Alendronic Acid
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Also known as Acide alendroniqueAcido alendronicoAlendronateBinostoFosamaxAendronateACIDE_ALENDRONIQUEALENDRONIC_acidALENDRONATE SODIUM TRIHYDRATE
Summary
Alendronic Acid (CHEMBL870) is an approved small-molecule EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor (ATC M05BA04) targeting FDPS; indicated across 17 conditions including bone disorder and osteoporosis.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: M05BA04
- Targets: 1 (FDPS)
- Indications: 17 conditions
- Clinical trials: 127
- Chemistry: 249.1 Da · C4H13NO7P2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL870 |
| Name | Alendronic Acid |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 2088 |
| ChEBI | CHEBI:2567 |
| ATC | M05BA04 |
| Molecular formula | C4H13NO7P2 |
| Molecular weight | 249.1 |
| InChIKey | OGSPWJRAVKPPFI-UHFFFAOYSA-N |
SMILES: C(CC(O)(P(=O)(O)O)P(=O)(O)O)CN
IUPAC name: (4-amino-1-hydroxy-1-phosphonobutyl)phosphonic acid
ChEBI definition: A 1,1-bis(phosphonic acid) that is methanebis(phosphonic acid) in which the two methylene hydrogens are replaced by hydroxy and 3-aminopropyl groups.
Pharmacological roles (ChEBI): EC 2.5.1.1 (dimethylallyltranstransferase) inhibitor, bone density conservation agent.
Also known as: Acide alendronique, Acido alendronico, Alendronate, Alendronic acid, Binosto, Fosamax, alendronate, Aendronate, Alendronic Acid, ACIDE_ALENDRONIQUE, ALENDRONIC ACID, ALENDRONIC_acid
Parent form; salt/anhydrous children: CHEMBL675, CHEMBL2367465
Patent coverage: 10,706 distinct patent families (36,141 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| FDPS | farnesyl diphosphate synthase | Inhibition | 6.34 | 72.4% | P14324 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Farnesyl pyrophosphate synthase, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A.
Bioactivity
ChEMBL activities: 11 potent at pChembl ≥ 5 of 11 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| FDPS | 7.36 | Ki | 44.2 | nM | CHEMBL_ACT_2155095 |
| FDPS | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_12049464 |
| FDPS | 7.3 | IC50 | 50 | nM | CHEMBL_ACT_899107 |
| FDPS | 7.04 | Ki | 91 | nM | CHEMBL_ACT_1077886 |
| FDPS | 6.58 | IC50 | 260 | nM | CHEMBL_ACT_2155094 |
| FDPS | 6.41 | Ki | 393.1 | nM | CHEMBL_ACT_2155051 |
| FDPS | 6.34 | IC50 | 460 | nM | CHEMBL_ACT_24973369 |
| FDPS | 6.02 | IC50 | 950 | nM | CHEMBL_ACT_1077885 |
| FDPS | 6.02 | IC50 | 955 | nM | CHEMBL_ACT_1077887 |
| PDE3A | 5.96 | AC50 | 1091 | nM | CHEMBL_ACT_25190900 |
| FDPS | 5.65 | IC50 | 2249 | nM | CHEMBL_ACT_2155050 |
Target pathways
Aggregated over 1 target gene(s): FDPS.
