Lunresertib is an experimental oral small molecule kinase inhibitor from Repare Therapeutics, in phase 2 trials for advanced solid tumours, ER-positive HER2-negative breast cancer resistant to CDK4/6 inhibitors and TP53-mutant ovarian and uterine cancer.
Lunresertib (RP-6306) is an oral small molecule kinase inhibitor from Repare Therapeutics, with Debiopharm as licensee. A first-in-class oral inhibitor of PKMYT1, a cell-cycle kinase; developed alone and with Debiopharm's WEE1 inhibitor Debio 0123 (zedoresertib). Its furthest stage is phase 2, for advanced solid tumours, ER-positive HER2-negative breast cancer resistant to CDK4/6 inhibitors (platform trial) and TP53-mutant ovarian and uterine cancer (with carboplatin and paclitaxel). ClinicalTrials.gov registers it in 6 studies linked below. Exclusively licensed worldwide to Debiopharm on 15 July 2025; Debiopharm took over sponsorship of the MYTHIC study (NCT04855656, recruiting). Phase 2 use is in the Canadian Cancer Trials Group platform NCT05601440 (recruiting) and NCT05605509 (completed). Whether it works in people has not been established unless a trial below reports it.
A first-in-class oral inhibitor of PKMYT1, a cell-cycle kinase; developed alone and with Debiopharm's WEE1 inhibitor Debio 0123 (zedoresertib).
1.Lunresertib slips into a pocket on its target.
Background: ADC sequencing, Antigen escape (antigen loss, lineage switch), BCG-unresponsive, Castration-resistant prostate cancer (CRPC), Circulating tumour DNA (ctDNA). Also on OnCo: Resistance: how tumours escape each drug class · Lines of therapy.
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Query for this drug: (TITLE:"Lunresertib" OR ABSTRACT:"Lunresertib" OR TITLE:"RP-6306" OR ABSTRACT:"RP-6306") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Lunresertib, not a curated reading list.
Shares Liquid-biopsy Informed Platform Trial to Evaluate CDK4/6-inhibitor Resistant ER+/HER2- Metastatic Breast Cancer, Breast cancer (all types), Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares Repare Therapeutics, Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares Repare Therapeutics, Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares Repare Therapeutics, Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares Liquid-biopsy Informed Platform Trial to Evaluate CDK4/6-inhibitor Resistant ER+/HER2- Metastatic Breast Cancer, Breast cancer (all types), Metastatic cancer (cancer that has spread) and the tag pipeline.
Shares Debiopharm and the tag pipeline.
Shares Debiopharm and the tag pipeline.
Shares Repare Therapeutics and the tag pipeline.
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