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DRUG:

camonsertib (RP-3500)

i
Other names: RP-3500, RG6526, RG 6526, RG-6526, RP 3500, RP3500
Associations
Company:
Repare Therap
Drug class:
ATR inhibitor
Associations
6d
Recent advances in small molecule ATR kinase inhibitors as anticancer agents. (PubMed, Future Med Chem)
Over the last decade, intensive medicinal chemistry efforts have generated a broad pipeline of ATR inhibitors, including ceralasertib, elimusertib, camonsertib, berzosertib, ART0380, and gartisertib, many of which are in Phase I/II clinical trials. Incorporating these strategies into adaptive platform trials with pharmacodynamic markers and patient-centered outcomes will speed up translation. Overall, ATR inhibitors highlight progress in DNA damage response therapies, from understanding mechanisms to biomarker-driven clinical use, with the potential to revolutionize treatment across various cancers.
Review • Journal • PARP Biomarker • IO biomarker
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RAD51 (RAD51 Homolog A)
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berzosertib (M6620) • ceralasertib (AZD6738) • elimusertib (BAY 1895344) • alnodesertib (ART0380) • camonsertib (RP-3500) • gartisertib (M4344)
11d
MYTHIC: Study of Lunresertib Alone or in Combination With RP-3500 or Debio 0123 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=464, Recruiting, Debiopharm International SA | Trial completion date: Dec 2026 --> Jun 2028 | Trial primary completion date: Jun 2026 --> Dec 2027
Trial completion date • Trial primary completion date
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CCNE1 (Cyclin E1) • FBXW7 (F-Box And WD Repeat Domain Containing 7) • MUC16 (Mucin 16, Cell Surface Associated) • PPP2R1A (Protein Phosphatase 2 Scaffold Subunit Aalpha)
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lunresertib (RP-6306) • Debio 0123 • camonsertib (RP-3500)
13d
Camonsertib, an ATRi, in Combination with Low-Dose Gemcitabine in Solid Tumors with DNA Damage Response (DDR) Aberrations: Preclinical and Phase 1b Results. (PubMed, Clin Cancer Res)
Camonsertib and low-dose gemcitabine demonstrated preliminary clinical activity, but due to challenging tolerability further evaluation is warranted to identify the optimal dosing regimen and subset of patients who may benefit most from this combination.
P1 data • Preclinical • Journal
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ATR (Ataxia telangiectasia and Rad3-related protein)
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gemcitabine • camonsertib (RP-3500)
1m
Rb1 deficiency induces synthetic lethality with ATR and PKMYT1 coinhibition in breast cancer cell lines and patient-derived xenografts. (PubMed, Sci Transl Med)
Here, we demonstrate that coinhibition of ATR (RP-3500) and PKMYT1 (RP-6306) induces synthetic lethality in Rb1-deficient breast cancers by disrupting both S-G2 and G2-M checkpoints...Clinically, a retrospective analysis of stage IV breast cancer datasets revealed that Rb1-low tumors display reduced DNA repair pathway activity in triple-negative and CDK4/6 inhibitor-resistant luminal breast cancers. These results identify Rb1 loss as a predictive biomarker for ATR/PKMYT1-targeted therapy, offering a potential precision treatment strategy for advanced breast cancers.
Preclinical • Journal
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RB1 (RB Transcriptional Corepressor 1) • PKMYT1 (Protein Kinase Membrane Associated Tyrosine/Threonine 1)
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camonsertib (RP-3500)
2ms
A Study of RP-3500 in Combination With Standard Radiation Therapy in People With Solid Tumor Cancer (clinicaltrials.gov)
P1/2, N=49, Active, not recruiting, Memorial Sloan Kettering Cancer Center | Recruiting --> Active, not recruiting | N=84 --> 49
Enrollment closed • Enrollment change
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ATM (ATM serine/threonine kinase)
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ATM mutation
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camonsertib (RP-3500)
2ms
Testing the Addition of an Anti-Cancer Drug, Camonsertib, to Radiation Therapy for Recurrent Head and Neck Squamous Cell Carcinoma (clinicaltrials.gov)
P1, N=39, Not yet recruiting, National Cancer Institute (NCI) | Initiation date: Dec 2025 --> Mar 2026
Trial initiation date • Tumor mutational burden
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camonsertib (RP-3500)
2ms
Trial completion
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PD-L1 (Programmed death ligand 1)
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PD-L1 expression
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • carboplatin • gemcitabine • docetaxel • Cotellic (cobimetinib) • pemetrexed • ipatasertib (RG7440) • Trodelvy (sacituzumab govitecan-hziy) • Actemra IV (tocilizumab) • tiragolumab (RG6058) • Repatha (evolocumab) • camonsertib (RP-3500) • cibisatamab (RG7802) • ciforadenant (CPI-444) • zanzalintinib (XL092)
3ms
A Study of RP-3500 in Combination With Standard Radiation Therapy in People With Solid Tumor Cancer (clinicaltrials.gov)
P1/2, N=84, Recruiting, Memorial Sloan Kettering Cancer Center | Trial completion date: Sep 2025 --> Sep 2026 | Trial primary completion date: Sep 2025 --> Sep 2026
Trial completion date • Trial primary completion date
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ATM (ATM serine/threonine kinase)
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ATM mutation
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camonsertib (RP-3500)
3ms
Trial completion date
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PD-L1 (Programmed death ligand 1)
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PD-L1 expression
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Avastin (bevacizumab) • Tecentriq (atezolizumab) • carboplatin • gemcitabine • docetaxel • Cotellic (cobimetinib) • pemetrexed • ipatasertib (RG7440) • Trodelvy (sacituzumab govitecan-hziy) • Actemra IV (tocilizumab) • tiragolumab (RG6058) • Repatha (evolocumab) • camonsertib (RP-3500) • cibisatamab (RG7802) • ciforadenant (CPI-444) • zanzalintinib (XL092)
3ms
ATTACC: Study of RP-3500 (Camonsertib) With Niraparib or Olaparib in Advanced Solid Tumors (clinicaltrials.gov)
P1/2, N=156, Terminated, Repare Therapeutics | Trial completion date: Dec 2025 --> Nov 2024 | Active, not recruiting --> Terminated | Trial primary completion date: Mar 2025 --> Nov 2024; Sponsor decided to terminate study early therefore, the Phase 2 portion was not conducted
Trial completion date • Trial termination • Trial primary completion date
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Lynparza (olaparib) • Zejula (niraparib) • camonsertib (RP-3500)
5ms
TRESR: Study of RP-3500, Camonsertib, in Advanced Solid Tumors (clinicaltrials.gov)
P1/2, N=276, Completed, Repare Therapeutics | Trial completion date: Dec 2025 --> Jun 2025 | Active, not recruiting --> Completed
Trial completion • Trial completion date
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gemcitabine • Talzenna (talazoparib) • camonsertib (RP-3500)
7ms
RP-6306 in Patients With Advanced Cancer (clinicaltrials.gov)
P2, N=28, Active, not recruiting, Canadian Cancer Trials Group | Recruiting --> Active, not recruiting | N=78 --> 28
Enrollment closed • Enrollment change
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • CCNE1 (Cyclin E1) • UGT1A1 (UDP glucuronosyltransferase family 1 member A1)
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TP53 mutation • KRAS mutation • HER-2 amplification • RAS mutation
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Herceptin (trastuzumab) • gemcitabine • 5-fluorouracil • irinotecan • leucovorin calcium • lunresertib (RP-6306) • camonsertib (RP-3500)