KC1086 / Konruns Pharma - LARVOL DELTA

A highly selective KAT6/7 dual inhibitor with best-in-class potential and favorable pharmacokinetic profile (AACR 2026) - "In ER+ breast cancer cells, KC1086 durably suppressed H3K23ac/H3K14ac, which outperformed PF-07248144 on biomarker depth and duration...Combinations of KC1086 further demonstrated enhanced efficacy: (i) with Palbociclib (CDK4/6 inhibitor) (TGI 101%) in ZR-75-1 ER+ breast cancer xenograft model; (ii) with Fulvestrant (Estrogen Receptor Antagonist) (TGI 83%) in xxT47D breast cancer models yielding tumor regressions and survival benefit. Furthermore, KC1086 demonstrated favorable PK profile and significant safety window: linear PK, high oral bioavailability, minimum drug accumulation and clean safety pharmacology (eg. CV, CNS and respiratory).In conclusion, we demonstrated equipotent dual inhibition of KAT6/7 delivering potentially deeper chromatin closure than KAT6-selective blockade, which translated into robust monotherapy activity and combination synergy across ER+ breast cancer, ovarian cancer as well as other tumor models, with favorable preclinical safety. These data..."

PK/PD data • Breast Cancer • Estrogen Receptor Positive Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Hormone Receptor Breast Cancer • Oncology • Ovarian Cancer • Solid Tumor • HER-2 • KAT6A

A Study of KC1086 in Patients With Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=66 | Not yet recruiting | Sponsor: Beijing Konruns Pharmaceutical Co., Ltd.

New P1 trial • Oncology • Solid Tumor