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Carfilzomib Drug Description

Shanghai Chiral Chemicals Inc | Updated: Sep 28, 2017

Carfilzomib Drug Description

Mechanism

Carfilzomib is a tetrapeptide-based epoxy skeleton proteasome inhibitor that is irreversibly bound to the 20S proteasome containing threonine at the N-terminal active site of the 26S protease in vivo by proteolytic core particles. Carfilzomib has anti-proliferative and apoptotic activity in vitro in solid and hematopoietic granulocytes. In animals, carfilzomib inhibits proteasome activity in blood and tissue and delays tumor growth in multiple myeloma, hematology, and solid tumor models.

Indications and uses

Carfilzomib is a proteasome inhibitor for the treatment of patients with multiple myeloma who have received at least two previous treatments including bortezomib and an immunomodulatory drug and have confirmed the progression of the disease or the last treatment completed within 60 days. Approval is based on response rate. Has not yet proven clinical benefits, such as survival or symptom improvement.

Administration

(1, 2, 8, 9, 15, and 16 days), followed by 12-day rest periods (days 17 to 28) for 2 to 10 minutes per week for 2 consecutive days.

(2) Recommended treatment 1 dose is 20 mg / m2 / day and if the tolerance increases the dose of the second course of treatment and the subsequent treatment dose to 27 mg / m2 / day.

(3) before and after hydration patients.

(4) Pretreatment with dexamethasone prior to all first course doses. In the first course of treatment, and if the infusion reaction occurs or occurs again.

(5) Administration according to toxicity.

Precautions

(1) Cardiac adverse reactions include heart failure and ischemia: monitoring of cardiac complications. Timely treatment and suspension of Carfilzomib.

(2) pulmonary hypertension: if suspected to stop the administration.

(3) Pulmonary complications: Surveillance and immediate treatment of dyspnea, interruption of Carfilzomib until the symptoms have been resolved or restored to baseline.

(4) infusion reaction: pre-administration with dexamethasone prevention.

(5) advise patients if the symptoms immediately look for medical attention.

(6) thrombocytopenia: monitoring platelet count; when clinically instructed to reduce or discontinue administration.

(8) Embryonic fetal toxicity: Carfilzomib can cause fetal harm. Fertility women should be treated as a pregnancy should be avoided.

Adverse reactions

The most frequently reported adverse events (incidence ≥ 30%) are fatigue, anemia, nausea, thrombocytopenia, dyspnea, diarrhea, and fever.

Special people use

Patients are dialysis: After dialysis operation given Carfilzomib.

Storage

Unopened vials should be stored in the refrigerator (2 ° C to 8 ° C; 36 ° F to 46 ° F). Keep in the original packaging protected from light.