Drug intelligence / Profile preview

clomiphene + clarithromycin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

A drug combination consisting of clomiphene, a selective estrogen receptor modulator (SERM) used primarily for female infertility due to anovulation, and clarithromycin, a macrolide antibiotic. Clarithromycin is a strong CYP3A4 inhibitor that can increase the serum concentration of clomiphene, which is primarily metabolized through CYP3A4 and CYP2D6 pathways. This interaction has been studied in clinical settings to develop physiologically based pharmacokinetic (PBPK) models for predicting drug-drug-gene interaction scenarios. ## Drug Interaction Information Clomiphene and clarithromycin represent a drug combination with notable interaction potential. The search results indicate that clarithromycin, a macrolide antibiotic, can increase the serum concentration of clomiphene when used together[4]. This interaction occurs because clarithromycin is a strong CYP3A4 inhibitor[3], and clomiphene is primarily metabolized through CYP3A4 and CYP2D6 pathways[7]. A clinical study demonstrated this interaction, where participants received 500 mg clarithromycin twice daily for four days, followed by a single dose of clomiphene citrate together with 500 mg clarithromycin on day 5[3]. The study aimed to develop a physiologically based pharmacokinetic (PBPK) model to predict drug-drug-gene interaction scenarios involving clomiphene. ## Individual Drug Information **Clomiphene:** - A selective estrogen receptor modulator (SERM) used primarily for female infertility due to anovulation - Used in treatment of ovulatory dysfunction[4] - Acts by competing with estrogen for estrogen-receptor-binding sites[4] - Initiates a series of endocrine events leading to follicular rupture and ovulation[4] **Clarithromycin:** - A macrolide antibiotic used for various bacterial infections - Indicated for respiratory tract infections, skin infections, H. pylori infection, and others[1] - Strong inhibitor of CYP3A4 enzyme[3] ## Research Applications Interestingly, there's also research showing that clomiphene combined with amoxicillin (another antibiotic, different from clarithromycin) can boost the antibiotic's activity against resistant bacteria, specifically Streptococcus pneumoniae[5]. This suggests potential therapeutic applications for clomiphene in combination with antibiotics beyond its traditional use in fertility treatment. ## Clinical Implications The interaction between clomiphene and clarithromycin could potentially affect: 1. The exposure of clomiphene and its active metabolites 2. The efficacy and safety profile of clomiphene treatment 3. Treatment outcomes in patients requiring both medications This drug combination requires careful consideration in clinical settings, especially given that clomiphene therapy may be susceptible to drug-drug interactions (DDIs), drug-gene interactions (DGIs), and drug-drug-gene interactions (DDGIs)[7].

02

Targets

Bacterial 50S ribosomal subunitER (Estrogen receptor)CYP3A4 (Cytochrome P450 3A4)

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