed as reduction in tumor growth at 0.5 mg/kg, ip qd for 21 days administration starting from 10 days after tumor cell implantation measured every 2 or 4 days till the end of the trea	2020	Journal of medicinal chemistry, 01-23, Volume: 63, Issue:2	Scaffold Hopping of Natural Product Evodiamine: Discovery of a Novel Antitumor Scaffold with Excellent Potency against Colon Cancer.
AID481181	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay	2010	Bioorganic & medicinal chemistry, May-01, Volume: 18, Issue:9	Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities.
AID679628	TP_TRANSPORTER: drug resistance(Imatinib mesylate) in BCRP-expressing SaoS2 cells	2004	Cancer research, Apr-01, Volume: 64, Issue:7	Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro.
AID625282	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID684310	Antitumor activity against human A549 cells xenografted in BALB/c mouse assessed as decrease in tumor weight at 0.5 mg/kg, iv qd for 5 days measured after 14 days relative to control	2012	European journal of medicinal chemistry, Oct, Volume: 56	Synthesis and preliminary bioevaluation of novel E-ring modified acetal analog of camptothecin as cytotoxic agents.
AID22191	Excited-state lifetime value for lactone form of compound bound to human serum albumin	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID1211554	Biliary excretion index in sandwich cultured Sprague-Dawley rat hepatocytes after 15 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID1702895	Antitumor activity in FVB/N mouse model of pCMV/SB/pT3-Caggs-NRasV12/myr-AKT/pT3-EF1alpha plasmids-induced primary hepatocellular carcinoma assessed as suppression of tumor growth at 2 mg/kg, iv administered every other day for 2 weeks	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID1221956	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1405121	Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID46874	Cytotoxicity using camptothecin-resistant variant of RPM18402 (CPT-K5) possessing functional, but mutant TOP-1	2002	Bioorganic & medicinal chemistry letters, Nov-18, Volume: 12, Issue:22	Diaza- and triazachrysenes: potent topoisomerase-targeting agents with exceptional antitumor activity against the human tumor xenograft, MDA-MB-435.
AID1702826	Inhibition of human recombinant topoisomerase 1 expressed in baculovirus expression system at 0.5 uM using supercoiled plasmid DNA as substrate preincubated 20 mins followed by substrate addition and measured after 30 mins by SYBR-green staining based aga	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID1702897	Antitumor activity in FVB/N mouse model of pCMV/SB/pT3-Caggs-NRasV12/myr-AKT/pT3-EF1alpha plasmids-induced primary hepatocellular carcinoma assessed as reduction in number of nodules on liver surface at 2 mg/kg, iv administered every other day for 2 weeks	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID311524	Oral bioavailability in human	2007	Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24	Hologram QSAR model for the prediction of human oral bioavailability.
AID600061	Inhibition of serotonin-induced MAPK phosphorylation in human PC3 cells at 2 uM after 48 hrs by Western blotting	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID1274799	Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for human HuH7 cells	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID1410937	Induction of apoptosis in human A498 cells assessed as increase in caspase-3/7 activity at 1 uM after 24 hrs by Caspase-Glo 3/7 assay relative to control	2018	Journal of medicinal chemistry, Jul-26, Volume: 61, Issue:14	Small Molecule Inhibition of MicroRNA miR-21 Rescues Chemosensitivity of Renal-Cell Carcinoma to Topotecan.
AID431836	Cell cycle distribution in human HT-29 cells assessed as accumulation at S phase at 0.1 uM after 6 hrs by flow cytometry	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID1826601	Antiproliferative activity against HEL cells assessed as cell growth inhibition incubated for 8 hrs by CCK8 assay	2022	Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6	Evodiamine-Inspired Topoisomerase-Histone Deacetylase Dual Inhibitors: Novel Orally Active Antitumor Agents for Leukemia Therapy.
AID1182909	Cytotoxicity against multidrug-resistant human KBVIN cells after 72 hrs sulforhodamine B colorimetric assay	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Design and synthesis of new 7-(N-substituted-methyl)-camptothecin derivatives as potent cytotoxic agents.
AID1211555	In vitro apparent biliary clearance in sandwich cultured Sprague-Dawley rat hepatocytes after 15 mins by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID540211	Fraction unbound in human after iv administration	2008	Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7	Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID1811233	Antiproliferative activity against rat C6 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation.
AID527983	Antiproliferative activity against human HCT116 cells by [3H]thymidine incorporation assay	2010	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 20, Issue:22	Development of novel inhibitors targeting HIF-1α towards anticancer drug discovery.
AID409908	Cytotoxicity against human KBH5.0 cells by MTT method	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
AID22192	Excited-state lifetime value for free carboxylate form of compound in solution	1994	Journal of medicinal chemistry, Jan-07, Volume: 37, Issue:1	The structural basis of camptothecin interactions with human serum albumin: impact on drug stability.
AID1255449	Induction DNA DSBs in human M21 cells assessed as increase in gamma H2AX foci at 0.75 uM incubated for 24 hrs by DAPI staining based immunocytochemistry	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Synthesis and biological evaluation of novel N-phenyl ureidobenzenesulfonate derivatives as potential anticancer agents. Part 2. Modulation of the ring B.
AID113238	In vivo efficacy of tumor growth ratio(T/B) of compound was calculated by using the HT-29 Human colon Xenograft model in mice at a dose of 11 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID760269	Effective permeability of the compound in human Caco2 cells at 50 uM after 15 to 90 mins in presence of sodium azide	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID586339	Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID1433674	Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 8 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 8.36%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID1600554	Inhibition of DNA topoisomerase 2 in human MCF7 cells incubated for 18 to 24 hrs by kinase assay	2019	Bioorganic & medicinal chemistry, 10-01, Volume: 27, Issue:19	Design, Synthesis and Anticancer Evaluation of New Substituted Thiophene-Quinoline Derivatives.
AID1079941	Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID143189	Log 10 cell kill induced in mice with human Non-Small-Cell tumor xenograft at a oral dose of 5 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID269233	Toxicity in nude athymic mouse at 15 mg/kg, po	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID586347	Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID373529	Cytotoxicity against mouse P388 cells by MTT method	2009	European journal of medicinal chemistry, Apr, Volume: 44, Issue:4	Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones.
AID1227810	Toxicity in BALB/c nude mouse assessed as body weight at 0.023 mmol/kg, ip administered every 2 days for 3 times measured on day 6 (Rvb = 17.5 to 17.9 gms)	2015	Bioorganic & medicinal chemistry letters, Jan-01, Volume: 25, Issue:1	The biological characteristics of a novel camptothecin-artesunate conjugate.
AID277801	Cytotoxicity against human Bel7402 cells	2007	Journal of natural products, Feb, Volume: 70, Issue:2	Structures, biogenesis, and biological activities of pyrano[4,3-c]isochromen-4-one derivatives from the Fungus Phellinus igniarius.
AID321332	Antitumor activity against human MCF7 cells after 4 hrs by MTT assay	2008	Bioorganic & medicinal chemistry, Feb-01, Volume: 16, Issue:3	New homocamptothecins: synthesis, antitumor activity, and molecular modeling.
AID490173	Cytotoxicity against human HCT8 cells after 3 days by MTT assay	2010	European journal of medicinal chemistry, Jul, Volume: 45, Issue:7	Cytotoxicity and topo I targeting activity of substituted 10--nitrogenous heterocyclic aromatic group derivatives of SN-38.
AID625279	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID143188	Complete response in CD1 mice with human Non-Small-Cell tumor at a oral dose of 9 mg/kg after treatment with compound	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID760270	Effective permeability of the compound in human Caco2 cells at 50 uM after 15 to 90 mins	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID250096	Topoisomerase I-mediated cleavage value on the plasmid DNA	2005	Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3	5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
AID1143389	Antiproliferative activity against human U87 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81	Novel N-substituted sophoridinol derivatives as anticancer agents.
AID1254842	Cytotoxicity against normal human astrocytes assessed as cell viability incubated for 72 hrs by WST-1 method	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID1079943	Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID247613	Cytotoxicity against camptothecin-resistant RPMI 8402	2005	Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3	5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
AID111715	The body weight loss was measured in mice in vivo by using the HT-29 Human colon Xenograft model at a dose of 9 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1221970	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID601001	Cytotoxicity against human A549 cells after 3 days by MTT assay	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis and biological evaluation of novel 7-acyl homocamptothecins as Topoisomerase I inhibitors.
AID1127188	Antiproliferative activity against human MDA-MB-231 cells after 3 days by XTT assay	2014	European journal of medicinal chemistry, May-22, Volume: 79	Synthesis, antiproliferative and anti-dengue virus evaluations of 2-aroyl-3-arylquinoline derivatives.
AID113228	Efficacy against HT-29 human colon xenograft infected mice expressed as tumor growth ratio at dose 5 mg/Kg	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1702898	Antitumor activity in FVB/N mouse model of pCMV/SB/pT3-Caggs-NRasV12/myr-AKT/pT3-EF1alpha plasmids-induced primary hepatocellular carcinoma assessed as reduction in size of nodules on liver surface at 2 mg/kg, iv administered every other day for 2 weeks	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID431856	Antitumor activity against human HT-29 cells xenografted in athymic BALB/c nude mouse at 5 mg/kg, ip for 2 days measured after 30 days relative to placebo control	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID102166	Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line	2002	Journal of medicinal chemistry, Nov-07, Volume: 45, Issue:23	Novel tricyclic poly(ADP-ribose) polymerase-1 inhibitors with potent anticancer chemopotentiating activity: design, synthesis, and X-ray cocrystal structure.
AID1079936	Choleostatic 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]
AID1405131	Cell cycle arrest in human M21 cells assessed as accumulation at G0/G1 phase at 1.8 uM after 24 hrs by DAPI staining based flow cytometry relative to control	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID586406	Antitumor activity against human HT-29 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 2 mg/kg, po QD for 5 days followed by 4 days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID714170	Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of HIF-1-mediated hypoxia-induced VEGF expression after 24 hrs by luciferase reporter gene assay	2012	European journal of medicinal chemistry, Mar, Volume: 49	Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
AID1254841	Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID7475	Potentiation of growth inhibition of A2780 cells by compound alone in experiment 2	2000	Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22	Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
AID586410	Antitumor activity against human PC3 cells xenografted in nu/nu mouse assessed as tumor growth inhibition at 2 mg/kg, po QD for 5 days followed by 2days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID586348	Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID431822	Cytotoxicity against human THP1 cells expressing p53 mutant after 48 hrs by SRB assay	2009	Journal of medicinal chemistry, Sep-24, Volume: 52, Issue:18	Discovery of a novel series of quinolone and naphthyridine derivatives as potential topoisomerase I inhibitors by scaffold modification.
AID221333	In Vitro cytotoxicity against human lung cancer cell line (H128)	2001	Journal of medicinal chemistry, May-10, Volume: 44, Issue:10	Synthesis and biological evaluation of novel A-ring modified hexacyclic camptothecin analogues.
AID389684	Cytotoxicity against human RPMI8402 cells after MTT assay	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.
AID409905	Cytotoxicity against camptothecin-resistant mouse P388 cells by MTT method	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
AID599600	Cell cycle arrest in human PC3 cells assessed as accumulation at S phase at 2 uM after 48 hrs using propidium iodide staining by flow cytometry (Rvb = 38.16 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID1823977	Antiproliferative activity against human HGC-27 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID133755	Maximally tolerated dose in mice bearing L1210 leukemia.	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Synthesis of water-soluble (aminoalkyl)camptothecin analogues: inhibition of topoisomerase I and antitumor activity.
AID1228609	Growth inhibition of human SN12C cells by five-dose growth inhibition assay	2015	Journal of medicinal chemistry, May-14, Volume: 58, Issue:9	Discovery of potent indenoisoquinoline topoisomerase I poisons lacking the 3-nitro toxicophore.
AID111704	Mean body weight loss for animals in all experimental conditions at dose 9 mg/Kg in HT-29 human colon xenograft infected mice	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID600073	Cell cycle arrest in human PC3 cells assessed as accumulation at G2 phase at 2 uM after 24 hrs using propidium iodide staining by flow cytometry (Rvb = 18.19 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID684302	Antiproliferative activity against human MDA-MB-435 cells after 3 days by MTT assay	2012	European journal of medicinal chemistry, Oct, Volume: 56	Synthesis and preliminary bioevaluation of novel E-ring modified acetal analog of camptothecin as cytotoxic agents.
AID409903	Cytotoxicity against camptothecin-resistant human CPT-K5 cells by MTT method	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
AID1211549	Unbound fraction in Sprague-Dawley rat plasma at 100 uM by equilibrium dialysis method	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID1211548	In vivo apparent biliary clearance in iv dosed Sprague-Dawley rat by LC-MS/MS analysis	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID586351	Cytotoxicity against human bone marrow cell by CFU-GM assay	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID453827	Antiproliferative activity against human A549 cells after 72 hrs by XTT assay	2009	Bioorganic & medicinal chemistry, Nov-01, Volume: 17, Issue:21	Synthesis and antiproliferative evaluation of 6-arylindeno[1,2-c]quinoline derivatives.
AID247623	Inhibitory concentration against human HCT116 colon cancer cell line	2005	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 15, Issue:8	Synthesis and antitumor activity of 7-ethyl-9-alkyl derivatives of camptothecin.
AID389683	Inhibition of human topoisomerase 1 mediated DNA cleavage assessed as effective drug concentration causing 10% YepG plasmid cleavage relative to camptothecin	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.
AID1433713	Toxicity in BALB/c nude mouse xenografted with human Bel7402 cells assessed as body volume at 5 mg/kg, ip administered once in a week for two weeks starting from 6 days post tumor transplantation measured every 3 days for 21 days (Rvb = 511 g)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID586412	Antitumor activity against human PC3 cells xenografted in nu/nu mouse assessed as tumor growth delay at 2 mg/kg, po QD for 5 days followed by 2days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID78395	Tumor volume index was measured on non-small-cell lung carcinoma H460 cells at a dose of 15 mg/kg perorally in mice	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID331825	Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs	2008	Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9	E-ring-modified 7-oxyiminomethyl camptothecins: Synthesis and preliminary in vitro and in vivo biological evaluation.
AID760278	Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID699540	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting	2012	Journal of medicinal chemistry, May-24, Volume: 55, Issue:10	Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1817012	Cytotoxicity against human MCF-7 cells assessed as cell growth inhibition after 72 hrs by MTT assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID586403	Antitumor activity against human H460 cells xenografted in nu/nu mouse assessed as tumor growth delay at 2 mg/kg, po QD for 5 days followed by 2days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID1433698	Antitumor activity against human Bel7402 cells xenografted in BALB/c nude mouse assessed as tumor growth inhibition at 5 mg/kg, ip administered once in a week for two weeks starting from 6 days post tumor transplantation measured 27 to 30 days post tumor	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID1817016	Induction of DNA damage in human MCF7/TDP1 cells assessed as increase in gammaH2AX foci measured after 6 hrs by DAPI staining based immunofluorescence assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID1255453	Antiproliferative activity against human MCF7 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Synthesis and biological evaluation of novel N-phenyl ureidobenzenesulfonate derivatives as potential anticancer agents. Part 2. Modulation of the ring B.
AID269232	Toxicity in nude athymic mouse at 9 mg/kg, po	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID625281	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1702899	Toxicity in FVB/N mouse model of pCMV/SB/pT3-Caggs-NRasV12/myr-AKT/pT3-EF1alpha plasmids-induced primary hepatocellular carcinoma assessed as decrease in body weight at 2 mg/kg, iv administered every other day for 2 weeks	2020	European journal of medicinal chemistry, Feb-01, Volume: 187	Design, synthesis and antineoplastic activity of novel 20(S)-acylthiourea derivatives of camptothecin.
AID44517	Percentage of body weight loss CD1 mice with human Non-Small-Cell tumor xenograft at a oral dose of 9 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1656686	Induction of apoptosis in human LNCAP cells assessed as up regulation of p53 expression at 10 uM measured after 24 hrs by immunoblot analysis	2020	Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3	Molecular mechanism of C-phycocyanin induced apoptosis in LNCaP cells.
AID1387387	Cytotoxicity in human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID269205	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 9 mg/kg, po measured as tumor volume inhibition relative to control	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID634879	Growth inhibition of human MCF7 cells after 72 hrs by XTT assay	2011	Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24	Synthesis and antiproliferative evaluation of 6-aryl-11-iminoindeno[1,2-c]quinoline derivatives.
AID1405119	Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID1824001	Induction of apoptosis in human SGC-7901 cells assessed as viable cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 99.95%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID1174156	Reduction of hypoxia-induced HIF-1 beta expression in human Hep3B cells at 10 uM after 48 hrs by Western blotting analysis	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Novel chalcone derivatives as hypoxia-inducible factor (HIF)-1 inhibitor: synthesis, anti-invasive and anti-angiogenic properties.
AID409904	Cytotoxicity against mouse P388 cells by MTT method	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
AID599607	Cell cycle arrest in human PC3 cells assessed as accumulation at G2 phase at 2 uM after 72 hrs using propidium iodide staining by flow cytometry (Rvb = 20.18 %)	2011	European journal of medicinal chemistry, Jun, Volume: 46, Issue:6	Synthesis of 1-naphtylpiperazine derivatives as serotoninergic ligands and their evaluation as antiproliferative agents.
AID248159	Concentration required to inhibit cell proliferation in KBH5.0 tumor cell line; overexpress BCRP	2004	Bioorganic & medicinal chemistry letters, Nov-15, Volume: 14, Issue:22	Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
AID377273	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay	2006	Journal of natural products, Jun, Volume: 69, Issue:6	Mono-, Bi-, and triphenanthrenes from the tubers of Cremastra appendiculata.
AID389687	Cytotoxicity against camptothecin-resistant and TOP1 deficient mouse P388/CPT45 cells after MTT assay	2008	Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20	Synthesis of N-substituted 5-[2-(N-alkylamino)ethyl]dibenzo[c,h][1,6]naphthyridines as novel topoisomerase I-targeting antitumor agents.
AID78407	In vitro cytotoxic activity against human non small cell lung carcinoma H460 cell line	2000	Journal of medicinal chemistry, Oct-19, Volume: 43, Issue:21	Novel 7-substituted camptothecins with potent antitumor activity.
AID1143390	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay	2014	European journal of medicinal chemistry, Jun-23, Volume: 81	Novel N-substituted sophoridinol derivatives as anticancer agents.
AID1811232	Antiproliferative activity against human U-251 cells assessed as inhibition of cell growth measured after 72 hrs by CCK-8 assay	2021	European journal of medicinal chemistry, Dec-15, Volume: 226	N-2-(phenylamino) benzamide derivatives as novel anti-glioblastoma agents: Synthesis and biological evaluation.
AID1464541	Cytotoxicity against human KBVIN cells after 72 hrs by SRB assay	2017	Bioorganic & medicinal chemistry letters, 10-15, Volume: 27, Issue:20	Design, semisynthesis and potent cytotoxic activity of novel 10-fluorocamptothecin derivatives.
AID7474	Potentiation of growth inhibition of A2780 cells by compound alone in experiment 1	2000	Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22	Resistance-modifying agents. 9. Synthesis and biological properties of benzimidazole inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase.
AID1433680	Cell cycle arrest in human A549 cells assessed as accumulation at G2/M phase at 75 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 8.36%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID380252	Antiproliferative activity against human NCI-H460 cells after 72 hrs	2006	Journal of natural products, Dec, Volume: 69, Issue:12	Cucurbitane triterpenes from the fruiting bodies and cultivated mycelia of Leucopaxillus gentianeus.
AID83595	Cytotoxicity was determined in vitro in HT-29 cells(colon) of human tumor cell lines by using MTT assay	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID586408	Antitumor activity against human HT-29 cells xenografted in nu/nu mouse assessed as tumor growth delay at 2 mg/kg, po QD for 5 days followed by 4 days without treatment for 2 weeks	2011	Journal of medicinal chemistry, Mar-24, Volume: 54, Issue:6	14-Aminocamptothecins: their synthesis, preclinical activity, and potential use for cancer treatment.
AID343604	Cytotoxicity against human BXPC3 cells after 4 days by MTT assay	2008	Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14	Novel hexacyclic camptothecin derivatives. Part 1: synthesis and cytotoxicity of camptothecins with an A-ring fused 1,3-oxazine ring.
AID147799	In vitro anti-cancer activity against OVCAR 8(Ovarian) human tumor cell line	1999	Bioorganic & medicinal chemistry letters, Jun-21, Volume: 9, Issue:12	Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.
AID1221961	Apparent permeability from basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1254838	Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability at 10 uM incubated for 72 hrs by WST-1 method	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID625288	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID97700	Percentage of L1210 leukemia cells arrested in G2+ M phase of cell cycle by 0.28 uM concentration	2003	Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16	Synthesis and pharmacological evaluation of novel non-lactone analogues of camptothecin.
AID1172292	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay	2014	Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22	Design and synthesis of novel spin-labeled camptothecin derivatives as potent cytotoxic agents.
AID1544076	Poison activity at TOP1 in human MCF7 cells assessed as decrease in relaxed supercoiled pBS(SK+) DNA mobility measured after 30 mins by ethidium bromide staining based agarose gel electrophoresis	2019	Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7	Discovery and Mechanistic Study of Tailor-Made Quinoline Derivatives as Topoisomerase 1 Poison with Potent Anticancer Activity.
AID634880	Growth inhibition of human MDA-MB-231 cells after 72 hrs by XTT assay	2011	Bioorganic & medicinal chemistry, Dec-15, Volume: 19, Issue:24	Synthesis and antiproliferative evaluation of 6-aryl-11-iminoindeno[1,2-c]quinoline derivatives.
AID269206	Antitumor activity against human MKN28 cell line xenografted in nude athymic mouse at 15 mg/kg, po measured as tumor volume inhibition relative to control	2006	Journal of medicinal chemistry, Aug-24, Volume: 49, Issue:17	Synthesis and cytotoxic activity of polyamine analogues of camptothecin.
AID1740932	Inhibition of recombinant human Top1 expressed in baculovirus infected sf9 insect cells using supercoiled pBS (SK+) DNA as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis analysis	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Development of a metabolically stable topoisomerase I poison as anticancer agent.
AID1656667	Induction of apoptosis in human LNCAP cells assessed as increase in cleaved PARP expression at 500 ug/ml measured after 24 hrs by western blot analysis	2020	Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3	Molecular mechanism of C-phycocyanin induced apoptosis in LNCaP cells.
AID625286	Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis	2011	PLoS computational biology, Dec, Volume: 7, Issue:12	Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID760277	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID1079946	Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID745327	Cytotoxicity against human DU145 cells	2013	European journal of medicinal chemistry, May, Volume: 63	Evolution in medicinal chemistry of E-ring-modified Camptothecin analogs as anticancer agents.
AID1079938	Chronic 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]
AID1221962	Efflux ratio of permeability from apical to basolateral side over basolateral to apical side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1221963	Transporter substrate index ratio of permeability from apical to basolateral side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of P-gp inhibitor LY335979	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1127189	Antiproliferative activity against human MCF7 cells after 3 days by XTT assay	2014	European journal of medicinal chemistry, May-22, Volume: 79	Synthesis, antiproliferative and anti-dengue virus evaluations of 2-aroyl-3-arylquinoline derivatives.
AID143199	Complete response CD1 mice with human Non-Small-Cell tumor xenograft at a oral dose of 15 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1211547	Biliary excretion in rat	2012	Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3	In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
AID111712	The body weight loss was measured in mice in vivo by using the HT-29 Human colon Xenograft model at a dose of 5 mg/kg	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID690722	Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay	2012	Bioorganic & medicinal chemistry letters, Oct-15, Volume: 22, Issue:20	Camptothecins in tumor homing via an RGD sequence mimetic.
AID136694	The compound (5 mg/kg) administered intravenously was tested for antitumor activity against A-498 (renal) xenograft model in mice	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID486937	Cytotoxicity against human A549 cells after 3 days by MTT assay	2010	European journal of medicinal chemistry, Jun, Volume: 45, Issue:6	Synthesis and evaluation of 9-benzylideneamino derivatives of homocamptothecin as potent inhibitors of DNA topoisomerase I.
AID8675	In vitro cytotoxicity against A549 (human lung cancer)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions.
AID1182906	Cytotoxicity against human A549 cells after 72 hrs sulforhodamine B colorimetric assay	2014	Bioorganic & medicinal chemistry letters, Aug-15, Volume: 24, Issue:16	Design and synthesis of new 7-(N-substituted-methyl)-camptothecin derivatives as potent cytotoxic agents.
AID1668357	Induction of apoptosis in human S1 cells assessed as early apoptotic cells at 5 uM incubated for 48 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 2%)	2020	Journal of natural products, 05-22, Volume: 83, Issue:5	Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.
AID1824036	Induction of cell cycle arrest in human SGC-7901 cells assessed as accumulation at S phase at 0.9 uM after 24 hrs by propidium iodide staining based flow cytometry	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID1221979	Transporter substrate index ratio of permeability from basolateral to apical side in human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 10 uM of MRP2 inhibitor MK571	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID83600	Human tumor cell cytotoxicity assay was performed using MTT (HT-29 cell line )	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1675244	Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 3 days by fluorometric assay	2020	Journal of natural products, 08-28, Volume: 83, Issue:8	Usnic Acid Conjugates with Monoterpenoids as Potent Tyrosyl-DNA Phosphodiesterase 1 Inhibitors.
AID1269398	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay	2016	Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3	Design, synthesis and biological evaluation of 3-substituted indenoisoquinoline derivatives as topoisomerase I inhibitors.
AID588979	Substrates of transporters of clinical importance in the absorption and disposition of drugs, MRP4	2010	Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3	Membrane transporters in drug development.
AID1823975	Antiproliferative activity against human SGC-7901 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID1405133	Cell cycle arrest in human M21 cells assessed as accumulation at G2/M phase at 1.8 uM after 24 hrs by DAPI staining based flow cytometry relative to control	2018	European journal of medicinal chemistry, Jul-15, Volume: 155	Preparation, characterisation and biological evaluation of new N-phenyl amidobenzenesulfonates and N-phenyl ureidobenzenesulfonates inducing DNA double-strand breaks. Part 3. Modulation of ring A.
AID1740933	Inhibition of Top1 in human MCF7 cells using supercoiled pBS (SK+) DNA as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis analysis	2020	European journal of medicinal chemistry, Sep-15, Volume: 202	Development of a metabolically stable topoisomerase I poison as anticancer agent.
AID208681	Cytotoxicity was determined in vitro in T47D cells(breast) of human tumor cell lines by using MTT assay	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID1656687	Induction of apoptosis in human LNCAP cells assessed as up regulation of p21 expression at 10 uM measured after 24 hrs by immunoblot analysis	2020	Bioorganic & medicinal chemistry, 02-01, Volume: 28, Issue:3	Molecular mechanism of C-phycocyanin induced apoptosis in LNCaP cells.
AID760273	Cytotoxicity against human A549 cells after 72 hrs by MTT assay	2013	ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7	Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
AID202503	Cytotoxicity was determined in vitro in SK-OV-3 cells (ovarian) of human tumor cell lines by using MTT assay	1995	Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3	Synthesis and antitumor activity of novel water soluble derivatives of camptothecin as specific inhibitors of topoisomerase I.
AID84358	Tested in vitro for cytotoxicity against human tumor cell line HOP62 (lung)	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID590484	Cell cycle arrest in human A549 cells assessed as accumulation at S phase at 25 uM after 24 hrs by flow cytometry (Rvb = 27.52%)	2011	Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7	Synthesis and antitumor activity of 10-arylcamptothecin derivatives.
AID1274790	Binding affinity to Escherichia coli negative supercoiled pBR322 DNA at 10 uM after 12 hrs by ethidium bromide staining based agarose gel electrophoresis	2016	European journal of medicinal chemistry, Jan-27, Volume: 108	Discovery of indeno[1,2-b]quinoxaline derivatives as potential anticancer agents.
AID1668355	Induction of apoptosis in human S1 cells assessed as necrotic cells at 5 uM incubated for 48 hrs by annexin V/propidium iodide staining based flow cytometry (Rvb = 0.2%)	2020	Journal of natural products, 05-22, Volume: 83, Issue:5	Licochalcone A Selectively Resensitizes ABCG2-Overexpressing Multidrug-Resistant Cancer Cells to Chemotherapeutic Drugs.
AID1433672	Cell cycle arrest in human A549 cells assessed as accumulation at G0/G1 phase at 8 nM after 24 hrs by propidium iodide staining based flow cytometry (Rvb = 58.84%)	2017	European journal of medicinal chemistry, Jan-05, Volume: 125	Synthesis and antitumor activity of novel substituted uracil-1'(N)-acetic acid ester derivatives of 20(S)-camptothecins.
AID1817000	Synergistic cytotoxicity against human MCF7/TDP1 cells at 100 nM after 96 hrs by MTT assay	2021	Journal of medicinal chemistry, 06-10, Volume: 64, Issue:11	Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer.
AID200289	Human tumor cell cytotoxicity assay was performed using MTT (SKVLB cell line )	1996	Journal of medicinal chemistry, Feb-02, Volume: 39, Issue:3	Water soluble inhibitors of topoisomerase I: quaternary salt derivatives of camptothecin.
AID1387388	Cytotoxicity in human KB cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID1254843	Selectivity index, ratio of IC50 for normal human astrocytes to IC50 for human GBM1 cells	2015	European journal of medicinal chemistry, Oct-20, Volume: 103	Discovery of potent and selective cytotoxic activity of new quinazoline-ureas against TMZ-resistant glioblastoma multiforme (GBM).
AID101469	Complete response in mice bearing lung carcinoma LX-1 at a oral dose of 15 mg/kg	2001	Journal of medicinal chemistry, Sep-27, Volume: 44, Issue:20	Novel 7-oxyiminomethyl derivatives of camptothecin with potent in vitro and in vivo antitumor activity.
AID1239204	Toxicity in human A549 cells xenografted BALB/C mouse assessed as change in body weight at 0.5 mg/kg, ip for 5 days	2015	Journal of medicinal chemistry, Aug-27, Volume: 58, Issue:16	Scaffold Diversity Inspired by the Natural Product Evodiamine: Discovery of Highly Potent and Multitargeting Antitumor Agents.
AID248146	Inhibitory concentration against lymphoblast RPMI 8402 cell line was determined	2005	Journal of medicinal chemistry, Feb-10, Volume: 48, Issue:3	5-(2-aminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones: variation of n-alkyl substituents modulates sensitivity to efflux transporters associated with multidrug resistance.
AID145076	The compound (10 mg/kg) administered intravenously was tested for antitumor activity against NCI-H23 (lung) xenograft model in mice	2000	Bioorganic & medicinal chemistry letters, Feb-21, Volume: 10, Issue:4	Novel C-ring analogues of 20(S)-camptothecin. Part 3: synthesis and their in vitro cytotoxicity of A-, B- and C-ring analogues.
AID489627	Toxicity in C57BL/6 mouse assessed as body weight at 0.5 mg/kg, ip qd for 5 days ( RVb = 19.06 +/- 1.35 g)	2010	European journal of medicinal chemistry, Jul, Volume: 45, Issue:7	Trifluoromethyl-promoted homocamptothecins: synthesis and biological activity.
AID1079948	Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID1221968	Apparent permeability from apical to basolateral side of human Caco2 cells at 10 uM up to 120 mins by HPLC-MC analysis in presence of 1 uM of BCRP inhibitor Ko143	2011	Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 39, Issue:2	Attenuation of intestinal absorption by major efflux transporters: quantitative tools and strategies using a Caco-2 model.
AID1824014	Induction of apoptosis in human MGC-803 cells assessed as early apoptic cells at 0.9 uM after 24 hrs by Annexin V-FITC/PI staining based flow cytometry method (Rvb = 0%)	2022	European journal of medicinal chemistry, Jan-15, Volume: 228	Design, synthesis and bioactivity evaluation of novel evodiamine derivatives with excellent potency against gastric cancer.
AID1387393	Cytotoxicity in human QGY7703 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay	2018	Journal of medicinal chemistry, 10-11, Volume: 61, Issue:19	Structure-Based Drug Design and Identification of H
AID1172293	Cytotoxicity against human KB cells after 72 hrs by SRB assay	2014	Bioorganic & medicinal chemistry, Nov-15, Volume: 22, Issue:22	Design and synthesis of novel spin-labeled camptothecin derivatives as potent cytotoxic agents.
AID425652	Total body clearance in human	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Physicochemical determinants of human renal clearance.
AID409901	Cytotoxicity against human RPMI8402 cells by MTT method	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	11-Substituted 2,3-dimethoxy-8,9-methylenedioxybenzo[i]phenanthridine derivatives as novel topoisomerase I-targeting agents.
AID1174154	Reduction of hypoxia-induced HIF-1 alpha expression in human Hep3B cells at 10 uM after 48 hrs by Western blotting analysis	2015	European journal of medicinal chemistry, Jan-07, Volume: 89	Novel chalcone derivatives as hypoxia-inducible factor (HIF)-1 inhibitor: synthesis, anti-invasive and anti-angiogenic properties.
AID41736	In vitro cytotoxicity against Bel7402 (human liver cancer)	2003	Bioorganic & medicinal chemistry letters, Nov-03, Volume: 13, Issue:21	Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions.
AID721754	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	2013	Journal of medicinal chemistry, Feb-14, Volume: 56, Issue:3	Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.
AID721719	Antiproliferative activity against human H184B5F5/M10 cells after 72 hrs by XTT assay	2013	European journal of medicinal chemistry, Jan, Volume: 59	Synthesis and antiproliferative evaluation of 3-phenylquinolinylchalcone derivatives against non-small cell lung cancers and breast cancers.
AID1346987	P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1296008	Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening	2020	SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1	Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1347160	Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1346986	P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen	2019	Molecular pharmacology, 11, Volume: 96, Issue:5	A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347159	Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347093	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347089	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630	Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay	2021	Cell reports, 04-27, Volume: 35, Issue:4	A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347107	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154	Primary screen GU AMC qHTS for Zika virus inhibitors	2020	Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49	Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347106	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083	qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen	2020	Antiviral research, 01, Volume: 173	A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347104	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1347090	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	2018	Oncotarget, Jan-12, Volume: 9, Issue:4	Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID686947	qHTS for small molecule inhibitors of Yes1 kinase: Primary Screen	2013	Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15	Identification of potent Yes1 kinase inhibitors using a library screening approach.
AID1159607	Screen for inhibitors of RMI FANCM (MM2) intereaction	2016	Journal of biomolecular screening, Jul, Volume: 21, Issue:6	A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	1 (0.04)	18.7374
1990's	386 (16.81)	18.2507
2000's	1022 (44.51)	29.6817
2010's	729 (31.75)	24.3611
2020's	158 (6.88)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	626 (26.17%)	5.53%
Reviews	275 (11.50%)	6.00%
Case Studies	97 (4.06%)	4.05%
Observational	6 (0.25%)	0.25%
Other	1,388 (58.03%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (388)

