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buparlisib + olaparib
- Development stage
- Unknown
- Lead developer
- Adlai Nortye
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination therapy consisting of buparlisib, a pan-class I PI3K inhibitor, and olaparib, a PARP inhibitor. This combination targets complementary pathways involved in DNA damage response and repair. Buparlisib inhibits all four isoforms of PI3K (PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ) by competitively binding to the ATP site, while olaparib inhibits PARP enzymes involved in DNA repair. The combination has shown synergistic effects in preclinical and early clinical studies, particularly in BRCA-mutated cancers and those with defects in DNA repair pathways.
02
Targets
PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)
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