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DRUG:

topotecan

i
Other names: NK 211, NK-211, NK211, NSC 609699, SKF 104864
Company:
Generic mfg.
Drug class:
Topoisomerase I inhibitor
Related drugs:
2d
Multi-omics analysis revealed significant metabolic changes in brain cancer cells treated with paclitaxel and/or topotecan. (PubMed, Heliyon)
Overall, this study underscores the effectiveness of multi-omics approaches in revealing the molecular mechanisms driving chemotherapy responses in cancer cells. Additionally, this work generates a comprehensive list of molecular alterations that can serve as a foundation for further investigations and inform personalized healthcare strategies to enhance patient outcomes.
Journal
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HIF1A (Hypoxia inducible factor 1, alpha subunit) • RACK1 (Receptor For Activated C Kinase 1) • RPA3 (Replication Protein A3)
|
paclitaxel • topotecan
8d
New P3 trial • Combination therapy
|
paclitaxel • topotecan • BNT327
8d
New P3 trial
|
topotecan • pegylated irinotecan (SSS22)
11d
Retinoblastoma Phase II Expanded Access Clinical Trial (clinicaltrials.gov)
P2, N=30, Not yet recruiting, Targeted Therapy Technologies, LLC
New P2 trial
|
topotecan • topotecan episcleral
17d
Rapid Administration Pilot for Infusing Dinutuximab (clinicaltrials.gov)
P4, N=11, Suspended, Children's Hospital Los Angeles | Trial completion date: Aug 2024 --> Jun 2025 | Recruiting --> Suspended | Trial primary completion date: Aug 2024 --> Jun 2025
Trial completion date • Trial suspension • Trial primary completion date
|
temozolomide • cyclophosphamide • irinotecan • topotecan • Unituxin (dinutuximab)
17d
Mobocertinib antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells: in vitro and in vivo studies. (PubMed, Cancer Lett)
In the tumor-bearing mouse model, mobocertinib boosted the antitumor effect of paclitaxel and topotecan, resulting in tumor regression. In summary, our study uncovers a novel potential for repurposing mobocertinib as a dual inhibitor of ABCB1 and ABCG2, and suggests the combination of mobocertinib with substrate drugs as a strategy to counteract MDR.
Preclinical • Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
|
EGFR mutation • EGFR exon 20 insertion • EGFR exon 20 mutation • ABCB1 overexpression • ABCG2 expression
|
paclitaxel • topotecan • Exkivity (mobocertinib)
26d
Enrollment closed
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gemcitabine • paclitaxel • pegylated liposomal doxorubicin • topotecan • raludotatug deruxtecan (DS-6000)
28d
MEF2C is a Potential Prognostic Biomarker and is Correlated with Immune Infiltrates in Lung Adenocarcinoma. (PubMed, Curr Med Chem)
The results imply that MEF2C could be a valuable indicator for predicting outcomes and a possible target for immunotherapy for LUAD patients.
Journal • Tumor mutational burden • IO biomarker
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TMB (Tumor Mutational Burden) • MEF2C (Myocyte Enhancer Factor 2C)
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Tasigna (nilotinib) • irinotecan • topotecan • Farydak (panobinostat)
1m
New P3 trial • Surgery
|
TP53 (Tumor protein P53) • DICER1 (Dicer 1 Ribonuclease III)
|
doxorubicin hydrochloride • cyclophosphamide • ifosfamide • vincristine • daunorubicin • topotecan • dactinomycin • dexrazoxane
1m
NCI-2018-03732: Dinutuximab, Sargramostim, and Combination Chemotherapy in Treating Patients With Newly Diagnosed High-Risk Neuroblastoma (clinicaltrials.gov)
P2, N=42, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Sep 2024 --> Sep 2025
Trial completion date
|
MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • IL6 (Interleukin 6) • CXCL9 (Chemokine (C-X-C motif) ligand 9)
|
MYCN amplification • IL6 expression
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cisplatin • carboplatin • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • vincristine • daunorubicin • topotecan • melphalan • thiotepa • Qarziba (dinutuximab beta) • Unituxin (dinutuximab) • Leukine (sargramostim) • dexrazoxane
1m
ARTEMIS-008:HS-20093 Compared With Topotecan in Subjects With Relapsed Small Cell Lung Cancer (clinicaltrials.gov)
P3, N=460, Recruiting, Hansoh BioMedical R&D Company | Not yet recruiting --> Recruiting
Enrollment open
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topotecan • GSK5764227
2ms
New P3 trial
|
gemcitabine • paclitaxel • pegylated liposomal doxorubicin • topotecan • rinatabart sesutecan (PRO1184)
2ms
ATR inhibition activates cancer cell cGAS/STING-interferon signaling and promotes antitumor immunity in small-cell lung cancer. (PubMed, Sci Adv)
This study shows that targeting ATR up-regulates major histocompatibility class I expression in preclinical models and SCLC clinical samples collected from a first-in-class clinical trial of ATR inhibitor, berzosertib, with topotecan in patients with relapsed SCLC. Targeting ATR represents a transformative vulnerability of SCLC and is a complementary strategy to induce STING-interferon signaling-mediated immunogenicity in SCLC.
Journal • PD(L)-1 Biomarker • IO biomarker
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STING (stimulator of interferon response cGAMP interactor 1)
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berzosertib (M6620) • topotecan
2ms
New P3 trial • Combination therapy
|
paclitaxel • topotecan • BNT327
2ms
New P3 trial
|
topotecan • YL201
2ms
Veliparib and Topotecan Hydrochloride in Treating Patients With Solid Tumors, Relapsed or Refractory Ovarian Cancer, or Primary Peritoneal Cancer (clinicaltrials.gov)
P1/2, N=88, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Aug 2024 --> Aug 2025
Trial completion date
|
BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
|
veliparib (ABT-888) • topotecan
2ms
Trial completion date • Combination therapy
|
PD-L1 (Programmed death ligand 1)
|
topotecan • obrixtamig (BI 764532)
2ms
NCI-2015-00693: 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 (clinicaltrials.gov)
P1, N=221, Terminated, M.D. Anderson Cancer Center | Trial completion date: Dec 2024 --> Sep 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Dec 2024 --> Sep 2024; Administratively Complete
Trial completion date • Trial termination • Trial primary completion date • Combination therapy • IO biomarker • Metastases
|
Keytruda (pembrolizumab) • Opdivo (nivolumab) • Lynparza (olaparib) • Yervoy (ipilimumab) • carboplatin • paclitaxel • doxorubicin hydrochloride • capecitabine • cyclophosphamide • pemetrexed • oxaliplatin • irinotecan • Halaven (eribulin mesylate) • Xpovio (selinexor) • daunorubicin • topotecan • leucovorin calcium • fluorouracil topical • Pemfexy (pemetrexed)
2ms
New trial
|
Loqtorzi (toripalimab-tpzi) • topotecan
2ms
Study Of Palbociclib Combined With Chemotherapy In Pediatric Patients With Recurrent/Refractory Solid Tumors (clinicaltrials.gov)
P2, N=128, Active, not recruiting, Pfizer | Phase classification: P1/2 --> P2 | Trial completion date: Feb 2025 --> Oct 2025
Phase classification • Trial completion date • Combination therapy
|
EWSR1 (EWS RNA Binding Protein 1) • FUS (FUS RNA Binding Protein)
|
Ibrance (palbociclib) • temozolomide • cyclophosphamide • irinotecan • topotecan
2ms
A Study of GSK5764227 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=260, Not yet recruiting, GlaxoSmithKline | N=100 --> 260
Enrollment change • Metastases
|
topotecan • GSK5764227
3ms
New P3 trial
|
topotecan • pegylated irinotecan (SSS22)
3ms
Trial completion date • Trial primary completion date
|
FOLR1 ( Folate receptor alpha )
|
gemcitabine • paclitaxel • pegylated liposomal doxorubicin • topotecan • luveltamab tazevibulin (STRO-002) • Neulasta (pegfilgrastim)
3ms
A Study of LY3295668 Erbumine in Participants With Relapsed/Refractory Neuroblastoma (clinicaltrials.gov)
P1, N=71, Active, not recruiting, Eli Lilly and Company | Trial completion date: Aug 2024 --> Aug 2025
Trial completion date
|
cyclophosphamide • topotecan • LY3295668
3ms
BL-B01D1-304: A Study Comparing BL-B01D1 With Topotecan in Patients With Recurrent Small Cell Lung Cancer (clinicaltrials.gov)
P3, N=652, Recruiting, Sichuan Baili Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open
|
topotecan • izalontamab brengitecan (BL-B01D1)
3ms
Ubiquitin-specific protease 22 controls melanoma metastasis and vulnerability to ferroptosis through targeting SIRT1/PTEN/PI3K signaling. (PubMed, MedComm (2020))
Finally, we found that both pharmacological and genetic silence of USP22 sensitize RSL3-induced ferroptosis through suppressing the PI3K/Akt/mTOR pathway and its downstream SCD, and ferroptosis inhibitor could partly rescued the decreased lung metastasis by topotecan in vivo. Overall, our findings reveal a prometastatic role of USP22 and identify topotecan as a potent USP22-targeting drug to limit melanoma metastasis.
