Drug intelligence / Profile preview

olaparib + gemcitabine

Development stage
Unknown
Lead developer
AstraZeneca
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Olaparib + gemcitabine is a combination of two anticancer agents: olaparib, an oral small-molecule inhibitor of poly(ADP-ribose) polymerase (PARP) enzymes (PARP-1 and PARP-2), and gemcitabine, an intravenous nucleoside analog that inhibits DNA synthesis. Olaparib exploits synthetic lethality in cancers with homologous recombination repair defects, such as those harboring BRCA mutations, potentiating the effects of DNA-damaging chemotherapy. Gemcitabine is incorporated into DNA and inhibits DNA polymerase, leading to apoptosis of tumor cells. The combination has been studied in patients with advanced solid tumors, including pancreatic and other cancers, to determine safety, tolerability, and optimal dosing schedules. While activity has been observed, the combination is associated with frequent dose-limiting hematologic toxicities, particularly myelosuppression, requiring intermittent dosing strategies for tolerability[1][2].

Brand names
LynparzaGemzar
Other names
olaparib + gemcitabine
02

Targets

PARP3 (Poly(adp-ribose) polymerase 3)DNA polymerase familyPARP2 (Poly (adp-ribose) polymerase 2)

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