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

Stem definition	Drug id	CAS RN
ribofuranyl-derivatives of the "pyrazofurin" type	667	4291-63-8

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: mavenclad litak cladribine cladarabine leustatin	An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia. Molecular weight: 285.69 Formula: C10H12ClN5O3 CLOGP: -0.10 LIPINSKI: 0 HAC: 8 HDO: 3 TPSA: 119.31 ALOGS: -1.65 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

mavenclad
litak
cladribine
cladarabine
leustatin

An antineoplastic agent used in the treatment of lymphoproliferative diseases including hairy-cell leukemia.

Molecular weight: 285.69
Formula: C10H12ClN5O3
CLOGP: -0.10
LIPINSKI: 0
HAC: 8
HDO: 3
TPSA: 119.31
ALOGS: -1.65
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
0.34	mg	O

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	7.70 L/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	45 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
EoM (Fraction excreted unchanged in urine)	18 %	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	16 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	14 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Bocci G, Oprea TI, Benet LZ
fu (Fraction unbound in plasma)	0.79 %	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.32 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
S (Water solubility)	0.10 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Feb. 26, 1993	FDA

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
Lymphopenia	368.30	26.02	102	3498	18225	63467197
Lymphocyte count decreased	305.52	26.02	99	3501	30158	63455264
Multiple sclerosis relapse	270.74	26.02	102	3498	48376	63437046
Leukopenia	88.87	26.02	55	3545	77235	63408187
Neutropenia	63.76	26.02	63	3537	174942	63310480
Febrile neutropenia	61.43	26.02	52	3548	118397	63367025
Alanine aminotransferase increased	56.78	26.02	47	3553	103723	63381699
Drug reaction with eosinophilia and systemic symptoms	51.78	26.02	29	3571	33807	63451615
COVID-19	49.30	26.02	45	3555	113058	63372364
Dysmenorrhoea	48.23	26.02	15	3585	3958	63481464

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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	101.51	30.40	45	3263	19163	34934460
Multiple sclerosis relapse	93.42	30.40	38	3270	13095	34940528
Pancytopenia	87.29	30.40	72	3236	95085	34858538
Febrile neutropenia	84.89	30.40	83	3225	136766	34816857
Rash maculo-papular	65.47	30.40	38	3270	28413	34925210
Lymphopenia	54.76	30.40	28	3280	16307	34937316
Acute generalised exanthematous pustulosis	49.50	30.40	20	3288	6756	34946867
Neutropenia	47.75	30.40	66	3242	156712	34796911
Face oedema	42.28	30.40	21	3287	11495	34942128
Leukaemia recurrent	40.53	30.40	12	3296	1603	34952020

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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
Lymphopenia	268.96	21.58	97	5908	30460	79707923
Multiple sclerosis relapse	246.16	21.58	102	5903	46431	79691952
Lymphocyte count decreased	176.14	21.58	81	5924	47208	79691175
Febrile neutropenia	151.97	21.58	131	5874	230868	79507515
Myelodysplastic syndrome	106.83	21.58	50	5955	30251	79708132
Rash maculo-papular	103.71	21.58	60	5945	56018	79682365
Neutropenia	102.74	21.58	117	5888	287593	79450790
Pancytopenia	96.83	21.58	88	5917	165657	79572726
Leukopenia	90.78	21.58	73	5932	116440	79621943
Thrombocytopenia	70.47	21.58	93	5912	265166	79473217

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L01BB04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ANTINEOPLASTIC AGENTS ANTIMETABOLITES Purine analogues
ATC	L04AA40	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
CHEBI has role	CHEBI:35610	antineoplastic agents
CHEBI has role	CHEBI:35705	immunosuppressive agents
FDA EPC	N0000175712	Purine Antimetabolite
MeSH PA	D000970	Antineoplastic Agents
MeSH PA	D007155	Immunologic Factors
MeSH PA	D007166	Immunosuppressive 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
Hairy cell leukemia	indication	118613001
Relapsing remitting multiple sclerosis	indication	426373005	DOID:2378
Langerhans cell histiocytosis	off-label use	65399007	DOID:2571
Waldenström macroglobulinemia	off-label use	190818004	DOID:0050747
Hyperuricemia	contraindication	35885006	DOID:1920
Kidney disease	contraindication	90708001	DOID:557
Anemia	contraindication	271737000	DOID:2355
Pregnancy, function	contraindication	289908002
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Peripheral nerve disease	contraindication	302226006

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.14	acidic
pKa2	13.72	acidic
pKa3	3.11	Basic
pKa4	2.3	Basic

