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

Stem definition	Drug id	CAS RN
antineoplastic, alkylating agents, (beta-chloroethyl)amine derivatives	512	154-93-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: carmustine becenun carmubris carmustin nitrumon	A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed) Molecular weight: 214.05 Formula: C5H9Cl2N3O2 CLOGP: 1.32 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 61.77 ALOGS: -2.15 ROTB: 5 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

carmustine
becenun
carmubris
carmustin
nitrumon

A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed)

Molecular weight: 214.05
Formula: C5H9Cl2N3O2
CLOGP: 1.32
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 61.77
ALOGS: -2.15
ROTB: 5

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
CL (Clearance)	78 mL/min/kg	Lombardo F, Berellini G, Obach RS
S (Water solubility)	3.80 mg/mL	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	11.50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.20 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.55 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	0.37 hours	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.23 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
March 7, 1977	FDA	EMCURE PHARMS LTD

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
Myelodysplastic syndrome	251.59	39.83	73	3244	16681	63469024
Malignant transformation	137.23	39.83	23	3294	394	63485311
Mucosal inflammation	134.81	39.83	60	3257	46868	63438837
Febrile neutropenia	131.77	39.83	80	3237	118369	63367336
Brain oedema	124.50	39.83	41	3276	14154	63471551
Haematotoxicity	110.82	39.83	34	3283	9342	63476363
Acute myeloid leukaemia	101.77	39.83	37	3280	17110	63468595
Diffuse large B-cell lymphoma recurrent	82.30	39.83	20	3297	2300	63483405
Second primary malignancy	82.06	39.83	26	3291	7927	63477778
Stem cell transplant	81.78	39.83	19	3298	1803	63483902

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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
Myelodysplastic syndrome	334.51	30.83	125	5848	19083	34931875
Venoocclusive liver disease	260.10	30.83	83	5890	7883	34943075
Acute myeloid leukaemia	219.67	30.83	91	5882	18179	34932779
Malignant transformation	219.14	30.83	46	5927	805	34950153
Febrile neutropenia	170.73	30.83	159	5814	136690	34814268
Second primary malignancy	150.59	30.83	55	5918	7831	34943127
Off label use	143.16	30.83	255	5718	419269	34531689
Brain oedema	120.74	30.83	55	5918	13766	34937192
Pneumocephalus	104.58	30.83	19	5954	148	34950810
Blood stem cell transplant failure	87.01	30.83	19	5954	403	34950555

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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
Myelodysplastic syndrome	540.35	30.82	178	8339	30123	79705748
Malignant transformation	333.07	30.82	64	8453	1154	79734717
Acute myeloid leukaemia	326.24	30.82	123	8394	30762	79705109
Febrile neutropenia	303.88	30.82	227	8290	230772	79505099
Venoocclusive liver disease	279.07	30.82	86	8431	11685	79724186
Second primary malignancy	230.40	30.82	78	8439	14272	79721599
Brain oedema	221.79	30.82	88	8429	25175	79710696
Mucosal inflammation	167.87	30.82	103	8414	75477	79660394
Haematotoxicity	153.61	30.82	59	8458	15460	79720411
Off label use	151.32	30.82	311	8206	906904	78828967

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01AD01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ALKYLATING AGENTS Nitrosoureas
CHEBI has role	CHEBI:35610	antineoplastic agents
FDA EPC	N0000175558	Alkylating Drug
FDA MoA	N0000000236	Alkylating Activity
MeSH PA	D000477	Alkylating Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018906	Antineoplastic Agents, Alkylating
MeSH PA	D009676	Noxae

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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
Glioma, malignant	indication	74532006
Diffuse non-Hodgkin's lymphoma, large cell	indication	109969005
Multiple myeloma	indication	109989006	DOID:9538
Hodgkin's disease	indication	118599009
Non-Hodgkin's lymphoma	indication	118601006
Glioblastoma multiforme of brain	indication	276828006	DOID:3073
Malignant neoplasm of brain	indication	428061005	DOID:1319
Astrocytoma, anaplastic	off-label use	55353007	DOID:3078
Allogeneic bone marrow transplantation	off-label use	58390007
Mycosis fungoides	off-label use	118618005

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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	11.09	acidic

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	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Glutathione reductase, mitochondrial	Enzyme	P00390	GSHR_HUMAN	INHIBITOR	IC50	5.09		CHEMBL	CHEMBL

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External reference:

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ID	Source
002640	NDDF
2105	RXNORM
251354	MMSL
2578	PUBCHEM_CID
2959	INN_ID
387281007	SNOMEDCT_US
4018136	VANDF
4020993	VUID
4020993	VANDF
4360	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Gliadel	HUMAN PRESCRIPTION DRUG LABEL	1	24338-050	WAFER	7.70 mg	INTRACAVITARY	NDA	25 sections

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