Trial Overview

Trial	Phase	Enrollment	Study Type	Start Date	Status
NCI 10147: A Phase II Randomized Study of Topotecan/Carboplatin With or Without Veliparib in Advanced Myeloproliferative Disorders and Chronic Myelomonocytic Leukemia (CMML) [NCT03289910]	Phase 2	60 participants (Anticipated)	Interventional	2018-06-08	Active, not recruiting
A Randomized Phase II Trial of Triplet Therapy (A PD-L1 Inhibitor Durvalumab (MEDI4736) in Combination With Olaparib and Cediranib) Compared to Olaparib and Cediranib or Durvalumab (MEDI4736) and Cediranib or Standard of Care Chemotherapy in Women With Pl [NCT04739800]	Phase 2	164 participants (Anticipated)	Interventional	2021-06-10	Active, not recruiting
A Randomized Phase II/III Study of the Combination of Cediranib and Olaparib Compared to Cediranib or Olaparib Alone, or Standard of Care Chemotherapy in Women With Recurrent Platinum-Resistant or -Refractory Ovarian, Fallopian Tube, or Primary Peritoneal [NCT02502266]	Phase 2/Phase 3	562 participants (Anticipated)	Interventional	2016-05-03	Active, not recruiting
Avatar-Directed Chemotherapy in Platinum-Resistant Ovarian, Primary Peritoneal and Fallopian Tube Cancers [NCT02312245]	Phase 2	13 participants (Actual)	Interventional	2015-07-21	Completed
A Randomized Phase III Trial Of Paclitaxel Plus Cisplatin Versus Vinorelbine Plus Cisplatin Versus Gemcitabine Plus Cisplatin Versus Topotecan Plus Cisplatin In Stage IVB, Recurrent Or Persistent Carcinoma of the Cervix [NCT00064077]	Phase 3	513 participants (Actual)	Interventional	2003-05-31	Completed
A Randomized, Double-blind, Phase III Study of BD0801 Injection Combined With Chemotherapy Versus Placebo Combined With Chemotherapy in Patients With Recurrent, Platinum-resistant Epithelial Ovarian, Fallopian Tube , or Primary Peritoneal Cancer. [NCT04908787]	Phase 3	357 participants (Anticipated)	Interventional	2021-06-11	Recruiting
A Phase 2/3, Multicenter, Randomized Study of Raludotatug Deruxtecan (R-DXd), a CDH6-directed Antibody-drug Conjugate, in Subjects With Platinum-resistant, High Grade Ovarian, Primary Peritoneal, or Fallopian Tube Cancer [NCT06161025]	Phase 2/Phase 3	650 participants (Anticipated)	Interventional	2024-02-29	Not yet recruiting
A Phase II Study of Pazopanib and Oral Topotecan in Women With Recurrent Cervical Cancer [NCT02348398]	Phase 2	0 participants (Actual)	Interventional	2016-08-31	Withdrawn
NANT N2013-02 A Phase I Study of Sorafenib and Cyclophosphamide/Topotecan in Patients With Relapsed and Refractory Neuroblastoma [NCT02298348]	Phase 1	18 participants (Anticipated)	Interventional	2015-04-30	Active, not recruiting
N2012-01: Phase 1 Study of Difluoromethylornithine (DFMO) and Celecoxib With Cyclophosphamide/Topotecan for Patients With Relapsed or Refractory Neuroblastoma [NCT02030964]	Phase 1	30 participants (Anticipated)	Interventional	2013-12-31	Active, not recruiting
RAPID Feasibility Study: A Pilot Study for the Rapid Infusion of Dinutuximab [NCT05421897]	Phase 4	11 participants (Anticipated)	Interventional	2022-10-24	Recruiting
A Randomized, Open-label, Parallel Group, Multi-center Phase II Clinical Trial Evaluating Effect of Addition of DCVAC/OvCa to Standard Chemotherapy in Women With Relapsed Platinum (Pt)-Resistant Epithelial Ovarian Carcinoma [NCT02107378]	Phase 2	22 participants (Actual)	Interventional	2014-01-31	Terminated(stopped due to sponsor decision)
Ocular Conservative Treatment for Retinoblastoma: Efficacy of the New Management Strategies and Visual Outcome - RETINO 2018 [NCT04681417]	Phase 2/Phase 3	225 participants (Anticipated)	Interventional	2021-03-25	Recruiting
[NCT01342237]	Phase 2	33 participants (Anticipated)	Interventional	2011-03-31	Recruiting
Indirect Comparison of the Efficacy Between Topotecan and Other Treatments for Recurrent Carcinoma of the Cervix [NCT01345279]		1 participants (Actual)	Observational	2009-06-30	Completed
Oral Topotecan, Utilization for a Metronomic Dosing Schedule to Treat Recurrent or Persistent Solid Tumors [NCT00382733]	Phase 1/Phase 2	26 participants (Actual)	Interventional	2006-11-30	Completed
A Phase II Study of Oxaliplatin Combined With Continuous Infusion Topotecan as Chemotherapy for Patients With Previously Treated Ovarian Cancer [NCT00313612]	Phase 2	39 participants (Actual)	Interventional	2006-01-31	Terminated
Phase II Study of High-Dose Topotecan, Cyclophosphamide and Melphalan for the Treatment of Multiple Myeloma [NCT01039025]	Phase 2	60 participants (Actual)	Interventional	2002-02-18	Completed
A Randomized Phase II Study: Sequencing Topoisomerase Inhibitors for Extensive Stage Small Cell Lung Cancer (SCLC): Topotecan Sequenced With Etoposide/Cisplatin, and Irinotecan/Cisplatin Sequenced With Etoposide [NCT00057837]	Phase 2	140 participants (Actual)	Interventional	2004-07-14	Completed
PHASE 1/2 STUDY TO EVALUATE PALBOCICLIB (IBRANCE®) IN COMBINATION WITH IRINOTECAN AND TEMOZOLOMIDE OR IN COMBINATION WITH TOPOTECAN AND CYCLOPHOSPHAMIDE IN PEDIATRIC PATIENTS WITH RECURRENT OR REFRACTORY SOLID TUMORS [NCT03709680]	Phase 2	184 participants (Anticipated)	Interventional	2019-05-24	Recruiting
An Open-label, Multicenter, Phase I/II Study of AT-101 in Combination With Topotecan in Patients With Relapsed or Refractory Small Cell Lung Cancer After Prior Platinum Containing First Line Chemotherapy [NCT00397293]	Phase 1/Phase 2	36 participants (Actual)	Interventional	2006-11-30	Completed
Pilot Study Using Myeloablative Busulfan/Melphalan (BuMel) Consolidation Following Induction Chemotherapy for Patients With Newly Diagnosed High-Risk Neuroblastoma [NCT01798004]	Phase 1	150 participants (Actual)	Interventional	2013-04-08	Active, not recruiting
A COG Pilot Study of Intensive Induction Chemotherapy and 131I-MIBG Followed by Myeloablative Busulfan/Melphalan (Bu/Mel) for Newly Diagnosed High-Risk Neuroblastoma [NCT01175356]	Phase 1	99 participants (Actual)	Interventional	2010-10-04	Active, not recruiting
A Phase I and Enrichment Study of Low-dose Metronomic Topotecan and Pazopanib in Pediatric Patients With Recurrent or Refractory Solid Tumours [NCT02303028]	Phase 1/Phase 2	30 participants (Actual)	Interventional	2015-03-31	Completed
A Two Part, Phase I-IIa Study Evaluating MK1775 in Combination With Topotecan/Cisplatin in Adult Patients With Cervical Cancer [NCT01076400]	Phase 1/Phase 2	7 participants (Actual)	Interventional	2010-05-31	Terminated(stopped due to The sponsor permanently suspended new enrollment into the trial and discontinued the study; which was not related to any concerns over product safety.)
Open-label Multicenter Trial of Glivec® (Imatinib Mesylate, Formerly Known as STI571) in Combination With Chemotherapy (MTC) in Patients With Refractory or Relapsed Acute Myeloid Leukemia (AML) [NCT00744081]	Phase 2	130 participants (Anticipated)	Interventional	2004-07-31	Completed
Phase I Dose-escalation Study of Topotecan in Moderate-severe COVID-19 Patients [NCT05083000]	Phase 1	24 participants (Anticipated)	Interventional	2021-08-16	Recruiting
A Phase II Trial of Nifurtimox for Refractory or Relapsed Neuroblastoma or Medulloblastoma. [NCT00601003]	Phase 2	112 participants (Actual)	Interventional	2008-01-14	Completed
International, Multi-Center, Open-label, Treatment Extension Study of Iniparib as Monotherapy or in Combination Chemotherapeutic Regimens in Cancer Patients Who Have Derived Clinical Benefit From Iniparib Following Completion of a Phase 1, 2 or 3 Parental [NCT01593228]	Phase 3	37 participants (Actual)	Interventional	2012-05-31	Completed
Choice of Topotecan or Melphalan in Retinoblastoma Patients [NCT04799002]	Phase 3	50 participants (Anticipated)	Interventional	2021-03-11	Recruiting
Intra-Arterial (IA) Chemotherapy for Newly Diagnosed, Residual, or Recurrent Atypical Choroid Plexus Papilloma (ACPP) and Choroid Plexus Carcinoma (CPC) Prior to Second-Look Surgery [NCT04994977]	Phase 1	6 participants (Anticipated)	Interventional	2023-05-04	Recruiting
Phase I, Traditional 3+3, Trial of PO Sorafenib and Topotecan in Refractory or Recurrent Pediatric Solid Malignancies [NCT01683149]	Phase 1	13 participants (Actual)	Interventional	2013-01-31	Completed
A Multicenter, Randomized, Open-label, Parallel-design Phase 3 Study to Evaluate the Efficacy and Safety of LY01610 (Irinotecan Hydrochloride Liposome Injection) Versus Topotecan in Patients With Recurrent Small Cell Lung Cancer (SCLC) [NCT06128837]	Phase 3	686 participants (Anticipated)	Interventional	2024-01-31	Not yet recruiting
Treatment of Newly Diagnosed Diffuse Anaplastic Wilms Tumors (DAWT) and Relapsed Favorable Histology Wilms Tumors (FHWT) [NCT04322318]	Phase 2	221 participants (Anticipated)	Interventional	2020-10-19	Recruiting
Phase 1 Trial of the LSD1 Inhibitor Seclidemstat (SP 2577) With and Without Topotecan and Cyclophosphamide in Patients With Relapsed or Refractory Ewing Sarcoma and Select Sarcomas [NCT03600649]	Phase 1	50 participants (Anticipated)	Interventional	2018-06-04	Active, not recruiting
Meta-analysis of Efficacy of Topotecan and Other Treatments for Recurrent Carcinoma of the Cervix [NCT01160185]		1 participants (Actual)	Observational	2009-06-30	Completed
Phase I Trial of High-dose Topotecan in Association With Carboplatin, With Peripheral Blood Stem Cell Support in Patients With First Relapsed Ovarian Carcinoma Without Platinum-treatment Since 6-12 Months [NCT01177501]	Phase 1	3 participants (Actual)	Interventional	2009-04-30	Terminated(stopped due to choice of the principal investigator)
A Phase 3 Study of 131I-Metaiodobenzylguanidine (131I-MIBG) or ALK Inhibitor Therapy Added to Intensive Therapy for Children With Newly Diagnosed High-Risk Neuroblastoma (NBL) [NCT03126916]	Phase 3	724 participants (Anticipated)	Interventional	2018-05-14	Active, not recruiting
A Two-part, Open-label, Randomized, Phase 2/3 Study of Dinutuximab and Irinotecan Versus Irinotecan for Second Line Treatment of Subjects With Relapsed or Refractory Small Cell Lung Cancer [NCT03098030]	Phase 2/Phase 3	483 participants (Actual)	Interventional	2017-06-01	Completed
A Phase Ib, Dose Escalation Study to Assess the Safety, Tolerability, and Pharmacokinetics of Humanized Anti-VEGF Monoclonal Antibody(Sevacizumab) Injection Plus Chemotherapy in Chinese Patients With Platinum-Resistant Recurrent Ovarian Cancer. [NCT03763123]	Phase 1	48 participants (Anticipated)	Interventional	2018-04-24	Recruiting
Clinical Research of Allogeneic Hematopoietic Stem Cell Transplantation for Treatment of Children With Stage 4/M Neuroblastoma: A Prospective, Single-arm, Phase II, Multi-center Trial [NCT05303727]	Phase 2	64 participants (Anticipated)	Interventional	2022-08-31	Not yet recruiting
A Phase II Prospective International Multicenter Clinical Trial for Eyes With Relapsed Retinoblastoma, With Randomization Depending on the Site of Relapse or on Previous Treatment [NCT04455139]	Phase 2	2 participants (Actual)	Interventional	2021-11-15	Terminated(stopped due to Difficulties in recruiting patients due to changing in treatment standards for the target population)
A Randomized Phase II Trial Comparing the Combination of PI3K Inhibitor Copanlisib (BAY 80-6946) and PARP Inhibitor Olaparib (AZD2281) to Standard Chemotherapy in Patients With Recurrent Platinum Resistant Ovarian, Fallopian Tube, or Primary Peritoneal Ca [NCT05295589]	Phase 2	0 participants (Actual)	Interventional	2022-06-30	Withdrawn(stopped due to Drug supply issues)
A Phase I Study of Weekly Doxorubicin and Oral Topotecan for Patients With Relapsed or Refractory Small Cell Lung Cancer (SCLC) [NCT00856037]	Phase 1	22 participants (Actual)	Interventional	2009-02-02	Completed
A Pharmacokinetic and Phase II Study of Oral Cyclophosphamide and Oral Topotecan in Children With Recurrent and or Refractory Solid Tumors [NCT00628732]	Phase 2	36 participants (Anticipated)	Interventional	2005-01-31	Completed
A Randomised Phase II Study Of Nintedanib (BIBF1120) Compared To Chemotherapy in Patients With Recurrent Clear Cell Carcinoma Of The Ovary Or Endometrium [NCT02866370]	Phase 2	120 participants (Anticipated)	Interventional	2015-04-30	Recruiting
A Phase 1 Study of Topotecan Liposomes Injection (TLI) in Subjects With Small Cell Lung Cancer (SCLC), Ovarian Cancer and Other Advanced Solid Tumors [NCT00765973]	Phase 1	14 participants (Actual)	Interventional	2008-11-10	Completed
A Phase I Study of Temsirolimus, Topotecan, and Bortezomib in Patients With Advanced Malignancy [NCT00770731]	Phase 1	80 participants (Actual)	Interventional	2008-09-30	Completed
A Randomized, Double-blind, Placebo-controlled, Multi-center Phase 3 Study Evaluating Efficacy, Safety and Pharmacokinetics of Trilaciclib In Extensive-Stage Small Cell Lung Cancer Patients Receiving Carboplatin Combined With Etoposide or Topotecan [NCT04902885]	Phase 3	95 participants (Actual)	Interventional	2021-05-25	Completed
Phase I/II Study of Carboplatin in Association With Weekly Oral Topotecan in Patients With Metastatic or Recurrent Cervical Cancer [NCT00807079]	Phase 1/Phase 2	12 participants (Actual)	Interventional	2008-09-30	Completed
Phase II Study of Cisplatin Combined With Topotecan in Advanced (Stage IVB) Recurrent or Persistent Cervical Cancer [NCT00826891]	Phase 2	40 participants (Anticipated)	Interventional	2009-02-28	Not yet recruiting
AMR PH GL 2007 CL001 Phase 3 A Randomized, Open-Label, Multinational Phase 3 Trial Comparing Amrubicin Versus Topotecan in Patients With Extensive or Limited and Sensitive or Refractory Small Cell Lung Cancer After Failure of First-Line Chemotherapy [NCT00547651]	Phase 3	637 participants (Actual)	Interventional	2007-09-01	Completed
A Randomized Phase 2 Trial Comparing Amrubicin Versus Topotecan as Second-Line Treatment in Patients With Extensive Small Cell Lung Cancer Sensitive to First-Line Chemotherapy [NCT00319969]	Phase 2	76 participants (Actual)	Interventional	2006-04-30	Completed
Liposomal Doxorubicin Versus Carboplatin/Paclitaxel in Patients With Ovarian Cancer Recurrence Between 6 and 12 Months After Previous Platinum Based Therapy: Phase III Randomized Multicenter Study Amendment Title Protocol Version 2.0: Phase III Internatio [NCT00657878]	Phase 3	215 participants (Actual)	Interventional	2008-11-30	Active, not recruiting
Phase 1 Study of Cabozantinib in Combination With Topotecan-Cyclophosphamide for Patients With Relapsed Ewing Sarcoma or Osteosarcoma [NCT04661852]	Phase 1	12 participants (Actual)	Interventional	2020-12-23	Completed
A Randomized Phase II Study Evaluating Pembrolizumab vs Topotecan in the Second-Line Treatment of Patients With Small Cell Lung Cancer [NCT02963090]	Phase 2	9 participants (Actual)	Interventional	2017-05-20	Terminated(stopped due to Lack of enrollment)
A Phase 3 Study of Dinutuximab Added to Intensive Multimodal Therapy for Children With Newly Diagnosed High-Risk Neuroblastoma [NCT06172296]	Phase 3	478 participants (Anticipated)	Interventional	2024-02-14	Not yet recruiting
N9: Pilot Study of Novel Shortened Induction Chemotherapy for High-Risk Neuroblastoma [NCT04947501]	Early Phase 1	30 participants (Anticipated)	Interventional	2021-06-22	Recruiting
A Phase I Study of Sequestered Transscleral, Controlled-Release Topotecan Delivered From an Episcleral Reservoir in Retinoblastoma Eyes [NCT04156347]	Phase 1	42 participants (Anticipated)	Interventional	2021-06-16	Active, not recruiting
A Randomized Phase II/III Study to Assess the Efficacy of Trametinib (GSK 1120212) in Patients With Recurrent or Progressive Low-Grade Serous Ovarian Cancer or Peritoneal Cancer [NCT02101788]	Phase 2/Phase 3	260 participants (Actual)	Interventional	2014-02-27	Active, not recruiting
Phase 1 Study of Lorlatinib (PF-06463922), an Oral Small Molecule Inhibitor of ALK/ROS1, for Patients With ALK-Driven Relapsed or Refractory Neuroblastoma [NCT03107988]	Phase 1	65 participants (Actual)	Interventional	2017-09-05	Active, not recruiting
Protocol for the Study and Treatment of Participants With Intraocular Retinoblastoma [NCT01783535]	Phase 2	174 participants (Anticipated)	Interventional	2013-06-19	Active, not recruiting
Avastin in Combination With Radiation and Temozolomide Followed by Avastin, Temozolomide, and Topotecan for Glioblastoma Multiformes and Gliosarcomas [NCT01004874]	Phase 2	80 participants (Actual)	Interventional	2009-12-30	Completed
Study EGF107671 - a Phase II Study of Lapatinib Plus Topotecan or Lapatinib Plus Capecitabine in the Treatment of Recurrent Brain Metastases From ErbB2-Positive Breast Cancer Following Cranial Radiotherapy [NCT00437073]	Phase 2	22 participants (Actual)	Interventional	2007-05-31	Terminated(stopped due to Lapatinib-topotecan arm enrollment closed early per protocol amendment 2. Then enrollment into remaining arm terminated due to operational issues.)
A Multicenter, Randomized, Open-Label Phase 2b Study to Investigate the Efficacy and Safety of Aldoxorubicin Compared to Topotecan in Subjects With Metastatic Small Cell Lung Cancer Who Either Relapsed or Were Refractory to Prior Chemotherapy [NCT02200757]	Phase 2	132 participants (Anticipated)	Interventional	2014-09-30	Recruiting
Randomized Study Comparing Two Strategies Carboplatin and Etoposide Topotecan in Patients With SCLC on the Second Row With Relapsed at Least Three Months After Initial Response to Chemotherapy With Platinum-etoposide 6 Cycles [NCT02738346]	Phase 3	164 participants (Anticipated)	Interventional	2013-07-31	Recruiting
Phase I Trial of Oral Topotecan Plus Temodar in the Treatment of Patients With Malignant Gliomas [NCT00610571]	Phase 1	62 participants (Actual)	Interventional	2004-04-30	Completed
A Phase II Trial of Twice Daily Oral Topotecan as a Radiation Sensitizer With Twice Daily Radiotherapy for Newly Diagnosed Small Cell Lung Cancer [NCT00043862]	Phase 2	60 participants (Actual)	Interventional	2002-08-31	Completed
Phase I/II Multicenter Study to Assess Efficacy and Safety of Ribociclib (LEE011) in Combination With Topotecan and Temozolomide (TOTEM) in Pediatric Patients With Relapsed or Refractory Neuroblastoma and Other Solid Tumors [NCT05429502]	Phase 1/Phase 2	231 participants (Anticipated)	Interventional	2022-12-27	Recruiting
Phase II Study of the Association of Iodobenzylguanidine Meta-I131 (I131 MIBG) and Topotecan in the Treatment of Refractory or Relapsed Metastatic Neuroblastoma [NCT00960739]	Phase 2	30 participants (Actual)	Interventional	2008-11-30	Completed
Phase II Study of Weekly Topotecan in Patients Treated for Metastatic Colorectal Cancer [NCT00193167]	Phase 2	40 participants	Interventional	2004-01-31	Completed
A Pilot Study of Intravenous Topotecan and Vincristine in Combination With Subconjunctival Carboplatin for Patients With a History of Bilateral Retinoblastoma and Refractory/Recurrent Intraocular Disease (IND# 104,942) [NCT00980551]		0 participants (Actual)	Interventional	2010-05-31	Withdrawn(stopped due to No enrollment and competing studies)
European Proof-of-Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory Tumors [NCT02813135]	Phase 1/Phase 2	460 participants (Anticipated)	Interventional	2016-08-03	Recruiting
Phase I/II Study of Obatoclax Mesylate (GX15-070MS), a Bcl-2 Antagonist, Plus Topotecan in Relapsed Small Cell Lung Carcinoma [NCT00521144]	Phase 1/Phase 2	22 participants (Actual)	Interventional	2007-08-31	Completed
A Phase 1 Study of FF-10850 Topotecan Liposome Injection in Advanced Solid Tumors Including Ovarian and Cervical Carcinoma, Sarcomas, and Neuroendocrine Tumors Including Small Cell Lung Cancer and Merkel Cell Carcinoma [NCT04047251]	Phase 1	96 participants (Anticipated)	Interventional	2019-11-14	Recruiting
Response- and Biology-Based Therapy for Intermediate-Risk Neuroblastoma [NCT00499616]	Phase 3	464 participants (Actual)	Interventional	2007-10-08	Completed
An Open-label Phase II Study of Weekly Intravenous Hycamtin and Carboplatin as First-line Treatment of Chemonaive Subjects With Extensive Disease Small Cell Lung Cancer [NCT00316186]	Phase 2	33 participants (Actual)	Interventional	2005-06-30	Completed
Phase II Clinical Study of Weekly Topotecan in Combination With Avastin™ in Patients With Stage IIIB/IV Non-Small Cell Lung Cancer Who Have Failed Prior Systemic Chemotherapy [NCT00365547]	Phase 2	46 participants (Actual)	Interventional	2006-09-30	Completed
A Phase II Study of Topotecan in Patients With Anaplastic Oligodendroglioma or Anaplastic Mixed Oligoastrocytoma [NCT00003372]	Phase 2	17 participants (Actual)	Interventional	1997-12-08	Completed
Phase Ib Dose-Escalation Study of LCL161 in Combination With Oral Topotecan for Patients With Relapsed/Refractory Small Cell Lung Cancer (SCLC) and Select Gynecologic Malignancies [NCT02649673]	Phase 1	34 participants (Actual)	Interventional	2016-03-23	Terminated(stopped due to Clinical program was discontinued by Novartis)
A Phase 3 Study of Safety and Efficacy of Karenitecin Versus Topotecan Administered for 5 Consecutive Days Every 3 Weeks in Patients With Advanced Epithelial Ovarian Cancer [NCT00477282]	Phase 3	509 participants (Actual)	Interventional	2007-08-31	Completed
A Dose Seeking Trial of Topotecan Combined With High-Dose Cyclophosphamide and Carboplatin With Peripheral Blood Stem Cell Transplant for the Treatment of Relapsed Ovarian Cancer and Primary Peritoneal Cancer [NCT00652691]	Phase 1	48 participants (Anticipated)	Interventional	1998-08-31	Completed
Neuroblastoma Protocol 2008: Therapy for Children With Advanced Stage High Risk Neuroblastoma [NCT00808899]	Phase 2	4 participants (Actual)	Interventional	2008-12-31	Terminated(stopped due to Voluntarily closed and terminated by the PI due to lack of feasibility)
A Pilot Prospective Trial Of Genomic Directed Salvage Chemotherapy With Either Liposomal Doxorubicin Or Topotecan In Recurrent Or Persistent Ovarian Cancer Within 12 Months Of Platinum-Based Chemotherapy [NCT00720096]		4 participants (Actual)	Interventional	2008-07-31	Terminated(stopped due to Funds for this project have been spent, and it is thereby terminated.)
Randomized Phase III Trial of Topotecan and Cisplatin Versus Etoposide and Carboplatin in the Treatment of Patients With Previously Untreated Small Cell Lung Cancer and Extensive Disease [NCT00812266]	Phase 3	281 participants (Actual)	Interventional	2006-01-31	Terminated(stopped due to Slow accrual)
Phase 2 Single- Arm Studies of Temozolomide in Combination With Topotecan in Refractory and Relapsed Neuroblastoma and Other Paediatric Solid Tumours [NCT00918320]	Phase 2	129 participants (Actual)	Interventional	2009-06-30	Completed
AURELIA: A Multi-center, Open-label, Randomised, Two-arm Phase III Trial of the Effect on Progression Free Survival of Bevacizumab Plus Chemotherapy Versus Chemotherapy Alone in Patients With Platinum-resistant, Epithelial Ovarian, Fallopian Tube or Prima [NCT00976911]	Phase 3	361 participants (Actual)	Interventional	2009-10-29	Completed
A Randomized, Double-Blind, Multicenter, Phase Ⅲ Study of Anlotinib Hydrochloride Capsule Combined With Topotecan Versus Placebo Combined With Topotecan in Subjects With Small Cell Lung Cancer [NCT04073550]	Phase 3	184 participants (Anticipated)	Interventional	2019-10-31	Not yet recruiting
Phase II Randomized Trial of the Polo-like Kinase 1 Inhibitor BI 6727 Monotherapy Versus Investigator´s Choice Chemotherapy in Ovarian Cancer Patients Resistant or Refractory to Platinum-based Cytotoxic Therapy [NCT01121406]	Phase 2	110 participants (Actual)	Interventional	2010-04-30	Completed
A Phase I Study of Weekly Oral Topotecan in Gynecologic Malignancies [NCT00842452]	Phase 1	26 participants (Actual)	Interventional	2009-02-28	Completed
A Randomized, Multicenter, Open-label, Phase III Study of Lurbinectedin Single-Agent or Lurbinectedin in Combination With Irinotecan Versus Investigator's Choice (Topotecan or Irinotecan) in Relapsed Small Cell Lung Cancer Patients (LAGOON Trial) [NCT05153239]	Phase 3	705 participants (Anticipated)	Interventional	2022-07-22	Recruiting
Protocol for the Study and Treatment of Patients With Intraocular Retinoblastoma [NCT00186888]	Phase 3	107 participants (Actual)	Interventional	2005-04-07	Active, not recruiting
An Open-label, Multicenter, Non-Comparative Phase II Study of the Combination of Intravenous Topotecan and Gemcitabine Administered Once Weekly for Three Weeks Every 28 Days as Second-line Treatment in Patients With Recurrent Platinum Sensitive Ovarian Ca [NCT00061308]	Phase 2	75 participants	Interventional	2002-12-31	Completed
