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tiludronic acid 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| calcium metabolism regulator, pharmaceutical aid | 2666 | 89987-06-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a bone resorption inhibitor; an antihypercalcemic agent; used in the tratment of Paget's disease; used in the treatment and prevention of osteoporosis; structure given in first source
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.40 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 60 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 17.52 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 6 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.23 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 0.40 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.10 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 7.70 hours | Lombardo F, Berellini G, Obach RS |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKC,AXL,BMX,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHUK,CSF1R,DDR1,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHB4,ERBB2,FLT1,FLT3,FLT4,GRK2,GSK3B,IGF1R,IKBKB,ITK,JAK1,JAK2,JAK3,KDR,MAP2K6,MAP3K1,MAP3K14,MAP3K2,MAP3K21,MAP3K3,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MTOR,NTRK1,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CD,PIM1,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,SRC,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 | 79 | |||
| kinase-selectivity-class | AURKA,AXL,BRAF,CDK4,CDK9,DDR1,DYRK1B,EPHB4,ERBB2,GRK2,IKBKB,JAK2,MAP2K6,MAP3K14,MAP3K2,MAPK7,MAPK8,PIK3CD,PIK3CG,PRKDC,STK33,SYK,TEK,TGFBR1,ZAP70 | 25 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 7, 1997 | FDA |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | M05BA05 | MUSCULO-SKELETAL SYSTEM DRUGS FOR TREATMENT OF BONE DISEASES DRUGS AFFECTING BONE STRUCTURE AND MINERALIZATION Bisphosphonates |
| FDA CS | M0006519 | Diphosphonates |
| FDA EPC | N0000175579 | Bisphosphonate |
| MeSH PA | D050071 | Bone Density Conservation Agents |
Related Drugs by ATC class:
M05BA Bisphosphonates 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Osteitis deformans | indication | 2089002 | DOID:5408 |
| Gastritis | contraindication | 4556007 | DOID:4029 |
| Hypocalcemia | contraindication | 5291005 | |
| Peptic ulcer | contraindication | 13200003 | DOID:750 |
| Hyperphosphatemia | contraindication | 20165001 | DOID:0050459 |
| Vitamin D deficiency | contraindication | 34713006 | |
| Dysphagia | contraindication | 40739000 | |
| Periodontitis | contraindication | 41565005 | DOID:824 |
| Acute nephropathy | contraindication | 58574008 | |
| Stricture of esophagus | contraindication | 63305008 | |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Hyperparathyroidism | contraindication | 66999008 | DOID:13543 |
| Fracture of femur | contraindication | 71620000 | |
| Duodenitis | contraindication | 72007001 | DOID:8643 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Bed-ridden | contraindication | 160685001 | |
| Esophageal dysmotility | contraindication | 266434009 | DOID:9192 |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Primary malignant neoplasm | contraindication | 372087000 | |
| Aseptic necrosis of bone of jaw | contraindication | 441809006 | |
| Esophageal Obstruction | contraindication | ||
| Invasive Dental Procedure | contraindication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Horses | Navicular syndrome | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Tildren | Bimeda Animal Health Limited | 1 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 2.19 | acidic |
| pKa2 | 6.26 | acidic |
| pKa3 | 7.24 | acidic |
| pKa4 | 11.31 | acidic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Tyrosine-protein phosphatase non-receptor type 1 | Enzyme | WOMBAT-PK | |||||||
| V-type proton ATPase 116 kDa subunit a isoform 3 | Enzyme | WOMBAT-PK | |||||||
| 72 kDa type IV collagenase | Enzyme | IC50 | 5.14 | CHEMBL | |||||
| Matrix metalloproteinase-14 | Enzyme | IC50 | 4.52 | CHEMBL | |||||
| Interstitial collagenase | Enzyme | IC50 | 4.30 | CHEMBL | |||||
| Neutrophil collagenase | Enzyme | IC50 | 4.49 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D02285 | KEGG_DRUG |
| 149845-07-8 | SECONDARY_CAS_RN |
| 4021043 | VANDF |
| 4024072 | VANDF |
| C0043611 | UMLSCUI |
| CHEBI:9598 | CHEBI |
| CHEMBL1350 | ChEMBL_ID |
| DB01133 | DRUGBANK_ID |
| CHEMBL1200448 | ChEMBL_ID |
| C058651 | MESH_SUPPLEMENTAL_RECORD_UI |
| 60937 | PUBCHEM_CID |
| 7604 | IUPHAR_LIGAND_ID |
| 6325 | INN_ID |
| 6PNS59HP4Y | UNII |
| 11476 | RXNORM |
| 5583 | MMSL |
| d04124 | MMSL |
| 006071 | NDDF |
| 006072 | NDDF |
| 395905009 | SNOMEDCT_US |
| 422263009 | SNOMEDCT_US |
| 426050007 | SNOMEDCT_US |
| 96286006 | SNOMEDCT_US |
Pharmaceutical products:
None