alendronic acid
Trade name: fosamax
Approved
Sep 29, 1995
Alendronic acid is a bisphosphonate drug used for osteoporosis, osteogenesis imperfecta, and several other bone diseases. It is marketed alone as well as in combination with vitamin D. Alendronate inhibits osteoclast-mediated bone-resorption. Like all bisphosphonates, it is chemically related to inorganic pyrophosphate, the endogenous regulator of bone turnover. But while pyrophosphate inhibits both osteoclastic bone resorption and the mineralization of the bone newly formed by osteoblasts, alendronate specifically inhibits bone resorption without any effect on mineralization at pharmacologically achievable doses. Its inhibition of bone-resorption is dose-dependent and approximately 1,000 times stronger than the equimolar effect of the first bisphosphonate drug, etidronate. Under therapy, normal bone tissue develops, and alendronate is deposited in the bone-matrix in a pharmacologically inactive form. For optimal action, enough calcium and vitamin D are needed in the body in order to promote normal bone development. Hypocalcemia should, therefore, be corrected before starting therapy. Treatment of post-menopausal women and people with osteogenesis imperfecta over the age of 22 with alendronic acid has demonstrated normalization of the rate of bone turnover, significant increase in BMD (bone mineral density) of the spine, hip, wrist and total body, and significant reductions in the risk of vertebral (spine) fractures, wrist fractures, hip fractures, and all non-vertebral fractures. In the Fracture Intervention Trial, the women with the highest risk of fracture (by virtue of pre-existing vertebral fractures) were treated with Fosamax 5 mg/day for two years followed by 10 mg/day for the third year. This resulted in approximately 50% reductions in fractures of the spine, hip, and wrist compared with the control group taking placebos. Both groups also took calcium and vitamin D. — NCATS
Clinical trial activity
163 trials · 155 clinical orgs · 24 marketing orgs
Earliest trial started Sep 1, 1987 (NCT00005006)
Timeline
1980s
- Jan 1, 1987
Earliest Phase 2 Sponsor(trial)
1990s
2000s
- Jan 1, 2000
- Apr 7, 2005
Organon — NDA Secondary Org
- Feb 6, 2008
Impax Laboratories — Marketing Organization
- Feb 6, 2008
Teva — Marketing Organization
- Aug 4, 2008
Apotex — Marketing Organization
- Aug 4, 2008
Aurobindo Pharma — Marketing Organization
- Aug 4, 2008
Cipla — Marketing Organization
- Aug 4, 2008
Mylan — Marketing Organization
- Aug 4, 2008
Neopharma — Marketing Organization
- Aug 4, 2008
Watson Pharmaceuticals — Marketing Organization
- Aug 4, 2008
US Antibiotics — Marketing Organization
- Aug 4, 2008
Picket Pharms — Marketing Organization
- Aug 4, 2008
Rising Pharmaceuticals — Marketing Organization
- Sep 10, 2008
Sun Pharmaceuticals — Marketing Organization
- Apr 22, 2009
Upsher-Smith Laboratories — Marketing Organization
- Apr 22, 2009
Chartwell Pharmaceuticals — Marketing Organization
- Sep 24, 2009
Minsheng Binjiang Pharmaceuticals — Marketing Organization
2010s
- Feb 18, 2010
Jubilant Innovation Ltd. — Marketing Organization
- Mar 12, 2012
Mission Pharmacal — NDA Secondary Org
- Mar 12, 2012
Stamford Pharmaceuticals — Marketing Organization
- Mar 12, 2012
Stamford Pharmaceuticals — NDA Secondary Org
- Feb 25, 2013
West-Ward Pharmaceutical — Marketing Organization
- Feb 25, 2013
Hikma — Marketing Organization
2020s
- May 11, 2023
Novitium Pharma — Marketing Organization
- May 11, 2023
Ani Pharmaceuticals — Marketing Organization
