Drug intelligence / Profile preview

tranexamic acid + oral contraceptive pills + levonorgestrel-releasing intrauterine system

Development stage
Unknown
Lead developer
Shosuke Okamoto
Modality
Small Molecules
Administration
Oral (tranexamic Acid, Oral Contraceptive Pills), Intrauterine (levonorgestrel-releasing Intrauterine System)
01

Overview

This is a **combination therapy** consisting of three distinct agents: - **Tranexamic acid**: an antifibrinolytic agent that inhibits plasminogen activation, reducing the breakdown of fibrin clots and thereby minimizing menstrual bleeding. - **Oral contraceptive pills** (OCPs): typically contain a combination of estrogen and progestin, which suppress ovulation by inhibiting hypothalamic-pituitary-ovarian axis signaling, thicken cervical mucus, and alter the endometrial lining to prevent implantation[3][2]. - **Levonorgestrel-releasing intrauterine system** (LNG IUS): a device placed in the uterus that locally releases levonorgestrel, a progestin. Its contraceptive effect is primarily through thickening of cervical mucus (impeding sperm passage), glandular atrophy and decidualization of the endometrium (hindering implantation), and downregulation of endometrial estrogen receptors[1][2][4][5][6]. This therapy is used for menstrual disorders such as heavy menstrual bleeding (menorrhagia), contraception, and may also help reduce dysmenorrhea when all three modalities are required due to refractory symptoms or patient preference.

02

Targets

ESR1 (ERα)PLG (Plasminogen)PR (Progesterone receptor)ESR2 (ERβ)AR (Adrenergic receptors)

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