A Phase I, Open-label Study of the Safety, Tolerability, and Pharmacokinetics of Oral Topotecan in Combination With Lapatinib in Subjects With Advanced Solid Tumors [NCT00682279]	Phase 1	0 participants (Actual)	Interventional	2008-09-30	Withdrawn(stopped due to Cancelled before enrollment)
An Open Label, Multi-centre, Non-interventional Post-marketing Surveillance (PMS) to Monitor the Safety and Effectiveness of HYCAMTIN Administered in Korean Patients According to the Prescribing Information [NCT01037023]		92 participants (Actual)	Observational	2010-10-31	Completed
A Phase I Study of the Weekly Oral RAD001 in Combination With Oral Topotecan in Patients With Advanced or Recurrent Endometrial Cancers [NCT00703807]	Phase 1	10 participants (Actual)	Interventional	2008-12-31	Completed
A Pilot Study of Chemotherapy Intensification by Adding Vincristine, Topotecan and Cyclophosphamide to Standard Chemotherapy Agents With an Interval Compression Schedule in Newly Diagnosed Patients With Localized Ewing Sarcoma Family of Tumors [NCT00618813]		35 participants (Actual)	Interventional	2008-03-31	Completed
Phase I Trial of Tandem Chemotherapy Cycles as Consolidation Therapy for High-Risk Epithelial Ovarian and Primary Peritoneal Cancer Utilizing Intraperitoneal Paclitaxel/IV Cyclophosphamide Followed by IV Topotecan/Intraperitoneal Cisplatin/IV Melphalan Us [NCT00550784]	Phase 1	8 participants (Actual)	Interventional	2001-01-31	Completed
An Open-label, Multicenter, Non-comparative, Phase II Study of Oral Topotecan in Combination With Bevacizumab for Second-line Treatment in Subjects With Relapsed Small-cell Lung Cancer (SCLC) [NCT00698516]	Phase 2	50 participants (Actual)	Interventional	2008-07-31	Completed
Phase III Multicenter Study in Epithelial Ovarian Carcinoma FIGO Stage IIB-IV Comparing Treatment With Paclitaxel and Carboplatin to Paclitaxel and Carboplatin Sequentially Followed by Topotecan [NCT00102375]	Phase 3	900 participants	Interventional	1999-12-31	Completed
A Pilot Induction Regimen Incorporating Chimeric 14.18 Antibody (ch14.18, Dinutuximab) (NSC# 764038) and Sargramostim (GM-CSF) for the Treatment of Newly Diagnosed High-Risk Neuroblastoma [NCT03786783]	Phase 2	42 participants (Actual)	Interventional	2019-01-14	Active, not recruiting
Phase III Randomized Trial of Single vs. Tandem Myeloablative Consolidation Therapy for High-Risk Neuroblastoma [NCT00567567]	Phase 3	665 participants (Actual)	Interventional	2007-11-05	Completed
Circulating Tumor DNA Guiding (Olaparib) Lynparza® Treatment in Ovarian [NCT02822157]	Phase 2	160 participants (Actual)	Interventional	2016-08-31	Active, not recruiting
Oral Topotecan Combined With Anlotinib in Patients With Platinum-resistant Recurrent Ovarian Cancer： [NCT05736952]	Phase 2	0 participants (Actual)	Interventional	2023-03-01	Withdrawn(stopped due to Program changed)
An Open-Label, Randomized, Phase 2 Study Comparing TAS-102 Versus Topotecan or Amrubicin in Patients Requiring Second-Line Chemotherapy for Small Cell Lung Cancer That is Refractory or Sensitive to First-Line Platinum-Based Chemotherapy [NCT01904253]	Phase 2	18 participants (Actual)	Interventional	2013-07-31	Terminated(stopped due to The preliminary data does not suggest any safety signal, but an ad hoc interim analysis showed an imbalance of PFS between the two arms)
A Phase II Trial of Oral Pazopanib Plus Oral Topotecan Metronomic Antiangiogenic Therapy for Recurrent Glioblastoma Multiforme (A)Without Prior Bevacizumab Exposure and (B) After Failing Prior Bevacizumab [NCT01931098]	Phase 2	35 participants (Actual)	Interventional	2015-12-10	Completed
A Rollover Protocol to Allow for Continued Access to the LSD1 Inhibitor Seclidemstat (SP-2577) [NCT05266196]	Phase 1/Phase 2	10 participants (Anticipated)	Interventional	2022-01-15	Enrolling by invitation
A Phase II Study of Intensive-Dose Topotecan, Ifosfamide/Mesna and Etoposide (Vepesid)(TIME) Followed by Autologous Stem Cell Rescue in High Risk Lymphoma [NCT00006373]	Phase 2	27 participants (Actual)	Interventional	2000-02-29	Completed
A Phase II Study of Intensive-Dose Topotecan, Ifosfamide/Mesna and Etoposide (TIME) Followed by Autologous Stem Cell Rescue in Metastatic Breast Cancer [NCT00006032]	Phase 2	0 participants	Interventional	2000-03-31	Terminated(stopped due to low accrual)
A Phase I Study of CCI-779 (Temsirolimus) in Combination With Topotecan in Patients With Gynecologic Malignancies [NCT00523432]	Phase 1	15 participants (Actual)	Interventional	2007-08-31	Completed
Safety and Dose Finding Study of Oral MP470, a Multi-targeted Tyrosine Kinase Inhibitor, in Combination With Standard-of-Care Chemotherapy Regimens [NCT00881166]	Phase 1	101 participants (Actual)	Interventional	2007-11-30	Completed
A Phase II Study Evaluating the Association of Topotecan and Lapatinib in Early Recurrent (Less Than 12 Months)Ovarian or Peritoneal Cancer Patients After First Line of Platinum-Based Chemotherapy [NCT00888810]	Phase 2	39 participants (Actual)	Interventional	2008-03-31	Terminated(stopped due to lack of efficacy (intermediate analysis))
A Pilot Study of Tamoxifen, Carboplatin and Topotecan in the Treatment of Recurrent or Refractory Primary Brain or Spinal Cord Tumors or Metastatic Epithelial Cancers With Central Nervous System Metastases [NCT00541138]	Phase 2	50 participants (Anticipated)	Interventional	2003-05-31	Completed
A Phase II Trial of Lapatinib in Combination With Weekly Topotecan in Patients With Platinum-Refractory/Resistant Ovarian and Primary Peritoneal Carcinoma [NCT00436644]	Phase 2	18 participants (Actual)	Interventional	2007-03-31	Completed
SCOT Registry: Small Cell Lung Cancer Treatment and Outcome [NCT00997061]		500 participants (Actual)	Observational	2009-11-30	Completed
An Open-Label, Single-Arm, Phase II Study of IV Weekly (Days 1 and 8 Every 21 Days) HYCAMTIN in Combination With Carboplatin (Day 1 Every 21 Days) as Second-Line Therapy in Subjects With Potentially Platinum-Sensitive Relapsed Ovarian Cancer [NCT00316173]	Phase 2	77 participants (Actual)	Interventional	2005-03-31	Completed
A Randomized, Phase III, Open-Label Study of Oral Topotecan Plus Whole-Brain Radiation Therapy (WBRT) Compared With WBRT Alone in Patients With Brain Metastases From Non-Small Cell Lung Cancer [NCT00390806]	Phase 3	472 participants (Actual)	Interventional	2006-12-31	Completed
A Randomized Phase II Evaluation of Topotecan (NSC #609699) Administered Daily x 5 Every 3 Weeks vs Weekly Topotecan in the Treatment of Recurrent Platinum-Sensitive Ovarian, Fallopian Tube, or Primary Peritoneal Cancer [NCT00114166]	Phase 2	81 participants (Actual)	Interventional	2005-01-31	Completed
A Phase I/II Study of Sorafenib in Combination With Topotecan for the Treatment of Platinum-Resistant Recurrent Ovarian Cancer or Primary Peritoneal Carcinomatosis: Hoosier Oncology Group GYN06-111 [NCT00526799]	Phase 1/Phase 2	30 participants (Actual)	Interventional	2007-09-30	Terminated(stopped due to Study closed to accrual due unfavorable interim analysis)
A Phase I/II Study of Weekly Topotecan and Gefitinib (Iressa) in Patients With Platinum-Resistant Ovarian, Peritoneal, of Fallopian Tube Cancer [NCT00317772]	Phase 1/Phase 2	19 participants (Actual)	Interventional	2004-09-02	Completed
A Study of Intensive-Dose Melphalan and Topotecan (MT) Followed by Autologous Stem Cell Rescue in Patients With Multiple Myeloma. [NCT00325416]	Phase 1/Phase 2	177 participants (Actual)	Interventional	2001-11-19	Completed
WEEKLY IV TOPOTECAN/DOCETAXEL COMBINATION COMPARED TO DOCETAXEL IN PATIENTS WITH PRETREATED ADVANCED NSCLC: AN OPEN-LABEL MULTICENTER RANDOMIZED PHASE III TRIAL [NCT00065182]	Phase 2	399 participants (Actual)	Interventional	2003-08-14	Completed
Phase II Trial of Weekly Topotecan in the Second-Line Treatment of Small Cell Lung Cancer [NCT00193388]	Phase 2	100 participants	Interventional	2002-09-30	Completed
Evaluation of TRILACICLIB in Chinese Patients With Extensive-stage Small Cell Lung Cancer (ES-SCLC) for Chemotherapy-induced Myelosuppression, Antitumor Effects of Combination Regimens, and Safety in a Real-world Study [NCT05071703]	Phase 4	30 participants (Actual)	Interventional	2021-08-11	Completed
A Phase II Evaluation of ABT-888 (NCI Supplied Agent: ABT-888, NSC #737664), Topotecan (NSC # 609699) and Filgrastim or Pegfilgrastim in the Treatment of Persistent or Recurrent Squamous or Non-squamous Cell Carcinoma of the Cervix [NCT01266447]	Phase 2	27 participants (Actual)	Interventional	2011-02-28	Completed
Phase 1b/2a Safety and Pharmacokinetic Study of G1T28 in Patients With Previously Treated Extensive Stage Small Cell Lung Cancer (SCLC) Receiving Topotecan Chemotherapy [NCT02514447]	Phase 1/Phase 2	123 participants (Actual)	Interventional	2015-10-05	Terminated(stopped due to Primary Analysis and survival follow up completed per protocol. Not stopped due to safety concerns.)
A Study of Intratumorally-Administered Topotecan Using Convection-Enhanced Delivery (CED) in Patients With Suspected Recurrent/Progressive World Health Organization (WHO) Grade III or IV (High Grade) Glioma Undergoing Stereotactic Biopsy [NCT03927274]	Early Phase 1	3 participants (Actual)	Interventional	2019-06-20	Terminated(stopped due to Funding unavailable)
A Phase 2 Open-label Randomized Study of Farletuzumab Ecteribulin (MORAb-202), a Folate Receptor Alpha-targeting Antibody-drug Conjugate, Versus Investigator's Choice Chemotherapy in Women With Platinum-resistant High-grade Serous (HGS) Ovarian, Primary P [NCT05613088]	Phase 2	90 participants (Anticipated)	Interventional	2023-02-01	Recruiting
A Phase I Protocol for Relapsed Pediatric AML to Determine the Safety and Efficacy of the PARP Inhibitor Talazoparib in Combination With Chemotherapy [NCT05101551]	Phase 1	34 participants (Anticipated)	Interventional	2023-02-23	Recruiting
Positron Emission Tomography Using 11C Topotecan in Predicting Response to Treatment in Patients With Brain Metastases Due to Ovarian, Small Cell Lung, or Other Cancer [NCT00253461]	Early Phase 1	7 participants (Actual)	Interventional	2004-12-31	Terminated(stopped due to Drugs unavailable:unable to make radioactive topotecan)
Phase I Study to Evaluate the Mass Balance, PK, Metabolism and Excretion of Berzosertib (Intravenous) Containing Microtracer [14C]Berzosertib in Participants With Advanced Solid Tumors (DDRiver Solid Tumors 208) [NCT05246111]	Phase 1	6 participants (Actual)	Interventional	2022-02-15	Completed
Phase I-II Study of Topotecan and Paclitaxel Followed by High-Dose Thoracic Radiation Therapy With Concomitant Cisplatin/Etoposide and Amifostine in Limited-Stage Small Cell Lung Cancer [NCT00006012]	Phase 1/Phase 2	73 participants (Actual)	Interventional	2001-02-28	Completed
Phase I Study of Weekly Bortezomib (VELCADE, PS-341) and Weekly Topotecan (HYCAMTIN) in Solid Tumor Patients With an Emphasis on Small Cell Lung Cancer (SCLC) [NCT00388089]	Phase 1	24 participants (Actual)	Interventional	2004-12-31	Completed
[NCT00006199]	Phase 1	0 participants	Interventional		Recruiting
A Phase I Dose-Finding Study of Oxaliplatin (NSC #266046) Combined With Continuous Infusion Topotecan Hydrochloride as Chemotherapy for Patients With Previously Treated Ovarian Cancer [NCT00006391]	Phase 1	0 participants	Interventional	2000-08-31	Completed
Phase III Multicenter Study in Epithelial Ovarian Carcinoma FIGO Stage IIB-IV Comparing Treatment With Paclitaxel and Carboplatin to Paclitaxel and Carboplatin Sequentially Followed by Topotecan [NCT00006454]	Phase 3	0 participants	Interventional	1999-12-31	Completed
An Open-label, Phase II, Multicenter Study of Intravenous Weekly Topotecan in Subjects With Recurrent or Persistent Endometrial Cancer [NCT00267488]	Phase 2	70 participants (Actual)	Interventional	2005-10-31	Completed
A Phase 1 Study of Crizotinib in Combination With Conventional Chemotherapy for Relapsed or Refractory Solid Tumors or Anaplastic Large Cell Lymphoma [NCT01606878]	Phase 1	46 participants (Actual)	Interventional	2013-04-29	Completed
A Phase 1b Study of AMG 386 in Combination With Either Pegylated Liposomal Doxorubicin or Topotecan in Subjects With Advanced Recurrent Epithelial Ovarian Cancer [NCT00770536]	Phase 1	103 participants (Actual)	Interventional	2009-01-31	Completed
MIRASOL: A Randomized, Open-label, Phase 3 Study of Mirvetuximab Soravtansine vs. Investigator's Choice of Chemotherapy in Platinum-Resistant, Advanced High-Grade Epithelial Ovarian, Primary Peritoneal, or Fallopian Tube Cancers With High Folate Receptor- [NCT04209855]	Phase 3	453 participants (Actual)	Interventional	2019-12-31	Active, not recruiting
Phase IB Study to Evaluate the Safety of Selinexor (KPT-330) in Combination With Multiple Standard Chemotherapy or Immunotherapy Agents in Patients With Advanced Malignancies [NCT02419495]	Phase 1	221 participants (Actual)	Interventional	2015-06-26	Active, not recruiting
A Phase I Open-label Study of the Safety, Tolerability, and Pharmacokinetics of Two Schedules of Oral Topotecan in Combination With Pazopanib in Subjects With Advanced Solid Tumors [NCT00732420]	Phase 1	68 participants (Actual)	Interventional	2008-09-24	Completed
BAY 1895344 Plus Topoisomerase-1 (Top1) Inhibitors in Patients With Advanced Solid Tumors, Phase I Studies With Expansion Cohorts in Small Cell Lung Carcinoma (SCLC), Poorly Differentiated Neuroendocrine Carcinoma (PD-NEC) and Pancreatic Adenocarcinoma (P [NCT04514497]	Phase 1	96 participants (Anticipated)	Interventional	2021-10-20	Active, not recruiting
Phase I Study of Anti-GD2 3F8 Antibody and Allogeneic Natural Killer Cells for High-Risk Neuroblastoma [NCT00877110]	Phase 1	71 participants (Actual)	Interventional	2009-04-02	Completed
A Phase I Study of Weekly Topotecan With Cisplatin for the Management of Advanced Stage or Recurrent Carcinoma of the Cervix [NCT00322920]	Phase 1	30 participants (Anticipated)	Interventional	2005-07-31	Terminated(stopped due to Low accrual)
Phase I-II Study of Oral Suberoylanilide Hydroxamic Acid (Vorinostat) in Combination With Topotecan in Patients With Chemosensitive Recurrent Small Cell Lung Cancer (SCLC) [NCT00697476]	Phase 1/Phase 2	2 participants (Actual)	Interventional	2009-01-31	Terminated(stopped due to insufficient enrollment)
A Randomized Phase II Study of Bevacizumab (NSC 704865) Combined With Vincristine, Topotecan and Cyclophosphamide in Patients With First Recurrent Ewing Sarcoma [NCT00516295]	Phase 2	7 participants (Actual)	Interventional	2008-02-29	Completed
The Efficacy and Safety of Nab-paclitaxel Versus Topotecan As Second-Line Treatment for Patients With Extensive Stage Small Cell Lung Cancer: A Multicenter, Randomized Controlled Study [NCT04213937]	Phase 2	386 participants (Anticipated)	Interventional	2020-01-31	Recruiting
A Phase I Study of Topotecan by Intracerebral Clysis for the Treatment of Recurrent Primary Malignant Brain Tumors [NCT00308165]	Phase 1/Phase 2	18 participants (Actual)	Interventional	2004-03-31	Active, not recruiting
A Phase II Study of Intraventricular Methotrexate With Systemic Topotecan and Cyclophosphamide in Children With Recurrent or Progressive Malignant Brain Tumors [NCT02684071]	Phase 2	3 participants (Actual)	Interventional	2016-02-29	Terminated(stopped due to Lack of additional funding; patients (3) no longer receiving intervention.)
A Randomized Phase II Trial of Weekly Topotecan With and Without AVE0005 (Aflibercept; NSC-724770) in Patients With Platinum Treated Extensive Stage Small Cell Lung Cancer (E-SCLC) [NCT00828139]	Phase 2	189 participants (Actual)	Interventional	2009-05-31	Completed
A Dose Regimen-Finding Study to Evaluate the Safety, Tolerability, Pharmacokinetics, and Activity of Oral Topotecan With HM30181A Monotherapy in Patients With Advanced Malignancies [NCT03987685]	Phase 1	10 participants (Actual)	Interventional	2018-07-19	Completed
Randomized Phase III Trial on NIraparib-TSR-042 (Dostarlimab) vs Physician's Choice CHEmotherapy in Recurrent, Ovarian, Fallopian Tube or Primary Peritoneal Cancer Patients Not Candidate for Platinum Retreatment: NItCHE Trial (MITO 33) [NCT04679064]	Phase 3	427 participants (Anticipated)	Interventional	2020-12-01	Recruiting
A Phase II Trial of SOM230(PasireotideLAR) and Topotecan in Patients With Relapsed or Refractory Small Cell Lung Cancer [NCT01417806]	Phase 2	28 participants (Anticipated)	Interventional	2011-07-31	Recruiting
Topotecan Plus Carboplatin im Vergleich Zur Standardtherapie (Paclitaxel Plus Carboplatin Oder Gemcitabin Plus Carboplatin) in Der Therapie Von Patientinnen Mit Platin-sensitivem Rezidivierten Epithelialen Ovarialkarzinom, Peritonealkarzinom Oder Tubenkar [NCT00437307]	Phase 3	550 participants (Actual)	Interventional	2007-03-31	Completed
Open-label, Dose-escalation, Multiple Dosing Study to Evaluate the Safety, Tolerability, Immune Response and Pre Efficacy of BVAC-C in Patients With Multiple Metastatic Progressive or Recurrent HPV Type 16 or 18 Positive Cervical Cancer After Failure to S [NCT02866006]	Phase 1/Phase 2	32 participants (Actual)	Interventional	2016-10-31	Completed
International Phase II Studies of I-mIBG in Combination With Topotecan and Peripheral Blood Stem Cell Rescue for (A) Primary Resistant High Risk Neuroblastoma and (B) Relapsed Stage 4 Neuroblastoma [NCT00389766]	Phase 2	0 participants (Actual)	Interventional	2008-07-31	Withdrawn(stopped due to Withdrawn because protocol has been discontinued. It was never opened.)
A Limited Access Phase II Trial of Weekly Topotecan (NSC #609699), Paclitaxel (NSC #673089), and Cisplatin (NSC #119875) in the Treatment of Advanced, Persistent, or Recurrent Carcinoma of the Cervix [NCT00276796]	Phase 2	66 participants (Anticipated)	Interventional		Completed
A Randomized Trial of Oral Topotecan Versus Docetaxel in Second-Line Treatment of Non-Small Cell Lung Cancer [NCT00193245]	Phase 2	80 participants	Interventional	2000-11-30	Completed
Phase II Trial of Weekly Topotecan in the First-line Treatment of Elderly Patients With Small Cell Lung Cancer [NCT00193401]	Phase 2	40 participants	Interventional	2002-08-31	Completed
A Phase I Study of ABT-888 in Combination With Topotecan Hydrochloride in Adults With Refractory Solid Tumors and Lymphomas [NCT00553189]	Phase 1	31 participants (Actual)	Interventional	2007-08-09	Completed
Phase II Study of the Activity of Weekly Paclitaxel, Topotecan Plus Oral Estramustine Phosphate in Metastatic Hormone-Refractory Prostate Carcinoma [NCT00084565]	Phase 2	0 participants (Actual)	Interventional	2003-11-30	Withdrawn(stopped due to Study was never activated at Fox Chase Cancer Center.)
A PHASE I STUDY OF PELVIC RADIATION THERAPY WITH CONCOMITANT WEEKLY CISPLATIN AND TOPOTECAN CHEMOTHERAPY IN PATIENTS WITH CERVICAL CARCINOMA WITHOUT EXTRA-PELVIC METASTASIS [NCT00054444]	Phase 1	11 participants (Actual)	Interventional	2007-09-30	Completed
A Phase II Study of Sequential Doxorubicin and Topotecan (Dox/Topo) in Relapsed or Refractory Intermediate- or High-Grade Non-Hodgkin's Lymphoma (NHL) [NCT00006125]	Phase 2	0 participants	Interventional	2000-07-31	Completed
NB2004 Trial Protocol for Risk Adapted Treatment of Children With Neuroblastoma [NCT00410631]	Phase 3	642 participants (Anticipated)	Interventional	2004-10-31	Recruiting
A Phase I Pharmacokinetic Optimal Dosing Study of Intrathecal Topotecan for Children With Neoplastic Meningitis [NCT00674674]	Phase 1	22 participants (Actual)	Interventional	2005-10-31	Completed
DAREON™-9: A Phase Ib Open-label Dose Escalation and Dose Confirmation Safety Study of Intravenous BI 764532 in Combination With Topotecan for the Treatment of Patients With Small Cell Lung Cancer [NCT05990738]	Phase 1	44 participants (Anticipated)	Interventional	2024-01-11	Not yet recruiting
Therapy for Children With Advanced Stage High Risk Neuroblastoma [NCT00186849]	Phase 2	30 participants (Actual)	Interventional	1997-10-31	Completed
A Study of Children With Refractory or Relapsed Acute Lymphoblastic Leukemia (ALLR16) [NCT00187083]	Phase 3	40 participants (Actual)	Interventional	1997-02-28	Completed
Phase 3 Randomized Study of TLK286 (Telcyta) Versus Doxil/Caelyx or Hycamtin as Third-Line Therapy in Platinum Refractory or Resistant Ovarian Cancer [ASSIST-1 (Assessment of Survival In Solid Tumors-1)] [NCT00057720]	Phase 3	440 participants	Interventional	2003-06-30	Completed
A Phase I Study of Oral Topotecan as a Radiosensitizing Agent in Patients With Rectal Cancer [NCT00158886]	Phase 1	26 participants (Actual)	Interventional	2001-11-08	Terminated
A Phase II Study of Topotecan in Children With Recurrent Wilms Tumor [NCT00187031]	Phase 2	37 participants (Actual)	Interventional	2002-11-30	Completed
National, Randomized, Phase II Study Comparing Efficacy of Weekly Administration of Paclitaxel in Monotherapy or in Combination With Topotecan or Carboplatin in Patients With Epithelial Ovarian Cancer in Early Relapse [NCT00189566]	Phase 2	165 participants (Anticipated)	Interventional	2004-04-30	Completed
Phase 1 Study of Temozolomide Associated With Topotecan in Refractory or Relapsed Malignant Tumors in Children and Adolescents [NCT00412503]	Phase 1	0 participants	Interventional		Completed
FORWARD I: A Randomized, Open Label Phase 3 Study to Evaluate the Safety and Efficacy of Mirvetuximab Soravtansine (IMGN853) Versus Investigator's Choice of Chemotherapy in Women With Folate Receptor Alpha Positive Advanced Epithelial Ovarian Cancer, Prim [NCT02631876]	Phase 3	366 participants (Actual)	Interventional	2016-03-02	Completed
A Randomized, Open-Label, Multicenter, Phase 3 Study of Rovalpituzumab Tesirine Compared With Topotecan for Subjects With Advanced or Metastatic DLL3high Small Cell Lung Cancer (SCLC) Who Have First Disease Progression During or Following Front-Line Plati [NCT03061812]	Phase 3	444 participants (Actual)	Interventional	2017-04-11	Completed
Evaluation of Topotecan in the Treatment of Persistent or Recurrent Carcinosarcoma (Mixed Mesodermal Tumors) of the Uterus [NCT00003156]	Phase 2	0 participants	Interventional	1998-06-30	Terminated
A Phase I Dose-Escalation Study of Topotecan and Ifosfamide in Patients With Refractory Non-Hematologic Malignancies. [NCT00003198]	Phase 1	0 participants	Interventional	1997-11-30	Completed
Phase 2 Study of Alisertib as a Single Agent in Recurrent or Progressive Central Nervous System (CNS) Atypical Teratoid Rhabdoid Tumors (AT/RT) and Extra-CNS Malignant Rhabdoid Tumors (MRT) and in Combination Therapy in Newly Diagnosed AT/RT [NCT02114229]	Phase 2	125 participants (Actual)	Interventional	2014-05-14	Active, not recruiting
FLAT: Fludarabine, Cytarabine and Topotecan in Treating Patients With Refractory or Relapsed Acute Myeloid Leukemia [NCT00488709]	Phase 4	47 participants (Actual)	Interventional	2003-05-31	Completed
Phase I Study of Weekly Topotecan in Combination With Sorafenib in Treatment of Relapsed Small Cell Lung Cancer [NCT00466232]	Phase 1	16 participants (Actual)	Interventional	2007-04-30	Completed
A Phase I Study of Oral Topotecan in Subjects With Cancer and Impaired Renal Function [NCT00483860]	Phase 1	59 participants (Actual)	Interventional	2007-06-20	Completed
A Phase I Study of a Novel Chemotherapeutic Regimen: Topotecan, Ifosfamide and Carboplatin (TIC) in Children and Young Adults With Solid Tumors-- A Limited Multi-Institution Study [NCT00502892]	Phase 1	2 participants (Actual)	Interventional	2004-08-31	Completed
A Phase I, Open-Label, Study of the Safety and Tolerability of KU-0059436 and Topotecan in the Treatment of Patients With Advanced Solid Tumours [NCT00516438]	Phase 1	48 participants (Anticipated)	Interventional	2007-07-31	Completed
A Phase II Trial of Weekly Topotecan As Consolidation Therapy in Ovarian Cancer Patients After Initial Chemotherapy [NCT00194935]	Phase 2	32 participants	Interventional	2003-02-28	Terminated
Phase I Study of Concurrent Radiotherapy With Weekly Topotecan for Primary Treatment of Inoperable Localized Non-small Cell Lung Cancer (NSCLC) (Stage I to IIIA) [NCT00322751]	Phase 1	10 participants (Anticipated)	Interventional	2006-04-30	Completed
RESILIENT: A Randomized, Open Label Phase 3 Study of Irinotecan Liposome Injection (ONIVYDE®) Versus Topotecan in Patients With Small Cell Lung Cancer Who Have Progressed on or After Platinum-based First-Line Therapy [NCT03088813]	Phase 3	491 participants (Actual)	Interventional	2018-04-25	Completed
A Phase I Trial of PS-341 in Combination With Topotecan in Advanced Solid Tumor Malignancies [NCT00541359]	Phase 1	54 participants (Actual)	Interventional	2004-01-31	Completed
