alitretinoin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| retinol derivatives | 3862 | 5300-03-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 20 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 0.33 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 2, 1999 | FDA | EISAI INC |
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 |
|---|---|---|---|---|---|---|
| Diverticulum oesophageal | 54.45 | 48.51 | 7 | 450 | 144 | 63488421 |
| Mandibular mass | 53.14 | 48.51 | 7 | 450 | 175 | 63488390 |
FDA Adverse Event Reporting System (Male)
None
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 |
|---|---|---|---|---|---|---|
| Diverticulum oesophageal | 54.61 | 51.57 | 7 | 506 | 158 | 79743717 |
| Mandibular mass | 52.53 | 51.57 | 7 | 506 | 215 | 79743660 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | D11AH04 | DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Agents for dermatitis, excluding corticosteroids |
| ATC | L01XF02 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Retinoids for cancer treatment |
| FDA CS | M0018962 | Retinoids |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D003879 | Dermatologic Agents |
| FDA EPC | N0000175607 | Retinoid |
| CHEBI has role | CHEBI:25212 | metabolites |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:50176 | keratolytic drugs |
| CHEBI has role | CHEBI:63794 | retinoid X receptor agonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Kaposi's Sarcoma Skin Lesions | indication | ||
| Mycosis fungoides | contraindication | 118618005 | |
| 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 | 4.17 | 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 alpha | Nuclear hormone receptor | AGONIST | EC50 | 6.52 | WOMBAT-PK | CHEMBL | |||
| Retinoic acid receptor RXR-alpha | Nuclear hormone receptor | AGONIST | EC50 | 6.50 | WOMBAT-PK | CHEMBL | |||
| Retinoic acid receptor RXR-beta | Nuclear hormone receptor | AGONIST | EC50 | 6.70 | WOMBAT-PK | CHEMBL | |||
| Retinoic acid receptor RXR-gamma | Nuclear hormone receptor | AGONIST | EC50 | 6.66 | WOMBAT-PK | CHEMBL | |||
| Retinoic acid receptor beta | Nuclear hormone receptor | AGONIST | EC50 | 7.30 | WOMBAT-PK | CHEMBL | |||
| Retinoic acid receptor gamma | Nuclear hormone receptor | AGONIST | EC50 | 7.13 | WOMBAT-PK | CHEMBL | |||
| Nuclear receptor ROR-gamma | Nuclear hormone receptor | EC50 | 4.85 | CHEMBL | |||||
| Nuclear receptor subfamily 4 group A member 1 | Nuclear other | Kd | 6.09 | CHEMBL | |||||
| Oxysterols receptor LXR-beta | Nuclear other | EC50 | 5.76 | CHEMBL | |||||
| Oxysterols receptor LXR-alpha | Nuclear other | EC50 | 5.96 | CHEMBL | |||||
| Retinoic acid receptor RXR-beta | Transcription factor | Kd | 7.92 | CHEMBL | |||||
| Retinoic acid receptor RXR-gamma | Transcription factor | Kd | 8.40 | CHEMBL | |||||
| Retinoic acid receptor alpha | Transcription factor | Kd | 8.15 | CHEMBL | |||||
| Retinoic acid receptor RXR-alpha | Transcription factor | Kd | 7.49 | CHEMBL | |||||
| Retinoic acid receptor beta | Transcription factor | Kd | 8.15 | CHEMBL | |||||
| Retinoic acid receptor gamma | Transcription factor | Kd | 7.77 | CHEMBL | |||||
| Retinoic acid receptor RXR-alpha | Nuclear hormone receptor | EC50 | 6.96 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021155 | VUID |
| N0000148606 | NUI |
| D02815 | KEGG_DRUG |
| 4021155 | VANDF |
| C0281666 | UMLSCUI |
| CHEBI:50648 | CHEBI |
| CHEMBL705 | ChEMBL_ID |
| DB00523 | DRUGBANK_ID |
| D000077556 | MESH_DESCRIPTOR_UI |
| 449171 | PUBCHEM_CID |
| 2645 | IUPHAR_LIGAND_ID |
| 7781 | INN_ID |
| 1UA8E65KDZ | UNII |
| 219098 | RXNORM |
| 14093 | MMSL |
| 7957 | MMSL |
| 007747 | NDDF |
| 116086005 | SNOMEDCT_US |
| 409488005 | SNOMEDCT_US |
| 9CR | PDB_CHEM_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| PANRETIN | Human Prescription Drug Label | 1 | 59212-601 | GEL | 60 mg | TOPICAL | NDA | 22 sections |
| CLINDAMYCIN 1% / NIACINAMIDE 4% / TRETINOIN 0.05% | HUMAN PRESCRIPTION DRUG LABEL | 3 | 72934-2054 | CREAM | 0.05 g | TOPICAL | unapproved drug other | 4 sections |