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Association details:
| Biomarker: | CCNE1 amplification |
|---|---|
| Cancer: | Solid Tumor |
| Drug: | lunresertib (RP-6306) (PKMYT1 inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
A phase 1 trial to study how safe and tolerable RP-6306 is when administered in patients with certain types of cancer
Excerpt:
...CCNE1 amplification (non-equivocal) as determined by tumor NGS or FISHb. ...
Trial ID:
Source:
Title:
The PKMYT1 inhibitor RP-6306 has synergistic efficacy with carboplatin in CCNE1 amplified tumor models
Published date:
10/12/2022
Excerpt:
We demonstrate that combining carboplatin with the PKMYT1 inhibitor RP-6306 is synergistic in several preclinical models of CCNE1-amplified cancer. In vitro, strong synergistic effects are observed in a CCNE1-amplified ovarian model using low concentrations of carboplatin in cell growth inhibition assays...: Together, these results provide a strong rationale for clinical development of this combination in CCNE1-amplified cancer that has therapeutic potential across several solid tumor types where platins are used.
Secondary therapy:
carboplatin
Source:
Title:
5650 - RP-6306, a novel PKMYT1 inhibitor, demonstrates synthetic lethality as monotherapy and in combination with gemcitabine in CCNE1 amplified cancer cells
Published date:
03/09/2022
Excerpt:
In combination with gemcitabine, RP-6306 demonstrated tumor regression and superior efficacy compared to single agent treatment of either agent alone in multiple CCNE1 amplified models, including HCC1569 and OVCAR3....Our studies show that inhibition of PKMYT1 kinase activity impairs the growth of CCNE1 amplified cancer cell lines both in vitro and in vivo and stands to benefit cancer patients with CCNE1 amplification.
Secondary therapy:
gemcitabine
Title:
Repare Therapeutics to Highlight Program Progress for RP-6306 at Today’s Virtual Investor Day Event
Published date:
04/08/2021
Excerpt:
Repare Therapeutics Inc....will be reviewing the compelling pre-clinical anti-tumor activity of RP-6306, our first- in-class, selective, oral inhibitor of PKMYT1 to treat CCNE1-amplified, FBXW7-altered and other undisclosed PKMYT1 inhibitor-sensitive cancers. Our in vivo and other pre-clinical data indicate that RP-6306 can selectively inhibit tumors with these specific alterations when used as a monotherapy and in combination with other agents.
