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Carfilzomib

Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.

IDDRUG-CARFILZOMIB
TypeDrug
Aliases
KyprolisКарфілзоміб
Statusreviewed 2026-04-25 | pending_clinical_signoff
DiseasesDIS-MM DIS-WM
SourcesSRC-ESMO-MM-2023 SRC-NCCN-MM-2025

Drug Facts

ClassSecond-generation irreversible proteasome inhibitor (epoxyketone)
MechanismSelective irreversible inhibitor of the chymotrypsin-like activity of the 20S proteasome (β5 / LMP7 subunits). Binds covalently via epoxyketone — distinct from bortezomib's reversible boronate binding — conferring sustained inhibition + activity in bortezomib-refractory myeloma. Single doses can suppress proteasome activity >80% for >24h.
Typical dosingMultiple schedules. KRd: 27 mg/m² days 1, 2, 8, 9, 15, 16 of 28-day cycle (escalated from 20 mg/m² day 1, 2 of cycle 1). KdW (weekly, CHAMPION-1 / ARROW): 70 mg/m² IV days 1, 8, 15 of 28-day cycle. Hydration 250-500 mL pre + post infusion mandatory.
Ukraine registeredTrue
NSZU reimbursedTrue
Ukraine last verified2026-04-27

Notes

Cardiac toxicity is THE safety signal — baseline ECG + ECHO mandatory; blood pressure control critical (target <140/90 pre-dose); hydration protocol non-negotiable for first 2 cycles. ENDEAVOR / ASPIRE / CANDOR trials demonstrate superior PFS over bortezomib-based regimens but at the cost of higher cardiac AEs. Particularly active in early-relapse / early-PI-exposed setting. Weekly schedule (70 mg/m²) is now preferred over twice-weekly for tolerability without efficacy loss (ARROW trial).

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