Drug intelligence / Profile preview

XL309 + olaparib

Development stage
Unknown
Lead developer
Exelixis
Modality
Small Molecules
Administration
Oral
01

Overview

**XL309 + olaparib** is an investigational combination therapy being evaluated for the treatment of advanced solid tumors. XL309 is a potent, selective, orally bioavailable inhibitor of USP1, a deubiquitinating enzyme involved in DNA damage repair. Inhibiting USP1 impairs tumor cells' ability to repair DNA and may enhance cell death. Olaparib is a well-established oral small molecule inhibitor of PARP enzymes, which also play a key role in DNA repair. The combination aims to maximize anti-tumor efficacy by dual inhibition of DNA repair pathways, potentially increasing sensitivity to treatment in cancers with defective homologous recombination or DNA damage response. This combination is currently undergoing Phase 1 clinical investigation and is not FDA approved.

Other names
XL309XL-309XL 309olaparib
02

Targets

USP1 (Ubiquitin-specific protease 1)PARP3 (Poly(adp-ribose) polymerase 3)PARP2 (Poly (adp-ribose) polymerase 2)PARP1 (Poly (adp-ribose) polymerase 1)

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