Drug intelligence / Profile preview

indomethacin + levonorgestrel

Development stage
Phase 2
Lead developer
Bayer
Modality
Small Molecules
Administration
Intrauterine
01

Overview

**indomethacin + levonorgestrel** is a combination drug incorporated into an intrauterine system (IUS) designed for contraception and reduction of early post-placement bleeding. Indomethacin, a nonsteroidal anti-inflammatory drug (NSAID) and prostaglandin synthesis inhibitor, is added to a levonorgestrel-releasing IUS to reduce initial uterine bleeding/spotting associated with hormonal IUS use. The device includes a reservoir for controlled release of indomethacin together with standard levonorgestrel delivery. In clinical studies, this combination demonstrated a substantial reduction in bleeding and spotting days during the first 90 days after placement. The mechanism of action involves indomethacin suppressing prostaglandin-mediated endometrial bleeding and levonorgestrel exerting progestogenic effects on the endometrium, leading to contraceptive effect and endometrial suppression. Plasma levels of indomethacin remain low when administered intrauterinely, minimizing systemic exposure and side effects. Developed by Bayer, the indomethacin + levonorgestrel combination represents a novel improvement to existing hormonal IUS-based contraception, particularly for women experiencing unfavorable bleeding patterns post-insertion[1][3].

Other names
indomethacin + levonorgestrel
02

Targets

PR (Progesterone receptor)PGHS-1 (Prostaglandin G/H Synthase 1)PTGS2 (Prostaglandin-Endoperoxide Synthase 2)

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