A Phase 3, Multicenter, Open-Label, Randomized Study of Nemvaleukin Alfa in Combination With Pembrolizumab Versus Investigator's Choice Chemotherapy in Patients With Platinum-Resistant Epithelial Ovarian, Fallopian Tube, or Primary Peritoneal Cancer (ARTI [NCT05092360]	Phase 3	376 participants (Anticipated)	Interventional	2022-01-10	Recruiting
Randomized Phase III Trial on Trabectedin (ET-743) vs Clinician's Choice Chemotherapy in Recurrent Ovarian, Primary Peritoneal or Fallopian Tube Cancers of BRCA Mutated or BRCAness Phenotype Patients [NCT02903004]	Phase 3	242 participants (Actual)	Interventional	2016-04-11	Completed
A Phase I/II Study of Pazopanib and Weekly Topotecan in Patients With Platinum-resistant or Intermediate-sensitive Recurrent Ovarian Cancer [NCT01600573]	Phase 1/Phase 2	68 participants (Anticipated)	Interventional	2012-05-31	Recruiting
A Phase II Trial of Paclitaxel and Topotecan With Filgrastim in Patients With Recurrent or Refractory Glioblastoma Multiforme or Anaplastic Astrocytoma [NCT00002814]	Phase 2	20 participants (Actual)	Interventional	1996-08-31	Completed
A Phase I/II Study to Determine the Maximum Tolerated Doses of Oral Topotecan, Carboplatin and Paclitaxel Administered Every 21 Days to Patients With Epithelial Ovarian Cancer Stages IIb, IIc, III and IV [NCT00003732]	Phase 2	80 participants (Anticipated)	Interventional	1998-09-30	Completed
A Randomized Study of Purged Versus Unpurged Peripheral Blood Stem Cell Transplant Following Dose Intensive Induction Therapy for High Risk Neuroblastoma [NCT00004188]	Phase 3	495 participants (Actual)	Interventional	2001-02-28	Completed
A Phase 1B, Open-Label, Dose Escalation Study Evaluating the Safety of BSI-201 in Combination With Chemotherapeutic Regimens in Subjects With Advanced Solid Tumors [NCT00422682]	Phase 1	136 participants (Actual)	Interventional	2007-01-31	Completed
GSK - Doublet: A Phase I Study of Pegylated Liposomal Doxorubicin (Doxil) and Weekly Intravenous Topotecan in Patients With Advanced Solid Tumors [NCT00252889]	Phase 1	20 participants (Actual)	Interventional	2004-05-31	Completed
A Phase I Study of Adjuvant Topotecan and Cisplatin With Concurrent Radiation Therapy for Advanced Cervical Cancer [NCT00287911]	Phase 1	18 participants (Actual)	Interventional	2005-02-28	Completed
The Use Of Weekly Topotecan As Second Line Therapy In Small Cell Lung Cancer [NCT00087048]	Phase 2	1 participants (Actual)	Interventional	2004-04-30	Terminated(stopped due to Slow accrual)
A Phase II Study Of Higher Dose Weekly Topotecan In The Treatment Of Patients With Extensive Stage Small-Cell Lung Cancer [NCT00294190]	Phase 2	38 participants (Actual)	Interventional	2006-02-28	Completed
A Phase I Trial of the Dual Kinase Inhibitor GW572016 in Combination With Topotecan in Patients With Advanced Solid Malignancies [NCT00295243]	Phase 1	25 participants (Anticipated)	Interventional	2004-09-30	Completed
Topotecan-Monotherapy Vs. Topotecan + Etoposide Vs. Topotecan + Gemcitabine in Therapy in Patients With Recurrent Ovarian Cancer [NCT00312988]	Phase 3	450 participants	Interventional	2000-01-31	Completed
A Phase 3 Trial of Balstilimab Versus Investigator Choice Chemotherapy in Patients With Recurrent Cervical Cancer After Platinum-Based Chemotherapy (BRAVA) [NCT04943627]	Phase 3	0 participants (Actual)	Interventional	2021-08-02	Withdrawn(stopped due to Strategic Business Decision)
Phase 2 Study of Weekly Topotecan With Docetaxel for Recurrent Small Cell Lung Cancer [NCT00315211]	Phase 2	7 participants (Actual)	Interventional	2004-11-30	Terminated(stopped due to Slow Accrual)
An Open-Label, Multicentre, Randomised, Phase III Study Comparing Topotecan/Cisplatin and Topotecan/Etoposide Versus Etoposide/Cisplatin as Treatment for Chemotherapy-naive Patients With Extensive Disease-Small Cell Lung Cancer [NCT00320359]	Phase 3	700 participants (Actual)	Interventional	2002-08-31	Completed
A Phase I Study of Adjuvant Topotecan and Cisplatin With Concurrent Radiation Therapy for Advanced Cervical Cancer [NCT00320983]	Phase 1	11 participants (Actual)	Interventional	2002-03-31	Completed
A Phase III Randomized Trial of Adding Vincristine-Topotecan-Cyclophosphamide to Standard Chemotherapy in Initial Treatment of Non-Metastatic Ewing Sarcoma [NCT00334867]	Phase 3	0 participants (Actual)	Interventional	2005-12-31	Withdrawn(stopped due to withdrawn)
Weekly Administration of Topotecan in Combination With Gemcitabine in Patients With Platinum-resistant Ovarian Cancer [NCT00429559]	Phase 1/Phase 2	31 participants (Actual)	Interventional	2006-06-30	Completed
Neuroblastoma Protocol 2005: Therapy for Children With Advanced Stage High-Risk Neuroblastoma [NCT00135135]	Phase 2	23 participants (Actual)	Interventional	2005-08-31	Completed
A Phase I/II Study of Topotecan With G-CSF and Radiation Therapy in Children With Malignant Intrinsic Pontine Brainstem Gliomas of Childhood [NCT00107471]	Phase 1/Phase 2	7 participants (Actual)	Interventional	2005-10-31	Terminated(stopped due to The unpromising experience of the French group with topotecan given at a dosage of 0.4 mg/m2/day over 30 mins w/in 1 hr of radiation (Cancer 2005; 104: 2792).)
A Phase I Pharmacokinetic Optimal Dosing Study of Intraventricular Topotecan for Children With Neoplastic Meningitis [NCT00112619]	Phase 1	19 participants (Actual)	Interventional	2005-08-31	Terminated(stopped due to Slow accrual and company withdrawing support to supply the drug)
Toxicity and Activity of Periocular Topotecan in Children With Retinoblastoma [NCT00460876]	Phase 1	5 participants (Actual)	Interventional	2007-03-31	Completed
A Phase I Dose Escalation Trial of Clofarabine in Addition to Topotecan, Vinorelbine, Thiotepa, and Dexamethasone in Pediatric Patients With Relapsed or Refractory Acute Leukemia [NCT00462787]	Phase 1	23 participants (Actual)	Interventional	2007-04-30	Completed
Salvage Treatment With Topotecan in Patients With Irinotecan-Refractory Small Cell Lung Cancer [NCT00502762]	Phase 2	0 participants	Interventional	2004-09-30	Active, not recruiting
A Phase 3, Randomized, Open-Label Study of Combination Therapy With Avutometinib Plus Defactinib Versus Investigator's Choice of Treatment in Patients With Recurrent Low-Grade Serous Ovarian Cancer (LGSOC) (RAMP 301) [NCT06072781]	Phase 3	270 participants (Anticipated)	Interventional	2023-12-31	Recruiting
A Phase II Study of Intrathecal Topotecan (NSC #609699) in Patients With Refractory Meningeal Malignancies [NCT00005811]	Phase 2	77 participants (Actual)	Interventional	2000-04-30	Completed
Phase II Trial of Topotecan, Cisplatin and Bevacizumab for Recurrent/Persistent Cervical Cancer [NCT00548418]	Phase 2	27 participants (Actual)	Interventional	2007-02-28	Completed
A Phase Ib Open Label Study of the Safety and Tolerability of ME-344 Given in Combination With Topotecan (Hycamtin®) in Patients With Solid Tumors [NCT02100007]	Phase 1/Phase 2	46 participants (Actual)	Interventional	2014-04-30	Terminated(stopped due to lack of efficacy)
Continuous Infusion Topotecan With Erlotinib for Topotecan Pretreated Ovarian Cancer: Tumor Features and Phase II/Pharmacokinetic Evaluation [NCT01003938]	Phase 2	6 participants (Actual)	Interventional	2009-08-31	Terminated(stopped due to due to administrative issue and financial sponsor decision to suspend ovarian cancer studies)
Phase I and Pharmacokinetic Study of the Farnesyl Transferase Inhibitor, R115777, in Combination With Topotecan [NCT00005990]	Phase 1	0 participants	Interventional	2000-08-31	Completed
Trial Protocol for the Treatment of Children With High Risk Neuroblastoma (NB2004-HR) [NCT00526318]		360 participants (Anticipated)	Interventional	2007-01-31	Recruiting
Phase I/II Open-Label, Dose Escalation Study To Determine The Maximum Tolerated Dose And To Evaluate The Safety Profile of Lenalidomide (Revlimid®) With Topotecan In Subjects With Advanced Ovarian and Primary Peritoneal Carcinoma [NCT00179712]	Phase 1/Phase 2	60 participants	Interventional	2005-04-30	Completed
A Phase I Study of Weekly Topotecan in Combination With Carboplatin in Two Different Schedules for Patients With Refractory and/or Advanced Solid Tumors [NCT00193583]	Phase 1	18 participants	Interventional	2003-05-31	Completed
Phase II Trial- Weekly Taxotere and Topotecan for Recurrent Ovarian, Primary Peritoneal, Endometrial and Uterine Cancers [NCT00231855]	Phase 2	31 participants	Interventional	2004-11-30	Completed
A Phase 1/2 Trial of ABT-888, an Inhibitor of Poly(ADP-ribose) Polymerase (PARP), and Topotecan (TPT) in Patients With Solid Tumors (Phase 1) and Relapsed Ovarian Cancer or Primary Peritoneal Cancer (Phase 2) After Prior Platinum Containing First-Line Che [NCT01012817]	Phase 1/Phase 2	88 participants (Actual)	Interventional	2009-11-03	Active, not recruiting
Phase I Study of Intrathecal Topotecan [NCT00001333]	Phase 1	30 participants	Interventional	1993-02-28	Completed
Study of Topoisomerase Inhibition in the Treatment of Acute Leukemia [NCT00100477]	Phase 2	10 participants (Actual)	Interventional	1998-08-31	Completed
An Open-Label, Multicenter, Randomized, Phase II Study of Topotecan/Paclitaxel vs Etoposide/Cisplatin as First-Line Therapy for Patients With Extensive Disease Small Cell Lung Cancer [NCT00006374]	Phase 2	0 participants (Actual)	Interventional	1999-10-31	Withdrawn(stopped due to Slow accrual)
A Phase I/II Combination Study of Topotecan, Fludarabine, Cytosine Arabinoside and G-CSF (T-FLAG) Induction Therapy in Patients With Poor Prognosis AML, MDS and Relapsed/Refractory ALL Followed by Maintenance of Either PBSC Transplant or 13 Cis-Retinoic A [NCT00003619]	Phase 1/Phase 2	0 participants	Interventional	1998-02-28	Completed
Phase II Trial of Salvage Chemotherapy With Temozolomide in Combination With Topotecan for Primary CNS Lymphoma [NCT00109798]		0 participants (Actual)	Interventional	2005-03-31	Withdrawn(stopped due to Sub-Investigator reloacted to another institution)
A Pilot Trial of Oral Topotecan for the Treatment of Refractory Advanced Solid Neoplasms Expressing HIF-1 Alpha [NCT00117013]	Phase 1	16 participants (Actual)	Interventional	2005-06-28	Completed
A Prospective Matched Cohort Study of Intravitreal Topotecan in the Repair of Rhegmatogenous Retinal Detachment With Proliferative Vitreoretinopathy [NCT05523869]	Phase 2	50 participants (Anticipated)	Interventional	2023-02-23	Recruiting
An International Multicenter Phase II Randomised Trial Evaluating and Comparing Two Intensification Treatment Strategies for Metastatic Neuroblastoma Patients With a Poor Response to Induction Chemotherapy [NCT03165292]	Phase 2	34 participants (Actual)	Interventional	2018-10-01	Terminated(stopped due to The Sponsor has been notified of an interruption in the international supply, and there is a possibility that 131I-mlBG would be unavailable to patients randomised to arm A of the trial)
A Phase II Study of Paclitaxel and Topotecan With Filgrastim-SD/01 Support For Patients With Relapsed and Refractory Aggressive Non-Hodgkin's Lymphoma [NCT00038545]	Phase 2	25 participants (Actual)	Interventional	2001-05-18	Completed
An Open-Label, Multicenter, Randomized, Phase III Study Comparing Oral Topotecan/Cisplatin Versus Etoposide/Cisplatin as Treatment for Chemotherapy-naive Patients With Extensive Disease-Small Cell Lung Cancer. [NCT00043927]	Phase 3	760 participants	Interventional	2001-04-30	Completed
A Phase I Study of UCN-01 in Combination With Topotecan in Patients With Solid Tumors [NCT00045175]	Phase 1	33 participants (Actual)	Interventional	2002-06-30	Completed
A Study to Determine the Bioequivalence of an Oral Formulation of Topotecan Containing the Drug Substance Manufactured by New Process Relative to the Current Study Formulation of Topotecan in Patients With Advanced Solid Tumors [NCT00046111]	Phase 1	1 participants (Actual)	Interventional	2001-09-30	Completed
Phase II Study of Fludarabine, Carboplatin, and Topotecan With Thalidomide for Patients With Relapsed/Refractory or High Risk Acute Myelogenous Leukemia, Chronic Myeloid Leukemia and Advanced Myelodysplastic Syndromes [NCT00053287]	Phase 2	42 participants (Actual)	Interventional	2002-09-30	Completed
An Open-Label, Multicentre, Phase II Study of TVD as Treatment for Children With Stage 4 Neuroblastoma Failing to Respond to First-Line Treatment According to HR-NBL-01/ E-SIOP [Topotecan-Vincristine-Doxorubicin in Children With Stage 4 Neuroblastoma Fail [NCT00392340]	Phase 2	63 participants (Anticipated)	Interventional	2008-03-31	Active, not recruiting
Phase I/II Study of High Dose Topotecan, Mitoxantrone and Thiotepa (TMT) Followed by Autologous Stem Cell Transplant in Patients With Recurrent Platinum Resistant Ovarian Cancer [NCT00003297]	Phase 1/Phase 2	50 participants (Anticipated)	Interventional	1997-12-31	Completed
An Open-Label, Multicentre, Randomised, Phase III Comparator Study of Active Symptom Control Alone or in Combination With Oral Topotecan in Patients With Relapsed Resistant SCLC [NCT00276276]	Phase 3	141 participants	Interventional	2000-11-30	Completed
A Phase II, Open, Randomized Multicenter Trial to Assess the Efficacy and Tolerability of Intravenous ZD9331 Given as Monotherapy (at Two Doses) or in Combination With Topotecan, in Patients With Ovarian Cancer Refractory or Recurrent After Failing Platin [NCT00014690]	Phase 2	0 participants	Interventional	2001-03-31	Completed
Phase II Study of Sequential Topotecan-Carboplatin-Etoposide in Patients With Extensive Stage Small Cell Lung Cancer [NCT00025272]	Phase 2	14 participants (Actual)	Interventional	2001-11-01	Completed
A Phase I Study Of Seven Day Continuous Intrathecal/Intraventricular Infusion Of Topotecan For Patients With Recurrent, Progressive Or Refractory Leptomingeal Disease [NCT00025311]	Phase 1	0 participants	Interventional	2001-05-31	Completed
A Phase 1b Study of the Dual MDMX/MDM2 Inhibitor, ALRN-6924, for the Prevention of Chemotherapy-induced Myelosuppression [NCT04022876]	Phase 1	35 participants (Actual)	Interventional	2019-09-03	Terminated(stopped due to With a favorable safety profile the difference between treatment groups for the primary composite endpoint was not sufficient to generate statistically significant results with the targeted sample size)
A Phase III Study of Cisplatin Plus Topotecan Followed by Paclitaxel Plus Carboplatin Versus Paclitaxel Plus Carboplatin as First Line Chemotherapy in Women With Newly Diagnosed Advanced Epithelial Ovarian Cancer [NCT00028743]	Phase 3	819 participants (Actual)	Interventional	2001-08-31	Completed
Paclitaxel/Topotecan/Etoposide (EtopoTax) Induction Followed by Consolidation Chemoradiotherapy for Limited Stage Small Cell Lung Cancer: A Phase II Study [NCT00033696]	Phase 2	65 participants (Actual)	Interventional	2001-09-30	Completed
N8: Dose-Intensive Chemotherapy Plus Biologics in the Treatment of Neuroblastoma [NCT00040872]	Phase 2	0 participants	Interventional	2000-06-30	Completed
Phase II Study of Dose Attenuated Chemotherapy in Patients With Lung Cancer and Age > 70 and/or Comorbidities [NCT05800587]	Phase 2	280 participants (Anticipated)	Interventional	2023-02-22	Recruiting
An Open-Label, Multicentre, Randomised, Phase III Study Comparing Oral Topotecan to Intravenous Docetaxel in Patients With Pretreated Advanced Non Small Cell Lung Cancer [NCT00049998]	Phase 3	760 participants	Interventional	2001-10-31	Completed
Phase I Study of Oral Topotecan as Consolidation for Patients With Mullerian Origin Tumors (Ovary, Tube, Peritoneum) [NCT00055614]	Phase 1	20 participants (Anticipated)	Interventional	2002-05-31	Completed
Phase II Trial of Oral Topotecan and Intravenous Carboplatin With G-CSF (Filgrastim) Support in Previously Untreated Patients With Extensive Stage Small Cell Lung Cancer [NCT00028925]	Phase 2	27 participants (Actual)	Interventional	2001-11-30	Completed
Phase I Treatment of Adults With Primary Malignant Glioma With Topotecan (NSC #609699) Plus BCNU (NSC #409962) [NCT00002986]	Phase 1	36 participants (Anticipated)	Interventional	1997-02-28	Completed
Phase II Study of Continuous Infusion Carboplatin and Topotecan in the Treamtment of Relapsed Acute Myelogenous Leukemia (AML) [NCT00003255]	Phase 2	38 participants (Actual)	Interventional	1999-11-30	Completed
A Pilot Induction Regimen Incorporating Topotecan for Treatment of Newly Diagnosed High Risk Neuroblastoma [NCT00070200]	Phase 1	31 participants (Actual)	Interventional	2004-03-31	Completed
A Phase II Study of UCN-01 in Combination With Topotecan in Patients With Advanced Ovarian Cancer [NCT00072267]	Phase 2	0 participants	Interventional	2004-01-31	Completed
A Dose Finding Phase I Trial of the Combination of Topotecan and PS-341, a Novel Proteasome Inhibitor, in Advanced Malignancies [NCT00068484]	Phase 1	25 participants (Actual)	Interventional	2003-07-31	Completed
An Open-Label, Multicenter, Randomized, Phase III Study Comparing Oral Topotecan/Cisplatin Versus Etoposide/Cisplatin As Treatment For Chemotherapy-Naive Patients With Extensive Disease - Small Cell Lung [NCT00041015]	Phase 3	4 participants (Actual)	Interventional	2001-09-30	Completed
A Phase I Study of Oral Topotecan as a Radiosensitizing Agent in Patients With Rectal Carcinoma [NCT00215956]	Phase 1	31 participants (Actual)	Interventional	2001-11-30	Completed
Phase II Trial for the Treatment of Recurrent or Persistent Platinum-Refractory Ovarian, Fallopian Tube, or Primary Peritoneal Cancer With Gemcitabine and Topotecan [NCT00217555]	Phase 2	0 participants	Interventional	2002-07-31	Completed
a Multicenter Clinical Trial for the Treatment of Children and Adolescents With Soft Tissue Sarcoma Stage 4 [NCT00130858]	Phase 2	90 participants (Anticipated)	Interventional	2005-01-31	Completed
Topotecan Weekly Versus Topotecan Day 1-5 in Patient With Platin-resistant Ovarian Cancer [NCT00170677]	Phase 2	194 participants (Actual)	Interventional	2005-09-30	Completed
A Phase II Study of a Three-Day Schedule of Topotecan Plus Paclitaxel and Carboplatin on Day Three in the Initial Treatment of Advanced Ovarian and Primary Peritoneal Carcinoma [NCT00193297]	Phase 2	50 participants	Interventional	2002-02-28	Completed
A Phase I Study of Topotecan in Combination With Docetaxel in Patients With Refractory and/or Advanced Solid Tumors [NCT00193570]	Phase 1	20 participants	Interventional	2002-02-28	Completed
Phase II Evaluation of Three-Day Topotecan (NSC 609699) in Recurrent Platinum-Sensitive Ovarian or Primary Peritoneal Cancer [NCT00005029]	Phase 2	0 participants	Interventional	2000-02-29	Terminated
MC1365, A Randomized Phase II Trial of a Genetically Engineered NIS-Expressing Strain of Measles Virus Versus Investigator's Choice Chemotherapy for Patients With Platinum-Resistant Ovarian, Fallopian, or Peritoneal Cancer [NCT02364713]	Phase 2	66 participants (Anticipated)	Interventional	2015-03-13	Active, not recruiting
Pilot Trial of Intratumorally-Administered Topotecan Using Convection-Enhanced Delivery (CED) in Patients With Suspected Recurrent/Progressive World Health Organization (WHO) Grade III or IV (High Grade) Glioma Undergoing Stereotactic Biopsy (IND 117,240) [NCT03193463]	Early Phase 1	0 participants (Actual)	Interventional	2017-11-03	Withdrawn(stopped due to PI left institution)
A Phase I Trial of Oral Metronomic Topotecan in Combination With Oral Pazopanib Utilizing a Daily Dosing Schedule to Treat Recurrent or Persistent Gynecologic Tumors [NCT00800345]	Phase 1	33 participants (Actual)	Interventional	2009-04-30	Completed
Chronic Convection Enhanced Delivery of Topotecan for Recurrent High Grade Gliomas [NCT03154996]	Phase 1	5 participants (Actual)	Interventional	2018-01-18	Completed
Phase I/II Study in Patients With Small Cell Lung Cancer (SCLC) of Veliparib in Combination With Topotecan [NCT03227016]	Phase 1	30 participants (Anticipated)	Interventional	2016-10-31	Recruiting
A Phase III Randomized Trial of Adding Vincristine-Topotecan-Cyclophosphamide to Standard Chemotherapy in Initial Treatment of Non-Metastatic Ewing Sarcoma [NCT01231906]	Phase 3	642 participants (Actual)	Interventional	2010-11-22	Active, not recruiting
A Study to Determine the Bioequivalence of an Oral Formulation of Topotecan Containing the Drug Substance Manufactured by New Process Relative to the Current Study Formulation of Topotecan in Patients With Advanced Solid Tumors (4C) [NCT00259935]	Phase 1	107 participants (Actual)	Interventional	2004-10-04	Completed
A Pilot Trial of Intraparenchymally-Administered Topotecan Using Convection-Enhanced Delivery (CED) in Patients With Suspected Recurrent/Progressive WHO Grade III or IV (High Grade) Glioma Requiring Stereotactic Biopsy [NCT02278510]	Early Phase 1	3 participants (Actual)	Interventional	2014-12-09	Completed
Clinical Benefit of Topoisomerase Downregulation: A Phase I Pilot Study [NCT00250094]	Phase 1	15 participants (Actual)	Interventional	2004-05-31	Completed
Phase I Study of Weekly Topotecan in Women With Progressive or Recurrent Ovarian Cancer and a Poor Performance Status [NCT00287859]	Phase 1	5 participants (Actual)	Interventional	2004-08-31	Terminated(stopped due to Withdrawn due to low accrual)
A Pilot Study of Weekly IV Topotecan and Cisplatin With Concurrent Pelvic Radiation in the Treatment of Stages IB2 - IVA Cervical Carcinoma [NCT00257816]	Phase 2	12 participants (Actual)	Interventional	2004-01-31	Completed
A Phase I Study of Topotecan in Combination With Pemetrexed in Patients With Advanced Malignancies [NCT00315861]	Phase 1	15 participants (Anticipated)	Interventional	2006-03-31	Completed
A Phase I Study of Topotecan in Combination With Vinorelbine in Recurrent Lung Cancer [NCT00287963]	Phase 1	18 participants (Actual)	Interventional	2004-02-29	Completed
A Phase 1b, Multicenter Study to Determine the Dose, Safety, Efficacy and Pharmacokinetics of TRK-950 When Used in Combinations With Selected Anti-Cancer Treatment Regimens in Patients With Selected Advanced Solid Tumors [NCT03872947]	Phase 1	169 participants (Anticipated)	Interventional	2019-04-26	Recruiting
Cisplatin Induction Followed by Paclitaxel Consolidation for the Treatment of Stage III and IV Epithelial Ovarian Cancer and Primary Peritoneal Cancer With In Vitro Correlates of Response [NCT00314678]	Phase 2	40 participants (Anticipated)	Interventional	2005-09-30	Completed
A Phase IIb, Randomized, Open, Parallel-Group, Multi-Center Trial to Assess the Efficacy and Safety of Belotecan(CamtoBell Inj.) or Topotecan in Patients With Relapsed Small Cell Lung Cancer [NCT01497873]	Phase 2	164 participants (Actual)	Interventional	2010-09-30	Completed
A Phase Ⅱb, Randomized, Open, Parallel-Group, Multi-Center Trial to Assess the Efficacy and Safety of Belotecan(CamtoBell Inj.) or Topotecan in Patients With Recurrent or Refractory Ovarian Cancer [NCT01630018]	Phase 2	141 participants (Actual)	Interventional	2011-01-31	Completed
An Open Label, Multicenter, Randomized, Phase III Comparator Study of Oral Topotecan Versus Intravenous Topotecan for Second Line Therapy in Patients With Small Cell Lung Cancer Who Have Relapsed Greater Than or Equal to 90 Days After Completion of First [NCT00003917]	Phase 3	4 participants (Actual)	Interventional	1999-03-31	Completed
A Phase I Study of ARQ 197 in Combination With IV Topotecan in Advanced Solid Tumors With an Expansion Cohort in Small Cell Lung Cancer [NCT01654965]	Phase 1	17 participants (Actual)	Interventional	2012-07-24	Completed
Veliparib (ABT888) and Topotecan (Hycamtin®) for Patients With Platinum-Resistant or Partially Platinum-Sensitive Relapse of Epithelial Ovarian Cancer With Negative or Unknown BRCA Status [NCT01690598]	Phase 1/Phase 2	22 participants (Actual)	Interventional	2012-11-30	Completed
Phase II Individualized Therapies Selection Study for Patients With Metastatic Colorectal Carcinoma According to the Genomic Expression Profile in Tumor Samples. [NCT01703910]	Phase 2	29 participants (Actual)	Interventional	2012-11-30	Completed
Phase II Trial of Chemotherapy With Temozolomide in Combination With Topotecan for Central Nervous System (CNS) Metastasis of Solid Tumors [NCT01736800]	Phase 2	0 participants (Actual)	Interventional	2007-03-31	Withdrawn(stopped due to No enrollment and PI requested study termination per IRB system.)
A Phase III Randomized Trial Of Paclitaxel And Carboplatin Versus Triplet Or Sequential Doublet Combinations In Patients With Epithelial Ovarian Or Primary Peritoneal Carcinoma [NCT00011986]	Phase 3	4,312 participants (Actual)	Interventional	2001-01-31	Completed
