Product Name

Carfilzomib

Appearance

White to off-white powder

Dosage Form

For use in preparation of injectable formulations

Specifications

Purity ≥ 98.0% (by HPLC)

Indications

Carfilzomib is a potent, irreversible proteasome inhibitor primarily indicated for the treatment of multiple myeloma. It selectively inhibits the chymotrypsin-like activity of the 20S proteasome, leading to the accumulation of defective proteins within the cell and ultimately inducing apoptosis, particularly in rapidly dividing malignant plasma cells.

Relapsed or Refractory Multiple Myeloma:
Carfilzomib is approved for patients who have received one or more prior therapies.
It is typically administered:
As monotherapy with dexamethasone.
In combination with lenalidomide and dexamethasone (KRd regimen).
In combination with daratumumab and dexamethasone (KDd regimen).
Clinical trials (e.g., ASPIRE, ENDEAVOR studies) demonstrated significant improvements in progression-free survival (PFS), overall survival (OS), and response rates compared to standard treatments.

First-Line Therapy (Under Clinical Investigation):
Carfilzomib-based regimens are being evaluated as part of initial therapy for newly diagnosed multiple myeloma patients, especially in combination with immunomodulators and monoclonal antibodies.
Promising data suggest improved depth of response and minimal residual disease (MRD) negativity rates.

High-Risk Cytogenetic Multiple Myeloma:
Patients with high-risk cytogenetic features (e.g., t(4;14), t(14;16), del(17p)) often have poorer outcomes. Carfilzomib-based therapies have shown to mitigate the negative impact of these abnormalities to some extent.

Patients Intolerant to First-Generation Proteasome Inhibitors:
Compared with bortezomib, carfilzomib has a lower incidence of peripheral neuropathy, making it a preferred option for patients who are intolerant or at risk of severe neuropathic side effects.

Other Potential Investigational Uses:
Ongoing research is exploring carfilzomib in:
Combination with anti-CD38 antibodies (e.g., isatuximab)
Smoldering multiple myeloma (SMM) to delay disease progression
Relapsed/refractory light chain (AL) amyloidosis treatment