tegaserod 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| serotonin receptor antagonists and partial agonists | 2579 | 145158-71-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a nonbenzamide 5-hydroxytryptamine(4) agonist; used in treatment of irritable bowel syndrome; marketing suspended 2007 in US due to higher incidence of MI, stroke, and unstable angina; structure given in first source
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 12 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.50 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.66 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 11 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 5.30 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 18 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.02 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 11 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 24, 2002 | 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 | A06AX06 | ALIMENTARY TRACT AND METABOLISM DRUGS FOR CONSTIPATION DRUGS FOR CONSTIPATION Other drugs for constipation |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018490 | Serotonin Agents |
| MeSH PA | D017366 | Serotonin Receptor Agonists |
| FDA MoA | N0000193870 | Serotonin 4 Receptor Agonists |
| FDA EPC | N0000193871 | Serotonin-4 Receptor Agonist |
| CHEBI has role | CHEBI:35941 | serotonin agonists |
| CHEBI has role | CHEBI:55324 | gastrointestinal drugs |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic idiopathic constipation | indication | 82934008 | |
| Irritable bowel syndrome characterized by constipation | indication | 440630006 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Hypovolemia | contraindication | 28560003 | |
| Ischemic colitis | contraindication | 30588004 | DOID:0060181 |
| Dehydration | contraindication | 34095006 | |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Acute nephropathy | contraindication | 58574008 | |
| Diarrhea | contraindication | 62315008 | |
| Intestinal obstruction | contraindication | 81060008 | DOID:8437 |
| Disorder of biliary tract | contraindication | 105997008 | DOID:9741 |
| Angina pectoris | contraindication | 194828000 | |
| Cerebrovascular accident | contraindication | 230690007 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Adhesion of Gastrointestinal Tract | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.67 | acidic |
| pKa2 | 12.01 | Basic |
| pKa3 | 1.56 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 4 | GPCR | PARTIAL AGONIST | Ki | 8.40 | CHEMBL | CHEMBL | |||
| 5-hydroxytryptamine receptor 1A | GPCR | WOMBAT-PK | |||||||
| 5-hydroxytryptamine receptor 2B | GPCR | ANTAGONIST | Ki | 8.40 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1D | GPCR | WOMBAT-PK | |||||||
| 5-hydroxytryptamine receptor 3A | Ion channel | Ki | 5.60 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 4 | GPCR | EC50 | 7.90 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021352 | VUID |
| N0000148771 | NUI |
| D02730 | KEGG_DRUG |
| 189188-57-6 | SECONDARY_CAS_RN |
| 4021352 | VANDF |
| 4024281 | VANDF |
| CHEBI:51043 | CHEBI |
| CHEMBL76370 | ChEMBL_ID |
| C105050 | MESH_SUPPLEMENTAL_RECORD_UI |
| 226 | IUPHAR_LIGAND_ID |
| 7606 | INN_ID |
| DB01079 | DRUGBANK_ID |
| 458VC51857 | UNII |
| 139778 | RXNORM |
| 16842 | MMSL |
| 43157 | MMSL |
| d04798 | MMSL |
| 009658 | NDDF |
| 386035006 | SNOMEDCT_US |
| 386036007 | SNOMEDCT_US |
| 417025001 | SNOMEDCT_US |
| C0537147 | UMLSCUI |
| CHEMBL1516474 | ChEMBL_ID |
| 135409453 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| ZELNORM | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0525-0971 | TABLET | 6 mg | ORAL | NDA | 27 sections |
| Zelnorm | HUMAN PRESCRIPTION DRUG LABEL | 1 | 27505-090 | TABLET | 6 mg | ORAL | NDA | 30 sections |