Drug intelligence / Profile preview

rp12146

Development stage
Phase 1
Lead developer
Rhizen Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

RP12146 is an orally bioavailable, potent, next-generation small molecule inhibitor of poly (ADP-ribose) polymerase (PARP) 1 and PARP 2. It is being developed primarily for the treatment of solid tumors, including BRCA-mutated cancers such as breast, ovarian, fallopian tube, peritoneal cancer; extensive-stage small cell lung cancer; metastatic castration-resistant prostate cancer; bile duct cancer (cholangiocarcinoma); pancreatic; colorectal; gastric and endometrial cancers. Preclinical studies have shown that RP12146 demonstrates anti-proliferative activity in both BRCA and non-BRCA mutant cancer cell lines as well as in xenograft models. The drug has a wide therapeutic window with no evidence of dose-limiting toxicities reported for first-generation inhibitors and shows potential for use both as monotherapy and in combination with standard-of-care chemotherapeutics[1][2][3][4][5][7].

Other names
RP-12146RP12146RP 12146
02

Targets

PARP2 (Poly (adp-ribose) polymerase 2)

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