Tox | Related Drugs | 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:

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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value
kinase-safety-class	ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,EPHB4,ERBB2,GRK2,MAPK7,NTRK2,PDK1,PDK2,PDK4,PIK3CB,PRKDC,TEK	18
kinase-selectivity-class	AXL,BRAF,GRK2,STK33,TTK	5
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

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

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
Thrombocytopenia	109.19	30.84	65	2049	208660	90417673
Eastern Cooperative Oncology Group performance status worsened	72.16	30.84	15	2099	1924	90624409
Mucosal inflammation	71.01	30.84	32	2082	57593	90568740
Neutropenia	66.19	30.84	49	2065	224855	90401478
Platelet count decreased	62.08	30.84	39	2075	136930	90489403
Death	60.30	30.84	63	2051	456488	90169845
Off label use	56.03	30.84	95	2019	1102157	89524176
Tumour pseudoprogression	53.92	30.84	10	2104	711	90625622
Ototoxicity	49.37	30.84	11	2103	1953	90624380
Disease progression	47.98	30.84	35	2079	156580	90469753
Nausea	46.47	30.84	88	2026	1110228	89516105
Neoplasm progression	43.29	30.84	21	2093	44465	90581868
Geotrichum infection	42.61	30.84	8	2106	608	90625725
Full blood count abnormal	40.88	30.84	19	2095	36578	90589755
Acute myeloid leukaemia	40.60	30.84	16	2098	20624	90605709
Malignant neoplasm progression	35.25	30.84	25	2089	106845	90519488
Second primary malignancy	35.12	30.84	12	2102	10366	90615967
Aspergilloma	34.76	30.84	6	2108	283	90626050
Bone marrow failure	33.74	30.84	16	2098	32205	90594128
Myelodysplastic syndrome	33.53	30.84	14	2100	20889	90605444
Post procedural diarrhoea	33.17	30.84	6	2108	371	90625962

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
Disease progression	73.88	29.40	66	2662	143590	42475017
Aeromonas infection	63.11	29.40	12	2716	348	42618259
Thrombocytopenia	53.19	29.40	63	2665	190216	42428391
Eastern Cooperative Oncology Group performance status worsened	52.43	29.40	13	2715	1323	42617284
Second primary malignancy	43.51	29.40	18	2710	9557	42609050
Seizure	42.32	29.40	45	2683	120516	42498091
Death	41.48	29.40	92	2636	471093	42147514
Fatigue	37.11	29.40	84	2644	435557	42183050
Hepatitis cholestatic	36.46	29.40	16	2712	9808	42608799
Platelet count decreased	35.57	29.40	44	2684	138537	42480070
Toxic skin eruption	34.29	29.40	17	2711	13713	42604894
Nausea	33.18	29.40	76	2652	396723	42221884
Necrotising fasciitis	32.95	29.40	12	2716	4534	42614073
Neutropenia	31.29	29.40	50	2678	199381	42419226
Hypermutation	30.87	29.40	5	2723	55	42618552
Tumour pseudoprogression	30.31	29.40	8	2720	1042	42617565

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
Thrombocytopenia	144.74	26.93	113	4042	348772	110236372
Eastern Cooperative Oncology Group performance status worsened	126.92	26.93	28	4127	2941	110582203
Disease progression	114.15	26.93	85	4070	243949	110341195
Tumour pseudoprogression	84.55	26.93	18	4137	1598	110583546
Neutropenia	82.54	26.93	85	4070	374535	110210609
Death	82.07	26.93	115	4040	698754	109886390
Off label use	71.15	26.93	166	3989	1500019	109085125
Second primary malignancy	69.54	26.93	26	4129	18042	110567102
Seizure	69.24	26.93	61	4094	221124	110364020
Neoplasm progression	66.37	26.93	37	4118	64558	110520586
Aeromonas infection	64.70	26.93	12	4143	525	110584619
Platelet count decreased	61.27	26.93	58	4097	230385	110354759
Acute myeloid leukaemia	56.77	26.93	28	4127	38082	110547062
Malignant neoplasm progression	54.31	26.93	48	4107	174519	110410625
Geotrichum infection	49.42	26.93	11	4144	1201	110583943
Myelodysplastic syndrome	48.39	26.93	25	4130	37459	110547685
Ototoxicity	40.35	26.93	12	4143	4119	110581025
Mucosal inflammation	39.34	26.93	31	4124	96110	110489034
Product use in unapproved indication	38.65	26.93	64	4091	447313	110137831
Haematotoxicity	35.95	26.93	17	4138	21065	110564079
Bone marrow failure	35.87	26.93	24	4131	57824	110527320
Hepatitis cholestatic	35.70	26.93	16	4139	17550	110567594
Glioblastoma	33.98	26.93	9	4146	2031	110583113
Cholestasis	33.50	26.93	24	4131	64494	110520650
Necrotising fasciitis	33.18	26.93	12	4143	7579	110577565
Hypermutation	30.06	26.93	5	4150	115	110585029
Hepatocellular injury	28.99	26.93	20	4135	50622	110534522
Toxic skin eruption	28.89	26.93	16	4139	27499	110557645
Post procedural diarrhoea	28.74	26.93	6	4149	484	110584660
Large granular lymphocytosis	28.34	26.93	6	4149	518	110584626
Myxoid liposarcoma	27.86	26.93	4	4151	33	110585111

