clofazimine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	692	2030-63-9

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lamprene clofazimine chlofazimine	A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619) Molecular weight: 473.40 Formula: C27H22Cl2N4 CLOGP: 7.55 LIPINSKI: 1 HAC: 4 HDO: 1 TPSA: 39.99 ALOGS: -5.50 ROTB: 4 Status: OFM Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lamprene
clofazimine
chlofazimine

A fat-soluble riminophenazine dye used for the treatment of leprosy. It has been used investigationally in combination with other antimycobacterial drugs to treat Mycobacterium avium infections in AIDS patients. Clofazimine also has a marked anti-inflammatory effect and is given to control the leprosy reaction, erythema nodosum leprosum. (From AMA Drug Evaluations Annual, 1993, p1619)

Molecular weight: 473.40
Formula: C27H22Cl2N4
CLOGP: 7.55
LIPINSKI: 1
HAC: 4
HDO: 1
TPSA: 39.99
ALOGS: -5.50
ROTB: 4

Status: OFM

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.10	g	O

ADMET properties:

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Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	7.03 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	57 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.20 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.00 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 15, 1986	FDA	NOVARTIS

FDA Adverse Event Reporting System (Female)

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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
Electrocardiogram QT prolonged	508.26	26.46	188	4970	59342	63424522
Drug resistance	147.04	26.46	59	5099	22874	63460990
Neuropathy peripheral	109.02	26.46	83	5075	113584	63370280
Anaemia	98.69	26.46	120	5038	293310	63190554
Vomiting	85.53	26.46	158	5000	559459	62924405
Hepatotoxicity	85.37	26.46	47	5111	36994	63446870
Optic neuropathy	76.14	26.46	20	5138	2012	63481852
Off label use	72.88	26.46	165	4993	674297	62809567
Type 2 lepra reaction	70.33	26.46	10	5148	30	63483834
Polyneuropathy	64.98	26.46	29	5129	14560	63469304

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FDA Adverse Event Reporting System (Male)

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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
Electrocardiogram QT prolonged	645.45	25.83	245	5547	40707	34910432
Type 2 lepra reaction	245.02	25.83	40	5752	155	34950984
Hepatotoxicity	185.65	25.83	84	5708	21401	34929738
Neuropathy peripheral	135.07	25.83	111	5681	83152	34867987
Drug resistance	113.48	25.83	64	5728	25863	34925276
Intentional product use issue	108.07	25.83	85	5707	59731	34891408
Off label use	102.63	25.83	218	5574	419306	34531833
Anaemia	73.28	25.83	135	5657	233200	34717939
Ototoxicity	71.59	25.83	22	5770	1895	34949244
Skin hyperpigmentation	67.61	25.83	24	5768	3240	34947899

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FDA Adverse Event Reporting System (Geriatric)

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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
Electrocardiogram QT prolonged	1083.36	21.97	420	10421	89966	79643581
Type 2 lepra reaction	312.06	21.97	49	10792	179	79733368
Neuropathy peripheral	268.28	21.97	191	10650	141114	79592433
Hepatotoxicity	251.99	21.97	128	10713	51224	79682323
Drug resistance	218.14	21.97	109	10732	42104	79691443
Off label use	166.06	21.97	373	10468	906842	78826705
Anaemia	156.93	21.97	243	10598	444772	79288775
Intentional product use issue	137.68	21.97	134	10707	151978	79581569
Polyneuropathy	117.76	21.97	60	10781	24091	79709456
Optic neuropathy	116.12	21.97	35	10806	3449	79730098

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J04BA01	ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF LEPRA Drugs for treatment of lepra
ATC	J04BA51	ANTIINFECTIVES FOR SYSTEMIC USE ANTIMYCOBACTERIALS DRUGS FOR TREATMENT OF LEPRA Drugs for treatment of lepra
CHEBI has role	CHEBI:35475	non-steroidal anti-inflammatory agent
CHEBI has role	CHEBI:35816	leprostatic drugs
CHEBI has role	CHEBI:37958	dyes
FDA EPC	N0000175483	Antimycobacterial
MeSH PA	D000900	Anti-Bacterial Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D000893	Anti-Inflammatory Agents
MeSH PA	D007917	Leprostatic Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Pyoderma gangrenosum	indication	74578003	DOID:8553
Leprosy	indication	81004002	DOID:1024
Erythema nodosum leprosum	indication	240411003
Multibacillary leprosy	indication	416257001
Dapsone resistant leprosy	indication	416597004
Mycobacteriosis	off-label use	88415009
Nausea and vomiting	contraindication	16932000
Splenic infarction	contraindication	22996003	DOID:2533
Disorder of digestive system	contraindication	53619000	DOID:77
Diarrhea	contraindication	62315008

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.81	Basic
pKa2	5.53	Basic
pKa3	2.07	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN	IC50	5.50	CHEMBL
Uncharacterized oxidoreductase CzcO-like	Enzyme		CZCO_GEOKA			WOMBAT-PK
Cruzipain	Enzyme		CYSP_TRYCR	IC50	5.22	CHEMBL
Spike glycoprotein	Glycoprotein		SPIKE_SARS2	Kd	5.42	CHEMBL

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External reference:

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ID	Source
003007	NDDF
1685	MMSL
203021	RXNORM
2248	INN_ID
2794	PUBCHEM_CID
387410004	SNOMEDCT_US
4019504	VUID
4019504	VANDF
4473	MMSL
72924009	SNOMEDCT_US

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Pharmaceutical products:

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