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Ethinylestradiol | CAS No: 57-63-6 | GMP-certified suppliers
A medication that supports contraception, manages premenstrual dysphoric disorder, moderate acne, menopausal vasomotor symptoms, and helps prevent postmenopausal osteoporosis.
Therapeutic categories
Primary indications
- Ethinylestradiol is combined with other drugs for use as a contraceptive, premenstrual dysphoric disorder, moderate acne, moderate to severe vasomotor symptoms of menopause, prevention of postmenopausal osteoporosis
Product Snapshot
- Ethinylestradiol is available in multiple formulation types including oral tablets, transdermal patches, vaginal rings, and kits combining various dosage forms
- It is primarily indicated for contraceptive use, as well as treatment for premenstrual dysphoric disorder, moderate acne, vasomotor symptoms of menopause, and prevention of postmenopausal osteoporosis
- The product is approved for use in major regulatory markets including the US, Canada, and the European Union
Clinical Overview
Clinically, ethinylestradiol is primarily used in combination with progestogens for contraception. It is also indicated for treatment of premenstrual dysphoric disorder, moderate acne, vasomotor symptoms related to menopause, and prevention of postmenopausal osteoporosis. Its classification belongs to the class of estrogens and derivatives characterized by a 3-hydroxylated estrane steroid structure.
Pharmacodynamically, ethinylestradiol acts by decreasing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), thereby suppressing ovulation. It reduces endometrial vascularization and thickens cervical mucus, hindering sperm penetration and implantation of fertilized ova. It also increases levels of sex hormone-binding globulin, influencing the bioavailability of endogenous sex steroids. The compound exhibits a long duration of action with once-daily dosing and displays a wide therapeutic index; overdose rarely leads to serious adverse outcomes.
Ethinylestradiol is metabolized primarily via hepatic pathways involving cytochrome P450 isoenzymes, notably CYP3A4 and CYP2C19, and undergoes extensive first-pass metabolism. Its pharmacokinetics are characterized by reasonable oral bioavailability and enterohepatic recirculation. Caution is warranted due to associated risks of thromboembolic events, and patients should be appropriately counselled. Safety considerations include monitoring for cardiovascular risk factors and contraindications in thrombotic disorders.
Notable formulations include combined oral contraceptives marketed globally under numerous brand names with varying progestogen combinations, underscoring its widespread use in reproductive health management.
From an API sourcing perspective, quality assurance should focus on compliance with pharmacopeial standards for purity, identity, and residual solvents. Given its classification as a hormone, manufacturers must ensure consistent stereochemistry and absence of contaminating steroidal impurities. Regulatory-compliant documentation and supply chain transparency are critical for meeting global regulatory requirements.
Identification & chemistry
| Generic name | Ethinylestradiol |
|---|---|
| Molecule type | Small molecule |
| CAS | 57-63-6 |
| UNII | 423D2T571U |
| DrugBank ID | DB00977 |
Pharmacology
| Summary | Ethinylestradiol is a synthetic estrogen that primarily targets estrogen receptor alpha and related nuclear receptors to modulate hormonal activity. It suppresses gonadotrophic hormones and luteinizing hormone, leading to inhibition of ovulation, reduced endometrial vascularization, and altered cervical mucus properties. Therapeutically, it is used in combination regimens for contraception, management of menopausal symptoms, and prevention of osteoporosis. |
|---|---|
| Mechanism of action | Ethinylestradiol is a synthetic estrogenic compound. Use of estrogens have a number of effects on the body including reduced bone density. Combined oral contraceptives suppress ovulation by suppressing gonadotrophic hormone, thickening cervical mucus to prevent the travel of sperm, and preventing changes in the endometrium required for implantation of a fertilized egg. Ethinylestradiol decreases luteinizing hormone, decreasing vascularity in the endometrium. It also increases sex hormone binding globulin. |
| Pharmacodynamics | Ethinylestradiol is a synthetic estrogen that decreases luteinizing hormone to decrease endometrial vascularization, and decreases gonadotrophic hormone to prevent ovulation. It has a long duration of action as it is taken once daily, and a wide therapeutic index as overdoses are generally not associated with serious adverse effects. Patients should be counselled regarding the risks of thrombotic events. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Estrogen receptor alpha | Humans | agonist |
