Drug intelligence / Profile preview

EIS-12656 + olaparib

Development stage
Unknown
Lead developer
Eisbach Bio
Modality
Small Molecules
Administration
Oral
01

Overview

EIS-12656 + olaparib is a combination therapy under development for the treatment of solid tumors, particularly those with homologous recombination deficiency (HRD) or resistance to PARP inhibitors. EIS-12656 is a first-in-class small molecule allosteric inhibitor of ALC1 (also known as CHD1L), a chromatin helicase, which disrupts cancer cell DNA repair and enhances cell death. Olaparib is a targeted small molecule PARP1 and PARP2 inhibitor, approved for several BRCA-mutated or HRD-associated cancers, such as ovarian, breast, pancreatic, and prostate cancer. The rationale for this combination is that EIS-12656 may help overcome resistance to PARP inhibition and extend the benefit of treatment in hard-to-treat and resistant tumors. EIS-12656 is being developed by Eisbach Bio, and olaparib is marketed as Lynparza by AstraZeneca.

Other names
EIS-12656EIS12656EIS 12656AZD2281AZD-2281AZD 2281KU-0059436KU0059436KU 0059436KU-59436KU59436KU 59436
02

Targets

CHD1L (Chromodomain-helicase-DNA-binding protein 1-like)PARP1 (Poly (adp-ribose) polymerase 1)ABCB1 (P-glycoprotein)

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