A Phase I Study to Characterize the Pharmacokinetics of 4 mg/m2 Weekly Intravenous Topotecan in Patients With Cancer [NCT00361803]	Phase 1	15 participants (Actual)	Interventional	2006-09-12	Completed
A Phase II Study of UCN-01 in Combination With Topotecan in Patients With SCLC Who Relapsed or Progressed >= 3 Months After Completing First-Line Platinum-Based Chemotherapy [NCT00098956]	Phase 2	19 participants (Actual)	Interventional	2005-01-31	Completed
Phase III Randomized Clinical Trial of Lurbinectedin (PM01183) Versus Pegylated Liposomal Doxorubicin or Topotecan in Patients With Platinum-resistant Ovarian Cancer (CORAIL Trial) [NCT02421588]	Phase 3	442 participants (Actual)	Interventional	2015-05-31	Completed
A Phase 1 Study Using Simvastatin in Combination With Topotecan and Cyclophosphamide in Relapsed and/or Refractory Pediatric Solid and CNS Tumors [NCT02390843]	Phase 1	13 participants (Actual)	Interventional	2015-02-28	Completed
A Two-Part, Randomized Phase III, Double-Blind, Multicenter Trial Assessing The Efficacy And Safety of Pertuzumab In Combination With Standard Chemotherapy Vs. Placebo Plus Standard Chemotherapy In Women With Recurrent Platinum-Resistant Epithelial Ovaria [NCT01684878]	Phase 3	208 participants (Actual)	Interventional	2012-10-22	Completed
New Therapeutic Strategies for Patients With Ewing's Sarcoma Family of Tumors, High Risk Rhabdomyosarcoma, and Neuroblastoma [NCT00001335]	Phase 2	90 participants	Interventional	1993-04-30	Completed
PHASE I STUDY OF TOPOTECAN AND THORACIC RADIATION [NCT00002625]	Phase 1	5 participants (Actual)	Interventional	1995-03-31	Completed
INTENSIVE THERAPY WITH GROWTH FACTOR SUPPORT FOR PATIENTS WITH EWING'S TUMOR METASTATIC AT DIAGNOSIS: A PEDIATRIC ONCOLOGY GROUP PHASE II STUDY [NCT00002643]	Phase 2	130 participants (Actual)	Interventional	1995-04-30	Completed
Phase I Dose Escalation and Expansion Study of Tazemetostat in Combination With Topotecan and Pembrolizumab in Recurrent Small Cell Lung Cancer [NCT05353439]	Phase 1	60 participants (Anticipated)	Interventional	2022-07-27	Recruiting
PHASE I STUDY OF PACLITAXEL COMBINED WITH TOPOTECAN AND CISPLATIN AND G-CSF IN PATIENTS WITH NEWLY DIAGNOSED ADVANCED OVARIAN EPITHELIAL MALIGNANCIES [NCT00002913]	Phase 1	30 participants (Actual)	Interventional	1996-12-31	Completed
An Open-label, Randomized, Phase 3 Study of Nivolumab or Chemotherapy in Subjects With Relapsed Small-cell Lung Cancer After Platinum-based First Line Chemotherapy (CheckMate 331: CHECKpoint Pathway and nivoluMAb Clinical Trial Evaluation 331) [NCT02481830]	Phase 3	569 participants (Actual)	Interventional	2015-09-14	Completed
A Pilot Study of Intra-Ophthalmic Artery Topotecan Infusion for the Treatment of Retinoblastoma [NCT01466855]	Early Phase 1	36 participants (Actual)	Interventional	2011-10-31	Terminated(stopped due to Competing studies)
A Phase II Randomized Trial of Carboplatin and Topotecan; Flavopiridol, Mitoxantrone and Cytosine Arabinoside; and Sirolimus, Mitoxantrone, Etoposide and Cytosine Arabinoside for the Treatment of Adults With Primary Refractory or Initial Relapse of Acute [NCT00634244]	Phase 2	92 participants (Actual)	Interventional	2008-10-31	Completed
A Phase I Study of ABT-888 in Combination With Topotecan Plus Carboplatin for High-Risk Myeloproliferative Disorders and AML Out of Myeloproliferative Disorders [NCT00588991]	Phase 1	12 participants (Actual)	Interventional	2007-11-28	Active, not recruiting
PHASE I STUDY OF INTERFERON ENHANCED INTRAPERITONEAL RADIOIMMUNO-CHEMOTHERAPY FOR OVARIAN CANCER [NCT00002734]	Phase 1	30 participants (Actual)	Interventional	1996-03-31	Completed
Phase I/II Study of Topotecan (SKF 104864) With Recombinant GM-CSF (Sargramostim) Used as a Priming Agent in Advanced Malignancies [NCT00002950]	Phase 1/Phase 2	25 participants (Anticipated)	Interventional	1996-09-26	Completed
Phase I-II Study of Tandem Cycles of High Dose Chemotherapy Followed by Autologous Hematopoietic Stem Cell Support in Women With Persistent, Refractory or Recurrent Advanced (Stage III or IV), Epithelial Ovarian Cancer [NCT00003064]	Phase 1/Phase 2	30 participants (Anticipated)	Interventional	1997-01-31	Active, not recruiting
Randomized Study of Vincristine, Actinomycin-D, and Cyclophosphamide (VAC) Versus VAC Alternating With Vincristine, Topotecan and Cyclophosphamide for Patients With Intermediate Risk Rhabdomyosarcoma [NCT00003958]	Phase 3	702 participants (Actual)	Interventional	2002-09-30	Completed
Treatment for Extrachoroidal or Metastatic Retinoblastoma [NCT00004006]	Phase 2	4 participants (Actual)	Interventional	1997-11-30	Completed
A Phase II Study of Cyclophosphamide Followed by Topotecan in Patients With Refractory or Relapsed Acute Myelogenous Leukemia [NCT00003340]	Phase 2	0 participants	Interventional	1997-11-30	Completed
A Phase I Study of Gemcitabine/Topotecan in Combination in Refractory Ovarian Cancer or Cancer of the Fallopian Tube [NCT00003382]	Phase 1	0 participants	Interventional	1998-05-31	Terminated
Phase I/IIA Study of Sequential Ifosfamide and Topotecan in Patients With Small Cell Lung Cancer [NCT00004186]	Phase 1/Phase 2	55 participants (Anticipated)	Interventional	1996-12-31	Completed
A Phase I Feasibility Trial of Carboplatin and Topotecan Followed by Carboplatin and Paclitaxel (Sequential Doublets) in Patients With Previously Untreated Epithelial Ovarian Carcinoma and Primary Peritoneal Carcinoma [NCT00005026]	Phase 1	0 participants	Interventional	2000-02-29	Completed
A Randomised Phase IIb Trial of Bevacizumab Added to Temozolomide ± Irinotecan for Children With Refractory/Relapsed Neuroblastoma - BEACON-Neuroblastoma Trial [NCT02308527]	Phase 2	225 participants (Actual)	Interventional	2013-07-31	Active, not recruiting
Risk-Adapted Therapy for Young Children With Embryonal Brain Tumors, Choroid Plexus Carcinoma, High Grade Glioma or Ependymoma [NCT00602667]	Phase 2	293 participants (Actual)	Interventional	2007-12-17	Active, not recruiting
Phase 1 Study of 9-ING-41, a Glycogen Synthase Kinase 3 Beta (GSK 3β) Inhibitor, as a Single Agent or With Irinotecan, Irinotecan Plus Temozolomide, or With Cyclophosphamide Plus Topotecan in Pediatric Patients With Refractory Malignancies. [NCT04239092]	Phase 1	68 participants (Anticipated)	Interventional	2020-06-05	Active, not recruiting
Topotecan Plus Apatinib Versus Topotecan Alone as Second-line Therapy in Small-cell Lung Cancer [NCT02980809]	Phase 2	60 participants (Anticipated)	Interventional	2017-03-31	Not yet recruiting
Evaluation of the Addition of N-Acetylcysteine to Topotecan in the Tumor Microenvironment of Persistent or Recurrent High Grade Endometrioid or Serous Ovarian Carcinoma [NCT02569957]	Phase 2	1 participants (Actual)	Interventional	2015-10-02	Terminated(stopped due to The trial was halted prematurely due to slow accrual.)
Phase II Study of Weekly Topotecan With Bevacizumab in Platinum Resistant Recurrent Ovarian, Fallopian Tube and Primary Peritoneal Cancers [NCT00343044]	Phase 2	40 participants (Actual)	Interventional	2006-06-30	Completed
Pilot Study of High-Dose Chemotherapy With Busulfan, Melphalan, and Topotecan Followed by Autologous Hematopoietic Stem Cell Transplant in Advanced Stage and Recurrent Tumors [NCT00638898]	Phase 1	25 participants (Actual)	Interventional	2007-02-26	Active, not recruiting
A Phase I/II, Multicenter, Open-Label, Multi-Arm Study Evaluating the Safety, Tolerability, Pharmacokinetics, and Preliminary Activity of Idasanutlin in Combination With Either Chemotherapy or Venetoclax in the Treatment of Pediatric and Young Adult Patie [NCT04029688]	Phase 1/Phase 2	183 participants (Anticipated)	Interventional	2020-01-27	Recruiting
A Phase 3, Randomized, Open-Label, Comparative Bridging Study of CAELYX® Versus Topotecan HCl in Subjects With Epithelial Ovarian Carcinoma Following Failure of First-Line, Platinum-Based Chemotherapy [NCT01840943]	Phase 3	32 participants (Actual)	Interventional	2013-06-30	Terminated(stopped due to the study was terminated due to medication supply issue from current manufacturer)
Phase I Trial of Sequential Topotecan(NSC 609699)and Etoposide for Patients With Relapsed, Refractory,or High Risk Acute Myeloid or Lymphoid Leukemia [NCT00002588]	Phase 1	30 participants (Actual)	Interventional	1994-08-31	Completed
A Phase I Study of High Dose Topotecan With Filgrastim and Peripheral Blood Stem Cell Support for Patients With Refractory Malignancies [NCT00002948]	Phase 1	0 participants	Interventional	1996-10-31	Terminated
An Open, Comparative Phase II Study of Immediate Versus Delayed Treatment With Topotecan HCl Given as a Continuous 21-Day Infusion Every 28 Days to Patients With AIDS-Related Progressive Multifocal Leukoencephalopathy [NCT00002395]	Phase 2	54 participants	Interventional		Completed
Myeloablative Chemotherapy With Bone Marrow Rescue For Rare Poor-Prognosis Cancers [NCT00002515]	Phase 2	0 participants	Interventional	1992-10-31	Completed
A PHASE I STUDY OF PROLONGED LOW-DOSE TOPOTECAN INFUSION COMBINED WITH PACLITAXEL (TAXOL) [NCT00002587]	Phase 1	20 participants (Actual)	Interventional	1994-09-30	Completed
A Phase I Study of Thiotepa in Combination With Carboplatin and Topotecan With Peripheral Blood Progenitor Cell Support for the Treatment of Children With Recurrent or Refractory Solid Tumors. [NCT00003194]	Phase 1	24 participants (Anticipated)	Interventional	1997-07-31	Terminated(stopped due to Study enrollment did not meet expected goals)
A Phase II Trial Using Multiple Cycles of High Dose Sequential Carboplatin, Paclitaxel and Topotecan With Peripheral Blood Stem Cell (PBSC) Support as Initial Chemotherapy in Patients With Suboptimally Debulked Stage III or IV Ovarian, Fallopian Tube or P [NCT00003944]	Phase 2	3 participants (Actual)	Interventional	1998-08-31	Completed
Topotecan/Paclitaxel Induction Followed by Consolidation Chemoradiotherapy for Limited Stage Small Cell Lung Cancer: A Phase II Study [NCT00003812]	Phase 2	75 participants (Actual)	Interventional	1999-03-31	Completed
A Phase I/II Study of Intensive-Dose Etoposide, Topotecan and Carboplatin (ETC) Followed by Autologous Stem Cell Rescue in Chemosensitive Ovarian Cancer Patients With Either Minimal Residual Disease or at First Relapse [NCT00005612]	Phase 1/Phase 2	3 participants (Actual)	Interventional	1999-08-31	Terminated(stopped due to Low accrual)
A Study of Intensive-Dose Melphalan, Topotecan, and VP-16 Phosphate (MTV) Followed by Autologous Stem Cell Rescue in Patients With Multiple Myeloma [NCT00005792]	Phase 1	131 participants (Actual)	Interventional	1998-06-02	Completed
A Phase II Trial of High Dose Paclitaxel, Carboplatin and Topotecan With Peripheral Blood Stem Cell Support in Extensive Stage Small Cell Cancer [NCT00003943]	Phase 2	3 participants (Actual)	Interventional	1998-09-30	Completed
A Phase I Study of Sequential Prolonged Oral Topotecan (IND# 58,131) and Prolonged Oral Etoposide as Second Line Therapy in Ovarian, Peritoneal or Tubal Carcinoma [NCT00003967]	Phase 1	24 participants (Anticipated)	Interventional	1999-09-30	Completed
A Phase II Study of Sequential Carboplatin, Paclitaxel and Hycamtin in Patients With Previously Untreated Advanced Ovarian Cancer [NCT00003733]	Phase 2	40 participants (Anticipated)	Interventional	1997-12-31	Active, not recruiting
A Phase I Study of Low Dose Continuous Infusion Topotecan in Combination With 5-Fluorouracil and Leucovorin for Advanced Malignancies [NCT00003331]	Phase 1	30 participants (Anticipated)	Interventional	1998-01-31	Completed
Phase I Study of Fludarabine, Carboplatin, and Topotecan for Patients With Relapsed/Refractory Acute Leukemia and Advanced Myelodysplastic Syndromes [NCT00005593]	Phase 1	31 participants (Actual)	Interventional	1998-09-30	Completed
A Protocol For Nonmetastatic Rhabdomyosarcoma [RMS-2005] [NCT00379457]	Phase 3	600 participants (Anticipated)	Interventional	2006-06-30	Recruiting
A PHASE I STUDY OF PROLONGED LOW-DOSE TOPOTECAN INFUSION COMBINED WITH CHEST IRRADIATION [NCT00002537]	Phase 1	20 participants (Actual)	Interventional	1993-09-30	Completed
PHASE I STUDY OF CONTINUOUS INFUSION CARBOPLATIN AND TOPOTECAN IN THE TREATMENT OF RELAPSED ACUTE LEUKEMIA AND BLAST CRISIS CHRONIC MYELOGENOUS LEUKEMIA [NCT00002693]	Phase 1	0 participants	Interventional	1995-10-31	Completed
TOPOTECAN FOR CHILDREN WITH REFRACTORY LEUKEMIA, A PEDIATRIC ONCOLOGY GROUP PHASE I COOPERATIVE AGREEMENT STUDY [NCT00002705]	Phase 1	3 participants (Actual)	Interventional	1996-04-30	Completed
A Phase II, Open-label, Single-arm Study of Berzosertib (M6620) in Combination With Topotecan in Participants With Relapsed Platinum-resistant Small-Cell Lung Cancer (DDRiver SCLC 250) [NCT04768296]	Phase 2	76 participants (Actual)	Interventional	2021-03-29	Completed
A Randomized Phase III Study of Cisplatin Versus Cisplatin Plus Topotecan Versus MVAC in Stage IVB, Recurrent or Persistent Squamous Cell Carcinoma of the Cervix [NCT00003945]	Phase 3	400 participants (Anticipated)	Interventional	1999-06-30	Completed
A Randomized Phase II Trial of Oral Topotecan Given Twice a Day for 5 Days or Once a Day for 10 Days to Patients With Myelodysplastic Syndromes (MDS) [NCT00003675]	Phase 2	100 participants (Actual)	Interventional	1999-03-31	Completed
Phase II Trial of Paclitaxel, Carboplatin and Topotecan With G-CSF in Untreated Patients With Extensive Small Cell Lung Cancer [NCT00004137]	Phase 2	88 participants (Actual)	Interventional	1999-10-31	Completed
A Phase II Trial Using Multiple Cycles of High Dose Sequential Carboplatin, Paclitaxel and Topotecan With Peripheral Blood Stem Cell (PBSC) Support as Initial Chemotherapy in Patients With Optimally Debulked Stage III Ovarian and Primary Peritoneal Carcin [NCT00004221]	Phase 2	12 participants (Actual)	Interventional	1999-11-30	Terminated
A Phase II Study of Oral Topotecan in Children With Relapsed Acute Leukemia [NCT00003735]	Phase 2	11 participants (Actual)	Interventional	1998-12-31	Completed
A Phase I/II Study of Induction Chemotherapy With Daunorubicin, Cytarabine, Topotecan and Etoposide (DATE) for De Novo AML: In the Treatment of Young Patients Ages 16-59 [NCT00005793]	Phase 1/Phase 2	41 participants (Actual)	Interventional	1999-07-31	Completed
A Phase 1 Study of Aurora Kinase A Inhibitor LY3295668 Erbumine as a Single Agent and in Combination in Patients With Relapsed/Refractory Neuroblastoma [NCT04106219]	Phase 1	71 participants (Anticipated)	Interventional	2020-06-11	Active, not recruiting
A Safety Pilot Study of High Risk Induction Chemotherapy for Neuroblastoma Without Prophylactic Administration of Myeloid Growth Factors [NCT02786719]		13 participants (Actual)	Interventional	2016-06-30	Completed
Randomized Phase II Study of Single Agent OSI-906, an Oral, Small Molecule, Tyrosine Kinase Inhibitor (TKI) of the Insulin Growth Factor-1 Receptor (IGF-1R) Versus Topotecan for the Treatment of Patients With Relapsed Small Cell Lung Cancer (SCLC) [NCT01533181]	Phase 2	44 participants (Actual)	Interventional	2012-02-29	Completed
A Phase I/II Trial of Topotecan With VX-970 (M6620), an ATR Kinase Inhibitor in Small Cell Cancers [NCT02487095]	Phase 1/Phase 2	62 participants (Actual)	Interventional	2015-07-30	Active, not recruiting
A Randomized Non-comparative Phase II Study of Anti-PDL1 ATEZOLIZUMAB (MPDL3280A) or Chemotherapy as Second-line Therapy in Patients With Small Cell Lung Cancer (SCLC) [NCT03059667]	Phase 2	73 participants (Actual)	Interventional	2017-03-13	Completed
Combination Chemotherapy Followed by Stem Cell Transplant and Isotretinoin in Treating Young Patients With High-risk Neuroblastoma [NCT03042429]	Phase 3	360 participants (Actual)	Interventional	2007-01-01	Completed
Phase I Sustained-Release Topotecan Episcleral Plaque (Chemoplaque) for Retinoblastoma [NCT04428879]	Phase 1	30 participants (Anticipated)	Interventional	2020-06-16	Recruiting
Phase I/II Study of Combined Treatment With Amifostine (Ethyol) and Topotecan (Hycamtin MS) in Patients With Myelodysplastic Syndrome [NCT00003415]	Phase 1/Phase 2	26 participants (Anticipated)	Interventional	1998-09-30	Completed
A Phase II Study of Continuous 21 Day Infusion of Topotecan (NSC # 609699) in Children With Relapsed Solid Tumors [NCT00003745]	Phase 2	125 participants (Actual)	Interventional	1999-05-31	Completed
A Pilot Study Of Hycamtin (Topotecan) And Thalomid (Thalidomide) In Patients With Recurrent Malignant Gliomas [NCT00014443]	Phase 2	5 participants (Anticipated)	Interventional	2000-08-31	Terminated(stopped due to Poor enrollment)
Phase I/II Study of Oral Topotecan and Intravenous Paclitaxel in Patients With Advanced Non-Small Cell Lung Cancer (Phases I and II) and Other Advanced Solid Tumors (Phase I Only) [NCT00004979]	Phase 1/Phase 2	0 participants	Interventional		Completed
A Phase II Randomized Trial of Immunologic and Chemotherapeutic Agents for Treatment of Patients With Relapsed or Refractory Acute Myelogenous Leukemia [NCT00005962]	Phase 2	0 participants	Interventional	2000-10-04	Completed
A Phase II Trial of Topotecan and Carboplatin in the First-Line Treatment of Patients With Extensive Stage Small Cell Lung Cancer [NCT00305942]	Phase 2	61 participants (Actual)	Interventional	2006-03-31	Completed
Phase III Randomized Clinical Trial of Lurbinectedin (PM01183)/Doxorubicin Versus Cyclophosphamide, Doxorubicin and Vincristine (CAV) or Topotecan as Treatment in Patients With Small-Cell Lung Cancer (SCLC) Who Failed One Prior Platinum-containing Line (A [NCT02566993]	Phase 3	613 participants (Actual)	Interventional	2016-08-30	Completed
Safety Run-In and Phase II Trial of M7824 and Topotecan or Temozolomide in Relapsed Small Cell Cancers [NCT03554473]	Phase 1/Phase 2	67 participants (Anticipated)	Interventional	2018-09-11	Recruiting
A Randomized Phase III Trial of Cisplatin Plus Paclitaxel With and Without NCI-Supplied Bevacizumab (NSC #704865) Versus the Non-platinum Doublet, Topotecan Plus Paclitaxel, With and Without NCI-Supplied Bevacizumab, in Stage IVB, Recurrent or Persistent [NCT00803062]	Phase 3	452 participants (Actual)	Interventional	2009-04-30	Completed
Randomized Phase II Trial of Topotecan Plus M6620 (VX-970, Berzosertib) vs. Topotecan Alone in Patients With Relapsed Small-Cell Lung Cancer [NCT03896503]	Phase 2	98 participants (Anticipated)	Interventional	2019-08-23	Active, not recruiting
Neuroblastoma Protocol 2012: Therapy for Children With Advanced Stage High-Risk Neuroblastoma [NCT01857934]	Phase 2	153 participants (Actual)	Interventional	2013-07-05	Active, not recruiting
A Phase I Study of Sirolimus in Combination With Oral Cyclophosphamide and Oral Topotecan in Children and Young Adults With Relapsed and Refractory Solid Tumors [NCT01670175]	Phase 1	21 participants (Actual)	Interventional	2012-08-31	Completed
A Phase II Evaluation of Weekly Topotecan Hydrochloride (Hycamtin®, NSC #609699) in the Treatment of Persistent or Recurrent Carcinoma of the Cervix [NCT00087126]	Phase 2	27 participants (Actual)	Interventional	2005-02-28	Completed
A Randomized, Open-label, Phase 3 Study of Tarlatamab Compared With Standard of Care in Subjects With Relapsed Small Cell Lung Cancer After Platinum-based First-line Chemotherapy [NCT05740566]	Phase 3	700 participants (Anticipated)	Interventional	2023-05-31	Recruiting
Phase II Investigation of Topotecan and Taxol in Patients With Recurrent/Metastatic Cancer of the Cervix [NCT00003065]	Phase 2	25 participants (Anticipated)	Interventional	1997-01-31	Completed
Phase II Trial of Oral Topotecan and Paclitaxel With G-CSF (Filgrastim) Support in Patients With Previously Untreated Extensive-Stage Small Cell Lung Cancer [NCT00004055]	Phase 2	38 participants (Actual)	Interventional	1999-11-30	Completed
Phase II Trial of Topotecan and Paclitaxel in Previously Treated Patients With Relapsed Small Cell Lung Cancer [NCT00003281]	Phase 2	84 participants (Actual)	Interventional	1998-04-30	Completed
Phase I Evaluation of Topotecan in Combination With Paclitaxel and Carboplatin [NCT00005021]	Phase 1	17 participants (Actual)	Interventional	1996-07-31	Completed
Phase II Study of First-Line Therapy of Ovarian Cancer With Sequential Regimens: Cisplatin-Prolonged Oral Topotecan (C-PORT) Followed by Paclitaxel/Carboplatin (PC) [NCT00005051]	Phase 2	0 participants	Interventional	1999-08-31	Completed
Treatment of Poor Risk Myelodysplasia With the Combination of Amifostine, Topotecan and ARA-C: A Phase II Study [NCT00003827]	Phase 2	25 participants (Anticipated)	Interventional	1999-01-31	Active, not recruiting
A Randomized, Open-Label, Phase 3 Trial of Tisotumab Vedotin vs Investigator's Choice Chemotherapy in Second- or Third-Line Recurrent or Metastatic Cervical Cancer [NCT04697628]	Phase 3	556 participants (Anticipated)	Interventional	2021-02-22	Recruiting
A Pilot Study of Whole-body MRI-guided Intensity Modulated Radiation Therapy Combined With Systemic Chemotherapy Followed by High-Dose Chemotherapy With Busulfan, Melphalan and Topotecan and Stem Cell Rescue in Patients With Poor Risk Ewing's Sarcoma [NCT01795430]		0 participants (Actual)	Interventional	2013-07-31	Withdrawn(stopped due to No participants enrolled.)
A Phase I, Dosage-finding and Pharmacokinetic Study of Intravenous Topotecan and Oral Erlotinib in Adults With Refractory Solid Tumors [NCT00611468]	Phase 1	29 participants (Actual)	Interventional	2006-06-30	Completed
A Phase II Trial of Cyclophosphamide, Topotecan, and Bevacizumab (CTB) in Patients With Relapsed/Refractory Ewing's Sarcoma and Neuroblastoma [NCT01492673]	Phase 2	9 participants (Actual)	Interventional	2011-12-31	Completed
A Randomized Phase II Study of IV Topotecan Versus CRLX101 in the Second Line Treatment of Recurrent Small Cell Lung Cancer [NCT01803269]	Phase 2	29 participants (Actual)	Interventional	2013-01-16	Terminated(stopped due to Due to lack of activity and slow accrual)
Real-World Effectiveness of Bevacizumab Based on AURELIA in Platinum-resistant Recurrent Ovarian Cancer [NCT03367182]		50 participants (Actual)	Observational	2017-09-01	Completed
GALOP II Protocol for the Treatment of Unilateral Retinoblastoma [NCT03475121]	Phase 3	200 participants (Anticipated)	Interventional	2018-01-01	Recruiting
A Randomized, Controlled, Open-Label, Phase 2 Trial of SGI-110 and Carboplatin in Subjects With Platinum-Resistant Recurrent Ovarian Cancer [NCT01696032]	Phase 2	120 participants (Actual)	Interventional	2012-09-30	Completed
Randomized Phase II Study of Cabazitaxel Versus Topotecan in Small Cell Lung Cancer Patients With Progressive Disease During or After a First Line Platinum Based Chemotherapy [NCT01500720]	Phase 2	179 participants (Actual)	Interventional	2012-03-31	Completed
A Phase I Study of SGT-53, a TfRscFv-Liposome-p53 Complex, in Children With Refractory or Recurrent Solid Tumors [NCT02354547]	Phase 1	18 participants (Anticipated)	Interventional	2014-12-31	Suspended
A Randomized, Double-Blind, Placebo-Controlled Study of Trilaciclib vs Placebo in Patients With Extensive Stage Small Cell Lung Cancer (ES-SCLC) Receiving Topotecan Chemotherapy [NCT05874401]	Phase 4	302 participants (Anticipated)	Interventional	2023-10-18	Recruiting
SJiMB21: Phase 2 Study of Molecular and Clinical Risk-Directed Therapy for Infants and Young Children With Newly Diagnosed Medulloblastoma [NCT05535166]	Phase 2	120 participants (Anticipated)	Interventional	2022-12-20	Recruiting
A Phase 1/2a/3 Evaluation of the Safety and Efficacy of Adding AL3818 (Anlotinib, INN: Catequentinib), a Dual Receptor Tyrosine Kinase Inhibitor, to Standard Platinum-Based Chemotherapy in Subjects With Recurrent or Metastatic Endometrial, Ovarian, Fallop [NCT02584478]	Phase 3	294 participants (Actual)	Interventional	2015-12-31	Active, not recruiting
A Pilot Trial of Intraparenchymally-Administered Topotecan Using Convection-Enhanced Delivery (CED) in Patients With Suspected Recurrent/Progressive WHO Grade III or IV (High Grade) Glioma Undergoing A Clinically-Indicated Surgical Resection (IND 117,240) [NCT02500459]	Early Phase 1	9 participants (Actual)	Interventional	2015-07-06	Terminated(stopped due to PI Left institution)
A Phase II Study of Pazopanib With Oral Topotecan in Patients With Metastatic and Non-resectable Soft Tissue and Bone Sarcomas [NCT02357810]	Phase 2	178 participants (Actual)	Interventional	2015-03-21	Completed
Multicenter, Prospective Phase-I/II-study: Topotecan and Carboplatin in the Therapy of Patients With Relapsed Ovarian Cancer [NCT00170625]	Phase 1/Phase 2	28 participants (Actual)	Interventional	2004-06-30	Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

