Chlorambucil

Alkylating Drug — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Chlorambucil is an ofp drug in the Alkylating Drug class catalogued in DrugCentral. It was first approved by the FDA in 1957. Its mechanism of action is classified as Alkylating Activity. DrugCentral lists 5 molecular targets, including CTSD, CTSE and ADAM9. Recorded indications include Chronic lymphoid leukemia, disease, Follicular non-Hodgkin's lymphoma and Hodgkin's disease.

• Approval status: ofp (first approved 1957 by the FDA).
• Drug class: Alkylating Drug.
• Mechanism of action: Alkylating Activity.
• Molecular targets: CTSD, CTSE, ADAM9 and OPRD1 (5 listed in DrugCentral).
• Indications: Chronic lymphoid leukemia, disease, Follicular non-Hodgkin's lymphoma and Hodgkin's disease.
• ATC code: L01AA02 (Nitrogen mustard analogues).
• Molecular formula: C14H19Cl2NO2; molecular weight 304.21 g/mol.

Indications & contraindications

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

Indications (3)

• Chronic lymphoid leukemia, disease
• Follicular non-Hodgkin's lymphoma
• Hodgkin's disease

Off-label uses (4)

• Minimal change disease
• Mycosis fungoides
• Primary cutaneous T-cell lymphoma
• Waldenström macroglobulinemia

Contraindications (18)

• Acute infectious disease
• Acute leukemia, disease
• Anemia
• Bone marrow depression
• Breastfeeding (mother)
• Drug-induced hepatitis
• Fibrosis of lung
• Interstitial pneumonia
• Leukopenia
• Lowered convulsive threshold
• Lymphocytopenia
• Nephrotic syndrome
• Neutropenic disorder
• Pregnancy, function
• Radiation oncology AND/OR radiotherapy
• Secondary malignant neoplasm of bone marrow
• Seizure disorder
• Thrombocytopenic disorder

Mechanism & targets

• Mechanism of action (MoA): Alkylating Activity
• Established pharmacologic class: Alkylating Drug

Molecular targets (5)

Target	Gene	Action	Activity
Cathepsin D	CTSD	unknown	IC50 8.93
Cathepsin E	CTSE	unknown	IC50 8.78
Disintegrin and metalloproteinase domain-containing protein 9	ADAM9	unknown	IC50 7.25
Delta-type opioid receptor	OPRD1	unknown	IC50 5.55
Aldose reductase	Akr1b1	unknown	IC50 5.03

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1957-03-18	FDA	—	ASPEN GLOBAL INC

ATC classification

ATC code	Therapeutic hierarchy
L01AA02	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › ALKYLATING AGENTS › Nitrogen mustard 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
Acute myeloid leukaemia	312.6
Neutropenia	295.2
Progressive multifocal leukoencephalopathy	287.7
Microsporidia infection	245.1
Myelodysplastic syndrome	234.6
Myositis	216.8
Secondary immunodeficiency	191.0
Second primary malignancy	177.0
Thrombocytopenia	167.5
Hypogammaglobulinaemia	157.6
Pneumonia	144.1
Febrile neutropenia	142.1

Chemical structure

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

• Molecular formula: C₁₄H₁₉Cl₂NO₂
• Molecular weight: 304.21 g/mol
• CAS number: 305-03-3
• InChIKey: JCKYGMPEJWAADB-UHFFFAOYSA-N
• PubChem CID: 2708

OC(=O)CCCC1=CC=C(C=C1)N(CCCl)CCCl

Frequently asked questions

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

What is Chlorambucil used for?

DrugCentral lists the following indications for Chlorambucil: Chronic lymphoid leukemia, disease, Follicular non-Hodgkin's lymphoma and Hodgkin's disease.

How does Chlorambucil work?

Chlorambucil is classified as Alkylating Activity; its molecular targets in DrugCentral include CTSD, CTSE, ADAM9 and OPRD1.

When was Chlorambucil first approved?

Chlorambucil was first approved by the FDA in 1957.

What drug class does Chlorambucil belong to?

Chlorambucil is in the Alkylating Drug class.

What is the chemical formula of Chlorambucil?

Chlorambucil has the molecular formula C14H19Cl2NO2 and a molecular weight of 304.21 g/mol.

Sources

• DrugCentral drug card 588 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL515 — compound record and bioactivity
• PubChem CID 2708 — chemical identifiers
• DrugBank DB00291 — drug record
• FDA UNII 18D0SL7309 — substance identity
• DailyMed: FDA labels for Chlorambucil — current prescribing information (label search)
• UniProt P07339 (CTSD) — target protein
• UniProt P14091 (CTSE) — target protein
• UniProt Q13443 (ADAM9) — target protein
• UniProt P41143 (OPRD1) — 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.