protein synthesis inhibitors
Treatment of chronic or accelerated phase chronic myeloid leukemia (CML) that has become resistant or intolerant to at least 2 tyrosine kinase inhibitors.
Inhibits protein synthesis.
Improved hematologic parameters and survival in CML.
Absorption: Absorbed following subcutaneous administration.
Distribution: Widely distributed.
Metabolism and Excretion: Metabolized by enzymes in plasma; not metabolized by the liver; 37 % excreted unchanged in urine.
Half-life: 6 hr.
TIME/ACTION PROFILE (response in Chronic Phase CML)
|Subcut||3.5 mo||unknown||12.5 mo|
TIME/ACTION PROFILE (response in Accelerated Phase CML)
|Subcut||2.3 mo||unknown||4.7 mo|
Use Cautiously in:
CNS: fatigue, headache, insomnia, anxiety, depression, mental status changes
EENT: epistaxis, ear pain, tinnitus
CV: angina, arrhythmias, peripheral edema
GI: diarrhea, anorexia, mucositis, nausea, constipation, stomatitis, ↑ liver function tests, upper abdominal pain, vomiting
Derm: alopecia, rash, hyperpigmentation, pruritus
Hemat: ANEMIA, NEUTROPENIA, THROMBOCYTOPENIA, lymphopenia
Local: injection site reactions
MS: arthralgia, myalgia, musculoskeletal pain
Metabolic: INFECTION, fever
Misc: hypersensitivity reactions, night sweats
* CAPITALS indicate life-threatening.
Underline indicate most frequent.
SC (Adults): Induction– 1.25 mg/m2 twice daily for 14 consecutive days of a 28-day cycle; maintenance– 1.25 mg/m2 twice daily for 7 consecutive days of a 28-day cycle. Modifications required for toxicity, treatment should be continued as long as benefit is noted.
Lyophilized powder for subcutaneous injection: 3.5 mg/vial
Lab Test Considerations:
Monitor CBC and platelet count weekly during induction and maintenance cycles. After initial maintenance cycles, monitor CBC and platelet count every 2 wks or as clinically indicated. If Grade 4 neutropenia occurs (ANC <0.5 × 109 /L) or Grade 3 thrombocytopenia (platelet count <50 × 109 /L) during a cycle, delay starting next cycle until ANC is ≥1.0 × 109 /L and platelet count is ≥50 × 109 /L. For next cycle, also reduce number of days by 2 days (e.g. to 12 or 5 days).
Reconstitute with 1 mL of 0.9% NaCl prior to use. Swirl gently until solution is clear; usually <1 minute. Concentration: 3.5 mg/mL.Do not administer solutions that are discolored or contain particulate matter. Avoid contact with skin; immediately wash affected area with soap and water. Protect from light. Use solution within 12 hr at room temperature or 6 days if refrigerated. Discard unused solution.
Improved hematologic parameters in CML.
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