Drug reference

Chlorambucil

Antineoplastic

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

AdalimumabSevereDatabaseDDInter
BaricitinibSevereDatabaseDDInter
CertolizumabSevereDatabaseDDInter
CladribineSevereDatabaseDDInter

Mechanism

Chlorambucil is a nitrogen mustard alkylating agent that forms covalent bonds with DNA through its bis-(2-chloroethyl) groups, producing interstrand and intrastrand cross-links that prevent DNA replication and transcription. As a phenylbutyric acid derivative, it is well absorbed orally and produces gradual, moderate, and rapidly reversible myelosuppression — distinguishing it from more acutely toxic alkylating agents. It is primarily used in chronic lymphocytic leukemia where its slow onset allows flexible dose titration without overwhelming a compromised bone marrow.

Indications

Some lymphomas and chronic leukaemias (used either alone or in combination therapy)Symptomatic stage III and IV follicular lymphoma in previously untreated patients (in combination with cyclophosphamide, vincristine and prednisolone; cyclophosphamide, doxorubicin, vincristine and prednisolone; mitoxantrone, chlorambucil and prednisolone; cyclophosphamide, doxorubicin, etoposide, prednisolone and interferon-alfa; or chlorambucil alone with Rituximab)Untreated chronic lymphocytic leukaemia in patients who have comorbidities that make full-dose fludarabine-based therapy unsuitable for them (in combination with Obinutuzumab)chronic lymphocytic leukemia (CLL) (historically used, now for relapsed disease or when modern agents are unavailable or not tolerated)Chronic lymphatic leukaemiaNon-Hodgkin lymphomaFew solid tumours

Dosing

Adult: BY MOUTH: consult local protocol

Pharmacokinetics

Onset

not specified

Peak effect

not specified

Bioavailability

adequate and reliable oral absorption

Protein binding

not specified

Contraindications

Children with nephrotic syndrome (increased seizure risk)
History of epilepsy (increased seizure risk)

Side effects

Common

nausea (with single oral doses of 20 mg or greater)vomiting (with single oral doses of 20 mg or greater)myelosuppression (moderate, gradual, rapidly reversible)GI discomfortazoospermiaamenorrheapulmonary fibrosis (rare)seizures (rare)dermatitis (rare)hepatotoxicity (rare)

Serious

marked hypoplasia of the bone marrow (with excessive doses)
acute myeloid leukemia (AML) and other tumors (increased incidence when used historically in polycythemia vera and as adjuvant after breast cancer)
Bone marrow depression