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Cyclophosphamide

Nitrogen-mustard alkylating agent (oxazaphosphorine) · Antineoplastic

Also known as Cytoxan, Neosar, Endoxan, Genoxal, Revimmune

START
Regimen-specific; ensure hydration ± mesna for IV pulse/high dose; e.g. lupus nephritis 500–1000 mg/m² IV monthly
TYPICAL MAX
Regimen-defined (e.g. 50 mg/kg/day transplant)
STOP IF
Haemorrhagic cystitis, severe myelosuppression/infection, anaphylaxis
WATCH
CBC, urinalysis/haematuria, sodium (SIADH), hydration, infection; fertility counselling
CDSCO approvedSchedule HATC L01AA01
Dose laddermg/d
50start150titrate1kmax3.5kceiling
Renal dose adjustmenteGFR mL/min/1.73m²
FULLUsual regimen dose with hydration30REDUCEReduce dose; monitor to…10REDUCE~25% reduc…90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
2hONSET3hPEAK6h2wDURATION
ONSET
2h · metabolite activation
PEAK
3h · active metabolite peak
6h · parent t½
DURATION
2w · pulse interval (illustrative)
EXCRETION
Hepatic activation; renal parent + metabolites
route + CYP
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Avoid — teratogenic/embryotoxic; effective contraception both sexes; avoid 1st trimester especially
FDA category + note
Top interactionssee all 12
  • Live VaccinesContraindicatedDatabaseKimi deep-research + Cla
  • AdalimumabSevereDatabaseDDInter
  • BaricitinibSevereDatabaseDDInter
  • CertolizumabSevereDatabaseDDInter
Available in India

50 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Prodrug activated by hepatic CYP (mainly CYP2B6) to 4-hydroxycyclophosphamide/aldophosphamide → phosphoramide mustard, which crosslinks DNA (N7-guanine) inhibiting replication; acrolein by-product causes urothelial toxicity. Also potent immunosuppressant.

Indications

Lymphomas, leukaemias, multiple myelomaBreast, ovarian and other solid tumours (regimen-dependent)Severe autoimmune disease (e.g. lupus nephritis, ANCA vasculitis)Conditioning for haematopoietic stem-cell transplant

Dosing

Adult
Highly regimen-specific. Oral 1–5 mg/kg/day; IV pulses 500–1000 mg/m² (e.g. monthly in vasculitis/lupus); transplant conditioning up to 50 mg/kg/day ×4. Always with hydration ± mesna for higher doses.
Pediatric
Protocol-specific (oncology/rheumatology specialist).
Renal adjustment
Reduce dose in significant renal impairment (active metabolites accumulate); ~25% reduction CrCl <10 / dialysis.
Hepatic adjustment
Severe hepatic impairment may impair activation/clearance — caution, consider reduction.
Geriatric
Greater myelosuppression/toxicity; reduce/monitor.
Max dose
Regimen-defined (e.g. 50 mg/kg/day transplant); no universal ceiling

Pharmacokinetics

Onset
Counts nadir ~day 7–14
Peak effect
Active metabolite within hours
Duration
Cycle/pulse-based
Half-life
Parent ~3–12 h
Bioavailability
Oral >75%
Protein binding
Parent low; metabolites ~50%
Metabolism
Hepatic CYP2B6/3A4 activation; aldehyde dehydrogenase detox
Excretion
Renal (parent + metabolites)

Contraindications

  • Severe hypersensitivity to cyclophosphamide
  • Active severe infection / severe bone-marrow failure
  • Urinary outflow obstruction; active haemorrhagic cystitis

Side effects

Common
Myelosuppression (dose-limiting)Nausea/vomitingAlopeciaAmenorrhoea/azoospermia
Serious
  • Haemorrhagic cystitis (acrolein) — prevent with hydration/mesna
  • Secondary malignancy (bladder cancer, leukaemia)
  • Infertility/gonadal failure
  • Cardiotoxicity (high-dose), pulmonary fibrosis
  • SIADH/hyponatraemia; severe immunosuppression/opportunistic infection
  • Anaphylaxis

Pregnancy & lactation

Pregnancy

Avoid — teratogenic/embryotoxic; effective contraception both sexes; avoid 1st trimester especially

Lactation

Contraindicated — excreted in milk, infant toxicity

Drug interactions

Live Vaccines
Contraindicated
Database

Profound immunosuppression — disseminated vaccine infection

Avoid live vaccines during and after therapy

Source: Kimi deep-research + Cla

Adalimumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Baricitinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Certolizumab
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cidofovir
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Cladribine
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Clozapine
Severe
Database

Additive agranulocytosis risk

Avoid combination; monitor ANC

Source: Kimi deep-research + Cla

Deferiprone
Severe
Database

Clinical effect not specified

Source: DDInter

Fingolimod
Severe
Database

Clinical effect not specified

Source: DDInter

Golimumab
Severe
Database

Clinical effect not specified

Source: DDInter

Infliximab
Severe
Database

.

Source: DDInter

Inotersen
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Ask House about Cyclophosphamide

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19