Trial	Outcome
NCT00011986 (3) [back to overview]	Progression-free Survival
NCT00011986 (3) [back to overview]	Number of Participants With Observed Adverse Effects (Grade 3 and Above) Assessed by Common Toxicity Criteria Version 2.0
NCT00011986 (3) [back to overview]	Overall Survival
NCT00057837 (3) [back to overview]	Overall Survival
NCT00057837 (3) [back to overview]	Duration of Response
NCT00057837 (3) [back to overview]	Proportion of Patients With Objective Response by Solid Tumor Response Criteria (RECIST)
NCT00064077 (5) [back to overview]	Duration of Progression-free Survival (PFS)
NCT00064077 (5) [back to overview]	Pain, Assessed by Brief Pain Inventory
NCT00064077 (5) [back to overview]	Patient Reported Neurotoxicity Symptoms as Measured With the Functional Assessment of Cancer Therapy/Gynecologic Oncology Group - Neurotoxicity Subscale (Short Version) (FACT/GOG-Ntx Subscale).
NCT00064077 (5) [back to overview]	Patient-reported Quality of Life as Measured by the Functional Assessment of Cancer Therapy (FACT)-Cervical Trial Outcome of Index (FACT-Cx TOI)
NCT00064077 (5) [back to overview]	Duration of Overall Survival (OS)
NCT00065182 (5) [back to overview]	Number of Participants With Grade 3 or 4 Clinical Chemical Toxicities
NCT00065182 (5) [back to overview]	Number of Participants With Grade 1, 2, 3 or 4 Hematologic Toxicities
NCT00065182 (5) [back to overview]	Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00065182 (5) [back to overview]	Number of Participants With Clinically Significant Abnormal Vital Signs Data
NCT00065182 (5) [back to overview]	Median Time of Overall Survival
NCT00087126 (2) [back to overview]	Proportion of Patients With Objective Tumor Response Rate (Complete Response [CR] or Partial Response [PR]) Using RECIST Version 1.0
NCT00087126 (2) [back to overview]	Number of Participants With Adverse Effects as Assessed by Common Terminology Criteria for Adverse Events Version 3.0
NCT00098956 (3) [back to overview]	Adverse Events, Graded Using the CTCAE Version 3.0
NCT00098956 (3) [back to overview]	Objective Response Rates (Complete and Partial) Evaluated Using RECIST Criteria
NCT00098956 (3) [back to overview]	Stable Disease Rate Evaluated Using RECIST Criteria
NCT00114166 (3) [back to overview]	Number of Participants With Adverse Effects (Grade 3 or Higher) as Assessed by Common Toxicity Criteria for Adverse Events Version 2.0
NCT00114166 (3) [back to overview]	Objective Tumor Response
NCT00114166 (3) [back to overview]	Reason Off Study Therapy
NCT00170625 (2) [back to overview]	Toxicity
NCT00170625 (2) [back to overview]	Progression-free Survival
NCT00186888 (27) [back to overview]	Event-free Survival of Eyes in Stratum A and Stratum B Patients Based on IC Classification
NCT00186888 (27) [back to overview]	Event-free Survival of Eyes in Stratum B Patients Responding to Window Treatment
NCT00186888 (27) [back to overview]	Event-free Survival of Eyes of Stratum B Patients
NCT00186888 (27) [back to overview]	Event-free Survival of Stratum A Patients
NCT00186888 (27) [back to overview]	Event-free Survival of Stratum B Patients Responding to Window Treatment
NCT00186888 (27) [back to overview]	Event-free Survival Per Eye in Stratum A and Stratum B Patients Based on AJCC Classification
NCT00186888 (27) [back to overview]	Mean Primary Visual Cortex Function: Cluster Size
NCT00186888 (27) [back to overview]	Mean Primary Visual Cortex Function: Maximum T-value
NCT00186888 (27) [back to overview]	Ocular Survival of Eyes in Stratum A and Stratum B Patients Based on IC Classification
NCT00186888 (27) [back to overview]	Ocular Survival of Eyes in Stratum B Patients Responding to Window Treatment
NCT00186888 (27) [back to overview]	Ocular Survival of Eyes of Stratum B Patients
NCT00186888 (27) [back to overview]	Ocular Survival of Stratum A Patients
NCT00186888 (27) [back to overview]	Ocular Survival of Stratum B Patients Responding to Window Treatment
NCT00186888 (27) [back to overview]	Ocular Survival Per Eye in Stratum A and Stratum B Patients Based on AJCC Classification
NCT00186888 (27) [back to overview]	Relationship Between Topotecan Clearance (CL) and ABCG2/B1 Genotype in Stratum B Participants.
NCT00186888 (27) [back to overview]	Relationship Between Topotecan Clearance (CL) and CYP3A4/5 Genotype in Stratum B Participants.
NCT00186888 (27) [back to overview]	Change in Distortion Product Otoacoustic Emissions (DPOAEs)
NCT00186888 (27) [back to overview]	Change in Parenting Stress Index (PSI)
NCT00186888 (27) [back to overview]	Number of Participants With Change in Size of Pineal Gland
NCT00186888 (27) [back to overview]	Number of Participants With Development of Pineal Cysts
NCT00186888 (27) [back to overview]	Number of Patients Recommended for and Utilizing Rehabilitation Services
NCT00186888 (27) [back to overview]	Stratum B Response to Window Therapy
NCT00186888 (27) [back to overview]	Stratum B Response Rate of Early Stage Eyes to Window Therapy
NCT00186888 (27) [back to overview]	Assessment of School Readiness
NCT00186888 (27) [back to overview]	Change in Cognitive Functioning
NCT00186888 (27) [back to overview]	Change in Parent Report of Social-Emotional Factors
NCT00186888 (27) [back to overview]	Change in Relevant Daily Living Skills
NCT00267488 (4) [back to overview]	Best Overall Response
NCT00267488 (4) [back to overview]	Time to Progression
NCT00267488 (4) [back to overview]	Safety and Tolerability as Summarized Through Adverse Event Reporting
NCT00267488 (4) [back to overview]	Overall Survival
NCT00305942 (3) [back to overview]	Time to Progression (TTP), the Length of Time, in Months, That Patients Were Alive From Their First Date of Protocol Treatment Until Worsening of Their Disease
NCT00305942 (3) [back to overview]	Overall Survival (OS), the Length of Time, in Months, That Patients Were Alive From Their First Date of Protocol Treatment Until Death
NCT00305942 (3) [back to overview]	Overall Response Rate (ORR), the Percentage of Patients Who Experience an Objective Benefit From Treatment
NCT00313612 (2) [back to overview]	Time to Disease Progression by RECIST and/or CA 125
NCT00313612 (2) [back to overview]	Clinical Response Rate (Complete and Partial Response by RECIST and/or CA [Cancer Antigen] 125)
NCT00316173 (6) [back to overview]	Number of Participants Who Died From the Start of Treatment to Follow-up
NCT00316173 (6) [back to overview]	Number of Participants With the Indicated Response
NCT00316173 (6) [back to overview]	Duration of Response
NCT00316173 (6) [back to overview]	Progression-free Survival
NCT00316173 (6) [back to overview]	The Number of Participants Classified as Responders in Cancer Antigen 125 (CA-125)
NCT00316173 (6) [back to overview]	Time to Response
NCT00316186 (5) [back to overview]	Grade 1 (Mild) Hematological Toxicities
NCT00316186 (5) [back to overview]	Grade 2 (Moderate) Hematological Toxicities
NCT00316186 (5) [back to overview]	Grade 3 (Severe) Hematological Toxicities
NCT00316186 (5) [back to overview]	Grade 4 (Life-threatening or Disabling) Hematological Toxicities
NCT00316186 (5) [back to overview]	Overall Response Rate, as Determined by Radiologic Evaluation (Utilizing the World Health Organization [WHO] Criteria), Calculated as the Number of Participants With the Indicated Response
NCT00317772 (3) [back to overview]	Dose Limiting Toxicity (DLT)
NCT00317772 (3) [back to overview]	Maximum Tolerated Dose (MTD) of Topotecan
NCT00317772 (3) [back to overview]	Response Rate
NCT00325416 (4) [back to overview]	Phase II Event Free Survival (EFS)
NCT00325416 (4) [back to overview]	Phase II Overall Survival (OS)
NCT00325416 (4) [back to overview]	Phase II Participants - Overall Response Rate
NCT00325416 (4) [back to overview]	Phase I - Maximum Tolerated Dose (MTD) Level
NCT00343044 (4) [back to overview]	Number or Participants With Toxicity
NCT00343044 (4) [back to overview]	Objective Response Rate
NCT00343044 (4) [back to overview]	Evaluation of Overall Survival
NCT00343044 (4) [back to overview]	Progression Free Survival
NCT00365547 (5) [back to overview]	Median Duration of Response
NCT00365547 (5) [back to overview]	Number of Tumor Responders
NCT00365547 (5) [back to overview]	Median Time to Response
NCT00365547 (5) [back to overview]	Median Time to Disease Progression
NCT00365547 (5) [back to overview]	Median Overall Survival
NCT00382733 (3) [back to overview]	Best Overall Response
NCT00382733 (3) [back to overview]	Maximum Tolerated Dose (MTD) of Single Agent Metronomic Oral Topotecan
NCT00382733 (3) [back to overview]	Dose Limiting Toxicities (DLT)
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Strength (Right Lower Extremity) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Strength (Right Upper Extremity) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Worst-case Change From Baseline in the Indicated Chemistry Parameters With Respect to the Normal Range
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Vertigo at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants Who Died or Progressed
NCT00390806 (29) [back to overview]	Overall Survival
NCT00390806 (29) [back to overview]	Six-month Survival
NCT00390806 (29) [back to overview]	Time to Progression (TTP) (All Sites of Disease-radiologic)
NCT00390806 (29) [back to overview]	Time to Progression (TTP) (CNS-radiologic)
NCT00390806 (29) [back to overview]	Time to Response (TTR) (CNS-radiologic)
NCT00390806 (29) [back to overview]	Number of Participants Who Ranked Each Individual Indicated Neurological Sign and Symptom as None, Mild, Moderate, or Severe at Months 1 and 3
NCT00390806 (29) [back to overview]	Number of Participants With a Complete Response (CR) or a Partial Response (PR) (Central Nervous System [CNS]-Radiologic)
NCT00390806 (29) [back to overview]	Number of Participants With Any Adverse Event (AE; Both Serious and Non-serious) or Serious Adverse Event (SAE)
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Dizziness/Lightheadedness at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Headache at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Level of Consciousness at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Nausea/Vomiting at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Other Neurological Symptoms at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Seizure at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment for the Neurological Sign and Symptom of Visual Problem at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Ataxia (Balance) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Ataxia (Gait) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Ataxia (Left Upper Extremity: Finger to Nose Testing) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Ataxia (Right Upper Extremity: Finger to Nose Testing) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Cranial Nerves II-XII at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Language (Dysphasia or Aphasia) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Sensation at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Strength (Left Lower Extremity) at Baseline, Month 1, and Month 3
NCT00390806 (29) [back to overview]	Number of Participants With the Indicated Investigator Assessment of Strength (Left Upper Extremity) at Baseline, Month 1, and Month 3
NCT00436644 (4) [back to overview]	Overall Survival
NCT00436644 (4) [back to overview]	Response Rate (Complete Response (CR) or Partial Response (PR))
NCT00436644 (4) [back to overview]	Time to Progression
NCT00436644 (4) [back to overview]	Adverse Event Profile
NCT00437073 (2) [back to overview]	Number of Participants With the Indicated Central Nervous System (CNS) Objective Response (OR)
NCT00437073 (2) [back to overview]	Number of Participants With the Indicated CNS Responses
NCT00499616 (14) [back to overview]	Correlation Between Extent of Surgical Resection With the Maintenance of Local Control, Event Free Survival (EFS)
NCT00499616 (14) [back to overview]	Outcome of Patients With Stage 4S Neuroblastoma Who Are Unable to Undergo Biopsy for Biology-based Risk Assignment
NCT00499616 (14) [back to overview]	Definitive Determination of the Prognostic Ability of 1p and 11q
NCT00499616 (14) [back to overview]	Correlation Between Extent of Surgical Resection With the Maintenance of Local Control, Surgical Complication Rate
NCT00499616 (14) [back to overview]	Definitive Determination of the Prognostic Ability of 1p and 11q
NCT00499616 (14) [back to overview]	Correlation Between Extent of Surgical Resection With the Maintenance of Local Control, Overall Survival (OS) Rates
NCT00499616 (14) [back to overview]	Second-Overall Survival
NCT00499616 (14) [back to overview]	Second-event-free Survival (E2FS)
NCT00499616 (14) [back to overview]	Reduced Surgical Morbidity for Patients With Stage 4S Neuroblastoma
NCT00499616 (14) [back to overview]	Overall Survival (OS) Rates
NCT00499616 (14) [back to overview]	Neurologic Symptoms
NCT00499616 (14) [back to overview]	Image Defined Risk Factor (IDRF)
NCT00499616 (14) [back to overview]	Comparison Between Reduce Intensity of Therapy for Patients With Unfavorable Histology Neuroblastoma and Patients Unfavorable Histology Neuroblastoma Treated on COG-A3961
NCT00499616 (14) [back to overview]	Comparison Between Reduce Intensity of Therapy for Patients With Stage 4 Neuroblastoma and Favorable Biological Features and Patients < 1 Year of Age With Stage 4 Neuroblastoma Treated on COG-A3961
NCT00516295 (2) [back to overview]	The Occurrence of Limiting Toxicity in an Eligible and Evaluable Patient.
NCT00516295 (2) [back to overview]	Time to Disease Progression in Patients Receiving VTC With or Without Bevacizumab
NCT00521144 (1) [back to overview]	Overall Response Rate (Phase II)
NCT00526799 (5) [back to overview]	Maximum Tolerated Dose (MTD)
NCT00526799 (5) [back to overview]	Clinical Benefit
NCT00526799 (5) [back to overview]	Duration of Stable Disease
NCT00526799 (5) [back to overview]	Percentage of Participants With Response
NCT00526799 (5) [back to overview]	Progression-free Survival
NCT00548418 (3) [back to overview]	Anti-tumor Activity as Measured by Surviving Progression-free
NCT00548418 (3) [back to overview]	Overall Survival
NCT00548418 (3) [back to overview]	Frequency of Response as Measured by RECIST Criteria (Imaging)
NCT00567567 (14) [back to overview]	Intraspinal Extension
NCT00567567 (14) [back to overview]	Duration of Greater Than or Equal to Grade 3 Neutropenia
NCT00567567 (14) [back to overview]	Type of Surgical or Radiotherapy Complication
NCT00567567 (14) [back to overview]	Topotecan Systemic Clearance
NCT00567567 (14) [back to overview]	Surgical Response
NCT00567567 (14) [back to overview]	Duration of Greater Than or Equal to Grade 3 Thrombocytopenia
NCT00567567 (14) [back to overview]	Response After Induction Therapy
NCT00567567 (14) [back to overview]	Proportion of Patients With a Polymorphism
NCT00567567 (14) [back to overview]	Enumeration of Peripheral Blood Cluster of Differentiation (CD)3, CD4, and CD8 Cells
NCT00567567 (14) [back to overview]	Peak Serum Concentration of Isotretinoin in Patients Enrolled on Either A3973, ANBL0032, ANBL0931, ANBL0532 and Future High Risk Studies
NCT00567567 (14) [back to overview]	OS in Patients 12-18 Months, Stage 4, MYCN Nonamplified Tumor/Unfavorable Histopathology/Diploid DNA Content/Indeterminant Histology/Ploidy and Patients > 547 Days, Stage 3, MYCN Nonamplified Tumor AND Unfavorable Histopathology/Indeterminant Histology
NCT00567567 (14) [back to overview]	EFS Pts Non-randomly Assigned to Single CEM (12-18 Mths, Stg. 4, MYCN Nonamplified Tumor/Unfavorable or Indeterminant Histopathology/Diploid DNA Content & Pts>547 Days, Stg.3, MYCN Nonamplified Tumor AND Unfavorable or Indeterminant Histopathology).
NCT00567567 (14) [back to overview]	Event-free Survival Rate
NCT00567567 (14) [back to overview]	Incidence Rate of Local Recurrence
NCT00601003 (1) [back to overview]	Number of Participants With Related Adverse Events as a Measure of Safety and Tolerability
NCT00602667 (62) [back to overview]	Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 3
NCT00602667 (62) [back to overview]	Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 4
NCT00602667 (62) [back to overview]	Methotrexate Volume of Central Compartment in Induction Cycle 1
NCT00602667 (62) [back to overview]	Methotrexate Volume of Central Compartment in Induction Cycle 2
NCT00602667 (62) [back to overview]	Event-free Survival (EFS) Compared to Historical Controls
NCT00602667 (62) [back to overview]	Erlotinib AUC0-24h
NCT00602667 (62) [back to overview]	Erlotinib Apparent Volume of Central Compartment
NCT00602667 (62) [back to overview]	Erlotinib Apparent Oral Clearance
NCT00602667 (62) [back to overview]	Cyclophosphamide Clearance in Induction Chemotherapy
NCT00602667 (62) [back to overview]	Cyclophosphamide Clearance in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]	Cyclophosphamide Clearance in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]	Methotrexate Volume of Central Compartment in Induction Cycle 3
NCT00602667 (62) [back to overview]	Methotrexate Volume of Central Compartment in Induction Cycle 4
NCT00602667 (62) [back to overview]	OSI-420 AUC0-24h
NCT00602667 (62) [back to overview]	Overall Survival (OS) Compared to Historical Controls
NCT00602667 (62) [back to overview]	Participants With Empirical Dosage Achieving Target System Exposure of Intravenous Topotecan
NCT00602667 (62) [back to overview]	Cyclophosphamide AUC0-24h in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]	Cyclophosphamide AUC0-24h in Induction Chemotherapy
NCT00602667 (62) [back to overview]	Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]	Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]	Cyclophosphamide Apparent Oral Clearance in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]	Participants With PK-guided Dosage Adjustment Achieving Target System Exposure of Intravenous Topotecan
NCT00602667 (62) [back to overview]	Percent of Patients With Sustained Objective Responses Rate After Consolidation
NCT00602667 (62) [back to overview]	Percent Probability of Event-free Survival (EFS) for Medulloblastoma Patients
NCT00602667 (62) [back to overview]	4-OH Cyclophosphamide AUC0-24h in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]	Percent Probability of Progression-free Survival (PFS) for Medulloblastoma Patients
NCT00602667 (62) [back to overview]	Percent Probability of Progression-free Survival (PFS) for Medulloblastoma Patients by DNA Methylation Subgroup
NCT00602667 (62) [back to overview]	Percentage of Patients With Objective Responses Rate to Induction Chemotherapy
NCT00602667 (62) [back to overview]	Rate of Distant Disease Progression
NCT00602667 (62) [back to overview]	Rate of Local Disease Progression
NCT00602667 (62) [back to overview]	Topotecan Apparent Oral Clearance in Maintenance Chemotherapy
NCT00602667 (62) [back to overview]	Topotecan AUC0-24h in Consolidation Chemotherapy
NCT00602667 (62) [back to overview]	Topotecan AUC0-24h in Maintenance Chemotherapy
NCT00602667 (62) [back to overview]	Topotecan Clearance in Consolidation Chemotherapy
NCT00602667 (62) [back to overview]	Concentration of Cerebrospinal Fluid Neurotransmitters
NCT00602667 (62) [back to overview]	Number and Type of Genetic Polymorphisms
NCT00602667 (62) [back to overview]	Number of Participants With Chromosomal Abnormalities
NCT00602667 (62) [back to overview]	Number of Successful Collections for Frozen and Fixed Tumor Samples
NCT00602667 (62) [back to overview]	Numbers of Patients With Gene Alterations
NCT00602667 (62) [back to overview]	Numbers of Patients With Molecular Abnormalities by Tumor Type
NCT00602667 (62) [back to overview]	Pharmacogenetic Variation on Central Nervous System Transmitters
NCT00602667 (62) [back to overview]	Percent of PET Scans With Loss of Signal Intensity
NCT00602667 (62) [back to overview]	CEPM AUC0-24h in Maintenance Chemotherapy Cycle A1
NCT00602667 (62) [back to overview]	CEPM AUC0-24h in Induction Chemotherapy
NCT00602667 (62) [back to overview]	Methotrexate AUC0-66h in Induction Cycle 3
NCT00602667 (62) [back to overview]	CEPM AUC0-24h in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]	CEPM AUC0-24h in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]	Feasibility and Toxicity of Administering Oral Maintenance Therapy in Children <3 Years of Age as Measured by the Percentage of Total Scheduled Maintenance Doses Received
NCT00602667 (62) [back to overview]	4-OH Cyclophosphamide AUC0-24h in Induction Chemotherapy
NCT00602667 (62) [back to overview]	4-OH Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 2
NCT00602667 (62) [back to overview]	4-OH Cyclophosphamide AUC0-24h in Consolidation Chemotherapy Cycle 1
NCT00602667 (62) [back to overview]	Feasibility and Toxicity of Administering Consolidation Therapy Including Cyclophosphamide and Pharmacokinetically Targeted Topotecan to Patients With Metastatic Disease Based on the Percentage of Courses Delayed for More Than 7 Days Due to Toxicity
NCT00602667 (62) [back to overview]	Feasibility and Toxicity of Administering Vinblastine With Induction Chemotherapy for Patients With Metastatic Disease as Measured by the Percentage of Courses Delayed for More Than 7 Days Due to Toxicity
NCT00602667 (62) [back to overview]	Methotrexate AUC0-66h in Induction Cycle 1
NCT00602667 (62) [back to overview]	Methotrexate AUC0-66h in Induction Cycle 2
NCT00602667 (62) [back to overview]	Methotrexate AUC0-66h in Induction Cycle 4
NCT00602667 (62) [back to overview]	Methotrexate Clearance in Induction Cycle 1
NCT00602667 (62) [back to overview]	Methotrexate Clearance in Induction Cycle 2
NCT00602667 (62) [back to overview]	Methotrexate Clearance in Induction Cycle 3
NCT00602667 (62) [back to overview]	Methotrexate Clearance in Induction Cycle 4
NCT00602667 (62) [back to overview]	Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 1
NCT00602667 (62) [back to overview]	Methotrexate Concentration at 42 Hours Post-dose in Induction Cycle 2
NCT00611468 (7) [back to overview]	Pharmacokinetic Parameters of Intravenous Topotecan With and Without Erlotinib (Mean Clearance)
NCT00611468 (7) [back to overview]	Pharmacogenetic Analysis (CYP3A4/5 Polymorphisms, UGT1A1, BCRP, and MDR1 Genotypes)
NCT00611468 (7) [back to overview]	Objective Response (as Determined Using RECIST 1.0 Criteria)
NCT00611468 (7) [back to overview]	Dosage Limiting Toxicities
NCT00611468 (7) [back to overview]	Maximum Tolerated Dosage (MTD) of Intravenous Topotecan When Given in Combination With Oral Erlotinib
NCT00611468 (7) [back to overview]	Pharmacokinetic Parameters of Intravenous Topotecan With and Without Erlotinib (Renal Clearance)
NCT00611468 (7) [back to overview]	Pharmacokinetic Parameters of Intravenous Topotecan With and Without Erlotinib (Dose-Normalized AUC)
NCT00618813 (5) [back to overview]	Incidence Rate (Number of Participants) of Dose-limiting Toxicity (DLT) - Enrollment to Week 12
NCT00618813 (5) [back to overview]	Incidence Rate (Number of Participants) of Dose-limiting Toxicity (DLT) - Week 29 to Week 37
NCT00618813 (5) [back to overview]	Incidence of Death
NCT00618813 (5) [back to overview]	Incidence Rate (Number of Participants) of Dose-limiting Toxicity (DLT) - Week 23 to Week 28
NCT00618813 (5) [back to overview]	Incidence Rate (Number of Participants) of Dose-limiting Toxicity (DLT) - Week 13 to Week 22
NCT00634244 (2) [back to overview]	The Rate of Complete Remission (CR+CRi)
NCT00634244 (2) [back to overview]	The Rate of Treatment Failure
NCT00698516 (7) [back to overview]	Duration of Tumor Response (CR and PR)
NCT00698516 (7) [back to overview]	Time to Tumor Response (CR and PR)
NCT00698516 (7) [back to overview]	Number of Participants With a Tumor Response (CR and PR)
NCT00698516 (7) [back to overview]	Overall Survival
NCT00698516 (7) [back to overview]	Percentage of Participants With Progression-free Survival (PFS) at 3 Months
NCT00698516 (7) [back to overview]	PFS - Overall
NCT00698516 (7) [back to overview]	Number of Participants With Complete Response (CR), Partial Response (PR), Stable Disease (SD), or Progressive Disease (PD)
NCT00720096 (2) [back to overview]	Interpret Genomic Array
NCT00720096 (2) [back to overview]	Assess Feasibility
NCT00800345 (2) [back to overview]	Dose Limiting Toxicity (DLT)
NCT00800345 (2) [back to overview]	Treatment Response
NCT00803062 (4) [back to overview]	To Determine and Compare the Frequency and Severity of Adverse Events as Assessed by CTCAE Version 3.0 for the Regimens Administered on This Study.
NCT00803062 (4) [back to overview]	Progression-free Survival
NCT00803062 (4) [back to overview]	Overall Survival
NCT00803062 (4) [back to overview]	Tumor Response
NCT00828139 (4) [back to overview]	Number of Patients With Grade 3 Through 5 Adverse Events That Are Related to Study Drugs
NCT00828139 (4) [back to overview]	Progression-free Survival (PFS)
NCT00828139 (4) [back to overview]	Overall Survival
NCT00828139 (4) [back to overview]	Response Rate (Confirmed and Unconfirmed, Complete and Partial Responses)
