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Fulvestrant | CAS No: 129453-61-8 | GMP-certified suppliers
A medication that treats hormone receptor positive metastatic breast cancer in postmenopausal women, offering an option for disease progression after prior endocrine therapy.
Therapeutic categories
Primary indications
- For the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti-estrogen therapy, as monotherapy or in combination with other antineoplastic agents
Product Snapshot
- Fulvestrant is an intramuscular parenteral injectable endocrine agent
- It is used for hormone receptor–positive metastatic breast cancer after progression on prior anti‑estrogen therapy, as monotherapy or in combination with other antineoplastic agents
- It is approved in the US, EU, and Canada, with additional investigational use in some markets
Clinical Overview
Pharmacologically, fulvestrant is classified among estrogens and derivatives, derived structurally from 3‑hydroxylated estrane steroids. Despite this structural relationship, it displays no known estrogen agonist activity. Its pharmacodynamic profile is characterized by pure antagonism at the estrogen receptor, leading to suppression of estrogen‑mediated signaling in tumors dependent on this pathway.
The mechanism of action involves competitive and reversible binding to estrogen receptors in malignant cells. Fulvestrant downregulates receptor expression and promotes receptor degradation, thereby reducing cellular sensitivity to endogenous estrogens. These dual actions inhibit proliferation in both tamoxifen‑resistant and estrogen‑sensitive breast cancer cell lines.
Available clinical and pharmacokinetic data identify fulvestrant as a substrate of CYP3A pathways and UGT1A1, although extensive metabolism details beyond these classifications vary by study. Following intramuscular administration, absorption is gradual, and systemic exposure is influenced by depot release characteristics. Elimination is primarily hepatic, with no known active metabolites of clinical relevance reported in the provided data.
Safety considerations include injection‑site reactions, hepatic function monitoring, and evaluation for estrogen deprivation–related effects. Toxicity profiles generally reflect its endocrine mechanism, and use should consider comorbid hepatic impairment and potential interactions with strong CYP3A modulators.
Fulvestrant is widely recognized in clinical practice, with established use in metastatic settings where endocrine resistance has emerged. For API procurement, sourcing should prioritize compliance with regulatory standards, verified impurity controls, and consistent polymorphic form to support robust formulation performance and regulatory submissions.
Identification & chemistry
| Generic name | Fulvestrant |
|---|---|
| Molecule type | Small molecule |
| CAS | 129453-61-8 |
| UNII | 22X328QOC4 |
| DrugBank ID | DB00947 |
Pharmacology
| Summary | Fulvestrant is an estrogen receptor antagonist that binds competitively to estrogen receptor alpha and blocks estrogen‑driven signaling. It promotes receptor downregulation and degradation, reducing proliferation of estrogen‑dependent and tamoxifen‑resistant breast cancer cells. These pharmacologic actions support its use in hormone receptor–positive metastatic breast cancer after anti‑estrogen therapy. |
|---|---|
| Mechanism of action | Fulvestrant competitively and reversibly binds to estrogen receptors present in cancer cells and achieves its anti-estrogen effects through two separate mechanisms. First, fulvestrant binds to the receptors and downregulates them so that estrogen is no longer able to bind to these receptors. Second, fulvestrant degrades the estrogen receptors to which it is bound. Both of these mechanisms inhibit the growth of tamoxifen-resistant as well as estrogen-sensitive human breast cancer cell lines. |
| Pharmacodynamics | Fulvestrant for intramuscular administration is an estrogen receptor antagonist without known agonist effects. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Estrogen receptor alpha | Humans | antagonist |
ADME / PK
| Half-life | 40 days |
|---|---|
| Protein binding | 99% (mainly VLDL, LDL, and HDL) |
| Metabolism | Metabolism of fulvestrant appears to involve combinations of a number of possible biotransformation pathways analogous to those of endogenous steroids, including oxidation, aromatic hydroxylation, conjugation with glucuronic acid and/or sulphate at the 2, 3 and 17 positions of the steroid nucleus, and oxidation of the side chain sulphoxide. Identified metabolites are either less active or exhibit similar activity to fulvestrant in antiestrogen models. Studies using human liver preparations and recombinant human enzymes indicate that cytochrome P-450 3A4 (CYP 3A4) is the only P-450 isoenzyme involved in the oxidation of fulvestrant; however, the relative contribution of P-450 and non-P-450 routes in vivo is unknown. |
| Route of elimination | Fulvestrant was rapidly cleared by the hepatobiliary route with excretion primarily via the feces (approximately 90%). Renal elimination was negligible (less than 1%). |
| Volume of distribution | * 3 to 5 L/kg |
Formulation & handling
- Fulvestrant is a highly lipophilic small‑molecule steroid requiring intramuscular or parenteral delivery due to extremely low aqueous solubility.
