Drug intelligence / Profile preview

rucaparib + rosuvastatin

Development stage
Unknown
Lead developer
Clovis Oncology
Modality
Small Molecules
Administration
Oral
01

Overview

Rucaparib + rosuvastatin is a non-fixed-dose combination of rucaparib, a poly(ADP-ribose) polymerase (PARP) inhibitor for oncology indications, with rosuvastatin, a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitor used for hypercholesterolemia and prevention of major cardiovascular events. This combination does not represent a marketed co-formulation, but is of pharmacological interest due to potential drug–drug interactions mediated by the inhibition of breast cancer resistance protein (BCRP) by rucaparib, which may modestly increase the exposure of rosuvastatin, a BCRP substrate. Clinical studies in patients with advanced solid tumors show weak pharmacokinetic interaction when both are coadministered, without a significant impact on safety or requirement for dose adjustment. Rucaparib's mechanism relates to inhibiting DNA repair in tumor cells, while rosuvastatin inhibits HMG-CoA reductase to lower cholesterol synthesis[1][2].

02

Targets

ABCG2 (Breast cancer resistance protein)PARP3 (Poly(adp-ribose) polymerase 3)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)PARP2 (Poly (adp-ribose) polymerase 2)

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