Dosing & Uses
Dosage Forms & Strengths
lyophilized powder for injection
- 3.5mg/vial (3.5mg/mL following reconstitution)
Chronic Myeloid Leukemia
Indicated for treatment of chronic or accelerated phase chronic myeloid leukemia (CML) with resistance and/or intolerance to ≥2 tyrosine kinase inhibitors
Induction: 1.25 mg/m² SC BID for 14 consecutive days q28 days; repeat q28 days until hematologic response achieved
Maintenance: 1.25 mg/m² SC BID for 7 consecutive days q28 days; continue as long as clinically beneficial
Dosing Modifications
Nonhematologic toxicities: Manage symptomatically; may interrupt and/or delay treatment until toxicity resolved
Neutropenia or thrombocytopenia
- Dosage cycles may be delayed and/or the number of days during the cycle reduced for hematologic toxicities (eg, neutropenia, thrombocytopenia)
- Grade 4 neutropenia (AND < 0.5 x 10^9/L) or grade 3 thrombocytopenia (platelets < 50 x 10^9/L): Delay starting next cycle until ANC ≥1 X 10^9/L and platelets ≥50 x 10^9/L
- For next cycle, reduce number of dosing days by 2 days (eg, to 12 or 5 days)
Safety and efficacy not established
Adverse Effects
>10% (Chronic Phase CML)
Thrombocytopenia (74%)
Anemia (61%)
Neutropenia (50%)
Infections and infestations (46%)
Diarrhea (42%)
Injection site reactions (34%)
Nausea (32%)
Fatigue (26%)
Pyrexia (24%)
Asthenia (23%)
Arthralgia (19%)
Headache (19%)
Lymphopenia (17%)
Cough (16%)
Alopecia (15%)
Constipation (15%)
Epistaxis (15%)
Abdominal pain, upper (14%)
Pain in extremities (13%)
Peripheral edema (13%)
Vomiting (12%)
Back pain (11%)
Hyperglycemia, grade 4 (11%)
Bone marrow failure (10%)
Febrile neutropenia (10%)
Insomnia (10%)
Rash (10%)
>10% (Accelerated Phase CML)
Thrombocytopenia (56%)
Infections and infestations (56%)
Anemia (51%)
Diarrhea (35%)
Fatigue (31%)
Pyrexia (29%)
Nausea (27%)
Asthenia (24%)
Injection site reactions (22%)
Febrile neutropenia (20%)
Neutropenia (20%)
Cough (15%)
Vomiting (15%)
Abdominal pain (13%)
Anorexia (13%)
Chills (13%)
Headache (13%)
Dyspnea (11%)
Epistaxis (11%)
Pain in extremities (11%)
Postmarketing Reports
Myelosuppression
Bleeding
Warnings
Contraindications
None
Cautions
Monitor CBC panel for myelosuppression
Grade 3/4 neutropenia, thrombocytopenia and anemia commonly occur; avoid use of anticoagulants, aspirin, and NSAIDs when platelet count is <50,000/ mm³
Therapy may induce glucose intolerance; monitor glucose levels frequently, especially in patients with diabetes or with risk factors for diabetes; avoid use in patients with poorly controlled diabetes; may initiate after glycemic control established
Avoid pregnancy
Pregnancy & Lactation
Pregnancy
Based on mechanism of action and findings from animal studies, therapy can cause fetal harm when administered to pregnant women
There are no available data on pregnant women to evaluate for a drug- associated risk of major birth defects, miscarriage or adverse maternal or fetal outcomes; advise pregnant women of potential risk to a fetus
Pregnancy testing is recommended for females of reproductive potential prior to initiating therapy
Infertility
-
Males
- Based on findings from animal studies, therapy may impair male fertility; studies in mice demonstrated adverse effects on male reproductive organs where bilateral degeneration of seminiferous tubular epithelium in testes and hypospermia/aspermia were observed; long-term effects on male fertility, including reversibility of adverse effects, not studied
Contraception
-
Females
- Drug can cause embryo-fetal harm when administered to pregnant women; advise female patients of reproductive potential to use effective contraception during treatment and for 6 months after final dose
-
Males
- Based on genotoxicity findings, advise males with female partners of reproductive potential to use effective contraception during treatment and for 3 months after final dose.
Animal data
- In animal reproduction studies, subcutaneous administration of drug to pregnant mice during organogenesis at doses approximately 0.25-0.5 times the maximum recommended human doses (MRHD) resulted in embryo-fetal mortality, structural abnormalities, and alterations to growth
Lactation
There are no data on presence of drug in either human or animal milk, effects on breastfed child, or on milk production; because of potential for serious adverse reactions in breastfed child, advise patients that breastfeeding is not recommended during treatment and for 2 weeks after final dose
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibition of protein synthesis and is independent of direct Bcr-Abl binding; binds to the A-site cleft in the peptidyl-transferase center of the large ribosomal subunit from a strain of archaeabacteria
Absorption
Peak Plasma Time: 30 minutes
Distribution
Protein Bound: 50%
Vd: 141 ±93.4 L
Metabolism
Hydrolyzed to 4′-DMHHT via plasma esterases; little evidence of hepatic microsomal oxidative and/or esterase-mediated metabolism in vitro
Elimination
Half-life: 6 hr
Excretion: ≤15% unchanged in urine
Administration
Administration
Inject subcutaneously
Follow institutional guidelines for preparing, administering, and disposal of chemotherapy
Preparation
- Reconstitute with 1 mL of 0.9% NaCl
- After addition of the diluent, gently swirl until a clear solution obtained
- Lyophilized powder should be completely dissolved in <1 minute
- Resulting solution concentration is 3.5 mg/mL
- Does not contain antimicrobial preservatives
Home administration
Provide training on proper handling, storage conditions, administration, disposal, and clean-up of accidental spillage of the product
Ensure that patients receive the necessary supplies for home administration. at minimum these should include:
- Reconstituted omacetaxine with patient-specific dose in syringe with a capped needle for SC injection
- Protective eyewear
- Gloves
- An appropriate biohazard container
- Absorbent pad(s) for placement of administration materials and for accidental spillage
- Alcohol swabs
- Gauze pads
- Ice packs or cooler for transportation of reconstituted syringes
Storage
Reconstituted solution: Use within 12 hr when stored at room temperature and within 6 days if refrigerated between 2- 8 °C (36-46°F)
Protect reconstituted solution from light
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Formulary
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