mitotane 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antineoplastics, nucleotoxic agents | 1820 | 53-19-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A derivative of the insecticide DICHLORODIPHENYLDICHLOROETHANE that specifically inhibits cells of the adrenal cortex and their production of hormones. It is used to treat adrenocortical tumors and causes CNS damage, but no bone marrow depression.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 40 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| April 28, 2004 | EMA | HRA Pharma Rare Diseases | |
| July 8, 1970 | FDA | BRISTOL MYERS SQUIBB |
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 |
|---|---|---|---|---|---|---|
| Adrenal insufficiency | 113.41 | 51.00 | 31 | 1036 | 17884 | 63470071 |
| Febrile neutropenia | 59.29 | 51.00 | 32 | 1035 | 118417 | 63369538 |
| Drug clearance increased | 57.50 | 51.00 | 8 | 1059 | 125 | 63487830 |
| Adrenocortical carcinoma | 56.36 | 51.00 | 7 | 1060 | 42 | 63487913 |
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 |
|---|---|---|---|---|---|---|
| Adrenal insufficiency | 95.37 | 41.43 | 25 | 496 | 14022 | 34942388 |
| Adrenocortical carcinoma | 59.78 | 41.43 | 7 | 514 | 27 | 34956383 |
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 |
|---|---|---|---|---|---|---|
| Adrenal insufficiency | 185.25 | 48.51 | 52 | 1509 | 28435 | 79714392 |
| Adrenocortical carcinoma | 95.53 | 48.51 | 12 | 1549 | 67 | 79742760 |
| Febrile neutropenia | 58.85 | 48.51 | 43 | 1518 | 230956 | 79511871 |
| Drug clearance increased | 57.99 | 48.51 | 9 | 1552 | 261 | 79742566 |
| Neutropenia | 54.65 | 48.51 | 45 | 1516 | 287665 | 79455162 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | L01XX23 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS OTHER ANTINEOPLASTIC AGENTS Other antineoplastic agents |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D018931 | Antineoplastic Agents, Hormonal |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Carcinoma in situ of adrenal cortex | indication | 92526009 | |
| Hypercortisolism | off-label use | 47270006 | |
| Shock | contraindication | 27942005 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Adrenal cortical hypofunction | contraindication | 386584007 | DOID:10493 |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Traumatic injury | contraindication | 417746004 | |
| CNS Toxicity | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 11B1, mitochondrial | Enzyme | INHIBITOR | WOMBAT-PK | CHEMBL | |||||
| Cholesterol side-chain cleavage enzyme, mitochondrial | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 6.09 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2B | GPCR | Ki | 5.51 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.19 | DRUG MATRIX | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 5.56 | DRUG MATRIX | |||||
| Adenosine receptor A3 | GPCR | Ki | 5.38 | DRUG MATRIX | |||||
| Adrenodoxin, mitochondrial | Unclassified | WOMBAT-PK | |||||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 6.10 | DRUG MATRIX | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 5.80 | DRUG MATRIX |
External reference:
| ID | Source |
|---|---|
| 4018140 | VUID |
| N0000146477 | NUI |
| D00420 | KEGG_DRUG |
| 4018140 | VANDF |
| C0026256 | UMLSCUI |
| CHEBI:6954 | CHEBI |
| CHEMBL1670 | ChEMBL_ID |
| DB00648 | DRUGBANK_ID |
| D008939 | MESH_DESCRIPTOR_UI |
| 4211 | PUBCHEM_CID |
| 6957 | IUPHAR_LIGAND_ID |
| 2597 | INN_ID |
| 78E4J5IB5J | UNII |
| 204257 | RXNORM |
| 1449 | MMSL |
| 5123 | MMSL |
| d01378 | MMSL |
| 002669 | NDDF |
| 26288002 | SNOMEDCT_US |
| 404865004 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Lysodren | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76336-080 | TABLET | 500 mg | ORAL | NDA | 24 sections |
| Lysodren | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76336-080 | TABLET | 500 mg | ORAL | NDA | 24 sections |