Omacetaxine

Name: Omacetaxine

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

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

Omacetaxine and Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if omacetaxine is excreted in human breast milk. Because this medication may harm your nursing baby, you should not breastfeed while receiving omacetaxine.

Omacetaxine Overdose

Omacetaxine is usually administered by a healthcare provider in a medical setting making it unlikely for an overdose to occur. However, if overdose is suspected, seek emergency medical attention.

Omacetaxine side effects

Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat.

Call your doctor at once if you have:

  • easy bruising, unusual bleeding (nose, mouth, vagina, or rectum);

  • confusion, vision changes, slurred speech;

  • blood in your urine, bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;

  • severe skin rash;

  • high blood sugar--increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss; or

  • low blood cell counts--fever, chills, flu-like symptoms, swollen gums, mouth sores, skin sores, rapid heart rate, pale skin, easy bruising, unusual bleeding, feeling light-headed.

Common side effects may include:

  • stomach pain, nausea, vomiting;

  • diarrhea, constipation;

  • fever, infections;

  • bruising or bleeding;

  • hair loss;

  • weakness, tired feeling; or

  • pain, swelling, or irritation where the medicine was injected.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What do I need to tell my doctor BEFORE I take Omacetaxine?

  • If you have an allergy to omacetaxine or any other part of omacetaxine.
  • If you are allergic to any drugs like this one, any other drugs, foods, or other substances. Tell your doctor about the allergy and what signs you had, like rash; hives; itching; shortness of breath; wheezing; cough; swelling of face, lips, tongue, or throat; or any other signs.
  • If you have high blood sugar (diabetes).
  • If you are breast-feeding. Do not breast-feed while you take this medicine.

This is not a list of all drugs or health problems that interact with omacetaxine.

Tell your doctor and pharmacist about all of your drugs (prescription or OTC, natural products, vitamins) and health problems. You must check to make sure that it is safe for you to take this medicine with all of your drugs and health problems. Do not start, stop, or change the dose of any drug without checking with your doctor.

What are some other side effects of Omacetaxine?

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

  • Headache.
  • Belly pain.
  • Feeling tired or weak.
  • Not hungry.
  • Muscle or joint pain.
  • Back pain.
  • Hair loss.
  • Not able to sleep.
  • Irritation where the shot is given.

These are not all of the side effects that may occur. If you have questions about side effects, call your doctor. Call your doctor for medical advice about side effects.

You may report side effects to the FDA at 1-800-FDA-1088. You may also report side effects at http://www.fda.gov/medwatch.

Other Comments

Administration advice:
-For subcutaneous injection
-May be administered in the home setting. The manufacturer's product information should be consulted for further information.

Reconstitution/preparation techniques:
-Reconstitute with 1 mL of 0.9% sodium chloride injection, USP.
-The manufacturer's product information should be consulted for detailed reconstitution information.

Storage requirements (reconstituted):
-Room Temperature: Use within 12 hours of reconstitution.
-Refrigerated: Use within 6 days of reconstitution.
-Protect reconstituted solution from light.

(web3)