bexarotene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| arotinoid derivatives | 361 | 153559-49-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A tetrahydronaphthalene derivative and RETINOID X RECEPTOR antagonist that is used in the treatment of CUTANEOUS T-CELL LYMPHOMA.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 0.01 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 28.70 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| March 29, 2001 | EMA | ||
| Dec. 29, 1999 | FDA | VALEANT LUXEMBOURG |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Hypertriglyceridaemia | 101.57 | 35.78 | 20 | 456 | 6239 | 63482307 |
| Cutaneous T-cell lymphoma | 58.85 | 35.78 | 10 | 466 | 1370 | 63487176 |
| Hypothyroidism | 51.17 | 35.78 | 17 | 459 | 42615 | 63445931 |
| Diffuse large B-cell lymphoma | 37.81 | 35.78 | 9 | 467 | 6703 | 63481843 |
| Blood triglycerides increased | 36.91 | 35.78 | 10 | 466 | 12478 | 63476068 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Hypothyroidism | 151.87 | 29.75 | 45 | 937 | 20857 | 34935092 |
| Hypertriglyceridaemia | 115.88 | 29.75 | 30 | 952 | 8418 | 34947531 |
| Cutaneous T-cell lymphoma | 78.80 | 29.75 | 16 | 966 | 1522 | 34954427 |
| Thyroid stimulating hormone deficiency | 39.57 | 29.75 | 5 | 977 | 19 | 34955930 |
| Dyslipidaemia | 36.81 | 29.75 | 12 | 970 | 7476 | 34948473 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Hypertriglyceridaemia | 187.91 | 29.20 | 44 | 1401 | 12696 | 79730247 |
| Hypothyroidism | 178.47 | 29.20 | 57 | 1388 | 52335 | 79690608 |
| Cutaneous T-cell lymphoma | 131.15 | 29.20 | 25 | 1420 | 2678 | 79740265 |
| Blood triglycerides increased | 48.04 | 29.20 | 17 | 1428 | 21023 | 79721920 |
| Dyslipidaemia | 45.02 | 29.20 | 14 | 1431 | 11619 | 79731324 |
| Diffuse large B-cell lymphoma | 44.42 | 29.20 | 14 | 1431 | 12135 | 79730808 |
| Thyroid stimulating hormone deficiency | 40.02 | 29.20 | 5 | 1440 | 29 | 79742914 |
| Skin exfoliation | 29.46 | 29.20 | 16 | 1429 | 55084 | 79687859 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XF03 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Retinoids for cancer treatment |
| FDA CS | M0018962 | Retinoids |
| MeSH PA | D000970 | Antineoplastic Agents |
| FDA EPC | N0000175607 | Retinoid |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Primary cutaneous T-cell lymphoma | indication | 400122007 | |
| Alcoholism | contraindication | 7200002 | |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Hepatic failure | contraindication | 59927004 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Leukopenia | contraindication | 84828003 | DOID:615 |
| Bilateral cataracts | contraindication | 95722004 | |
| Disorder of biliary tract | contraindication | 105997008 | DOID:9741 |
| Acute pancreatitis | contraindication | 197456007 | DOID:2913 |
| Chronic pancreatitis | contraindication | 235494005 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Diabetic - poor control | contraindication | 268519009 | |
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.23 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Retinoic acid receptor RXR-beta | Nuclear hormone receptor | AGONIST | Ki | 8.23 | CHEMBL | CHEMBL | |||
| Retinoic acid receptor RXR-gamma | Nuclear hormone receptor | AGONIST | Ki | 8.08 | CHEMBL | CHEMBL | |||
| Retinoic acid receptor RXR-alpha | Nuclear hormone receptor | AGONIST | Kd | 7.85 | CHEMBL | CHEMBL | |||
| Retinoic acid receptor gamma | Nuclear hormone receptor | Ki | 6.89 | CHEMBL | |||||
| Cytochrome P450 26A1 | Enzyme | IC50 | 4.87 | CHEMBL | |||||
| Cytochrome P450 26B1 | Enzyme | IC50 | 5.23 | CHEMBL | |||||
| Oxysterols receptor LXR-beta | Nuclear other | EC50 | 6.36 | CHEMBL | |||||
| Retinoic acid receptor alpha | Nuclear hormone receptor | Ki | 6.74 | CHEMBL | |||||
| Oxysterols receptor LXR-alpha | Nuclear other | EC50 | 6.71 | CHEMBL | |||||
| Peroxisome proliferator-activated receptor gamma | Nuclear hormone receptor | ANTAGONIST | IC50 | 5.52 | IUPHAR | ||||
| Retinoic acid receptor beta | Nuclear hormone receptor | Ki | 7.30 | CHEMBL | |||||
| Retinoic acid receptor RXR-beta | Transcription factor | Kd | 7.68 | CHEMBL | |||||
| Retinoic acid receptor RXR-gamma | Transcription factor | Kd | 7.54 | CHEMBL | |||||
| Retinoic acid receptor RXR-alpha | Transcription factor | EC50 | 7.40 | CHEMBL | |||||
| Retinoic acid receptor RXR-alpha | Nuclear hormone receptor | EC50 | 7.40 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021197 | VUID |
| N0000148643 | NUI |
| D03106 | KEGG_DRUG |
| 233272 | RXNORM |
| C0765273 | UMLSCUI |
| CHEBI:50859 | CHEBI |
| 9RA | PDB_CHEM_ID |
| CHEMBL1023 | ChEMBL_ID |
| DB00307 | DRUGBANK_ID |
| D000077610 | MESH_DESCRIPTOR_UI |
| 82146 | PUBCHEM_CID |
| 2807 | IUPHAR_LIGAND_ID |
| 7782 | INN_ID |
| A61RXM4375 | UNII |
| 234760 | MMSL |
| 31640 | MMSL |
| 8604 | MMSL |
| d04507 | MMSL |
| 116346006 | SNOMEDCT_US |
| 387023000 | SNOMEDCT_US |
| 4021197 | VANDF |
| 008004 | NDDF |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0399 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 25 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0054-0399 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 25 sections |
| Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5525 | GEL | 1 g | TOPICAL | NDA | 21 sections |
| Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5525 | GEL | 1 g | TOPICAL | NDA | 21 sections |
| Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5525 | GEL | 1 g | TOPICAL | NDA | 21 sections |
| Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5526 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | NDA | 25 sections |
| Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5526 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | NDA | 25 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0378-6955 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 28 sections |
| bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-2832 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 27 sections |
| bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0591-2832 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 27 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-0285 | CAPSULE | 75 mg | ORAL | ANDA | 28 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0832-0285 | CAPSULE | 75 mg | ORAL | ANDA | 28 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42291-072 | CAPSULE | 75 mg | ORAL | ANDA | 27 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43975-315 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 27 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43975-315 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | ANDA | 27 sections |
| bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-002 | GEL | 1 g | TOPICAL | NDA authorized generic | 21 sections |
| bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-002 | GEL | 1 g | TOPICAL | NDA authorized generic | 21 sections |
| bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68682-003 | CAPSULE, LIQUID FILLED | 75 mg | ORAL | NDA authorized generic | 25 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1250 | CAPSULE | 75 mg | ORAL | ANDA | 27 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1250 | CAPSULE | 75 mg | ORAL | ANDA | 27 sections |
| Bexarotene | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-2088 | GEL | 10 mg | TOPICAL | ANDA | 21 sections |