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Dienogest | CAS No: 65928-58-7 | GMP-certified suppliers
A medication that treats endometriosis and supports reliable hormonal contraception, providing consistent symptom control and reproductive management for diverse formulation needs.
Therapeutic categories
Primary indications
- Indicated for use as the treatment of endometriosis alone and as a contraceptive in combination with ethinylestradiol
Product Snapshot
- Oral small‑molecule product supplied mainly as coated or film‑coated tablets
- Used for endometriosis management and for hormonal contraception when combined with ethinylestradiol
- Approved and marketed in the US and Canada
Clinical Overview
Dienogest provides potent progestogenic activity in endometrial tissue despite its relatively weak affinity for the progesterone receptor. Sustained administration induces endometrial atrophy and creates a hyperprogestogenic, moderately hypoestrogenic endocrine environment that supports decidualization and suppresses proliferation of eutopic and ectopic endometrium. Reduction of endogenous estradiol counters estrogen‑driven trophic stimulation. The compound also demonstrates antiandrogenic activity through androgen receptor antagonism.
Pharmacodynamic effects include inhibition of follicular development at a 2 mg dose and suppression of ovulation, with limited influence on FSH and LH. In clinical use for endometriosis, dienogest reduces pain and lesion burden. In combined oral contraceptives, it contributes to cycle control and improvement of androgen‑related symptoms such as acne and hirsutism.
Absorption is rapid after oral dosing, and metabolism occurs primarily via CYP3A pathways, with renal excretion of metabolites. As a CYP3A substrate, dienogest may be affected by strong enzyme inducers or inhibitors. No glucocorticoid or mineralocorticoid activity has been reported. Safety considerations include the potential for hypoestrogenic effects during long‑term use and class‑related risks associated with hormonal contraception.
For API procurement, suppliers should provide controlled stereochemistry, validated impurity profiles, and documentation supporting compliance with regional pharmacopoeial or regulatory specifications.
Identification & chemistry
| Generic name | Dienogest |
|---|---|
| Molecule type | Small molecule |
| CAS | 65928-58-7 |
| UNII | 46M3EV8HHE |
| DrugBank ID | DB09123 |
Pharmacology
| Summary | Dienogest is a synthetic progestin that acts primarily as a progesterone receptor agonist, producing antiproliferative, antiangiogenic, and immunologic effects that reduce endometrial growth. It lowers endogenous estradiol levels, generating a hypoestrogenic and hyperprogestogenic environment that suppresses trophic stimulation of both eutopic and ectopic endometrial tissue. Dienogest also antagonizes androgen receptors, contributing to its antiandrogenic pharmacodynamic profile. |
|---|---|
| Mechanism of action | Dienogest acts as an agonist at the progesterone receptor (PR) with weak affinity that is comparable to that of progesterone but has a very potent progestagenic effect in the endometrium, causing endometrial atrophy after prolonged use . It promotes antiproliferative, immunologic and antiangiogenic effects on endometrial tissue. Dienogest reduces the level of endogenous production of oestradiol and thereby suppressing the trophic effects of oestradiol on both the eutopic and ectopic endometrium . Continous administration of dienogest results in hyperprogestogenic and moderately hypoestrogenic endocrine environment, which causes initial decidualization of endometrial tissue . It is an antagonist at androgen receptors, improve androgenic symptoms such as acne and hirsutism . |
| Pharmacodynamics | Dienogest exhibits a very potent progestagenic effect in the endometrium, and causes endometrial atrophy after prolonged use . It also mediates an antiandrogenic effect that is equivalent to approximately one third that of cyproterone acetate . A dose of 2 mg inhibits the growth of ovarian follicles at 10 mm and maintains the concentration of progesterone at a low level, but has a weak inhibitory effect on FSH and LH. 1mg/kg of dienogest also directly inhibits ovulation . In clinical trials composing of patients with endometriosis, dienogest therapy effectively reduced painful symptoms and endometriotic lesions associated with the disorder . Dienogest displays no antiestrogenic activity as it activate neither estrogen receptor (ER) α nor ERβ , and causes hypoestrogenic effects instead as it is shown to decrease the relative expressions of ERβ and ERα . It has no glucocorticoid or mineralocorticoid effects. In combined oral contraceptive pills (COCP) with ethinyloestradiol, dienogest conjuction therapy effectively reduces the symptoms of acne and hirsutism, as well as improving excessively heavy or prolonged menstrual bleeding . |
Targets
| Target | Organism | Actions |
|---|---|---|
| Progesterone receptor | Humans | agonist |
| Androgen receptor | Humans | antagonist |
ADME / PK
| Absorption | Dienogest is rapidly absorbed following oral administration, with 91% bioavailability. The peak plasma concentration of 47 ng/mL is reached at about 1.5 hours after single ingestion of 2 mg . The stable concentrations of the drug are reached after two days of initial treatment . |
|---|---|
| Half-life | Elimination half-life of dienogest is around 9-10 hours. The half-life of urinary metabolites excretion is 14 hours . |
| Protein binding | Dienogest is 90% nonospecifically bound to albumin. It displays no binding to sex hormone binding globulin (SHBG) or corticoid binding globulin (CBG) . |
| Metabolism | Dienogest undergoes complete metabolism that is mainly mediated by CYP3A4. The metabolites are pharmacologically inactive and rapidly eliminated from the plasma. |
| Route of elimination | The ratio of renal elimination to fecal elimination of dienogest is 3:1, where dienogest is predominantly excreted in the form of inactive metabolites. Most of orally administered drug is excreted in the urine within the first 24 hours of ingestion . |
| Volume of distribution | The apparent volume of distribution (Vd/F) of dienogest is 40 L . |
| Clearance | The metabolic clearance rate from serum (Cl/F) is 64 mL/min . |
Formulation & handling
- Oral small‑molecule oxosteroid with low aqueous solubility, typically formulated as coated tablets to aid dissolution and protect from moisture.
