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

Stem definition	Drug id	CAS RN
antineoplastic, alkylating agents, (beta-chloroethyl)amine derivatives	1596	13010-47-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lomustine belustine chloroethylcyclohexylnitrosourea lomustin	An alkylating agent of value against both hematologic malignancies and solid tumors. Molecular weight: 233.70 Formula: C9H16ClN3O2 CLOGP: 2.75 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 61.77 ALOGS: -2.49 ROTB: 4 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

lomustine
belustine
chloroethylcyclohexylnitrosourea
lomustin

An alkylating agent of value against both hematologic malignancies and solid tumors.

Molecular weight: 233.70
Formula: C9H16ClN3O2
CLOGP: 2.75
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 61.77
ALOGS: -2.49
ROTB: 4

Status: OFP

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

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	99 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
MRTD (Maximum Recommended Therapeutic Daily Dose)	15.02 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.05 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Aug. 4, 1976	FDA	CORDEN PHARMA

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
Thrombocytopenia	69.29	32.12	46	1698	151111	63336167
Eastern Cooperative Oncology Group performance status worsened	64.22	32.12	13	1731	1241	63486037
Tumour pseudoprogression	61.32	32.12	10	1734	282	63486996
Platelet count decreased	57.21	32.12	37	1707	116085	63371193
Mucosal inflammation	56.61	32.12	27	1717	46901	63440377
Ototoxicity	51.59	32.12	11	1733	1351	63485927
Death	44.72	32.12	53	1691	374328	63112950
Geotrichum infection	43.40	32.12	8	1736	466	63486812
Full blood count abnormal	40.53	32.12	19	1725	31698	63455580
Nausea	40.02	32.12	78	1666	854393	62632885

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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
Disease progression	61.19	26.25	53	2239	108024	34846615
Aeromonas infection	52.90	26.25	10	2282	274	34954365
Eastern Cooperative Oncology Group performance status worsened	45.35	26.25	11	2281	997	34953642
Second primary malignancy	42.95	26.25	17	2275	7869	34946770
Seizure	39.34	26.25	41	2251	104816	34849823
Nausea	36.47	26.25	73	2219	339835	34614804
Platelet count decreased	34.87	26.25	41	2251	119676	34834963
Fatigue	33.25	26.25	74	2218	370579	34584060
Thrombocytopenia	32.11	26.25	45	2247	156202	34798437
Tumour pseudoprogression	30.59	26.25	7	2285	493	34954146

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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
Eastern Cooperative Oncology Group performance status worsened	110.41	28.08	24	3427	2041	79738896
Tumour pseudoprogression	91.20	28.08	17	3434	662	79740275
Disease progression	88.38	28.08	69	3382	184293	79556644
Thrombocytopenia	87.49	28.08	80	3371	265179	79475758
Seizure	60.29	28.08	56	3395	188778	79552159
Platelet count decreased	58.83	28.08	56	3395	194608	79546329
Aeromonas infection	54.24	28.08	10	3441	366	79740571
Acute myeloid leukaemia	52.59	28.08	26	3425	30859	79710078
Death	52.19	28.08	90	3361	566424	79174513
Neutropenia	51.97	28.08	63	3388	287647	79453290

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01AD02	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
Hodgkin's disease	indication	118599009
Neoplasm of brain	indication	126952004	DOID:1319
Allogeneic bone marrow transplantation	off-label use	58390007
Mycosis	contraindication	3218000	DOID:1564
Hyperbilirubinemia	contraindication	14783006	DOID:2741
Viral disease	contraindication	34014006	DOID:934
Fibrosis of lung	contraindication	51615001	DOID:3770
Leukopenia	contraindication	84828003	DOID:615
Bacterial infectious disease	contraindication	87628006
Kidney disease	contraindication	90708001	DOID:557

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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	12.87	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

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ID	Source
002639	NDDF
3184	INN_ID
387227009	SNOMEDCT_US
3950	PUBCHEM_CID
4018138	VUID
4018138	VANDF
40999006	SNOMEDCT_US
4991	MMSL
52513	MMSL
6466	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Gleostine	HUMAN PRESCRIPTION DRUG LABEL	1	58181-3040	CAPSULE, GELATIN COATED	10 mg	ORAL	NDA	24 sections
Gleostine	HUMAN PRESCRIPTION DRUG LABEL	1	58181-3040	CAPSULE, GELATIN COATED	10 mg	ORAL	NDA	24 sections
Gleostine	HUMAN PRESCRIPTION DRUG LABEL	1	58181-3041	CAPSULE, GELATIN COATED	40 mg	ORAL	NDA	24 sections
Gleostine	HUMAN PRESCRIPTION DRUG LABEL	1	58181-3041	CAPSULE, GELATIN COATED	40 mg	ORAL	NDA	24 sections
Gleostine	HUMAN PRESCRIPTION DRUG LABEL	1	58181-3042	CAPSULE, GELATIN COATED	100 mg	ORAL	NDA	24 sections
Gleostine	HUMAN PRESCRIPTION DRUG LABEL	1	58181-3042	CAPSULE, GELATIN COATED	100 mg	ORAL	NDA	24 sections

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