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Alendronic acid | CAS No: 66376-36-1 | GMP-certified suppliers
A medication that treats and prevents osteoporosis and Paget’s disease of bone, including glucocorticoid-induced osteoporosis, in adults with preserved renal function.
Therapeutic categories
Primary indications
- Alendronic acid is indicated for the treatment and prevention of osteoporosis in men and postmenopausal women, treatment of glucocorticoid-induced osteoporosis, and Paget's disease of bone
- However, alendronic acid is not indicated for use in pediatric populations or patients with a creatinine clearance <35mL/min
Product Snapshot
- Alendronic acid is available as oral tablets (including film-coated, effervescent, and delayed-release forms) and intravenous solutions
- It is primarily used for the treatment and prevention of osteoporosis, glucocorticoid-induced osteoporosis, and Paget's disease of bone
- Alendronic acid is approved for use in the US, EU, and Canada
Clinical Overview
Pharmacologically, alendronic acid belongs to the class of bisphosphonates characterized by two phosphonate groups linked through a carbon atom. After oral administration, the drug exhibits very low bioavailability. It distributes rapidly to bone and soft tissues and is not subject to metabolic transformation. The primary route of elimination is renal excretion.
The mechanism of action involves selective binding of alendronic acid to hydroxyapatite crystals in bone. Bone resorption by osteoclasts leads to localized acidification, facilitating the release and uptake of alendronic acid into osteoclasts through fluid-phase endocytosis. Once internalized, the drug induces osteoclast apoptosis by disrupting cellular functions within acidified endocytic vesicles. This osteoclast inhibition reduces bone resorption, as evidenced by decreased urinary biomarkers such as calcium, deoxypyridinoline, and cross-linked N-telopeptides of type I collagen.
Safety considerations include renal impairment, where dose adjustments or avoidance are necessary due to renal clearance as the drug is not metabolized. Muscle-related adverse effects have been reported with bisphosphonate class agents, although specific muscle toxicity risks should be evaluated in context. Monitoring for esophageal irritation associated with oral dosing is advised.
Notable brand names include Fosamax among others, with broad utilization in bone disease management globally. For API procurement, ensuring pharmaceutical-grade quality with stringent adherence to purity, stability, and particle size specifications is critical to guarantee consistent clinical performance and regulatory compliance. Verification of supplier certifications and detailed analytical data is recommended to support global regulatory submissions and manufacturing requirements.
Identification & chemistry
| Generic name | Alendronic acid |
|---|---|
| Molecule type | Small molecule |
| CAS | 66376-36-1 |
| UNII | X1J18R4W8P |
| DrugBank ID | DB00630 |
Pharmacology
| Summary | Alendronic acid is a bisphosphonate that targets bone hydroxyapatite and osteoclasts to inhibit bone resorption. It is internalized by osteoclasts via endocytosis, leading to apoptosis and reduced bone turnover markers. The drug distributes primarily to bone and is excreted unchanged in urine without metabolic transformation. |
|---|---|
| Mechanism of action | Alendronic acid binds to bone hydroxyapatite. Bone resorption causes local acidification, releasing alendronic acid which is that taken into osteoclasts by fluid-phase endocytosis. Endocytic vesicles are acidified, releasing alendronic acid to the cytosol of osteoclasts where they induce apoptosis. Inhibition of osteoclasts results in decreased bone resorption which is shown through decreased urinary calcium, deoxypyridinoline and cross-linked N-telopeptidases of type I collagen. |
| Pharmacodynamics | Alendronic acid tablets have a very low oral bioavialability. After administration it distributes into soft tissue and bone or is excreted in the urine. Alendronic acid does not undergo metabolism. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Farnesyl pyrophosphate synthase | Humans | inhibitor |
| Hydroxylapatite | Humans | antagonist |
| Tyrosine-protein phosphatase non-receptor type 4 | Humans | inhibitor |
ADME / PK
| Absorption | Mean oral bioavailability of alendronic acid in women is 0.64% and in men is 0.59%. Bioavailability of alendronic acid decreases by up to 40% if it is taken within an hour of a meal. |
|---|---|
| Half-life | Due to alendronic acid being incorporated into the skeleton, the terminal half life is estimated to be over 10 years. |
| Protein binding | 78%. Studies in rats show that plasma protein binding increases with decreasing alendronic acid plasma concentration and increasing pH. |
| Metabolism | Urinary excretion is the sole method of elimination of alendronic acid and no metabolites are detected upon urine collection. |
| Route of elimination | Administration of radiolabeled alendronic acid results in 50% recovery in urine within 72 hours. No alendronic acid is recovered in the feces. Men excrete less alendronic acid than women, though race and advanced age do not affect elimination. |
| Volume of distribution | 28L. |
| Clearance | 71mL/min. |
Formulation & handling
- Alendronic acid is a small molecule bisphosphonate administered primarily via oral tablets, with some intravenous formulations available.
- Its absorption is sensitive to food and divalent cations; it must be taken fasting with a full glass of water and before meals to avoid chelation.