Top Reactome pathways
3 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Cholesterol biosynthesis | 1 | FDPS |
| Activation of gene expression by SREBF (SREBP) | 1 | FDPS |
| Lanosterol biosynthesis | 1 | FDPS |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cholesterol biosynthetic process | 1 |
| geranyl diphosphate biosynthetic process | 1 |
| trans, trans-farnesyl diphosphate biosynthetic process | 1 |
| lipid metabolic process | 1 |
| steroid biosynthetic process | 1 |
| steroid metabolic process | 1 |
| cholesterol metabolic process | 1 |
| isoprenoid biosynthetic process | 1 |
| sterol biosynthetic process | 1 |
Indications & clinical
Indications
17 indications (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| bone disorder | 4 | MONDO:0005381 | EFO:0004260 |
| osteoporosis | 3 | MONDO:0005298 | EFO:0003882 |
| postmenopausal osteoporosis | 3 | MONDO:0008159 | EFO:0003854 |
| prostate adenocarcinoma | 3 | MONDO:0005082 | EFO:0000673 |
| bone Paget disease | 3 | MONDO:0005382 | EFO:0004261 |
| aortic valve stenosis | 2 | MONDO:0042981 | EFO:0000266 |
| periodontitis | 2 | MONDO:0005076 | EFO:0000649 |
| HIV infectious disease | 2 | MONDO:0005109 | EFO:0000764 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| asthma | 2 | MONDO:0004979 | MONDO:0004979 |
| osteoarthritis | 2 | MONDO:0005178 | MONDO:0005178 |
| polyostotic fibrous dysplasia | 2 | MONDO:0008274 | MONDO:0008274 |
| coronary stenosis | 2 | MONDO:0006715 | MONDO:0006715 |
| bone resorption disease | 2 | MONDO:0000837 | GO:0045453 |
| breast neoplasm | 1 | MONDO:0021100 | EFO:0003869 |
| hepatitis B virus infection | 1 | MONDO:0005344 | EFO:0004197 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 127.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE4 | 36 |
| PHASE2 | 30 |
| PHASE3 | 24 |
| Not specified | 20 |
| PHASE1 | 11 |
| PHASE2/PHASE3 | 6 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03623633 | PHASE4 | ACTIVE_NOT_RECRUITING | Comparative Antiresorptive Efficacy Discontinuation of Denosumab |
| NCT05151484 | PHASE4 | ACTIVE_NOT_RECRUITING | Novel Precision Medicine Approach to Treatment of Osteoporosis Based on Bone Turnover |
| NCT06264609 | PHASE4 | ENROLLING_BY_INVITATION | Precision Medicine Approach for Osteoporosis - Follow Up Study |
| NCT06856369 | PHASE4 | ACTIVE_NOT_RECRUITING | Clinical Efficacy of 1% Metformin and Alendronate Gel in Adjunct to Fibrin in Chronic Periodontitis |
| NCT00006180 | PHASE4 | COMPLETED | Bone Loss in Premenopausal Women With Depression |
| NCT00035971 | PHASE4 | COMPLETED | EVA: Evista Alendronate Comparison |
| NCT00157690 | PHASE4 | COMPLETED | Study of Alendronate to Prevent and Treat Osteoporosis in Cystic Fibrosis Patients |
| NCT00159419 | PHASE4 | COMPLETED | Bisphosphonate Therapy for Osteogenesis Imperfecta |
| NCT00261625 | PHASE4 | COMPLETED | Can Alendronate Suppress Calcification and Improve Bone Density in Chronic Peritoneal Dialysis Patients? |
| NCT00265252 | PHASE4 | UNKNOWN | Alendronate in the Prevention of Collapse of Femoral Head in Non-Traumatic Osteonecrosis |
| NCT00299572 | PHASE4 | UNKNOWN | Alendronate for Vascular Calcification in Peritoneal Dialysis Patients? |
| NCT00327990 | PHASE4 | COMPLETED | Evaluation Of Missed Osteoporosis Diagnoses, And Preference Between Once Monthly Ibandronate And Once Weekly Alendronate |
| NCT00395382 | PHASE4 | COMPLETED | Study of the Effect of Alendronate on Vascular Calcification and Arterial Stiffness in Chronic Kidney Disease |
| NCT00460057 | PHASE4 | COMPLETED | The Change of Bone Markers After Low Dose Alendronate in Postmenopausal Women With Bone Loss |
| NCT00503113 | PHASE4 | COMPLETED | A Study of Bonviva (Ibandronate) and Alendronate on Renal Function in Postmenopausal Women With Osteoporosis at High Risk for Renal Disease. |
