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Ospemifene | CAS No: 128607-22-7 | GMP-certified suppliers
A medication that treats moderate to severe dyspareunia and vaginal dryness associated with menopause, providing targeted relief for genitourinary symptoms in postmenopausal women.
Therapeutic categories
Primary indications
- Ospemifene is indicated for the treatment of moderate to severe dyspareunia and vaginal dryness associated with menopause
Product Snapshot
- Ospemifene is formulated as an oral tablet, including film-coated variants
- It is primarily indicated for managing moderate to severe dyspareunia and vaginal dryness associated with menopause
- The product is approved for use in the US, Canada, and the EU, with regulatory status ranging from approved to investigational
Clinical Overview
Pharmacodynamically, ospemifene exhibits binding affinity for estrogen receptors, with half maximal inhibitory concentrations (IC50) of approximately 0.8 μM for ER alpha and 1.7 μM for ER beta. It functions as a tissue-selective estrogen receptor modulator, exerting agonistic effects on the endometrium while modulating estrogenic activity in other tissues. This mechanism underlies its utility in addressing menopausal symptoms and suggests potential benefits in osteoporosis management through the modulation of osteoblast and osteoclast activity, resulting in reduced bone turnover. Preclinical evidence also indicates a dose-dependent reduction in tumor incidence, suggesting conceivable chemopreventive properties.
Ospemifene is metabolized primarily via cytochrome P450 enzymes, including CYP2B6, CYP2C19, CYP2C9, CYP2D6, and CYP3A4 isoforms, with weak inhibition noted on CYP2D6 activity. Its classification as both a substrate and inhibitor of cytochrome P450 enzymes necessitates careful consideration of potential drug-drug interactions in clinical use.
Safety considerations include the compound’s agonistic impact on estrogen receptors, warranting cautious use in patients with a history of estrogen-dependent neoplasms. Adverse effect profiles and long-term safety data remain integral to risk assessment.
Commercially, ospemifene is available under various proprietary formulations intended for oral administration. Procurement of the active pharmaceutical ingredient (API) requires attention to compliance with pharmacopeial standards, including purity, residual solvents, and stability. Due to its metabolism via multiple CYP enzymes, consistent batch quality is critical to ensure predictable pharmacokinetics and minimize variability in clinical response. Suppliers should demonstrate adherence to Good Manufacturing Practice (GMP) and provide robust analytical characterization data alongside their product.
Identification & chemistry
| Generic name | Ospemifene |
|---|---|
| Molecule type | Small molecule |
| CAS | 128607-22-7 |
| UNII | B0P231ILBK |
| DrugBank ID | DB04938 |
Pharmacology
| Summary | Ospemifene is a selective estrogen receptor modulator (SERM) that exhibits tissue-specific estrogen receptor agonist or antagonist activity, primarily targeting estrogen receptor alpha. It exerts agonistic effects on the endometrium and modulates bone remodeling by influencing osteoblast and osteoclast activity, leading to reduced bone turnover. Ospemifene’s pharmacological profile supports its use in managing menopausal symptoms and shows potential in osteoporosis treatment and breast cancer prevention. |
|---|---|
| Mechanism of action | Ospemifene is a next generation SERM (selective estrogen receptor modulator) that selectively binds to estrogen receptors and either stimulates or blocks estrogen's activity in different tissue types. It has an agonistic effect on the endometrium. |
| Pharmacodynamics | The half maximal inhibitory concentration (IC50) for estrogen receptor (ER) alpha and beta are 0.8 μM and 1.7 μM, respectively. Ospemifene has potential uses in the management of osteoporosis in postmenopausal women. It interacts with osteoblasts and osteoclasts in such a way that it reduces bone turnover. It also has potential uses in the prevention of breast cancer. Studies suggest that ospemifene, in a dose-dependent manner, reduces the incidence of tumours. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Estrogen receptor alpha | Humans | antagonist, agonist |
