Drug intelligence / Profile preview

olaparib + elacestrant

Development stage
Unknown
Lead developer
Menarini
Modality
Small Molecules
Administration
Oral
01

Overview

Olaparib + elacestrant is a combination of two oral small molecule drugs used in oncology, particularly for the treatment of hormone receptor (HR)-positive, HER2-negative advanced or metastatic breast cancer with germline BRCA1/2 mutations. Olaparib is a poly(ADP-ribose) polymerase (PARP) inhibitor that blocks DNA repair in cancer cells, leading to cell death—especially effective in tumors with BRCA mutations or homologous recombination deficiency[1][4][6]. Elacestrant is a selective estrogen receptor degrader (SERD), which binds to and degrades the estrogen receptor, thereby inhibiting estrogen-driven tumor growth[2][5][8]. The combination aims to address endocrine resistance and improve outcomes for patients with limited options after prior therapies.

Other names
olaparib + elacestrant
02

Targets

PARP1 (Poly (adp-ribose) polymerase 1)Pol II (RNA polymerase II elongation factors)ESR1 (ERα)Pol III (Dna-directed RNA polymerase III)

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