II. Indications

  1. Breast Cancer (locally advanced or metastatic)

III. Contraindications

  1. Liver transaminases (AST, ALT) >2.5 times the upper limit of normal
  2. Serum Bilirubin > upper limit of normal
  3. Polyoxyethylated Castor Oil (Cremophor EL) allergy

IV. Mechanism

  1. See Mitotic Inhibitor Chemotherapy
  2. Ixabepilone is a semisynthetic analog of epothilone B with antineoplastic properties
    1. Used in Taxane-resistant neoplasms
    2. Available in an enteric coated oral formulation with good Bioavailability
  3. Ixabepilone is an anti-tubulin agent
    1. Ixabepilone binds to tubulin
    2. Ixabepilone promotes tubulin polymerization and microtubule stabilization
    3. Arrests Cell Cycle at G2/M phase

V. Medications

  1. Ixabepilone 15 and 45 mg powder for injection

VI. Dosing

  1. See other references for disease specific dosing protocols
  2. Pretreatment (given 1 hour before Ixabepilone )
    1. Anthistamine (H1 Blocker) AND
    2. H2 Blocker (e.g. Famotidine) AND
    3. If prior reaction, Corticosteroid

VII. Adverse Effects

VIII. Safety

  1. Avoid in Lactation
  2. Avoid in pregnancy (all trimesters)
    1. Use reliable Contraception

IX. Drug Interactions

  1. Agents that increase Ixabepilone levels
    1. CYP3A4 Inhibitors (e.g. Ketoconazole)
  2. Agents that decrease Ixabepilone levels
    1. CYP3A4 Inducers (e.g. Rifampin)

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Ontology: ixabepilone (C1135132)

Definition (NCI_NCI-GLOSS) A drug used to treat metastatic or locally advanced breast cancer that has not improved after treatment with certain other anticancer drugs. It is also being studied in the treatment of other types of cancer. Ixempra stops the growth of tumor cells by blocking cell division. It is a type of epothilone analog.
Definition (NCI) An orally bioavailable semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines.
Definition (NCI) An enteric-coated formulation of ixabepilone, a semisynthetic analogue of epothilone B and a non-taxane tubulin inhibitor, with antineoplastic activity. Ixabepilone binds to and stabilizes tubulin molecules, thereby interfering with the dynamics of microtubule assembly/disassembly. This results in cell cycle arrest at the G2-M phase and leads to apoptosis within fast growing tumor cells. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. Compared to intravenously administered ixabepilone, the oral formulation provides a more manageable way to administer this agent.
Definition (PDQ) A semisynthetic analogue of epothilone B with antineoplastic activity. Ixabepilone (BMS-247550) binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arresting cells in the G2-M phase of the cell cycle and inducing tumor cell apoptosis. This agent demonstrates antineoplastic activity against taxane-resistant cell lines. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=37860&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=37860&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C37452" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C430592
SnomedCT 428282007, 429022006
English Epothilone, (1S,3S,7S,10R,11S,12S,16R)-7,11-Dihydroxy-8,8,10,12,16-pentamethyl-3-[(1E)-1-methyl-2-(2-methyl-4-thiazolyl)ethenyl]-17-oxa-4-azabicyclo[14.1.0]heptadecane-5,9-dione, ixabepilone, Azaepothilone B, ixabepilone (oral), Oral Ixabepilone, IXABEPILONE, Ixabepilone (substance), Ixabepilone, Ixabepilone (product), ixabepilone (medication), ixabepilone [Chemical/Ingredient]
Spanish ixabepilona (producto), ixabepilona, ixabepilona (sustancia)