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	L01AD02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ALKYLATING AGENTS Nitrosoureas
FDA MoA	N0000000236	Alkylating Activity
FDA EPC	N0000175558	Alkylating Drug
MeSH PA	D000477	Alkylating Agents
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D018906	Antineoplastic Agents, Alkylating
CHEBI has role	CHEBI:22333	alkylating agent
CHEBI has role	CHEBI:35610	antineoplastic agent

Related Drugs by ATC class:

L01AD Nitrosoureas 7 drugs

carmustine fotemustine nimustine ranimustine semustine streptozocin uracil mustard

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

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
Bleeding	contraindication	131148009
Liver function tests abnormal	contraindication	166603001
Drug-induced hepatitis	contraindication	235876009
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Bone marrow depression	contraindication	307762000
Breastfeeding (mother)	contraindication	413712001
Pulmonary Infiltrates	contraindication

🐶 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)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
100MG	LOMUSTINE	CARNEGIE	A219265	Oct. 27, 2025	RX	CAPSULE	ORAL	May 19, 2026	COMPETITIVE GENERIC THERAPY
10MG	LOMUSTINE	CARNEGIE	A219265	Oct. 27, 2025	RX	CAPSULE	ORAL	May 19, 2026	COMPETITIVE GENERIC THERAPY
40MG	LOMUSTINE	CARNEGIE	A219265	Oct. 27, 2025	RX	CAPSULE	ORAL	May 19, 2026	COMPETITIVE GENERIC THERAPY

Bioactivity Summary:

None

External reference:

ID	Source
4018138	VUID
N0000146475	NUI
D00363	KEGG_DRUG
4018138	VANDF
C0023972	UMLSCUI
CHEBI:6520	CHEBI
CHEMBL514	ChEMBL_ID
DB01206	DRUGBANK_ID
D008130	MESH_DESCRIPTOR_UI
3950	PUBCHEM_CID
7214	IUPHAR_LIGAND_ID
3184	INN_ID
7BRF0Z81KG	UNII
6466	RXNORM
4991	MMSL
52513	MMSL
d01341	MMSL
002639	NDDF
387227009	SNOMEDCT_US
40999006	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Gleostine	Human Prescription Drug Label	1	24338-340	CAPSULE, GELATIN COATED	10 mg	ORAL	NDA	24 sections
Gleostine	Human Prescription Drug Label	1	24338-341	CAPSULE, GELATIN COATED	40 mg	ORAL	NDA	24 sections
Gleostine	Human Prescription Drug Label	1	24338-342	CAPSULE, GELATIN COATED	100 mg	ORAL	NDA	24 sections
Lomustine	Human Prescription Drug Label	1	52536-340	CAPSULE, GELATIN COATED	10 mg	ORAL	NDA	24 sections
Lomustine	Human Prescription Drug Label	1	52536-341	CAPSULE, GELATIN COATED	40 mg	ORAL	NDA	24 sections
Lomustine	Human Prescription Drug Label	1	52536-342	CAPSULE, GELATIN COATED	100 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	58181-3042	CAPSULE, GELATIN COATED	100 mg	ORAL	NDA	24 sections
LOMUSTINE	HUMAN PRESCRIPTION DRUG LABEL	1	80005-114	CAPSULE	10 mg	ORAL	ANDA	25 sections
LOMUSTINE	HUMAN PRESCRIPTION DRUG LABEL	1	80005-115	CAPSULE	40 mg	ORAL	ANDA	25 sections
LOMUSTINE	HUMAN PRESCRIPTION DRUG LABEL	1	80005-116	CAPSULE	100 mg	ORAL	ANDA	25 sections

Ask DrugCentral

Try a sample question

lomustine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: