Clofarabine

Nucleoside Metabolic Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Clofarabine is an ofp drug in the Nucleoside Metabolic Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2004. Its mechanism of action is classified as Nucleic Acid Synthesis Inhibitors. DrugCentral lists 7 molecular targets, including RRM2, RRM1 and PDE2A. Recorded indications include Acute lymphoid leukemia.

• Approval status: ofp (first approved 2004 by the FDA).
• Drug class: Nucleoside Metabolic Inhibitor.
• Mechanism of action: Nucleic Acid Synthesis Inhibitors.
• Molecular targets: RRM2, RRM1, PDE2A and UCK2 (7 listed in DrugCentral).
• Indications: Acute lymphoid leukemia.
• ATC code: L01BB06 (Purine analogues).
• Molecular formula: C10H11ClFN5O3; molecular weight 303.68 g/mol.

Indications & contraindications

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

Indications (1)

• Acute lymphoid leukemia

Contraindications (18)

• Anemia
• Bacterial infectious disease
• Bone marrow depression
• Breastfeeding (mother)
• Capillary leak syndrome
• Chemotherapy-Induced Hyperuricemia
• Dehydration
• Disease of liver
• Hyperbilirubinemia
• Liver function tests abnormal
• Low blood pressure
• Mycosis
• Neutropenic disorder
• Pregnancy, function
• Renal failure syndrome
• Sepsis syndrome
• Thrombocytopenic disorder
• Viral disease

Mechanism & targets

• Mechanism of action (MoA): Nucleic Acid Synthesis Inhibitors
• Established pharmacologic class: Nucleoside Metabolic Inhibitor

Molecular targets (7)

Target	Gene	Action	Activity
Ribonucleoside-diphosphate reductase subunit M2	RRM2	inhibitor	IC50 8.30
Ribonucleoside-diphosphate reductase large subunit	RRM1	inhibitor	IC50 8.30
cGMP-dependent 3',5'-cyclic phosphodiesterase	PDE2A	unknown	IC50 5.51
Uridine-cytidine kinase 2	UCK2	unknown	—
Ribose-phosphate pyrophosphokinase 1	PRPS1	unknown	—
DNA polymerase alpha catalytic subunit	POLA1	inhibitor	—
Uridine-cytidine kinase 1	UCK1	unknown	—

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2019-11-14	EMA	—	ORPHELIA PHARMA SAS
2004-12-28	FDA	—	GENZYME	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01BB06	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ANTIMETABOLITES › Purine analogues

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
Febrile neutropenia	430.4
Multiple organ dysfunction syndrome	262.1
Mucosal inflammation	221.5
Haematotoxicity	194.6
Blood bilirubin increased	191.6
Capillary leak syndrome	186.4
Venoocclusive liver disease	162.3
Bone marrow failure	156.1
Sepsis	151.5
Palmar-plantar erythrodysaesthesia syndrome	148.0
Adenovirus infection	123.4
Graft versus host disease	114.3

Chemical structure

• Molecular formula: C₁₀H₁₁ClFN₅O₃
• Molecular weight: 303.68 g/mol
• CAS number: 123318-82-1
• InChIKey: WDDPHFBMKLOVOX-AYQXTPAHSA-N
• PubChem CID: 119182

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

Frequently asked questions

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

What is Clofarabine used for?

DrugCentral lists the following indications for Clofarabine: Acute lymphoid leukemia.

How does Clofarabine work?

Clofarabine is classified as Nucleic Acid Synthesis Inhibitors; its molecular targets in DrugCentral include RRM2 (inhibitor), RRM1 (inhibitor), PDE2A and UCK2.

When was Clofarabine first approved?

Clofarabine was first approved by the FDA in 2004.

What drug class does Clofarabine belong to?

Clofarabine is in the Nucleoside Metabolic Inhibitor class.

What is the chemical formula of Clofarabine?

Clofarabine has the molecular formula C10H11ClFN5O3 and a molecular weight of 303.68 g/mol.

Sources

• DrugCentral drug card 691 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1750 — compound record and bioactivity
• PubChem CID 119182 — chemical identifiers
• DrugBank DB00631 — drug record
• FDA UNII 762RDY0Y2H — substance identity
• DailyMed: FDA labels for Clofarabine — current prescribing information (label search)
• UniProt P31350 (RRM2) — target protein
• UniProt P23921 (RRM1) — target protein
• UniProt O00408 (PDE2A) — target protein
• UniProt Q9BZX2 (UCK2) — target protein
• UniProt P60891 (PRPS1) — target protein
• UniProt P09884 (POLA1) — 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.