- Formulations should consider stability in aqueous media due to high water solubility and the need for appropriate handling to prevent interaction with calcium or antacids.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient is marketed in Canada, the EU, and the US, with key patents having expired between 2012 and 2019, indicating a mature market with potential generic competition in these regions. |
|---|
| Markets | Canada, EU, US |
|---|
Supply Chain
| Supply chain summary | Alendronic acid is manufactured by multiple originator and generic companies, including both global and regional pharmaceutical firms. Branded products are distributed primarily across the US, EU, and Canadian markets. The listed patents have expired or are close to expiry, indicating a landscape with established generic competition. |
|---|
Safety
| Toxicity | In clinical studies, ≥3% of patients experience abdominal pain, acid regurgitation, constipation, diarrhea, dyspepsia, musculoskeletal pain, and nausea. No information for treatment of overdose is available, however patients should be given milk or antacids to bind alendronic acid and vomiting should not be induced. Patients may experience hypocalcemia, hypophosphatemia, and upper gastrointestinal events.. There are currently no studies for safety and efficacy in pregnancy, though studies in pregnant rats show fetal and maternal complications at 4 times the clinical dose and pregnant rabbits do not show complications at as high as 10 times the clincal dose. Excretion in breast milk, and therefore safety in lactation, is unknown. Alendronic acid has been studied for use in pediatric patients. The oral bioavailability is similar to that in adult patients, but an increase in the portion of patients experiencing vomiting. There is no significant difference in efficacy or safety of alendronic acid in geriatric populations, though there is potential for even greater sensitivity in patients at a further advanced age than those in the study. Alendronic acid is not recommended for patients with creatinine clearance <35mL/min, but no dosage adjustment is necessary in hepatic impairment. |
|---|
- Handling alendronic acid requires caution due to potential gastrointestinal irritation and musculoskeletal adverse effects observed in clinical use
- Avoid exposure in populations with severe renal impairment (creatinine clearance ‹35 mL/min) as safety is not established
- No established safety profile for use in pregnancy and lactation
Alendronic acid is a type of Means for diseases of the bone and muscular system
The pharmaceutical API subcategory known as "Means for diseases of the bone and muscular system" refers to a specialized class of active pharmaceutical ingredients (APIs) designed to target and treat various disorders related to the skeletal and muscular systems. These APIs play a crucial role in the development of medications that alleviate symptoms and improve the quality of life for individuals affected by bone and muscular conditions.
One common group of APIs in this subcategory includes bisphosphonates, which are widely used for the treatment of osteoporosis. These compounds inhibit bone resorption, thereby increasing bone density and reducing the risk of fractures. Bisphosphonates act by targeting specific enzymes involved in bone breakdown, preventing excessive bone loss.
Another significant class of APIs for bone and muscular diseases are muscle relaxants. These compounds help alleviate muscle spasms and stiffness associated with conditions such as muscle strains, sprains, and certain neurological disorders. Muscle relaxants work by interfering with the signals sent between the brain and the muscles, inducing relaxation and reducing pain.
Additionally, APIs like calcitonin analogs are utilized for the management of conditions such as Paget's disease and osteoporosis. Calcitonin analogs function by inhibiting osteoclast activity, reducing bone resorption, and promoting bone formation.
In summary, the subcategory of "Means for diseases of the bone and muscular system" encompasses APIs that target bone metabolism, muscle relaxation, and bone remodeling processes. These pharmaceutical ingredients play a vital role in the development of medications aimed at improving the well-being and mobility of individuals suffering from bone and muscular disorders.
Alendronic acid (Means for diseases of the bone and muscular system), classified under Metabolic Bone Disease Agents
Metabolic Bone Disease Agents are a category of pharmaceutical active pharmaceutical ingredients (APIs) that are specifically designed to treat and manage conditions related to the bones and their metabolism. These agents play a crucial role in the treatment of various metabolic bone diseases, including osteoporosis, Paget's disease, and rickets.
The primary function of Metabolic Bone Disease Agents is to regulate bone remodeling and maintain bone health. They achieve this by targeting specific pathways involved in bone metabolism, such as osteoclast and osteoblast activity, calcium regulation, and vitamin D metabolism.
These APIs are commonly used in the development of medications, including oral tablets, injectables, and topical formulations, for the effective treatment of metabolic bone diseases. They are carefully formulated to optimize their pharmacokinetic and pharmacodynamic properties, ensuring maximum efficacy and minimal side effects.
Metabolic Bone Disease Agents encompass a range of substances, including bisphosphonates, selective estrogen receptor modulators (SERMs), calcitonin, and vitamin D analogs. These APIs act through different mechanisms to address specific aspects of bone health, such as inhibiting bone resorption, promoting bone formation, or regulating calcium levels.
In conclusion, Metabolic Bone Disease Agents are a vital category of pharmaceutical APIs used in the development of medications for the treatment and management of various metabolic bone diseases. These agents target specific pathways involved in bone metabolism to regulate bone remodeling, enhance bone health, and alleviate the symptoms associated with these conditions.
Alendronic acid API manufacturers & distributors
Compare qualified Alendronic acid API suppliers worldwide. We currently have 11 companies offering Alendronic acid API, with manufacturing taking place in 4 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 |
|---|---|---|---|---|---|
| Apex Healthcare | Producer | India | India | CoA, WC | 9 products |
| Cipla | Producer | India | India | CoA, GMP, USDMF, WC | 164 products |
| Dr. Sahu's Laboratories | Producer | India | India | CoA | 70 products |
| InventyS Research Company... | Producer | India | India | CoA | 5 products |
| Ipca Labs. | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 69 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Mylan | Producer | India | India | CoA, GMP, JDMF, USDMF, WC | 201 products |
| Polpharma | Producer | Poland | Poland | BSE/TSE, cDMF, CEP, CoA, EDMF/ASMF, FDA, GMP, JDMF, KDMF, MSDS, USDMF | 64 products |
| Sanofi | Producer | France | Unknown | CEP, CoA, GMP | 93 products |
| Signa | Producer | Mexico | Mexico | CoA, USDMF | 42 products |
| Sun Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 219 products |
When sending a request, specify which Alendronic acid 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.).
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