- Batches require consideration of CYP3A‑mediated metabolism, as exposure is sensitive to co‑ingested CYP3A inhibitors or inducers during clinical use.
- Solid-state stability is generally good, but handling should limit humidity to prevent degradation and maintain consistent tablet performance.
Regulatory status
| Lifecycle | Most U.S. patent protection for the API has expired, with remaining patents extending to 2026 and 2028, indicating a market transitioning toward later‑stage exclusivity. With sales limited to the U.S. and Canada, the product is moving into a more mature phase as key protections near completion. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Dienogest is supplied through several branded products in the US and Canada, indicating participation from multiple manufacturers rather than a single dominant originator. Branded formulations combining dienogest with estradiol valerate show established market penetration in North America, with similar products available globally. With key U.S. patents already expired and the remaining ones nearing expiry in 2026 and 2028, the molecule is positioned for continued or expanding generic competition. |
|---|
Safety
| Toxicity | Oral LD50 in mouse is 4 mg/kg [MSDS]. In a long-term carcinogenicity study involving rats and mice, exposure of 10 times the dose of maximum recommended clinical dose of dienogest resulted in increased incidences of pituitary adenomas, fibroepithelial mammary tumours, stromal polyps of the uterus and malignant lymphoma . These tumors are thought to arise from marked species differences in the optimal oestrogen:progestogen ratio for reproductive function. In rat liver foci assay, dienogest did not induce tumor promotion activity . Dienogest does not display genotoxic potential. |
|---|
- Exhibits high acute oral toxicity in mice (LD50 ~4 mg/kg), indicating need for controlled handling and exposure minimization in manufacturing environments
- Chronic high‑dose exposure in rodents produced increased incidences of pituitary, mammary, uterine, and lymphoid tumors, reflecting species‑specific hormonal sensitivity rather than genotoxicity
- Demonstrates no genotoxic activity and showed no tumor‑promoting effects in rat liver foci assays, suggesting low intrinsic mutagenic or promotional risk under standard industrial exposure controls
Dienogest is a type of Progestagens
Progestagens are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in hormonal therapies and contraceptives. Also known as progestins, these synthetic compounds mimic the effects of the naturally occurring hormone progesterone in the body.
Progestagens are widely used in various medical applications due to their ability to regulate the menstrual cycle, support pregnancy, and prevent undesired conception. They function by binding to progesterone receptors and modulating the reproductive system's activity.
In addition to their contraceptive properties, progestagens are utilized in hormone replacement therapy (HRT) to alleviate symptoms associated with menopause, such as hot flashes and mood swings. They can also be prescribed to treat irregular menstruation, endometriosis, and certain types of cancer, including breast and uterine cancers.
Pharmaceutical companies develop progestagens in different formulations, including oral tablets, injections, and implants, to cater to diverse patient needs. These formulations offer varying durations of action, allowing healthcare professionals to tailor treatment regimens to individual patients.
While progestagens are generally well-tolerated, they may be associated with certain side effects, such as weight gain, bloating, and breast tenderness. It is essential for healthcare providers to assess patient medical history and monitor their response to progestagen therapy closely.
In conclusion, progestagens are a vital class of pharmaceutical APIs with significant therapeutic applications. Their versatility and effectiveness in hormonal regulation make them a cornerstone of various hormonal therapies, providing patients with safe and reliable options for contraception, HRT, and managing reproductive disorders.
Dienogest (Progestagens), 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.
Dienogest API manufacturers & distributors
Compare qualified Dienogest API suppliers worldwide. We currently have 10 companies offering Dienogest API, with manufacturing taking place in 6 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 | CoA, GMP, USDMF | 42 products |
| Gedeon Richter | Producer | Hungary | Hungary | CoA, GMP | 48 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
| Heyl Chemisch-Pharmazeuti... | Producer | Germany | Germany | CoA, JDMF | 1 products |
| Industriale Chimica | Producer | Italy | Unknown | CoA, JDMF, USDMF | 33 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Qinhuangdao Zizhu | Producer | China | China | CoA, USDMF | 10 products |
| Senova Technology Co., Lt... | Producer | China | China | CoA, ISO9001, USDMF | 157 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CEP, CoA, GMP, ISO9001, USDMF | 757 products |
When sending a request, specify which Dienogest 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 Dienogest 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.
Frequently asked questions about Dienogest API
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