ADME / PK
| Absorption | When a single oral dose of ospemifene 60 mg is given to postmenopausal women under fasted conditions, the pharmacokinetic parameters are as follows: Tmax = 2 hours (range of 1 - 8 hours); Cmax = 533 ng/mL; AUC (0-inf) = 4165 ng•hr/mL. When the same aforementioned dose is given to postmenopausal women under fed conditions, the pharmacokinetic parameters are as follows: Tmax = 2.5 hours (1 - 6 hours); Cmax = 1198 ng/mL; AUC (0-inf) = 7521 ng•hr/mL. Accumulation occurs following repeated doses. Time to steady state = 9 days. Although the bioavailability of ospemifene has not been formally evaluated, it is expected to have a low bioavailability because of its lipophilic nature. |
|---|---|
| Half-life | Terminal half-life = 26 hours . |
| Protein binding | >99% bound to serum proteins |
| Metabolism | Ospemifene is hepatically metabolized via CYP3A4, CYP2C9, CYP2C19, and CYP2B6. The major metabolite was 4-hydroxyospemifene, 25% of the parent compound will undergo this biotransformation. Other metabolites include 4'-hydroxy-ospemifene, <7% of the parent compound will undergo this biotransformation. In order of decreasing potency, ospemifene was suggested to be a weak inhibitor for CYP2B6, CYP2C9, CYP2C19, CYP2C8, CYP2D6 and CYP3A4. |
| Route of elimination | Following an oral administration of ospemifene, approximately 75% and 7% of the dose was excreted in feces and urine, respectively. Less than 0.2% of the ospemifene dose was excreted unchanged in urine. |
| Volume of distribution | 448 L |
| Clearance | Total body clearance = 9.16 L/hr. |
Formulation & handling
- Ospemifene is a small molecule administered orally as film-coated tablets with low water solubility.
- Formulations should consider its lipophilicity (LogP 5.56) to optimize bioavailability and absorption.
- Handling instructions include advising administration with food to enhance absorption and minimize variability.
Regulatory status
| Lifecycle | The API is approaching patent expirations in the United States between 2024 and 2026, indicating a transition toward a more mature market phase in the US, with established presence in the US, Canada, and EU markets. |
|---|
| Markets | US, Canada, EU |
|---|
Supply Chain
| Supply chain summary | Ospemifene is marketed under several branded products primarily in the US, Canada, and EU, indicating the presence of multiple originator companies involved in its supply. The existing patents are predominantly US-based with expiration dates ranging from 2020 to 2026, suggesting that while some generic competition may already exist, additional generic entries could enter the market as patents expire through 2026. This landscape supports a mixed supply environment with ongoing patent protection and emerging generic availability. |
|---|
Safety
| Toxicity | Adverse reactions (≥1 percent) include: hot flush, vaginal discharge, muscle spasms, genital discharge, hyperhidrosis. |
|---|
- Potential adverse reactions include hot flush, hyperhidrosis, muscle spasms, and genital or vaginal discharge
- Handle with appropriate protective equipment to minimize exposure and avoid dermal or mucosal contact
- Use in well-ventilated areas to reduce inhalation risk due to possible irritant properties
Ospemifene 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.
Ospemifene (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.
Ospemifene API manufacturers & distributors
Compare qualified Ospemifene API suppliers worldwide. We currently have 6 companies offering Ospemifene 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 |
|---|---|---|---|---|---|
| Cambrex | Producer | Italy | United States | CoA, GMP | 104 products |
| Cambrex, Karlskoga | Producer | Sweden | Sweden | CoA, USDMF | 8 products |
| Fermion | Producer | Finland | Finland | CoA, USDMF | 29 products |
| Honour Lab | Producer | India | India | CoA, GMP, USDMF, WC | 30 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Weijie Pharmaceuticals | Producer | China | China | CoA, USDMF | 15 products |
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