| Nuclear receptor subfamily 1 group I member 2 | Humans | agonist |
ADME / PK
| Absorption | A 30µg oral dose of ethinylestradiol reaches a C<sub>max</sub> of 74.1±35.6pg/mL, with a T<sub>max</sub> of 1.5±0.5h, and an AUC of 487.4±166.6pg\*h/mL. A 1.2mg dose delivered via a patch reaches a C<sub>max</sub> of 28.8±10.3pg/mL, with a T<sub>max</sub> of 86±31h, and an AUC of3895±1423pg\*h/mL. |
|---|---|
| Half-life | A 30µg oral dose has a half life of 8.4±4.8h and a 1.2mg topical dose has a half life of 27.7±34.2h. |
| Protein binding | Enthinylestradiol is 98.3-98.5% bound to albumin in serum but also exhibits binding to sex hormone binding globulin. |
| Metabolism | Ethinylestradiol can be glucuronidated by UGT1A1, UGT1A3, UGT1A4, UGT1A9, and UGT2B7. Ethinylestradiol is also sulfated by SULT1A1, SULT1A3, and SULT1E1. Ethinylestradiol can also be hydroxylated at positions 2, 4, 6, 7, and 16 by CYP3A4, CYP3A5, CYP2C8, CYP2C9, and CYP1A2. These hydroxylated metabolites can be methylated by catechol-O-methyltransferase. The methoxy metabolites can in turn be sulfated or glucuronidated. |
| Route of elimination | Ethinylestradiol is 59.2% eliminated in the urine and bile, while 2-3% is eliminated in the feces. Over 90% of ethinylestradiol is eliminated as the unchanged parent drug. |
| Volume of distribution | A 30µg oral dose has an apparent volume of distribution of 625.3±228.7L and a 1.2mg topical dose has an apparent volume of distribution of 11745.3±15934.8L. |
| Clearance | Ethinylestradiol has an intravenous clearance of 16.47L/h, and an estimated renal clearance of approximately 2.1L/h. A 30µg oral dose has a clearance of 58.0±19.8L/h and a 1.2mg topical dose has a clearance of 303.5±100.5L/h. |
Formulation & handling
- Ethinylestradiol is a small molecule estrogen commonly formulated for oral, transdermal, and vaginal routes, with diverse dosage forms including tablets, patches, and rings.
- The compound exhibits low water solubility and moderate lipophilicity (LogP 3.9), requiring formulation strategies to enhance bioavailability and stability in solid oral and transdermal dosage forms.
- Avoid co-administration with St. John's Wort due to potential reduction in systemic efficacy caused by metabolic interactions.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has multiple patent expirations in the United States between 2015 and 2020, indicating market exclusivity has ended in key regions including the US, Canada, and the EU. As a result, the API is currently in a mature phase across these markets. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Ethinylestradiol involves multiple originator companies with roles spanning production and packaging across various regions. Branded products are established primarily in the US, Canada, and EU markets, supported by a diverse range of packagers. Recent or upcoming patent expirations in the US indicate the presence of established and potential generic competition in these markets. |
|---|
Safety
| Toxicity | Female patients experiencing and overdose may present with withdrawal bleeding, nausea, vomiting, breast tenderness, abdominal pain, drowsiness, and fatigue. Overdose should be treated with symptomatic and supportive care including monitoring for potassium concentrations, sodium concentrations, and signs of metabolic acidosis. |
|---|
- Handle with appropriate protective equipment to minimize exposure, as overdose may induce withdrawal-like symptoms and systemic effects
- In case of accidental ingestion or exposure, implement monitoring protocols for electrolyte imbalances and metabolic acidosis
- Ensure controlled environment to prevent contamination and unintended exposure due to the compound’s potential systemic toxicity
Ethinyl Estradiol is a type of Estrogens
Estrogens are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in hormone therapy and women's health. Estrogens are a class of steroidal compounds that are primarily produced in the ovaries and play a significant role in the development and maintenance of female reproductive tissues and secondary sexual characteristics. These APIs are widely used in various pharmaceutical formulations, including oral contraceptives, hormone replacement therapies, and treatments for menopausal symptoms. They are also utilized in the management of conditions such as hypogonadism, infertility, and certain types of cancer.
