alendronic acid

Trade name: fosamax

Small moleculeapproved

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

Phase 1
13
Phase 2
83
Phase 3
54
Phase 4
45

Earliest trial started Sep 1, 1987 (NCT00005006)

Timeline

1980s

  1. Jan 1, 1987

    Earliest Phase 2 Sponsor(trial)

1990s

  1. Jan 1, 1995

    Merck — Earliest Phase 3 Sponsor(trial)

  2. Sep 29, 1995

    Merck — Earliest FDA Approval

  3. Sep 29, 1995

    Merck — NDA Organization

2000s

  1. Jan 1, 2000

    Teva — Earliest Phase 1 Sponsor(trial)

  2. Apr 7, 2005

    Organon — NDA Secondary Org

  3. Feb 6, 2008

    Impax Laboratories — Marketing Organization

  4. Feb 6, 2008

    Teva — Marketing Organization

  5. Aug 4, 2008

    Apotex — Marketing Organization

  6. Aug 4, 2008

    Aurobindo Pharma — Marketing Organization

  7. Aug 4, 2008

    Cipla — Marketing Organization

  8. Aug 4, 2008

    Mylan — Marketing Organization

  9. Aug 4, 2008

    Neopharma — Marketing Organization

  10. Aug 4, 2008

    Watson Pharmaceuticals — Marketing Organization

  11. Aug 4, 2008

    US Antibiotics — Marketing Organization

  12. Aug 4, 2008

    Picket Pharms — Marketing Organization

  13. Aug 4, 2008

    Rising Pharmaceuticals — Marketing Organization

  14. Sep 10, 2008

    Sun Pharmaceuticals — Marketing Organization

  15. Apr 22, 2009

    Upsher-Smith Laboratories — Marketing Organization

  16. Apr 22, 2009

    Chartwell Pharmaceuticals — Marketing Organization

  17. Sep 24, 2009

    Minsheng Binjiang Pharmaceuticals — Marketing Organization

2010s

  1. Feb 18, 2010

    Jubilant Innovation Ltd. — Marketing Organization

  2. Mar 12, 2012

    Mission Pharmacal — NDA Secondary Org

  3. Mar 12, 2012

    Stamford Pharmaceuticals — Marketing Organization

  4. Mar 12, 2012

    Stamford Pharmaceuticals — NDA Secondary Org

  5. Feb 25, 2013

    West-Ward Pharmaceutical — Marketing Organization

  6. Feb 25, 2013

    Hikma — Marketing Organization

2020s

  1. May 11, 2023

    Novitium Pharma — Marketing Organization

  2. May 11, 2023

    Ani Pharmaceuticals — Marketing Organization

Indications

Studied for

Mechanism of action

Combination products

Approval history

  • approvedPriority reviewSep 29, 1995

Chemistry & pharmacology

Loading structure…

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

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 IDPhaseStart dateSponsor(s)
NCT07216794Phase 2Jan 17, 2026National Institute of Allergy and Infectious Diseases (NIAID)
NCT07245381Phase 1/Phase 2 (Phase 2)Dec 31, 2025Tel Aviv University
NCT06973109Phase 2Dec 31, 2025Amgen, University of Pittsburgh
NCT07242612N/AOct 1, 2025Khyber Medical University Peshawar
NCT06864130Phase 4Feb 21, 2025University of Southern Denmark
NCT06856369Phase 4Jan 22, 2025Bahria University, Islamabad Medical and Dental College
NCT06772792Phase 1Apr 23, 2024Merck
NCT06264609Phase 4Feb 1, 2024University of Kentucky
NCT06264401N/AFeb 1, 2024Cairo University
NCT06016634Phase 2Jan 31, 2024Doris Duke Charitable Foundation, National Heart, Lung, and Blood Institute (NHLBI), University of California, Davis
NCT05645289Phase 4Jan 1, 2023Peking University
NCT05602493Phase 3Nov 16, 2022Xeolas Pharmaceuticals
NCT05527548Phase 4Nov 1, 2022Chinese University of Hong Kong
NCT05493761Phase 4Sep 30, 2022Aristotle University of Thessaloniki, Government of Greece, Hellenic Army
NCT05397938Phase 2Jun 15, 2022Shanghai JMT-Bio Inc.
NCT05305183Phase 3May 31, 2022Shandong New Time Pharmaceutical Co., LTD
NCT05151484Phase 4Dec 15, 2021National Institute on Aging (NIA), University of Kentucky
NCT07028320Phase 3Dec 3, 2021Jiao Tong University, Shenzhen Salubris Pharmaceuticals Co., Ltd.
NCT05091099Phase 4Nov 20, 2021National Taiwan University
NCT05325515Phase 4Oct 1, 2021Aarhus University
Showing 20 of 163 trials
Page 1 / 9