NCT00976911 (7) [back to overview]	Overall Survival (Data Cutoff 25 January 2013)
NCT00976911 (7) [back to overview]	Duration of Objective Response (Data Cutoff 14 November 2011)
NCT00976911 (7) [back to overview]	Percentage of Participants Who Died (Data Cutoff 25 January 2013)
NCT00976911 (7) [back to overview]	Percentage of Participants With Best Overall Confirmed Objective Response of Complete Response (CR) or Partial Response (PR) Per Modified RECIST (Data Cutoff 14 November 2011)
NCT00976911 (7) [back to overview]	Progression Free Survival (PFS; Data Cutoff 14 November 2011)
NCT00976911 (7) [back to overview]	Percentage of Participants With Disease Progression or Death (Data Cutoff 14 November 2011)
NCT00976911 (7) [back to overview]	European Organization for Research and Treatment of Cancer (EORTC) Quality of Life Questionnaire (QLQ) Ovarian (OV) 28 Abdominal/Gastrointestinal (AB/GI) Symptom Scale - Percentage of Responders (Data Cutoff 14 November 2011)
NCT01003938 (2) [back to overview]	CA125 Response Rate With Continuous-infusion Topotecan and Erlotinib
NCT01003938 (2) [back to overview]	Toxicity Profile
NCT01004874 (6) [back to overview]	Median Overall Survival
NCT01004874 (6) [back to overview]	One and Two Year Overall Survival
NCT01004874 (6) [back to overview]	6-month Progression-free Survival
NCT01004874 (6) [back to overview]	Number of Patients Experiencing a Greater Than or Equal to Grade 4 Hematologic or a Greater Than or Equal to Grade 3 Non-hematologic Toxicity
NCT01004874 (6) [back to overview]	Number of Patients Experiencing a Central Nervous System (CNS) Hemorrhage or a Systemic Hemorrhage
NCT01004874 (6) [back to overview]	Median Progression-free Survival
NCT01012817 (2) [back to overview]	Percent of Patients With Tumor Response, Defined as Complete Response or Partial Response as Assessed Using Response Evaluation Criteria In Solid Tumors
NCT01012817 (2) [back to overview]	Maximum Tolerated Dose of Topotecan Hydrochloride and Veliparib, Determined According to Incidence of Dose-limiting Toxicity, Graded Using National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.0 (Phase I)
NCT01076400 (1) [back to overview]	Part 1: Number of Participants With Dose Limiting Toxicities (DLTs)
NCT01121406 (26) [back to overview]	Incidence and Intensity of Adverse Events According to the United States National Cancer Institute (US NCI) Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0
NCT01121406 (26) [back to overview]	t1/2; Terminal Half-life of CD 10899 BS in Plasma
NCT01121406 (26) [back to overview]	Tmax; Time From Dosing to Maximum Measured Concentration of CD 10899 BS in Plasma
NCT01121406 (26) [back to overview]	AUC (0-24); Area Under the Concentration-time Curve in Plasma Over the Time Interval From 0 to 24 Hours for BI 6727 BS
NCT01121406 (26) [back to overview]	AUC (0-24); Area Under the Concentration-time Curve in Plasma Over the Time Interval From 0 to 24 Hours for CD 10899 BS
NCT01121406 (26) [back to overview]	AUC (0-inf); Area Under the Concentration-time Curve in Plasma Over the Time Interval From 0 Extrapolated to Infinity for BI 6727 BS
NCT01121406 (26) [back to overview]	AUC (0-inf); Area Under the Concentration-time Curve in Plasma Over the Time Interval From 0 Extrapolated to Infinity for CD 10899 BS
NCT01121406 (26) [back to overview]	Biological Progression-free Survival Based on Serum Cancer Antigen 125 (CA-125) According to the Gynaecologic Cancer Intergroup (GCIG) Criteria
NCT01121406 (26) [back to overview]	CL; Total Clearance of BI 6727 BS in Plasma After Intravenous Administration
NCT01121406 (26) [back to overview]	Cmax; Maximum Measured Concentration of BI 6727 BS in Plasma
NCT01121406 (26) [back to overview]	Cmax; Maximum Measured Concentration of CD 10899 BS in Plasma
NCT01121406 (26) [back to overview]	Disease Control Rate (DCR) at Week 24 According to Response Evaluation Criteria In Solid Tumours (RECIST) Version 1.1
NCT01121406 (26) [back to overview]	MRT; Mean Residence Time of BI 6727 BS in the Body
NCT01121406 (26) [back to overview]	Overall Survival (OS)
NCT01121406 (26) [back to overview]	Progression Free Survival (PFS)
NCT01121406 (26) [back to overview]	t1/2; Terminal Half-life of BI 6727 BS in Plasma
NCT01121406 (26) [back to overview]	Time to Deterioration in Abdominal Bloating/ Quality of Life (QOL)
NCT01121406 (26) [back to overview]	Time to Deterioration in Fatigue/Quality of Life (QOL)
NCT01121406 (26) [back to overview]	Time to Deterioration in Global Health Status/Quality of Life (QOL)
NCT01121406 (26) [back to overview]	Time to Deterioration in Pain/ Quality of Life (QOL)
NCT01121406 (26) [back to overview]	Time to Deterioration in the Three Most Troublesome Disease Specific Symptoms/ Quality of Life (QOL)
NCT01121406 (26) [back to overview]	Tmax; Time From Dosing to Maximum Measured Concentration of BI 6727 BS in Plasma
NCT01121406 (26) [back to overview]	Vss;Apparent Volume of Distribution at Steady State Following Intravenous Administration for BI 6727 BS
NCT01121406 (26) [back to overview]	Best Overall Response
NCT01121406 (26) [back to overview]	Biological Tumour Response Based on Serum Cancer Antigen 125 (CA-125) According to the Gynaecologic Cancer Intergroup (GCIG) Criteria
NCT01121406 (26) [back to overview]	Clinically Relevant Changes in Laboratory and ECG Data
NCT01175356 (3) [back to overview]	Incidence of Unacceptable Toxicity and Sinusoidal Obstruction Syndrome (SOS), Assessed by Common Terminology Criteria (CTV)v.4.0 for Toxicity Assessment and Grading for I-MIBG
NCT01175356 (3) [back to overview]	Percentage of MIBG Avid Patients Treated With MIBG Labeled With Iodine-131 and Bu/Mel Chemotherapy
NCT01175356 (3) [back to overview]	Percentage of MIBG Avid Patients Treated With Meta-iodobenxylguanide (MIBG) Labeled With Iodine-131
NCT01231906 (1) [back to overview]	Event-Free Survival
NCT01266447 (6) [back to overview]	Duration of Objective Response
NCT01266447 (6) [back to overview]	Number of Patients With Dose-limiting Toxicities (in Safety lead-in)
NCT01266447 (6) [back to overview]	Overall Survival
NCT01266447 (6) [back to overview]	Progression-free Survival
NCT01266447 (6) [back to overview]	Tumor Response
NCT01266447 (6) [back to overview]	Adverse Events (Grade 3 or Higher) During Treatment Period
NCT01492673 (1) [back to overview]	Number of Participants With Adverse Events
NCT01500720 (4) [back to overview]	Progression Free Survival (PFS)
NCT01500720 (4) [back to overview]	Overall Objective Tumor Response Rate
NCT01500720 (4) [back to overview]	Overall Survival
NCT01500720 (4) [back to overview]	Progression Free Rate at Week 12
NCT01533181 (4) [back to overview]	Disease Control Rate (DCR)
NCT01533181 (4) [back to overview]	Overall Survival (OS)
NCT01533181 (4) [back to overview]	Median Progression Free Survival (PFS)
NCT01533181 (4) [back to overview]	Incidence of Serious Adverse Events (SAEs) Possibly/Probably Definitely Related to Study Drugs
NCT01684878 (9) [back to overview]	Part 2: European Organization for Research and Treatment of Cancer (EORTC) Quality of Life (QoL) Questionnaire (QLQ) of Core 30 (C30) Score
NCT01684878 (9) [back to overview]	Part 2: Progression-free Survival (PFS) Assessed by the Investigator
NCT01684878 (9) [back to overview]	Part 2: Progression Free Survival (PFS) as Assessed by a Blinded Independent Review Committee (IRC) Including Malignant Bowel Obstruction (MBO)
NCT01684878 (9) [back to overview]	Part 2: Percentage of Participants With Adverse Events (AEs)
NCT01684878 (9) [back to overview]	Part 2: Overall Survival
NCT01684878 (9) [back to overview]	Part 2- Objective Response Rate (ORR)
NCT01684878 (9) [back to overview]	Part 1: PFS Assessed by the Investigator
NCT01684878 (9) [back to overview]	Part 1: Percentage of Participants With Adverse Events (AEs)
NCT01684878 (9) [back to overview]	Part 1- Objective Response Rate (ORR)
NCT01696032 (11) [back to overview]	Overall Survival
NCT01696032 (11) [back to overview]	Progression Free Survival at 6 Months
NCT01696032 (11) [back to overview]	Stage 1: Dose Limiting Toxicities
NCT01696032 (11) [back to overview]	Stage 2: Progression Free Survival
NCT01696032 (11) [back to overview]	Stage 1: Pharmacokinetic Parameter AUC0-8
NCT01696032 (11) [back to overview]	Stage 1: Pharmacokinetic Parameter Cmax
NCT01696032 (11) [back to overview]	Stage 1: Pharmacokinetic Parameter Tmax
NCT01696032 (11) [back to overview]	Duration of Response
NCT01696032 (11) [back to overview]	CA-125 Levels
NCT01696032 (11) [back to overview]	Clinical Benefit Rate
NCT01696032 (11) [back to overview]	Objective Response Rate
NCT01798004 (1) [back to overview]	The Tolerability of BuMel Regimen
NCT01803269 (5) [back to overview]	Progression-free Survival
NCT01803269 (5) [back to overview]	Continuous Change in Tumor Size.
NCT01803269 (5) [back to overview]	Frequency of Reported Side Effects
NCT01803269 (5) [back to overview]	Overall Survival
NCT01803269 (5) [back to overview]	Response Rates According to Response Evaluation Criteria in Solid Tumors (RECIST) Version 1.1 (Cohort A)
NCT01840943 (7) [back to overview]	Duration of Progression-free Survival
NCT01840943 (7) [back to overview]	Number of Participants With Progression-free Survival Incidence at Week 24
NCT01840943 (7) [back to overview]	Time to Response
NCT01840943 (7) [back to overview]	Number of Participants With Adverse Events
NCT01840943 (7) [back to overview]	Number of Participants With Overall Survival
NCT01840943 (7) [back to overview]	Number of Participants With Response
NCT01840943 (7) [back to overview]	Duration of Response
NCT01857934 (6) [back to overview]	Local Failure Rate and Pattern of Failure
NCT01857934 (6) [back to overview]	Dose Limiting Toxicity (DLT)
NCT01857934 (6) [back to overview]	Feasibility of Delivering hu14.18K322A to 6 Cycles of Induction Therapy
NCT01857934 (6) [back to overview]	Overall Response Rate [Complete Response + Very Good Partial Response + Partial Response (CR + VGPR + PR)]
NCT01857934 (6) [back to overview]	Dose Limiting Toxicity (DLT) or Severe (Grade 3 or 4) VOD With hu14.18K322A With Allogeneic NK Cells in Consolidation
NCT01857934 (6) [back to overview]	Event-free Survival (EFS)
NCT01931098 (7) [back to overview]	Proportion of Patients That Have Progressive Survival (PFS) at Six Months From Patient Registration for Bevacizumab Naive Patients and PFS at 3 Months for Patients With Prior Bevacizumab Treatment
NCT01931098 (7) [back to overview]	Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0)
NCT01931098 (7) [back to overview]	Mean Symptom Interference Score Between Responders and Non-responders at Baseline and by Cycle
NCT01931098 (7) [back to overview]	Overall Survival
NCT01931098 (7) [back to overview]	Mean Symptom Severity Score Between Responders and Non-responders at Baseline and by Cycle
NCT01931098 (7) [back to overview]	Mean Symptom Severity Score Between Responders and Non-responders at Baseline and by Cycle
NCT01931098 (7) [back to overview]	Mean Symptom Interference Score Between Responders and Non-responders at Baseline and by Cycle
NCT02100007 (8) [back to overview]	Estimate Overall Response Rate for ME-344 Given in Combination With Topotecan
NCT02100007 (8) [back to overview]	Number of Adverse Events
NCT02100007 (8) [back to overview]	Number of Serious Adverse Events
NCT02100007 (8) [back to overview]	Estimate the Overall Survival (OS)
NCT02100007 (8) [back to overview]	Time to Maximum Plasma Concentration for ME-344 (Tmax)
NCT02100007 (8) [back to overview]	Mean Terminal Half-life (t 1/2)
NCT02100007 (8) [back to overview]	Minimum Plasma Concentration (Cmin) of ME-344
NCT02100007 (8) [back to overview]	Maximum Plasma Concentration (Cmax)
NCT02101788 (7) [back to overview]	Progression Free Survival
NCT02101788 (7) [back to overview]	Objective Tumor Response Rate (Complete Response and Partial Response)
NCT02101788 (7) [back to overview]	Overall Survival
NCT02101788 (7) [back to overview]	Patients Reported Acute Quality of Life
NCT02101788 (7) [back to overview]	Patient Reported Acute Peripheral Neuropathy Symptoms
NCT02101788 (7) [back to overview]	Incidence of Adverse Events (AEs)
NCT02101788 (7) [back to overview]	Progression-free Survival (PFS)
NCT02357810 (11) [back to overview]	Clinical Benefit Rate (CBR) for Patients With Soft Tissue Sarcoma (STS) Treated With Combination Pazopanib and Topotecan.
NCT02357810 (11) [back to overview]	Duration of Best Response in Patients With Liposarcoma Treated With Pazopanib and Topotecan Combination
NCT02357810 (11) [back to overview]	Duration of Best Response in Patients With Soft Tissue Sarcoma Treated With Pazopanib and Topotecan Combination
NCT02357810 (11) [back to overview]	Median Progression Free Survival (PFS) for Patients With Soft Tissue Sarcoma (STS) Treated With Combination Pazopanib and Topotecan.
NCT02357810 (11) [back to overview]	Overall Response Rate (ORR) for Patients With Soft Tissue Sarcoma (STS) Treated With Combination Pazopanib and Topotecan.
NCT02357810 (11) [back to overview]	Overall Survival (OS) for Patients With Soft Tissue Sarcoma (STS) Treated With Combination Pazopanib and Topotecan.
NCT02357810 (11) [back to overview]	Overall Survival of Patients With Liposarcoma Treated With With Pazopanib and Oral Topotecan Combination
NCT02357810 (11) [back to overview]	Progression Free Survival at 12 Weeks for Patients With Soft Tissue Sarcoma (STS) Treated With Pazopanib and Oral Topotecan
NCT02357810 (11) [back to overview]	Progression Free Survival for Patients With Liposarcoma Treated With Combination Pazopanib and Topotecan.
NCT02357810 (11) [back to overview]	Progression Free Survival in Patients With Osteosarcoma Treated With Combination Pazopanib and Topotecan.
NCT02357810 (11) [back to overview]	Number of Patients With Significant Adverse Events, Assessed by National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.03
NCT02421588 (5) [back to overview]	Progression-free Survival by Independent Review Committee
NCT02421588 (5) [back to overview]	Overall Survival (OS)
NCT02421588 (5) [back to overview]	Progression-free Survival by Investigator's Assessment
NCT02421588 (5) [back to overview]	Duration of Response by Independent Review Committee
NCT02421588 (5) [back to overview]	Duration of Response by Investigator's Assessment
NCT02481830 (4) [back to overview]	Progression Free Survival (PFS)
NCT02481830 (4) [back to overview]	Overall Survival (OS) - Extended Collection
NCT02481830 (4) [back to overview]	Overall Survival (OS)
NCT02481830 (4) [back to overview]	Objective Response Rate (ORR)
NCT02487095 (11) [back to overview]	Phase I: Number of Participants With a Change in H2AX Phosphorylation (ƴH2AX) Levels in Peripheral Blood Mononuclear Cells (PBMCs) From Baseline (Day 1 Pre-Treatment)
NCT02487095 (11) [back to overview]	Phase I: Number of Participants With a Change in H2AX Phosphorylation (ƴH2AX) Levels in Hairs From Baseline (Day 1 Pre-Treatment)
NCT02487095 (11) [back to overview]	Ph II: Number of Participants With a Clinical Response
NCT02487095 (11) [back to overview]	Percentage of Peripheral Blood Mononuclear Cells (PBMCs): Cluster of Differentiation 14 (CD14)+ Monocytes Among Viable Cells, and Regulatory T Cells Among Cluster of Differentiation 4 (CD4)+ T Cells At Baseline and Post-Treatment
NCT02487095 (11) [back to overview]	Phase II: Progression-free Survival (PFS)
NCT02487095 (11) [back to overview]	Phase I Number of Participants With a Dose Limiting Toxicity (DLT)
NCT02487095 (11) [back to overview]	Phase I and Phase II: Duration of Response (DOR)
NCT02487095 (11) [back to overview]	Ph I: Maximum Tolerated Dose (MTD)/Recommended Phase 2 Dose (RP2D) of VX-970 (M6620)
NCT02487095 (11) [back to overview]	Ph I: Maximum Tolerated Dose (MTD)/Recommended Phase 2 Dose (RP2D) of Topotecan
NCT02487095 (11) [back to overview]	Number of Participants With Serious and Non-serious Adverse Events Assessed by the Common Terminology Criteria for Adverse Events (CTCAE v4.0)
NCT02487095 (11) [back to overview]	Ratio of Peripheral Blood Mononuclear Cells (PBMCs): Cluster of Differentiation 8 (CD8)/Cluster of Differentiation 4 (CD4) T Cells at Baseline and Post-Treatment
NCT02514447 (23) [back to overview]	Occurrence of Platelet Transfusions
NCT02514447 (23) [back to overview]	Occurrence of Intravenous (IV) Antibiotic Use
NCT02514447 (23) [back to overview]	Occurrence of Infection Serious Adverse Events (SAEs)
NCT02514447 (23) [back to overview]	Duration of Severe (Grade 4) Neutropenia in Cycle 1
NCT02514447 (23) [back to overview]	Duration of Response (DOR)
NCT02514447 (23) [back to overview]	Occurrence of Grade 3 and 4 Hematologic Toxicities
NCT02514447 (23) [back to overview]	Tumor Response Based on RECIST, Version 1.1
NCT02514447 (23) [back to overview]	Occurrence of Grade 4 and Grade 3/4 Decreased Platelet Count Laboratory Values (Thrombocytopenia)
NCT02514447 (23) [back to overview]	Chemotherapy Cycles and Modifications Overall
NCT02514447 (23) [back to overview]	Progression Free Survival (PFS)
NCT02514447 (23) [back to overview]	Pharmacokinetic Profile for Trilaciclib (G1T28) When Administered With Topotecan
NCT02514447 (23) [back to overview]	Pharmacokinetic Profile for Topotecan When Administered With Trilaciclib (G1T28)
NCT02514447 (23) [back to overview]	Occurrence of Febrile Neutropenia Adverse Events
NCT02514447 (23) [back to overview]	Occurrence of Erythropoietin-stimulating Agent (ESA) Administrations
NCT02514447 (23) [back to overview]	Need for Treatment With Hematopoietic Growth Factors
NCT02514447 (23) [back to overview]	Overall Survival (OS)
NCT02514447 (23) [back to overview]	Occurrence of Severe (Grade 4) Neutropenia
NCT02514447 (23) [back to overview]	Occurrence of Pulmonary Infection Serious Adverse Events (SAEs)
NCT02514447 (23) [back to overview]	Occurrence of RBC Transfusions
NCT02514447 (23) [back to overview]	Assess the Dose Limiting Toxicities (DLTs) of G1T28/Trilaciclib Administered With Topotecan in Part 1
NCT02514447 (23) [back to overview]	Assess the Hematologic Profile of G1T28/Trilaciclib Administered With Topotecan
NCT02514447 (23) [back to overview]	Chemotherapy Exposure
NCT02514447 (23) [back to overview]	Dose Reductions in Chemotherapy (Topotecan)
NCT02566993 (25) [back to overview]	Overall Response Rate in Patients With Chemotherapy-free Interval <90 Days
NCT02566993 (25) [back to overview]	Overall Response Rate in Patients With Chemotherapy-free Interval ≥ 90 Days
NCT02566993 (25) [back to overview]	Overall Response Rate in Patients Without Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Overall Survival (OS)
NCT02566993 (25) [back to overview]	Duration of Response in Patients Without Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Overall Survival in Patients With Chemotherapy-free Interval < 90 Days
NCT02566993 (25) [back to overview]	Overall Survival in Patients With Chemotherapy-free Interval ≥ 90 Days
NCT02566993 (25) [back to overview]	Overall Survival in Patients Without Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Progression-free Survival (PFS) by Independent Review Committee
NCT02566993 (25) [back to overview]	Progression-free Survival in Patients With Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Progression-free Survival in Patients With Chemotherapy-free Interval <90 Days
NCT02566993 (25) [back to overview]	Progression-free Survival in Patients With Chemotherapy-free Interval ≥90 Days
NCT02566993 (25) [back to overview]	Progression-free Survival in Patients Without Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Progression-free Survival Rate at 12 Months by Independent Review Committee
NCT02566993 (25) [back to overview]	Progression-free Survival Rate at 6 Months by Independent Review Committee
NCT02566993 (25) [back to overview]	Duration of Response in Patients With Chemotherapy-free Interval ≥ 90 Days
NCT02566993 (25) [back to overview]	Duration of Response in Patients With Chemotherapy-free Interval <90 Days
NCT02566993 (25) [back to overview]	Duration of Response in Patients With Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Duration of Response by Independent Review Committee
NCT02566993 (25) [back to overview]	Overall Survival in Patients With Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Difference in Overall Survival Between Lurbinectedin/Doxorubicin (DOX) and CAV in Patients With CAV as Best Investigator's Choice: Overall Survival Rate at 12 Months
NCT02566993 (25) [back to overview]	Difference in Overall Survival Between Lurbinectedin/DOX and CAV in Patients With CAV as Best Investigator's Choice: Overall Survival Rate at 24 Months
NCT02566993 (25) [back to overview]	Difference in Overall Survival Between Lurbinectedin/DOX and CAV in Patients With CAV as Best Investigator's Choice: Overall Survival Rate at 18 Months
NCT02566993 (25) [back to overview]	Overall Response Rate in Patients With Central Nervous System Involvement at Baseline
NCT02566993 (25) [back to overview]	Overall Response Rate by Independent Review Committee
NCT02631876 (11) [back to overview]	Progression-Free Survival (PFS), as Assessed by BIRC Per RECIST Version 1.1 in All Participants Randomized to the Study
NCT02631876 (11) [back to overview]	PFS, as Assessed by Investigator Per RECIST Version 1.1
NCT02631876 (11) [back to overview]	PFS, as Assessed by BIRC Per RECIST Version 1.1 in Participants With High Folate Receptor Alpha Level (≥ 75% of Tumor Staining)
NCT02631876 (11) [back to overview]	Overall Survival (OS)
NCT02631876 (11) [back to overview]	Objective Response Rate (ORR): Percentage of Participants With Objective Response, as Assessed by BIRC Per RECIST1.1
NCT02631876 (11) [back to overview]	Number of Participants With Anti-Drug Antibodies (ADA)
NCT02631876 (11) [back to overview]	Gynecologic Cancer Intergroup (GCIG) CA-125 Response Rate: Percentage of Participants With GCIG CA-125 Confirmed Clinical Responses
NCT02631876 (11) [back to overview]	Duration of Response (DOR), as Assessed by BIRC Per RECIST v1.1
NCT02631876 (11) [back to overview]	Number of Participants Achieving at Least a 15% (≥ 15-Point) Absolute Improvement From Baseline on the EORTC QLQ-OV28 Abdominal/Gastrointestinal (AB/GI) Symptom Subscale at Week 8/9 Assessment
NCT02631876 (11) [back to overview]	Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT02631876 (11) [back to overview]	Area Under the Plasma Concentration-Versus Time Curve From Time of Dose Until Tlast (AUClast) of Mirvetuximab Soravtansine,Total M9346A Antibody, DM4, and S-methyl DM4
NCT02786719 (2) [back to overview]	Delay in Chemotherapy Administration Due to Prolonged Neutrophil Recovery
NCT02786719 (2) [back to overview]	Incidence of Infection
NCT02963090 (3) [back to overview]	Progression Free Survival
NCT02963090 (3) [back to overview]	Overall Survival (OS)
NCT02963090 (3) [back to overview]	Overall Response Percentage
NCT03061812 (6) [back to overview]	Change From Baseline of the Physical Functioning Scale Score in European Organization for Research and Treatment of Cancer Quality of Life Questionnaire-Core 15-Palliative Care (EORTC QLQ-C15-PAL) at Week 7
NCT03061812 (6) [back to overview]	Progression Free Survival (PFS)
NCT03061812 (6) [back to overview]	Overall Survival (OS)
NCT03061812 (6) [back to overview]	Objective Response Rate (ORR)
NCT03061812 (6) [back to overview]	Clinical Benefit Rate (CBR)
NCT03061812 (6) [back to overview]	Duration of Objective Response (DOR)
NCT03088813 (12) [back to overview]	Part 1: Number of Participants With Dose-Limiting Toxicities (DLT)
NCT03088813 (12) [back to overview]	Change From Baseline in European Organization for Research and Treatment of Cancer Quality of Life Questionnaire - Core 30 (EORTC QLQ-C30)/Lung Cancer Supplement (LC13) Dyspnea Scale at Week 12
NCT03088813 (12) [back to overview]	Change From Baseline in EORTC QLQ-LC13 Cough Scale at Week 12
NCT03088813 (12) [back to overview]	Part 1: OS
NCT03088813 (12) [back to overview]	Part 1: Objective Response Rate (ORR)
NCT03088813 (12) [back to overview]	Part 1: Progression-Free Survival (PFS)
NCT03088813 (12) [back to overview]	Part 2: Median Duration of Response (DoR)
NCT03088813 (12) [back to overview]	Part 2: PFS
NCT03088813 (12) [back to overview]	Part 2: Median Time to Objective Response (OR)
NCT03088813 (12) [back to overview]	Part 2: ORR
NCT03088813 (12) [back to overview]	Part 2: Overall Survival (OS)
NCT03088813 (12) [back to overview]	Part 1: Number of Participants With Treatment-Emergent Adverse Events (TEAEs) and Treatment-Emergent Serious Adverse Events (SAEs)
NCT03098030 (4) [back to overview]	Progression-free Survival (PFS)
NCT03098030 (4) [back to overview]	Overall Survival (OS)
NCT03098030 (4) [back to overview]	Clinical Benefit Rate (CBR)
NCT03098030 (4) [back to overview]	Objective Response Rate (ORR)
NCT03786783 (5) [back to overview]	Overall Survival
NCT03786783 (5) [back to overview]	Event-free Survival
NCT03786783 (5) [back to overview]	"Percentage of Participants Who Are Feasibility Failure"
NCT03786783 (5) [back to overview]	Response Rate
NCT03786783 (5) [back to overview]	Percentage of Participants With Unacceptable Toxicity

