Drug intelligence / Profile preview

SYN818 + olaparib

Development stage
Phase 1
Lead developer
SynRx Therapeutics
Modality
Small Molecules
Administration
Oral
01

Overview

SYN818 + olaparib is an investigational oral combination therapy currently being evaluated in a Phase Ib clinical trial for adult patients with locally advanced or metastatic solid tumors harboring mutations in BRCA or defects in the homologous recombination repair (HRR) pathway[1][3][5][7]. Olaparib is a poly(ADP-ribose) polymerase (PARP) inhibitor, approved for the treatment of several cancers with DNA repair deficiencies, including BRCA-mutated ovarian, breast, pancreatic, and prostate cancers[2][6][8][10]. SYN818’s specific molecular profile and mechanism have not been disclosed; however, it is presumed to target a pathway synergistic with PARP inhibition in HRR-deficient tumors. The combination aims to enhance DNA repair inhibition and synthetic lethality in tumor cells with defective homologous recombination, leveraging olaparib’s mechanism as a selective inhibitor of PARP1 and PARP2, which induces DNA damage and cell death particularly in repair-deficient tumor cells[2][6][8][10].

Other names
AZD2281AZD-2281AZD 2281KU-59436KU59436KU 59436
02

Targets

POLQ (DNA polymerase theta)PARP1 (Poly (adp-ribose) polymerase 1)PARP2 (Poly (adp-ribose) polymerase 2)PARP3 (Poly(adp-ribose) polymerase 3)Pol II (RNA polymerase II elongation factors)

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