Drug reference

carfilzomib

Selective proteasome inhibitor (antineoplastic) · Antineoplastic agent

START

Cycle 1: 20 mg/m² IV d1,2; then 27–56 mg/m² escalation per schedule

TYPICAL MAX

56 mg/m² per dose

STOP IF

Severe cardiac/pulmonary event, thrombotic microangiopathy, or hepatic failure

WATCH

Cardiac (echo/BNP if symptoms), BP, LFTs, renal function, infusion reactions

CDSCO approvedATC L01XG02

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 6min · infusion start
PEAK: 30min · end infusion
t½: 30min · plasma t½
DURATION: 4w · q28d cycle

EXCRETION

Renal metabolites; minimal unchanged

route + CYP

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

Can cause fetal harm — avoid; effective contraception required.

FDA category + note

Top interactionssee all 12 →

AdalimumabSevereDatabaseDDInter
Aminocaproic AcidSevereDatabaseDDInter
AvatrombopagSevereDatabaseDDInter
BaricitinibSevereDatabaseDDInter

Mechanism

Irreversible epoxyketone-based selective inhibitor of the chymotrypsin-like activity of the 20S proteasome (CT-L/β5), accumulating polyubiquitinated proteins and inducing apoptosis in myeloma cells.

Indications

Relapsed/refractory multiple myeloma (mono- or combination)After bortezomib failure or with lenalidomide+dexamethasone or daratumumab

Dosing

Adult: Cycle 1: 20 mg/m² IV days 1, 2; 27–56 mg/m² days 8, 9, 15, 16. Cycles 2+: 27–56 mg/m² days 1, 2, 8, 9, 15, 16 (q28d). Infusion 10–30 min per regimen.
Pediatric: Not established.
Renal adjustment: No adjustment for CrCl ≥15; dialysis: dose after HD.
Hepatic adjustment: Mild–moderate: reduce starting dose. Severe: not studied.
Geriatric: Higher cardiac toxicity risk; monitor closely.
Max dose: 56 mg/m² per dose (28-day cycle, days 1/2/8/9/15/16 schedule)

Pharmacokinetics

Onset

Cytoreduction over cycles

Peak effect

End of infusion

Duration

28-day cycle

Half-life

Very short plasma t½ ~30 min; sustained proteasome inhibition

Bioavailability

IV 100%

Protein binding

~97%

Metabolism

Rapid extrahepatic peptidase cleavage

Excretion

Mainly renal (metabolites); minimal unchanged

Contraindications

Severe hypersensitivity
Caution: heart failure / arrhythmia, pulmonary hypertension, hepatic impairment

Side effects

Common

FatigueAnaemiaNauseaThrombocytopeniaDiarrhoeaDyspnoeaHypertension

Serious

Cardiac failure / ischaemia / arrhythmia
Pulmonary toxicity / hypertension
Thrombotic microangiopathy / TLS
Infusion reactions
Hepatic failure
Posterior reversible encephalopathy

Pregnancy & lactation

Pregnancy

Can cause fetal harm — avoid; effective contraception required.

Lactation

Avoid breastfeeding during therapy.