Drug intelligence / Profile preview

LPRI-421

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

Overview

**LPRI-421** is an investigational prolonged-release combined oral contraceptive developed by Exeltis. It contains the synthetic progestogen dienogest and the synthetic estrogen ethinyl estradiol in an extended-release oral tablet formulation. A completed single-center, open-label, randomized Phase II trial evaluated three prolonged-release dienogest/ethinyl estradiol formulations against flexible-regimen drospirenone plus ethinyl estradiol in 100 healthy women, using ovulation inhibition assessments. ([clinicaltrialsregister.eu](https://www.clinicaltrialsregister.eu/ctr-search/trial/2016-003830-26/DE)) The contraceptive effect is mediated through estrogen- and progesterone-receptor signaling, which suppresses ovulation and contributes to cervical-mucus changes that impede conception. ([ema.europa.eu](https://www.ema.europa.eu/en/documents/referral/dienogest-ethinylestradiol-article-31-referral-annex-ii_en.pdf))

02

Targets

ESR1 (ERα)GR (Glucocorticoid receptor)PR-A (Progesterone Receptor A)ESR2 (ERβ)RB1 (Retinoblastoma-associated Protein)AR (Adrenergic receptors)MR (Mineralocorticoid receptor)

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