- Formulations rely on solvent or oil-based systems to solubilize the API and ensure uniform dosing given its high LogP and solid-state properties.
- Handling requires attention to precipitation risk and viscosity management to maintain stability and injectability during manufacturing and filling.
Regulatory status
| Lifecycle | Most core patents for the API expired in 2021 across Canada and the United States, indicating that the product is now in a mature post‑exclusivity phase. With availability in Canada, the US, and the EU, the market is likely characterized by established competition and generic participation. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Fulvestrant is supplied primarily by a single originator company, with additional packagers supporting distribution in North America and Europe. Branded products are established in the US, EU, and Canada, indicating broad global availability. Key patents expired in 2021, suggesting that generic competition is already present or likely to expand. |
|---|
Safety
| Toxicity | There is no clinical experience with overdosage in humans. |
|---|
- Human overdosage data are unavailable
- Handling protocols should account for unknown acute toxicity margins
- Monitor for class‑consistent endocrine and hepatic liabilities common to hormone‑modulating antineoplastic agents during development or scale‑up work
Fulvestrant is a type of Anti-estrogens
Anti-estrogens are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the field of medicine. These compounds are specifically designed to counteract the effects of estrogens, a group of hormones primarily responsible for regulating various physiological processes in the body, particularly in females.
Anti-estrogens act by binding to estrogen receptors, either blocking or reducing the effects of estrogen in target tissues. This mechanism of action makes them valuable in the treatment of estrogen-related conditions, such as certain types of breast cancer, endometriosis, and infertility. Additionally, anti-estrogens are commonly used in hormone replacement therapy and as an adjunct in assisted reproductive technologies.
One widely used anti-estrogen API is Tamoxifen, which selectively inhibits estrogen receptors in breast tissue, thus impeding the growth of estrogen-sensitive breast cancers. Another notable anti-estrogen is Clomiphene, which is employed in the management of female infertility by promoting ovulation.
The development and utilization of anti-estrogen APIs have significantly advanced medical treatment options, providing improved outcomes for patients dealing with estrogen-related disorders. These compounds are typically synthesized through complex chemical processes, ensuring high purity and pharmaceutical grade standards.
In summary, anti-estrogen APIs offer targeted therapy for conditions influenced by estrogens. Their ability to modulate estrogen receptor activity makes them essential tools in cancer treatment, reproductive medicine, and hormone therapy, ultimately contributing to better patient care and overall well-being.
Fulvestrant (Anti-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.
Fulvestrant API manufacturers & distributors
Compare qualified Fulvestrant API suppliers worldwide. We currently have 17 companies offering Fulvestrant API, with manufacturing taking place in 10 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 |
|---|---|---|---|---|---|
| Apino Pharma Co., Ltd. | Producer | China | China | BSE/TSE, CoA, GMP, USDMF | 229 products |
| AXXO GmbH | Distributor | Germany | World | CoA, GMP, GDP, MSDS, USDMF | 243 products |
| Cambrex | Producer | Italy | United States | CoA, GMP | 104 products |
| Farmabios | Producer | Italy | Italy | CEP, CoA, GMP, ISO9001, USDMF | 58 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 |
| KRKA | Producer | Slovenia | Slovenia | CoA, GMP | 81 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Lianyungang Runzhong | Producer | China | China | CoA, USDMF | 6 products |
| Minakem | Producer | France | Belgium | CEP, CoA, FDA, GMP, USDMF | 31 products |
| Natco Pharma | Producer | India | India | CoA, WC | 40 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, CoA, FDA, GMP, MSDS | 64 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sicor | Producer | Italy | Italy | CoA, GMP | 47 products |
| Sun Pharma | Producer | India | India | CoA, GMP, WC | 219 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 146 products |
| Xi’an Libang | Producer | China | China | CoA, WC | 2 products |
When sending a request, specify which Fulvestrant 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 Fulvestrant 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 Fulvestrant API
Sourcing
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Technical
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Regulatory
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Pharmaoffer
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