Organizations

Research & Development (155)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
MerckFor profit322141995
AmgenFor profit13822002
Harvard UniversityAcademic/Hospital12941999
National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)Government8131987
Government Dental College and Research Institute, BangaloreAcademic/Hospital5522009
Columbia UniversityAcademic/Hospital4431997
Eli LillyFor profit4422001
Chinese University of Hong KongAcademic/Hospital3322006
GlaxoSmithKlineFor profit3232005
National Cancer Institute (NCI)Government3131999
National Institute of Allergy and Infectious Diseases (NIAID)Government3312003
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)Government3122002
National Institutes of Health (NIH)Government3121998
National Taiwan UniversityAcademic/Hospital3212005
University of California, San FranciscoAcademic/Hospital3231999
University of KentuckyAcademic/Hospital3322015
University of PittsburghAcademic/Hospital3222002
Aarhus UniversityAcademic/Hospital2222015
BIOrest Ltd.For profit2212008
Elizabeth Glaser Pediatric AIDS FoundationAcademic/Hospital2012002
155 organizations
Page 1 / 8

Marketing (30)

OrganizationOrg typeRelationshipDate
Ani PharmaceuticalsFor profitMKTGMay 11, 2023
ApotexFor profitMKTGAug 4, 2008
Aurobindo PharmaFor profitMKTGAug 4, 2008
Chartwell PharmaceuticalsFor profitMKTGApr 22, 2009
CiplaFor profitMKTGAug 4, 2008
HikmaFor profitMKTGFeb 25, 2013
HikmaFor profitSYNFeb 25, 2013
Impax LaboratoriesFor profitMKTGFeb 6, 2008
Jubilant Innovation Ltd.For profitMKTGFeb 18, 2010
MerckFor profitSYNSep 29, 1995
MerckFor profitNDASep 29, 1995
Minsheng Binjiang PharmaceuticalsFor profitMKTGSep 24, 2009
Mission PharmacalFor profitNDA2Mar 12, 2012
MylanFor profitMKTGAug 4, 2008
NeopharmaFor profitMKTGAug 4, 2008
Novitium PharmaFor profitMKTGMay 11, 2023
OrganonFor profitNDA2Apr 7, 2005
OrganonFor profitSYNApr 7, 2005
Picket PharmsFor profitMKTGAug 4, 2008
Rising PharmaceuticalsFor profitMKTGAug 4, 2008
Rising PharmaceuticalsFor profitSYNAug 4, 2008
Stamford PharmaceuticalsFor profitMKTGMar 12, 2012
Stamford PharmaceuticalsFor profitNDA2Mar 12, 2012
Sun PharmaceuticalsFor profitMKTGSep 10, 2008
Sun PharmaceuticalsFor profitSYNSep 10, 2008
TevaFor profitMKTGFeb 6, 2008
US AntibioticsFor profitMKTGAug 4, 2008
Upsher-Smith LaboratoriesFor profitMKTGApr 22, 2009
Watson PharmaceuticalsFor profitMKTGAug 4, 2008
West-Ward PharmaceuticalFor profitMKTGFeb 25, 2013