APL-2302 / Asieris - LARVOL DELTA

ASN-3186 is a potent and selective inhibitor of USP1 for the treatment of BRCA1/2 mut and HRD+ cancers (AACR 2024) - "MDA-MB-436 CDX mouse model confirmed dose-dependent, single-agent inhibitory activity of ASN-3186 in vivo with higher potency than KSQ4279, possibly due to ASN-3186's higher oral bioavailability...The combination of ASN-3186 and PARPi Olaparib yielded a more robust and durable anti-tumor response, with near-complete tumor regression demonstrated at higher combination dose...Synthetic lethal activity was also observed when ASN-3186 was combined with DNA damage drug Gemcitabine. Furthermore, ASN-3186 displayed desirable ADME and PK profiles with high oral bioavailabilities (>75%) across species. These data support further clinical development of ASN-3186 as a potential best-in-class USP1 inhibitor, both as a single agent as well as in combination with PARPi, for treatment of BRCA1/2 mut and HRD+ cancers."

Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • BRCA • BRCA1 • BRCA2 • HRD • PCNA • USP1

Clinical Study of ASN-3186 in Patients with Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=200 | Not yet recruiting | Sponsor: Jiangsu Yahong Meditech Co., Ltd aka Asieris

New P1/2 trial • Oncology • Solid Tumor