Indications
Studied for
- Alveolar Bone Loss · Phase 3
- Anemia, Sickle Cell · Phase 2
- Anorexia Nervosa · Phase 3
- Anterior Cruciate Ligament Injuries · Phase 4
- Aortic Stenosis, Subvalvular · Phase 2
- Arteriosclerosis · Phase 4
- Arthritis, Rheumatoid · Phase 4
- Asthma · Phase 2/Phase 3
- Back Pain · Phase 4
- Bone Diseases · Phase 4
- Bone Diseases, Metabolic · Phase 4
- Bone Resorption · Phase 4
- Breast Neoplasms · Phase 3
- Cerebral Palsy · Phase 3
- Chronic Periodontitis · Phase 2/Phase 3
- Coronary Stenosis · Phase 2
- Cystic Fibrosis · Phase 4
- Depression · Phase 4
- Depressive Disorder · Phase 4
- Diabetes Mellitus · Phase 2
- Drug-Related Side Effects and Adverse Reactions · Phase 3
- Feeding and Eating Disorders · Phase 3
- Fibrous Dysplasia, Polyostotic · Phase 2
- Gaucher Disease · Phase 2
- Giant Cell Arteritis · Phase 3
- Granulomatosis with Polyangiitis · Phase 3
- Healthy Volunteers · Phase 4
- Heart Transplantation · Phase 3
- Hepatitis B · Phase 1
- HIV · Phase 2
- HIV Infections · Phase 3
- Hyperparathyroidism · Phase 4
- Hyperparathyroidism, Primary · Phase 4
- Hypogonadism · Phase 3
- Intraocular Pressure · Phase 2
- Kidney Failure, Chronic · Phase 4
- Kidney Transplantation · Phase 2/Phase 3
- Liver Transplantation · Phase 2/Phase 3
- Multiple Myeloma · Phase 3
- Necrosis · Phase 2
- Neoplasm Metastasis · Phase 2
- Non-alcoholic Fatty Liver Disease · Phase 4
- Osteitis Deformans · Phase 4
- Osteoarthritis · Phase 2
- Osteoarthritis, Knee · Phase 4
- Osteogenesis Imperfecta · Phase 4
- Osteonecrosis · Phase 2
- Osteoporosis · Phase 4
- Osteoporosis, Postmenopausal · Phase 4
- Ovarian Neoplasms · Phase 2
- Paralysis · Phase 2
- Periodontal Diseases · Phase 4
- Periodontitis · Phase 4
- Peritoneal Dialysis · Phase 4
- Polymyalgia Rheumatica · Phase 3
- Polymyositis · Phase 3
- Prostatic Neoplasms · Phase 3
- Spinal Cord Injuries · Phase 2
- Spondylitis, Ankylosing · Phase 4
- Traumatology · Phase 4
- Uterine Cervical Neoplasms · Phase 1/Phase 2
- Vascular Calcification · Phase 4
- Vascular Diseases · Phase 2
- Vitamin D Deficiency · Phase 3
Mechanism of action
- Geranylgeranyl pyrophosphate synthaseANTAGONIST
BTS1 antagonist
Combination products
fosamax plus
with vitamin d3
Approval history
- approvedPriority reviewSep 29, 1995
Chemistry & pharmacology
SMILES
NCCCC(O)(P(=O)(O)O)P(=O)(O)O- Mol. weight
- 249.1 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL870 ↗
- WikipediaAlendronic acid ↗
- NCATSX1J18R4W8P ↗
- ChEMBLCHEMBL675 ↗
Also known as
- 4-amino-1-hydroxybutane-1,1-diphosphonic acid
- 4-amino-1-hydroxybutane-1,1-diphosphonic acid
- (4-amino-1-hydroxybutane-1,1-diyl)bis(phosphonic acid)
- (4-amino-1-hydroxybutane-1,1-diyl)bis(phosphonic acid)
- (4-amino-1-hydroxybutylidene)bisphosphonic acid
- (4-amino-1-hydroxybutylidene)bisphosphonic acid
- abdp
- abdp
- acide alendronique
- acide alendronique
- acido alendronico
- acido alendronico
- acidum alendronicum
- acidum alendronicum
- aldrenodate
- alendronate
- alendronate
- alendronate
- alendronate
- alendronate
- alendronate
- alendronate sodium
- alendronate sodium
- alendronate sodium
- alendronate sodium
- alendronate sodium trihydrate / colecalciferol
- alendronic acid
- alendronic acid
- alendronic acid
- alendronic acid
- alendronic acid
- alendronic acid
- alendronic acid / colecalciferol
- binosto
- binosto
- biphosphonate
- biphosphonate
- bisphosphonate
- bisphosphonate
- bisphosphonates
- fosamax
- fosamax
- fosamax
- fosamax
- g-704650
- g-704650
