Stem definition | Drug id | CAS RN |
---|---|---|
arotinoid derivatives | 361 | 153559-49-0 |
None
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 ยตM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Date | Agency | Company | Orphan |
---|---|---|---|
March 29, 2001 | EMA | ||
Dec. 29, 1999 | FDA | VALEANT LUXEMBOURG |
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 | 89.88 | 41.92 | 18 | 406 | 5473 | 50599227 |
Cutaneous T-cell lymphoma | 51.81 | 41.92 | 9 | 415 | 1255 | 50603445 |
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 | 123.22 | 29.35 | 36 | 795 | 15870 | 29557826 |
Hypertriglyceridaemia | 104.77 | 29.35 | 27 | 804 | 7448 | 29566248 |
Cutaneous T-cell lymphoma | 75.52 | 29.35 | 15 | 816 | 1278 | 29572418 |
Dyslipidaemia | 39.32 | 29.35 | 12 | 819 | 6049 | 29567647 |
Thyroid stimulating hormone deficiency | 32.92 | 29.35 | 4 | 827 | 10 | 29573686 |
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 | 168.95 | 29.17 | 40 | 1227 | 11165 | 64486300 |
Hypothyroidism | 142.30 | 29.17 | 46 | 1221 | 40411 | 64457054 |
Cutaneous T-cell lymphoma | 126.34 | 29.17 | 24 | 1243 | 2328 | 64495137 |
Dyslipidaemia | 47.09 | 29.17 | 14 | 1253 | 9228 | 64488237 |
Diffuse large B-cell lymphoma | 45.51 | 29.17 | 14 | 1253 | 10347 | 64487118 |
Blood triglycerides increased | 40.97 | 29.17 | 15 | 1252 | 18851 | 64478614 |
Thyroid stimulating hormone deficiency | 34.35 | 29.17 | 4 | 1263 | 10 | 64497455 |
Skin exfoliation | 31.35 | 29.17 | 16 | 1251 | 44869 | 64452596 |
None
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 |
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 4.23 | acidic |
None
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
1% | BEXAROTENE | AMNEAL | A215398 | April 27, 2022 | RX | GEL | TOPICAL | Nov. 13, 2022 | COMPETITIVE GENERIC THERAPY |
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 |
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 |
008004 | NDDF |
116346006 | SNOMEDCT_US |
387023000 | SNOMEDCT_US |
4021197 | VANDF |
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 |
Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5525 | GEL | 1 g | TOPICAL | NDA | 20 sections |
Targretin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0187-5525 | GEL | 1 g | TOPICAL | NDA | 20 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 | 0832-0285 | CAPSULE | 75 mg | ORAL | ANDA | 28 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 | 20 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 | 69238-2088 | GEL | 10 mg | TOPICAL | ANDA | 21 sections |