Drug intelligence / Profile preview

celecoxib + exemestane

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

Overview

Celecoxib + exemestane is a combination of two small molecule drugs used in clinical research for the treatment of hormone receptor-positive breast cancer, particularly in postmenopausal women. Celecoxib is a selective cyclooxygenase-2 (COX-2) inhibitor classified as a nonsteroidal anti-inflammatory drug (NSAID), primarily used for its analgesic, anti-inflammatory, and antipyretic properties. It inhibits prostaglandin synthesis by selectively blocking COX-2, reducing inflammation and pain; it also has demonstrated anticancer effects through additional mechanisms such as binding to cadherin-11 and inhibiting 3-phosphoinositide-dependent kinase 1 (PDK1)[3][6][8]. Exemestane is an irreversible steroidal aromatase inhibitor that blocks the conversion of androgens to estrogens by covalently binding to the aromatase enzyme ("suicide" inhibition), leading to estrogen deprivation in hormone-sensitive tumors[4]. The combination has been studied in neoadjuvant settings for breast cancer with evidence suggesting tolerability and potential anti-tumor activity[1][2][3][5].

Other names
none
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)CYP19A1 (Aromatase)

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