| NCT00713258 | PHASE4 | TERMINATED | The Effect of PTH(1-84) or Alendronate on Reduction of Back Pain in Postmenopausal Women With an Osteoporosis Related Vertebral Fracture(s) (FP-005-IM) |
| NCT00729651 | PHASE4 | COMPLETED | Efficacy and Safety Study of Fosamax Plus D in Postmenopausal Women With Osteoporosis (0217A-263) |
| NCT01350934 | PHASE4 | COMPLETED | A Study to Evaluate Alendronate Sodium /Vitamin D3 Combination Tablets(FOSAMAX PLUS) Versus Calcitriol in the Treatment of Osteoporosis in Postmenopausal Women in China (MK-0217A-264) |
| NCT01535027 | PHASE4 | COMPLETED | Combined Administration of Teripapartide and Antiresorptive Agents in Postmenopausal Osteoporosis |
| NCT01750086 | PHASE4 | COMPLETED | Acute Effect of Teriparatide With Bisphosphonate or Denosumab on Bone Resorption |
| NCT01770106 | PHASE4 | COMPLETED | RA Denosumab on Bone Microstructure Study |
| NCT02139007 | PHASE4 | COMPLETED | Effectiveness of DiscontinuinG bisphosphonatEs Study: R21 Pilot Study |
| NCT02303873 | PHASE4 | COMPLETED | Efficacy and Safety of Alendronate in Chinese Children or Adolescents With Osteogenesis Imperfecta |
| NCT02322099 | PHASE4 | TERMINATED | Alendronate for Prevention of AntiRetroviral Therapy-associated Bone Loss |
| NCT02371252 | PHASE4 | COMPLETED | Efficacy and Safety of Brand Versus Generic Alendronate for Osteoporosis Treatment |
| NCT02416271 | PHASE4 | COMPLETED | The Forteo Alendronate Comparator Trial |
| NCT02417389 | PHASE4 | COMPLETED | Efficacy of Cinacalcet in the Control of Primary Hyperparathyroidism |
| NCT02598440 | PHASE4 | COMPLETED | A Study of Ibandronate (Bonviva) in Patients With Post-Menopausal Osteoporosis |
| NCT03005678 | PHASE4 | COMPLETED | Denosumab Versus Bisphosphonates (Alendronate) in GIOP |
| NCT03006003 | PHASE4 | UNKNOWN | Osteoporosis Treatment in Post-menopausal Women |
| NCT04739592 | PHASE4 | UNKNOWN | A Study of Alendronate Sodium Vitamin D3 Tablets on Knee Osteoarthritis |
| NCT05091099 | PHASE4 | COMPLETED | The Optimal Sequential Therapy After Long Term Denosumab Treatment |
| NCT05325515 | PHASE4 | COMPLETED | The Effect of Effervescent Alendronate on Bone Turnover |
| NCT05387200 | PHASE4 | UNKNOWN | Phase IV Clinical Trial to Evaluate Efficacy and Safety of MASI BONE S (Alendronate Sodium Trihydrate) in Postmenopausal Women With Osteoporosis |
| NCT05527548 | PHASE4 | UNKNOWN | A Single-blind RCT to Investigate the Effect of Alendronate on Knee Function Following ACLR |
| NCT05645289 | PHASE4 | UNKNOWN | Efficacy and Safety of Minodronate in Patients With Low Back Pain |
| NCT00000412 | PHASE3 | COMPLETED | Osteoporosis Prevention After Heart Transplant |
| NCT00000427 | PHASE3 | COMPLETED | Effects of Parathyroid Hormone in Men With Osteoporosis |
| NCT00000430 | PHASE3 | TERMINATED | Low-Dose Hormone Replacement Therapy and Alendronate for Osteoporosis |
| NCT00048841 | PHASE3 | COMPLETED | Prevention of Osteoporosis in Men With Prostate Cancer |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 2 clinical and 18 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
10 molecules share ≥1 primary target. Top 10 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| IBANDRONIC ACID | ChEMBL + PubChem | Phase 4 (approved) | FDPS |
| PAMIDRONIC ACID | ChEMBL + PubChem | Phase 4 (approved) | FDPS |
| RISEDRONIC ACID | ChEMBL + PubChem | Phase 4 (approved) | FDPS |
| ZOLEDRONIC ACID | ChEMBL + PubChem | Phase 4 (approved) | FDPS |
| MINODRONIC ACID | ChEMBL | Phase 4 (approved) | FDPS |
| NERIDRONIC ACID | ChEMBL | Phase 3 | FDPS |
| PYROPHOSPHORIC ACID | ChEMBL + PubChem | Phase 2 (approved) | FDPS |
| INCADRONIC ACID | ChEMBL | Phase 2 | FDPS |
| PIRIDRONIC ACID | ChEMBL | Phase 2 | FDPS |
| Lovastatin | PubChem | Approved | FDPS |