Last reviewed 2026-05-14 · How we verify

ethinyl estradiol and levonorgestrel

ethinyl estradiol and levonorgestrel is a Small molecule drug developed by Proteostasis Therapeutics, Inc.. It is currently in Phase 1 development.

12.1 Mechanism of action COCs lower the risk of becoming pregnant primarily by suppressing ovulation. Other possible mechanisms may include cervical mucus changes that inhibit sperm penetration and endometrial changes that reduce the likelihood of implantation.

At a glance

Mechanism of action

1. INDICATIONS AND USAGE AMETHIA tablets are indicated for use by women to prevent pregnancy. AMETHIA tablets are an estrogen/progestin COC indicated for use by women to prevent pregnancy. ( 1 )

Approved indications

No approved indications tracked.

Boxed warnings

• WARNING: CIGARETTE SMOKING AND SERIOUS CARDIOVASCULAR EVENTS Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptives (COC) use. This risk increases with age, particularly in women over 35 years of age, and with the number of cigarettes smoked. For this reason, COCs should not be used by women who are over 35 years of age and smoke. [See Contraindications (4) .] WARNING: CIGARETTE SMOKING AND SERIOUS CARDIOVASCULAR EVENTS See full prescribing information for complete boxed warning. Women who are over 35 years old and smoke should not use AMETHIA tablets. Cigarette smoking increases the risk of serious cardiovascular events from combination oral contraceptive (COC) use.

Common side effects

• Dysmenorrhoea
• Acne
• Cervical dysplasia
• Headache
• Abdominal pain
• Cystitis
• Nasopharyngitis
• Ovarian cyst
• Vulvovaginal candidiasis
• Pelvic pain
• Urinary tract infection
• Abdominal pain lower

Drug interactions

• 7. DRUG INTERACTIONS No drug-drug interaction studies were conducted with AMETHIA tablets. Drugs or herbal products that induce certain enzymes, including CYP3A4, may decrease the effectiveness of COCs or increase breakthrough bleeding. Counsel patients to use a back-up method or alternative method of contraception when enzyme inducers are used with COCs. ( 7.1 ) 7.1 Changes in Contraceptive Effectiveness Associated with Co-Administration of Other Products If a woman on hormonal contraceptives takes a drug or herbal product that induces enzymes, including CYP3A4, that metabolize contraceptive hormones, counsel her to use additional contraception or a different method of contraception. Drugs or herbal products that induce such enzymes may decrease the plasma concentrations of contraceptive hormones, and may decrease the effectiveness of hormonal contraceptives or increase breakthrough bleeding. Some drugs or herbal products that may decrease the effectiveness of hormonal contraceptives include: barbiturates bosentan carbamazepine felbamate griseofulvin oxcarbazepine phenytoin rifampin St. John's wort topiramate HIV protease inhibitors and non-nucleoside reverse transcriptase inhibitors : Significant changes (increase or decrease) in the plasma levels of the estrogen and progestin have been noted in some cases of co-administration of HIV protease inhibitors or with non-nucleoside reverse transcriptase inhibitors. Antibiotics : There have been reports of pregnancy while taking hormonal contraceptives and antibiotics, but clinical pharmacokinetic studies have not shown consistent effects of antibiotics on plasma concentrations of synthetic steroids. Consult the labeling of all concurrently-used drugs to obtain further information about interactions with hormonal contraceptives or the potential for enzyme alterations. 7.2 Increase in Plasma Levels of Estradiol Associated with Co-Administered Drugs Co-administration of atorvastatin and certain COCs containing ethinyl estradiol increase AUC values for ethinyl estradiol by approximately 20%. Ascorbic acid and acetaminophen may increase plasma ethinyl estradiol levels, possibly by inhibition of conjugation. CYP3A4 inhibitors such as itraconazole or ketoconazole may increase plasma hormone levels. 7.3 Concomitant Use with Hepatitis C Vaccine (HCV) Combination Therapy – Liver Enzyme Elevation Do not co-administer AMETHIA tablets with HCV drug combinations containing ombitasvir/paritaprevir/ritonavir, with or without dasabuvir, due to potential for ALT elevations [see Warnings and Precautions (5.4) ] . 7.4 Changes in Plasma Levels of Co-Administered Drugs COCs containing some synthetic estrogens (e.g., ethinyl estradiol) may inhibit the metabolism of other compounds. COCs have been shown to significantly decrease plasma concentrations of lamotrigine likely due to induction of lamotrigine glucuronidation. This may reduce seizure control; therefore, dosage adjustments of lamotrigine may be necessary. Consult the labeling of the concurrently-used drug to obtain further information about interactions with COCs or the potential for enzyme alterations.

Key clinical trials

• Multi-Center, Double-Blind, Double-Dummy, Randomized, Parallel-Group Study to Evaluate Cycle Control, Bleeding Pattern, Blood Pressure, Lipid and Carbohydrate Metabolism of the Transdermal Contracepti (Phase 3)
• An Open, Repeat Dose Study to Investigate the Effect of Co-administration of the Combined Oral Contraceptive Pill (COC) and GW273225 on the Pharmacokinetics of the COC and to Investigate the Effects o (Phase 1)
• Functional Study of the Hypothalamus in High-resolution Magnetic Resonance Imaging (MRI) in Women With Polycystic Ovary Syndrome (PCOS): a Comparative Study (NA)
• A Phase I Trial to Investigate the Effect of Nintedanib on the Pharmacokinetics of a Combination of Ethinylestradiol and Levonorgestrel in Female Patients With Systemic Sclerosis Associated Interstiti (Phase 1)
• Multi-center, Double-blind, Randomized Study to Investigate the Impact of a Sequential Oral Contraceptive Containing Estradiol Valerate and Dienogest (SH T00658ID) Compared to a Monophasic Contracepti (Phase 3)
• Phase3, Placebo Controlled, Randomized, Double-blinded, Long-Term, NSAID-Add-on, Clinical Trial of NPC-16 for Treatment of Dysmenorrhea (Phase 3)
• A Multicenter, Open-label Study to Evaluate the Efficacy and Safety of an Extended-cycle, Low Dose, Combination Oral Contraceptive, Which Utilizes Ethinyl Estradiol During the Seven Day Interval Betwe (Phase 3)
• Levonorgestrel Intrauterine System Versus Oral Contraceptives for Heavy Menses (NA)

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• ethinyl estradiol and levonorgestrel CI brief — competitive landscape report
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• Proteostasis Therapeutics, Inc. portfolio CI

Frequently asked questions about ethinyl estradiol and levonorgestrel

Related

• Manufacturer: Proteostasis Therapeutics, Inc. — full pipeline
• Therapeutic area: All drugs in Other

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing