All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Molfile Inchi Smiles Synonyms: mitotane chloditan chlodithane lysodren mitotan opeprim

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. Molecular weight: 320.03 Formula: C14H10Cl4 CLOGP: 6.06 LIPINSKI: 1 HAC: 0 HDO: 0 TPSA: ALOGS: -7.53 ROTB: 3 Status: OFP 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

Approvals:

Date	Agency	Company	Orphan
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	107.00	52.96	29	950	15668	56275420
Adrenocortical carcinoma	72.91	52.96	9	970	49	56291039
Drug clearance increased	60.17	52.96	8	971	84	56291004
Febrile neutropenia	56.06	52.96	30	949	105515	56185573

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	97.45	44.52	25	458	12634	31684227
Adrenocortical carcinoma	59.63	44.52	7	476	27	31696834

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	189.15	47.59	52	1405	25143	70901844
Adrenocortical carcinoma	111.28	47.59	14	1443	75	70926912
Drug clearance increased	58.33	47.59	9	1448	239	70926748
Febrile neutropenia	57.11	47.59	41	1416	204277	70722710
Neutropenia	55.08	47.59	44	1413	257112	70669875

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	P15538	C11B1_HUMAN	INHIBITOR				WOMBAT-PK	CHEMBL
Cholesterol side-chain cleavage enzyme, mitochondrial	Enzyme	P05108	CP11A_HUMAN	INHIBITOR				CHEMBL	CHEMBL
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	6.09		DRUG MATRIX
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN		Ki	5.51		DRUG MATRIX
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	6.19		DRUG MATRIX
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.56		DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.38		DRUG MATRIX
Adrenodoxin, mitochondrial	Unclassified	P10109	ADX_HUMAN					WOMBAT-PK
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	6.10		DRUG MATRIX
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN		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