Estrogens exert their effects by binding to estrogen receptors, which are present in various tissues throughout the body. This binding initiates a cascade of cellular and molecular events that regulate gene expression and modulate physiological processes.
Some common examples of estrogens used in pharmaceutical formulations include estradiol, estrone, and estriol. These compounds are typically synthesized from natural sources or derived from plant-based substances through a series of chemical reactions and purification processes.
As with any pharmaceutical API, the production of estrogens follows strict quality control guidelines to ensure purity, potency, and safety. Stringent regulatory standards and rigorous testing protocols are employed to guarantee consistent quality and adherence to pharmaceutical industry regulations.
In conclusion, estrogens are a vital subcategory of pharmaceutical APIs with a wide range of applications in women's health and hormone therapy. Their role in maintaining hormonal balance and addressing various medical conditions underscores their importance in modern medicine.
Ethinyl Estradiol (Estrogens), classified under Hormonal Agents
Hormonal agents are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These substances play a crucial role in regulating and modulating hormonal functions within the body. Hormonal agents are designed to mimic or manipulate the effects of naturally occurring hormones, allowing healthcare professionals to treat various endocrine disorders and hormonal imbalances.
Hormonal agents are commonly employed in the treatment of conditions such as hypothyroidism, hyperthyroidism, diabetes, and hormonal cancers. These APIs work by interacting with specific hormone receptors, either by stimulating or inhibiting their activity, to restore the balance of hormones in the body. They can be administered orally, intravenously, or through other routes depending on the specific medication and patient needs.
Pharmaceutical companies employ rigorous manufacturing processes and quality control measures to ensure the purity, potency, and safety of hormonal agent APIs. These APIs are synthesized using chemical or biotechnological methods, often starting from natural hormone sources or through recombinant DNA technology. Stringent regulatory guidelines are in place to guarantee the efficacy and safety of hormonal agent APIs, ensuring that patients receive high-quality medications.
As the demand for hormone-related therapies continues to grow, ongoing research and development efforts focus on enhancing the effectiveness and reducing the side effects of hormonal agent APIs. This includes the exploration of novel delivery systems, advanced formulations, and targeted drug delivery methods. By continuously advancing our understanding and capabilities in hormonal agents, the medical community can improve patient outcomes and quality of life for individuals with hormonal disorders.
Ethinyl Estradiol API manufacturers & distributors
Compare qualified Ethinyl Estradiol API suppliers worldwide. We currently have 13 companies offering Ethinyl Estradiol API, with manufacturing taking place in 3 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Bayer | Producer | Germany | Unknown | CEP, CoA, GMP, JDMF, USDMF | 42 products |
| Dr. Sahu's Laboratories | Producer | India | India | CoA, GMP | 70 products |
| Flavine | Distributor | Germany | Unknown | CoA | 83 products |
| Gedeon Richter | Producer | Hungary | Unknown | CEP, CoA, FDA, GMP | 48 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Industriale Chimica | Producer | Italy | Unknown | CEP, CoA, FDA, GMP, USDMF | 33 products |
| Lupin | Producer | India | Unknown | CEP, CoA, FDA, GMP, USDMF | 155 products |
| Qinhuangdao Zizhu | Producer | China | China | CEP, CoA, FDA | 10 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001 | 757 products |
| Symbiotec Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 50 products |
| Zhejiang Xianju | Producer | China | China | CEP, CoA, FDA | 17 products |
| Zhejiang Xianju Junye | Producer | China | China | CoA, JDMF | 7 products |
When sending a request, specify which Ethinyl Estradiol API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Ethinyl Estradiol API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