- labr-312
- mk0217
- mk-217
- mk-217
- mk-217
- sodium alendronate
- sodium alendronate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07216794 | Phase 2 | Jan 17, 2026 | National Institute of Allergy and Infectious Diseases (NIAID) |
| NCT07245381 | Phase 1/Phase 2 (Phase 2) | Dec 31, 2025 | Tel Aviv University |
| NCT06973109 | Phase 2 | Dec 31, 2025 | Amgen, University of Pittsburgh |
| NCT07242612 | N/A | Oct 1, 2025 | Khyber Medical University Peshawar |
| NCT06864130 | Phase 4 | Feb 21, 2025 | University of Southern Denmark |
| NCT06856369 | Phase 4 | Jan 22, 2025 | Bahria University, Islamabad Medical and Dental College |
| NCT06772792 | Phase 1 | Apr 23, 2024 | Merck |
| NCT06264609 | Phase 4 | Feb 1, 2024 | University of Kentucky |
| NCT06264401 | N/A | Feb 1, 2024 | Cairo University |
| NCT06016634 | Phase 2 | Jan 31, 2024 | Doris Duke Charitable Foundation, National Heart, Lung, and Blood Institute (NHLBI), University of California, Davis |
| NCT05645289 | Phase 4 | Jan 1, 2023 | Peking University |
| NCT05602493 | Phase 3 | Nov 16, 2022 | Xeolas Pharmaceuticals |
| NCT05527548 | Phase 4 | Nov 1, 2022 | Chinese University of Hong Kong |
| NCT05493761 | Phase 4 | Sep 30, 2022 | Aristotle University of Thessaloniki, Government of Greece, Hellenic Army |
| NCT05397938 | Phase 2 | Jun 15, 2022 | Shanghai JMT-Bio Inc. |
| NCT05305183 | Phase 3 | May 31, 2022 | Shandong New Time Pharmaceutical Co., LTD |
| NCT05151484 | Phase 4 | Dec 15, 2021 | National Institute on Aging (NIA), University of Kentucky |
| NCT07028320 | Phase 3 | Dec 3, 2021 | Jiao Tong University, Shenzhen Salubris Pharmaceuticals Co., Ltd. |
| NCT05091099 | Phase 4 | Nov 20, 2021 | National Taiwan University |
| NCT05325515 | Phase 4 | Oct 1, 2021 | Aarhus University |
Organizations
Research & Development (155)
Marketing (30)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Ani Pharmaceuticals | For profit | MKTG | May 11, 2023 |
| Apotex | For profit | MKTG | Aug 4, 2008 |
| Aurobindo Pharma | For profit | MKTG | Aug 4, 2008 |
| Chartwell Pharmaceuticals | For profit | MKTG | Apr 22, 2009 |
| Cipla | For profit | MKTG | Aug 4, 2008 |
| Hikma | For profit | MKTG | Feb 25, 2013 |
| Hikma | For profit | SYN | Feb 25, 2013 |
| Impax Laboratories | For profit | MKTG | Feb 6, 2008 |
| Jubilant Innovation Ltd. | For profit | MKTG | Feb 18, 2010 |
| Merck | For profit | SYN | Sep 29, 1995 |
| Merck | For profit | NDA | Sep 29, 1995 |
| Minsheng Binjiang Pharmaceuticals | For profit | MKTG | Sep 24, 2009 |
| Mission Pharmacal | For profit | NDA2 | Mar 12, 2012 |
| Mylan | For profit | MKTG | Aug 4, 2008 |
| Neopharma | For profit | MKTG | Aug 4, 2008 |
| Novitium Pharma | For profit | MKTG | May 11, 2023 |
| Organon | For profit | NDA2 | Apr 7, 2005 |
| Organon | For profit | SYN | Apr 7, 2005 |
| Picket Pharms | For profit | MKTG | Aug 4, 2008 |
| Rising Pharmaceuticals | For profit | MKTG | Aug 4, 2008 |
| Rising Pharmaceuticals | For profit | SYN | Aug 4, 2008 |
| Stamford Pharmaceuticals | For profit | MKTG | Mar 12, 2012 |
| Stamford Pharmaceuticals | For profit | NDA2 | Mar 12, 2012 |
| Sun Pharmaceuticals | For profit | MKTG | Sep 10, 2008 |
| Sun Pharmaceuticals | For profit | SYN | Sep 10, 2008 |
| Teva | For profit | MKTG | Feb 6, 2008 |
| US Antibiotics | For profit | MKTG | Aug 4, 2008 |
| Upsher-Smith Laboratories | For profit | MKTG | Apr 22, 2009 |
| Watson Pharmaceuticals | For profit | MKTG | Aug 4, 2008 |
| West-Ward Pharmaceutical | For profit | MKTG | Feb 25, 2013 |