Lunresertib

Lunresertib is an investigational new drug that is being evaluated for the treatment of cancer. It is an oral small molecule inhibitor of PKMYT1, developed by Repare Therapeutics.^[1] This drug targets cell cycle regulation in tumors with specific genetic alterations, including CCNE1 amplifications or FBXW7 and PPP2R1A loss of function mutations. It is currently in phase 1/2 clinical trials, both as monotherapy or in combination with camonsertib, an ATR inhibitor.^[2]

References

↑ "Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306". Journal of Medicinal Chemistry 65 (15): 10251–10284. August 2022. doi:10.1021/acs.jmedchem.2c00552. PMID 35880755.
↑ "New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives". Journal of Medicinal Chemistry 67 (14): 11488–11521. July 2024. doi:10.1021/acs.jmedchem.4c00113. PMID 38955347.

0.00

(0 votes)

Original source: https://en.wikipedia.org/wiki/Lunresertib. Read more

[Szychowski_2022-1] "Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306". Journal of Medicinal Chemistry 65 (15): 10251–10284. August 2022. doi:10.1021/acs.jmedchem.2c00552. PMID 35880755.

[Previtali_2024-2] "New Horizons of Synthetic Lethality in Cancer: Current Development and Future Perspectives". Journal of Medicinal Chemistry 67 (14): 11488–11521. July 2024. doi:10.1021/acs.jmedchem.4c00113. PMID 38955347.

[1]

[2]

Lunresertib

Topic: Chemistry

References