Drug intelligence / Profile preview

clomiphene citrate + letrozole

Development stage
Preclinical
Lead developer
Novartis
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Oral
01

Overview

Clomiphene citrate + letrozole is a combination of two oral ovulation induction agents used primarily in the treatment of infertility associated with polycystic ovary syndrome (PCOS), especially in women who are resistant to either drug alone. Clomiphene citrate is a selective estrogen receptor modulator (SERM) that induces ovulation by blocking estrogen receptors at the hypothalamus, leading to increased secretion of gonadotropins (FSH and LH). Letrozole is an aromatase inhibitor that reduces estrogen synthesis, also resulting in increased FSH and LH production. The combination has been shown to improve ovulation rates compared to monotherapy with either agent and may be considered for patients who do not respond adequately to single-agent therapy[1][2][4]. This regimen is typically used off-label as there are no fixed-dose combination products commercially available; both drugs are administered together during specific days of the menstrual cycle.

Other names
clomiphene + letrozoleCC + letrozoleclomid + letrozolefemara + clomid
02

Targets

ER (Estrogen receptor)CYP19A1 (Aromatase)

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