Cladribine

Purine Antimetabolite — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Cladribine is an ofp drug in the Purine Antimetabolite class catalogued in DrugCentral. It was first approved by the FDA in 1993. DrugCentral lists 5 molecular targets, including PNP, PDE4A and Adora1. Recorded indications include Hairy cell leukemia and Relapsing remitting multiple sclerosis.

• Approval status: ofp (first approved 1993 by the FDA).
• Drug class: Purine Antimetabolite.
• Molecular targets: PNP, PDE4A, Adora1 and Adora2a (5 listed in DrugCentral).
• Indications: Hairy cell leukemia and Relapsing remitting multiple sclerosis.
• ATC code: L01BB04 (Purine analogues).
• Molecular formula: C10H12ClN5O3; molecular weight 285.69 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Hairy cell leukemia
• Relapsing remitting multiple sclerosis

Off-label uses (2)

• Langerhans cell histiocytosis
• Waldenström macroglobulinemia

Contraindications (10)

• Anemia
• Bone marrow depression
• Breastfeeding (mother)
• Hyperuricemia
• Kidney disease
• Neutropenic disorder
• Peripheral nerve disease
• Pregnancy, function
• Thrombocytopenic disorder
• Uric Acid Nephropathy Gout

Mechanism & targets

• Established pharmacologic class: Purine Antimetabolite

Molecular targets (5)

Target	Gene	Action	Activity
Purine nucleoside phosphorylase	PNP	unknown	Ki 8.64
cAMP-specific 3',5'-cyclic phosphodiesterase 4A	PDE4A	unknown	IC50 5.44
Adenosine receptor A1	Adora1	unknown	Ki 5.14
Adenosine receptor A2a	Adora2a	unknown	Ki 4.69
Deoxycytidine kinase	DCK	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1993-02-26	FDA	—	—	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01BB04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ANTIMETABOLITES › Purine analogues
L04AA40	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Selective immunosuppressants

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Multiple sclerosis relapse	665.1
Lymphopenia	565.3
Lymphocyte count decreased	529.3
Febrile neutropenia	212.2
Pancytopenia	191.7
Rash maculo-papular	163.4
Myelodysplastic syndrome	148.0
Neutropenia	121.8
Hairy cell leukaemia recurrent	120.8
Leukopenia	105.5
Maternal exposure before pregnancy	96.1
Thrombocytopenia	86.9

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Cladribine is on its molecule page.

• Molecular formula: C₁₀H₁₂ClN₅O₃
• Molecular weight: 285.69 g/mol
• CAS number: 4291-63-8
• InChIKey: PTOAARAWEBMLNO-KVQBGUIXSA-N
• PubChem CID: 20279

NC1=C2N=CN([C@H]3C[C@H](O)[C@@H](CO)O3)C2=NC(Cl)=N1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Cladribine used for?

DrugCentral lists the following indications for Cladribine: Hairy cell leukemia and Relapsing remitting multiple sclerosis.

How does Cladribine work?

Its molecular targets in DrugCentral include PNP, PDE4A, Adora1 and Adora2a.

When was Cladribine first approved?

Cladribine was first approved by the FDA in 1993.

What drug class does Cladribine belong to?

Cladribine is in the Purine Antimetabolite class.

What is the chemical formula of Cladribine?

Cladribine has the molecular formula C10H12ClN5O3 and a molecular weight of 285.69 g/mol.

Sources

• DrugCentral drug card 667 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1619 — compound record and bioactivity
• PubChem CID 20279 — chemical identifiers
• DrugBank DB00242 — drug record
• FDA UNII 47M74X9YT5 — substance identity
• DailyMed: FDA labels for Cladribine — current prescribing information (label search)
• UniProt P00491 (PNP) — target protein
• UniProt P27815 (PDE4A) — target protein
• UniProt P27707 (DCK) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.