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Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
10MG	MAVENCLAD	EMD SERONO INC	N022561	March 29, 2019	RX	TABLET	ORAL	7888328	April 11, 2024	TREATMENT OF MS WITH A TABLET WITH AN ADMIXTURE OF (A) AN AMORPHOUS INCLUSION COMPLEX OF CLADRIBINE AND HYDROXYPROPYL-B-CYCLODEXTRIN AND (B) AMORPHOUS FREE CLADRIBINE AND CYCLODEXTRIN AS A NON-INCLUSION COMPLEX, CLADRIBINE/CYCLODEXTRIN 1:10-1:16 W/W
10MG	MAVENCLAD	EMD SERONO INC	N022561	March 29, 2019	RX	TABLET	ORAL	8785415	April 11, 2024	TREATMENT OF MS WITH AN ADMIXTURE OF (A) AN AMORPHOUS INCLUSION COMPLEX OF CLADRIBINE (2CDA) AND CYCLODEXTRIN AND (B) AMORPHOUS FREE 2CDA AND CYCLODEXTRIN AS A NON-INCLUSION COMPLEX, FORMULATED AS A SOLID ORAL FORM, W/O SIGN. AMOUNTS OF CRYST. 2CDA
10MG	MAVENCLAD	EMD SERONO INC	N022561	March 29, 2019	RX	TABLET	ORAL	8377903	May 31, 2026	TREATING RRMS OR SPMS WITH ORAL CLADRIBINE: (I) 2-4 MONTHS INDUCTION WITH 1.7 MG/KG - 3.5 MG/KG CLADRIBINE; (II) CLADRIBINE-FREE PERIOD OF ABOUT 8-10 MONTHS; (III) 2-4 MONTHS MAINTENANCE WITH ABOUT 1.7 MG/KG CLADRIBINE; (IV) CLADRIBINE-FREE PERIOD
10MG	MAVENCLAD	EMD SERONO INC	N022561	March 29, 2019	RX	TABLET	ORAL	7713947	Oct. 16, 2026	TREATING MS WITH ORAL CLADRIBINE ACC. TO THE STEPS (I) INDUCTION PERIOD WITH ABOUT 1.7 MG/KG-3.5 MG/KG CLADRIBINE; (II) CLADRIBINE-FREE PERIOD OF ABOUT 8-10 MONTHS; (III) MAINTENANCE PERIOD WITH ABOUT 1.7 MG/KG CLADRIBINE; (IV) CLADRIBINE-FREE PERIOD
10MG	MAVENCLAD	EMD SERONO INC	N022561	March 29, 2019	RX	TABLET	ORAL	10849919	Nov. 23, 2038	TREATING NON-EARLY SPMS BY ADMINISTERING ORAL CLADRIBINE AT A FIXED DOSE PER PATIENT, PER BODY WEIGHT AND PER TREATMENT YEAR, WHICH FIXED DOSE IS 1.75 +/- 0.2 MG/KG, TO BE ADMINISTERED WITHIN MONTHS 1 AND 2 IN EACH OF 2 ADJACENT TREATMENT YEARS

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Orange Book exclusivity data (new drug applications)

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Type	Activity value (-log[M])	Bioact source
Deoxycytidine kinase	Kinase	P27707	DCK_HUMAN			WOMBAT-PK
cAMP-specific 3',5'-cyclic phosphodiesterase 4A	Enzyme	P27815	PDE4A_HUMAN	IC50	5.44	DRUG MATRIX
Adenosine receptor A1	GPCR		AA1R_RAT	Ki	5.14	CHEMBL
Adenosine receptor A2a	GPCR		AA2AR_RAT	Ki	4.69	CHEMBL

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External reference:

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ID	Source
004145	NDDF
108800000	SNOMEDCT_US
1760	MMSL
20279	PUBCHEM_CID
2122636	RXNORM
262155	MMSL
31821	MMSL
386916009	SNOMEDCT_US
4020629	VUID
4020629	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Cladribine	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9871	INJECTION	1 mg	INTRAVENOUS	ANDA	23 sections
Cladribine	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9871	INJECTION	1 mg	INTRAVENOUS	ANDA	23 sections
Cladribine	HUMAN PRESCRIPTION DRUG LABEL	1	42658-010	INJECTION, SOLUTION	1 mg	INTRAVENOUS	ANDA	26 sections
Cladribine	HUMAN PRESCRIPTION DRUG LABEL	1	42658-010	INJECTION, SOLUTION	1 mg	INTRAVENOUS	ANDA	26 sections
Cladribine	HUMAN PRESCRIPTION DRUG LABEL	1	63323-140	INJECTION	1 mg	INTRAVENOUS	ANDA	15 sections
Cladribine	HUMAN PRESCRIPTION DRUG LABEL	1	67457-450	INJECTION	1 mg	INTRAVENOUS	ANDA	23 sections
Cladribine	HUMAN PRESCRIPTION DRUG LABEL	1	67457-450	INJECTION	1 mg	INTRAVENOUS	ANDA	23 sections
Mavenclad	HUMAN PRESCRIPTION DRUG LABEL	1	44087-4000	TABLET	10 mg	ORAL	NDA	34 sections
Mavenclad	HUMAN PRESCRIPTION DRUG LABEL	1	44087-4000	TABLET	10 mg	ORAL	NDA	34 sections

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