Journal
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PTEN (Phosphatase and tensin homolog) • USP22 (Ubiquitin Specific Peptidase 22)
|
topotecan • RSL3
3ms
New P1 trial • Metastases
|
topotecan • GSK5764227
3ms
Synergistic antitumor effect of liposomal-based formulations of olaparib and topotecan in primary epithelial ovarian cancer cells. (PubMed, Cancer Cell Int)
The concentration-dependent response of different ovarian cancer cell types to combination therapy confirms the need for in vitro optimization to maximize drug cytotoxicity. The OLL and TLL combination is a promising formulation for further animal studies, especially for eliminating epithelial ovarian cancer with wild-type BRCA1/2.
Journal • BRCA Biomarker • PARP Biomarker
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BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
|
Lynparza (olaparib) • topotecan
3ms
Trial primary completion date • Combination therapy
|
MYCN (MYCN Proto-Oncogene BHLH Transcription Factor) • SMARCB1 (SWI/SNF Related, Matrix Associated, Actin Dependent Regulator Of Chromatin, Subfamily B, Member 1)
|
temozolomide • Kisqali (ribociclib) • topotecan
3ms
New P2 trial • Combination therapy • Metastases
|
Loqtorzi (toripalimab-tpzi) • topotecan
3ms
SHR-A1921-303: SHR-A1921 for Injection in Patients With Platinum-Resistant Recurrent Epithelial Ovarian Cancer (clinicaltrials.gov)
P3, N=440, Recruiting, Suzhou Suncadia Biopharmaceuticals Co., Ltd. | Not yet recruiting --> Recruiting
Enrollment open
|
paclitaxel • doxorubicin hydrochloride • topotecan • SHR-A1921
3ms
Mechanism and rational combinations with GP-2250, a novel oxathiazine derivative, in ovarian cancer. (PubMed, Cancer Med)
Taken together, our data indicate that GP-2250 exerts profound effects on tumor metabolism and, in combination with PARP inhibitors or bevacizumab, showed promising anti-tumor efficacy. These findings could have implications for the clinical development of GP-2250.
Journal • PARP Biomarker
|
HIF1A (Hypoxia inducible factor 1, alpha subunit) • HK2 (Hexokinase 2) • ANXA5 (Annexin A5)
|
Avastin (bevacizumab) • cisplatin • paclitaxel • topotecan • misetionamide (GP-2250)
3ms
NRG-GY023: Comparison of Standard of Care Treatment With a Triplet Combination of Targeted Immunotherapeutic Agents (clinicaltrials.gov)
P2, N=120, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Jan 2025 --> Jun 2025
Trial completion date • Combination therapy
|
PD-L1 (Programmed death ligand 1) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
|
Avastin (bevacizumab) • Lynparza (olaparib) • Imfinzi (durvalumab) • paclitaxel • pegylated liposomal doxorubicin • topotecan • Recentin (cediranib) • Myocet (non-pegylated liposomal doxorubicin) • Duomeisu (pegylated liposomal doxorubicin)
4ms
Enrollment closed
|
topotecan • Zepzelca (lurbinectedin) • Imdelltra (tarlatamab-dlle) • Calsed (amrubicin)
4ms
Trial completion date • Metastases
|
FOLR1 ( Folate receptor alpha )
|
paclitaxel • pegylated liposomal doxorubicin • Elahere (mirvetuximab soravtansine-gynx) • topotecan
4ms
RN486, a Bruton's Tyrosine Kinase inhibitor, antagonizes multidrug resistance in ABCG2-overexpressing cancer cells. (PubMed, J Transl Int Med)
Non-toxic concentrations of RN486 remarkably increased the sensitivity of ABCG2-overexpressing cancer cells to conventional anticancer drugs mitoxantrone and topotecan. Our studies propose that RN486 can antagonize ABCG2-mediated MDR in cancer cells via down-regulating the expression level of ABCG2 protein, reducing ATPase activity of ABCG2 transporter, and inhibiting the transporting function. RN486 could be potentially used in conjunction with chemotherapy to alleviate MDR mediated by ABCG2 in cancer.
Journal
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ABCB1 (ATP Binding Cassette Subfamily B Member 1) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
|
mitoxantrone • topotecan
4ms
Enrollment open • Metastases
|
gemcitabine • pemetrexed • irinotecan • vinorelbine tartrate • topotecan • sacituzumab tirumotecan (MK-2870) • Tivdak (tisotumab vedotin-tftv)
4ms
New P2 trial
|
carboplatin • temozolomide • doxorubicin hydrochloride • cyclophosphamide • ifosfamide • etoposide IV • irinotecan • vincristine • topotecan • Danyelza (naxitamab-gqgk) • Leukine (sargramostim)
4ms
Trial suspension • Combination therapy
|
CD4 (CD4 Molecule)
|
Keytruda (pembrolizumab) • Tazverik (tazemetostat) • topotecan
4ms
Phase III MIRASOL trial: Updated overall survival results of mirvetuximab soravtansine (MIRV) vs. investigator's choice chemotherapy (ICC) in patients (pts) with platinum-resistant ovarian cancer (PROC) and high folate receptor-alpha (FRα) expression (ESMO 2024)
Here, we report updated nonanalytical results based on a median follow-up of 16.7 months. 453 PROC pts with high FRα expression (VENTANA FOLR1 [FOLR1-2.1] RxDx Assay) with 1-3 prior therapies were randomized 1:1 to MIRV 6 mg/kg, adjusted ideal body weight, Day 1 of a 21-day cycle or ICC: paclitaxel (PAC), pegylated liposomal doxorubicin (PLD), or topotecan (Topo). With a median follow-up of 16.7 months, MIRV demonstrated improved efficacy vs ICC in pts with PROC. The efficacy data, along with the well-characterized safety profile, supports MIRV as the standard of care for pts with FRα positive PROC. Clinical Trial Information: NCT04209855.
P3 data • Clinical
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FOLR1 ( Folate receptor alpha )
|
FOLR1 expression
|
VENTANA FOLR1 RxDx Assay
|
paclitaxel • pegylated liposomal doxorubicin • Elahere (mirvetuximab soravtansine-gynx) • topotecan
4ms
Consenso de expertos basado en la evidencia: perfilamiento y manejo del carcinoma epitelial de ovario de alto grado avanzado. (PubMed, Rev Colomb Obstet Ginecol)
Se sugiere utilizar bevacizumab u olaparib más bevacizumab en pacientes con CEO estadios III/IV BRCA1/2 negativo o desconocido (HRD positivo) que recibieron quimioterapia basada en platino más bevacizumab y obtuvieron RC/RP...Para pacientes con CEO de alto grado avanzado o metastásico en recaída platino-sensibles se sugiere: • Quimioterapia combinada basada en platino: carboplatino/doxorrubicina liposomal o carboplatino/paclitaxel o carboplatino/ nab-paclitaxel o carboplatino/docetaxel o carboplatino/gemcitabina, por seis ciclos. Si no se tolera la terapia combinada, dar carboplatino o cisplatino solo. • Quimioterapia combinada: carboplatino/gemcitabina o carboplatino/paclitaxel o carboplatino/doxorubicina liposomal, más bevacizumab, seguida de bevacizumab como mantenimiento (hasta progresión o toxicidad)...El paclitaxel semanal o la doxorrubicina liposomal pegilada o el topotecan pueden ser administrados con o sin bevacizumab. • Existen otros agentes que se consideran potencialmente act ivos (capecitabina, ciclofosfamida, ifosfamida, irinotecán, oxaliplatino, pemetrexed, vinorelbina, ciclofosfamida), que se podrían recomendar para líneas posteriores. • Las pacientes con receptores hormonales positivos que no toleran o no tienen respuesta a los regímenes citotóxicos pueden recibir terapia hormonal con tamoxifeno u otros agentes, incluidos los inhibidores de la aromatasa (anastrozol y letrozol) o acetato de leuprolide o acetato de megestrol...El niraparib podría ser útil en pacientes BRCA 1/2 +/-/desconocido, al igual que el rucaparib, sin embargo, este último no tiene aún aprobación del ente regulador en Colombia. Conclusiones: se espera que las recomendaciones emitidas en este consenso contribuyan a mejorar la atención clínica, el impacto oncológico y la calidad de vida de estas mujeres.
Clinical guideline • Journal
|
BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • HRD (Homologous Recombination Deficiency) • BRCA (Breast cancer early onset) • PARP1 (Poly(ADP-Ribose) Polymerase 1)
|
Avastin (bevacizumab) • Lynparza (olaparib) • cisplatin • carboplatin • gemcitabine • tamoxifen • Zejula (niraparib) • Rubraca (rucaparib) • albumin-bound paclitaxel • pemetrexed • topotecan • megestrol • leuprolide acetate for depot suspension
4ms
Trial completion • Trial completion date
|
MYCN (MYCN Proto-Oncogene BHLH Transcription Factor)
|
cisplatin • doxorubicin hydrochloride • cyclophosphamide • etoposide IV • vincristine • topotecan • melphalan • busulfan • Neupogen (filgrastim)