Progression-free Survival

Median duration in months of progression free survival. (NCT00011986)
Timeframe: From the date of enrollment to first progression or death or last contact, if alive and progression free.

Intervention	months (Median)
Carbo/Taxol	16.0
Carbo/Taxol/Gemcitabine	16.3
Carbo/Taxol/Doxil	16.4
Carbo/Topotecan - Carbo/Taxol	15.4
Carbo/Gemcitabine - Carbo/Taxol	15.4

Intervention	Participants (Count of Participants)
	Leukopenia	Neutropenia	Thrombocytopenia	Anemia	Other Hematologic	Allergy	Auditory	Cardiovascular	Coagulation	Constitutional	Dermatologic	Endocrine	Gastrointestinal	Genitourinary/Renal	Hemorrhage	Hepatic	Infection/Fever	Metabolic	Musculoskeletal	Neurologic	Peripheral Neurologic	Ocular/Visual	Pain	Pulmonary	Sexual	Second Primary
Grade 3 and Above on Carbo/Gemcitabine - Carbo/Taxol	513	761	486	203	315	26	1	23	7	57	8	1	92	9	30	25	82	45	10	35	24	3	52	37	0	57
Grade 3 and Above on Carbo/Taxol/Doxil	595	782	320	160	244	28	3	34	4	84	11	2	124	13	20	11	134	55	13	43	45	1	75	39	1	51
Grade 3 and Above on Carbo/Taxol/Gemcitabine	686	798	520	196	338	20	2	36	10	96	6	4	145	8	29	32	138	55	18	47	59	3	75	37	0	66
Grade 3 and Above on Carbo/Topotecan - Carbo/Taxol	476	779	303	167	246	21	2	17	9	73	6	1	105	6	8	13	84	37	8	28	35	3	66	21	1	41
Grade 3 and Above on ToxicityCarbo/Taxol	438	749	193	102	156	38	5	20	5	54	13	0	90	9	8	13	76	61	7	34	45	1	53	19	0	34

Intervention	Months (Median)
PET (Topotecan/Etoposide/Cisplatin/G-CSF)	11.9
PIE (Irinotecan/Cisplatin/Etoposide)	11.0

Intervention	proportion of participants (Number)
PET (Topotecan/Etoposide/Cisplatin/G-CSF)	0.697
PIE (Irinotecan/Cisplatin/Etoposide)	0.576

Intervention	months (Median)
Arm I (Paclitaxel, Cisplatin)	5.82
Arm II (Vinorelbine, Cisplatin)	3.98
Arm III (Gemcitabine, Cisplatin)	4.70
Arm IV (Topotecan, Cisplatin)	4.57

Intervention	units on a scale (Mean)
	Baseline	Pre-cycle 2	Pre-cycle 5	9 months post cycle 1
Arm I (Paclitaxel, Cisplatin)	4.0	3.5	3.6	2.3
Arm II (Vinorelbine, Cisplatin)	3.9	3.5	4.0	3.2
Arm III (Gemcitabine, Cisplatin)	3.3	3.4	3.5	3.7
Arm IV (Topotecan, Cisplatin)	3.6	3.6	2.5	2.9

Intervention	months (Median)
Arm I (Paclitaxel, Cisplatin)	12.87
Arm II (Vinorelbine, Cisplatin)	9.99
Arm III (Gemcitabine, Cisplatin)	10.28
Arm IV (Topotecan, Cisplatin)	10.25

Intervention	Participants (Count of Participants)
	Albumin, Grade 3	BUN/Urea, Grade 3	Creatinine, Grade 3	Alkaline Phosphatase, Grade 3	AST, Grade 3	AST, Grade 4	ALT, Grade 3	ALT, Grade 4	Bilirubin, Grade 3	Sodium, Grade 3	Sodium, Grade 4	Calcium, Grade 3	Calcium, Grade 4	Potassium, Grade 3	Potassium, Grade 4	Magnesium, Grade 3
IV Docetaxel	3	2	1	1	1	0	0	0	2	9	1	2	1	3	1	2
IV Topotecan + IV Docetaxel	3	4	0	1	0	1	1	1	1	12	0	2	0	7	1	4

Intervention	Participants (Count of Participants)
	Hemoglobin, Grade 1	Hemoglobin, Grade 2	Hemoglobin, Grade 3	Neutrophils, Grade 1	Neutrophils, Grade 2	Neutrophils, Grade 3	Neutrophils, Grade 4	Platelets, Grade 1	Platelets, Grade 2	Platelets, Grade 3	Platelets, Grade 4	White blood cell, Grade 1	White blood cell, Grade 2	White blood cell, Grade 3	White blood cell, Grade 4
IV Docetaxel	107	46	11	14	7	7	11	10	3	0	0	28	14	13	2
IV Topotecan + IV Docetaxel	76	95	18	27	37	47	20	75	20	18	1	38	51	50	15

Intervention	Participants (Count of Participants)
	Any AEs	Any SAEs
IV Docetaxel	172	49
IV Topotecan + IV Docetaxel	186	58

Intervention	Participants (Count of Participants)
	Partial Response	Stable Disease	Increase Disease	Indeterminate
Regimen I (Topotecan 1.25 mg/m2)	4	8	2	1
Regimen II (Topotecan 4.0 mg/m2)	8	32	21	4

Intervention	Participants (Count of Participants)
	Disease Progression	Refused further treatment	Toxicity as permitted	Other
Regimen I (Topotecan 1.25 mg/m2)	9	3	3	0
Regimen II (Topotecan 4.0 mg/m2)	47	7	2	9

Intervention	probability (Number)
Stratum A-Early Disease	0.839
Stratum A-Advanced Disease	0.667
Stratum B-Early Disease	1.0
Stratum B-Advanced Disease	0.743

Intervention	probability (Number)
Stratum A-Early Disease	0.857
Stratum A-Advanced Disease	0.500
Stratum B-Early Disease	1.0
Stratum B-Advanced Disease	0.719

Intervention	dB (Mean)
	1000 Hz	1400 Hz	2000 Hz	2800 Hz	4000 Hz	6000 Hz	8000 Hz
Additional Evaluation	4.5	8.2	11.0	8.4	3.4	5.7	-9.9
Baseline	17.7	16.6	15.1	11.6	15.3	13.3	5.0
Interim Evaluation	5.5	9.4	13.0	12.2	11.3	12.9	-2.0

Intervention	units on a scale (Mean)
	Child Domain	Parent Domain	Overall Total Stress
1 Year	93.27	105.84	200.51
2 Years	92.77	105.84	198.61
3 Years	94.60	105.92	200.23
5 Years	92.49	102.74	194.68
6 Months	93.08	101.56	194.84
Baseline	96.76	109.38	207.25

Intervention	Participants (Count of Participants)
	Prominent or mildly enlarged pineal glands	Pineal growth over time	No change in pineal gland size
Participants With Bilateral Retinoblastoma	12	8	23

Intervention	Participants (Count of Participants)
	Developed new solitary cyst(s)	Developed multiple new cysts	Growth of pineal cyst	Decrease in size (resolution) of pineal cyst	No change
Participants With Bilateral Retinoblastoma	12	15	5	1	11

Intervention	participants (Number)
	Received rehabilitation services	Did not receive rehabilitation services
Occupational Therapy Did Not Recommend Rehabilitation Services	1	5
Occupational Therapy Recommended Rehabilitation Services	12	4

Intervention	Participants (Number)
	Partial response	Progressive Disease or New Lesion	Failure due to Toxicity
Stratum B	24	2	1

Intervention	Participants (Number)
	Partial response	Progressive Disease / New lesion	Failure due to Toxicity
Stratum B	11	0	1

topotecan

Description

Cross-References

Synonyms (134)

Research Excerpts

Overview

Effects

Actions

Treatment

Toxicity

Pharmacokinetics

Compound-Compound Interactions

Bioavailability

Dosage Studied

Roles (2)

Drug Classes (1)

Protein Targets (16)

Potency Measurements

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (194)

Molecular Functions (91)

Ceullar Components (39)

Bioassays (821)

Research

Studies (2,296)

Market Indicators

Research Demand Index: 64.57

Study Types

Clinical Trials (388)

Trial Overview

Trial Outcomes

Progression-free Survival

Number of Participants With Observed Adverse Effects (Grade 3 and Above) Assessed by Common Toxicity Criteria Version 2.0

Overall Survival

Overall Survival

Duration of Response

Proportion of Patients With Objective Response by Solid Tumor Response Criteria (RECIST)

Duration of Progression-free Survival (PFS)

Pain, Assessed by Brief Pain Inventory

Patient Reported Neurotoxicity Symptoms as Measured With the Functional Assessment of Cancer Therapy/Gynecologic Oncology Group - Neurotoxicity Subscale (Short Version) (FACT/GOG-Ntx Subscale).

Patient-reported Quality of Life as Measured by the Functional Assessment of Cancer Therapy (FACT)-Cervical Trial Outcome of Index (FACT-Cx TOI)

Duration of Overall Survival (OS)

Number of Participants With Grade 3 or 4 Clinical Chemical Toxicities

Number of Participants With Grade 1, 2, 3 or 4 Hematologic Toxicities

Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

Number of Participants With Clinically Significant Abnormal Vital Signs Data

Median Time of Overall Survival

Proportion of Patients With Objective Tumor Response Rate (Complete Response [CR] or Partial Response [PR]) Using RECIST Version 1.0

Number of Participants With Adverse Effects as Assessed by Common Terminology Criteria for Adverse Events Version 3.0

Adverse Events, Graded Using the CTCAE Version 3.0

Objective Response Rates (Complete and Partial) Evaluated Using RECIST Criteria

Stable Disease Rate Evaluated Using RECIST Criteria

Number of Participants With Adverse Effects (Grade 3 or Higher) as Assessed by Common Toxicity Criteria for Adverse Events Version 2.0

Objective Tumor Response

Reason Off Study Therapy

Toxicity

Progression-free Survival

Event-free Survival of Eyes in Stratum A and Stratum B Patients Based on IC Classification

Event-free Survival of Eyes in Stratum B Patients Responding to Window Treatment

Event-free Survival of Eyes of Stratum B Patients

Event-free Survival of Stratum A Patients

Event-free Survival of Stratum B Patients Responding to Window Treatment

Event-free Survival Per Eye in Stratum A and Stratum B Patients Based on AJCC Classification

Mean Primary Visual Cortex Function: Cluster Size

Mean Primary Visual Cortex Function: Maximum T-value

Ocular Survival of Eyes in Stratum A and Stratum B Patients Based on IC Classification

Ocular Survival of Eyes in Stratum B Patients Responding to Window Treatment

Ocular Survival of Eyes of Stratum B Patients

Ocular Survival of Stratum A Patients

Ocular Survival of Stratum B Patients Responding to Window Treatment

Ocular Survival Per Eye in Stratum A and Stratum B Patients Based on AJCC Classification

Relationship Between Topotecan Clearance (CL) and ABCG2/B1 Genotype in Stratum B Participants.

Relationship Between Topotecan Clearance (CL) and CYP3A4/5 Genotype in Stratum B Participants.

Change in Distortion Product Otoacoustic Emissions (DPOAEs)

Change in Parenting Stress Index (PSI)

Number of Participants With Change in Size of Pineal Gland

Number of Participants With Development of Pineal Cysts

Number of Patients Recommended for and Utilizing Rehabilitation Services

Intervention	units on a scale (Mean)
Baseline	91.61
6 Months	90.96
1 Year	95.91
2 Years	88.40
3 Years	82.12
5 Years	86.00

Intervention	units on a scale (Mean)
Baseline	40
6 Months	19.42
1 Year	26.28
2 Years	29.67
3 Years	40.61
5 Years	39.93

Intervention	units on a scale (Mean)
Baseline	97.48
6 Months	104.73
1 Year	106.06
2 Years	94.22
3 Years	96.45
5 Years	93.03

Intervention	Participants (Number)
	Complete Response	Partial Response	Stable Disease	Progressive Disease	Unknown
Topotecan Hydrochloride	0	1	9	23	4

Intervention	Weeks (Mean)
	25th percentile	Median percentile	75th percentile
Topotecan Hydrochloride	7.3	8.7	15.3

Intervention	Number of Events (Number)
	AE: Fatigue	AE: Nausea	AE: Constipation	AE: Abdominal Pain	AE: Vomiting	AE: Hypokalemia	AE: Anorexia	AE: Dyspnea	AE: Diarrhea	AE: Dizziness	AE: Headache	AE: Insomnia	SAE: Abdominal Pain	SAE: Gastrointestinal hemorrhage	SAE: Intestinal obstruction	SAE: Rectal Hemorrhage	SAE: Vomiting	SAE: Pulmonary Embolism	SAE: Dyspnea	SAE: Bacteremia	SAE: Streptococcal Bacteremia	SAE: Cerebral ischemia	SAE: Cerebral infarction	SAE: Incisional hernia, obstructive	SAE: Dehydration	SAE: Embolism venous	Alive at last contact-when follow-up ended	Deaths - any subject	Cause of Death - Disease of Study	Cause of Death - Non-Hematological toxicity	Cause of Death - Other-Brain Metastases
Topotecan Hydrochloride	15	14	12	11	8	7	6	6	6	6	6	6	2	1	1	1	1	3	1	1	1	1	1	1	1	1	9	28	25	2	1

Intervention	months (Median)
Treatment Stratum I (Oxaliplatin Plus Topotecan)	6.3
Treatment Stratum II (Oxaliplatin Plus Topotecan)	12.6

Intervention	Dose Limiting Toxicities (Number)
Phase 1 Dose Level 1	2
Phase 1 Dose Level 2	3
Phase 1 Dose Level 3	4

Intervention	months (Median)
Age Group A - Melphalan and Topotecan Plus Stem Cell Rescue	13.3
Age Group B - Melphalan and Topotecan Plus Stem Cell Rescue	21.3

Intervention	percentage of participants (Number)
	Overall Response Rate	Complete Response Rate	Partial Response Rate
Age Group A - Melphalan and Topotecan Plus Stem Cell Rescue	65	26	39
Age Group B - Melphalan and Topotecan Plus Stem Cell Rescue	57	18	39