Ixabepilone

Ixabepilone is a semi-synthetic analog of epothilone B. Ixabepilone binds directly to β-tubulin subunits on microtubules, leading to suppression of microtubule dynamics.

• IXEMPRA is indicated in combination with capecitabine for the treatment of patients with metastatic or locally advanced breast cancer resistant to treatment with an anthracycline and a taxane, or whose cancer is taxane resistant and for whom further anthracycline therapy is contraindicated. Anthracycline resistance is defined as progression while on therapy or within 6 months in the adjuvant setting or 3 months in the metastatic setting.ICD-10: C50.919

• IXEMPRA is contraindicated in patients who have: a neutrophil count <1500 cells/mm 3 or a platelet count <100,000 cells/mm 3 [see Warnings and Precautions ( 5.2 )]. a history of severe hypersensitivity to agents containing Cremophor ® EL or its derivatives (e.g., polyoxyethylated castor oil) [see Warnings and Precautions ( 5.4 )].contraindicated

The recommended dosage of IXEMPRA is 40 mg/m 2 administered as a 3-hour intravenous infusion once every 3 weeks ( 2.2 ). Dose reduction is required in patients with elevated AST, ALT, or bilirubin.( 2.3, 8.6 ) IXEMPRA must be reconstituted with the supplied DILUENT and further diluted to a concentration of 0.2 mg/mL to 0.6 mg/mL prior to administration ( 2.6 ). 2.1 Premedication All patients must be premedicated approximately 1 hour before the infusion of IXEMPRA with: An H 1 antagonist (eg, diphenhydramine 50 mg orally or equivalent) and An H 2 antagonist (eg, ranitidine 150 - 300 mg orally or equivalent). Patients who experienced a hypersensitivity reaction to IXEMPRA require premedication with corticosteroids (eg, dexamethasone 20 mg intravenously, 30 minutes before infusion or orally, 60 minutes before infusion) in addition to pretreatment with H 1 and H 2 antagonists [see Warnings and Precautions ( 5.4 )] . 2.2 Recommended Dosage The recommended dosage of IXEMPRA is 40 mg/m 2 administered intravenously over 3 hours every 3 weeks. Calculate doses for patients with body surface area (BSA) greater than 2.2 m 2 should be calculated based on 2.2 m 2 . 2.3 Dosage Modification for Adverse Reactions Evaluate patients during treatment by periodic clinical observation and laboratory tests including complete blood cell counts [see the Warnings and Precautions ( 5 )]. Dosage modifications for IXEMPRA for adverse reactions are shown in Table 1. If adverse reactions recur, reduce dose by an additional 20%.

Peripheral Neuropathy: Monitor for symptoms of neuropathy (sensory and motor neuropathy).) Withhold, reduce, or discontinue IXEMPRA depending on severity. ( 2.3 , 5.1 ). Myelosuppression: Neutropenia, febrile neutropenia, and infections have occurred. Monitor blood cell counts before and during treatment with IXEMPRA. Withhold, reduce, or discontinue IXEMPRA depending on severity ( 2.3 , 5.2 ). Increased Toxicity in Patients with Hepatic Impairment: Grade 4 neutropenia, febrile neutropenia, and serious adverse reactions may occur in patients with hepatic impairment during treatment with IXEMPRA. Reduce dose depending on severity. ( 2.3 , 5.3 , 6.1 ). Hypersensitivity Reactions: Severe hypersensitivity reactions (including anaphylaxis) have occurred. Premedicate all patients before treatment with IXEMPRA. Withhold, reduce, or discontinue IXEMPRA depending on severity ( 2.1 , 2.3 , 5.4 ). Cardiac Adverse Reactions: Myocardial ischemia and ventricular dysfunction have occurred. Closely monitor patients with a history of cardiac disease during treatment with IXEMPRA. Consider discontinuation of IXEMPRA in patients who develop cardiac ischemia or impaired cardiac function ( 2.3 , 5.5 ). Embryo-Fetal Toxicity: Can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception ( 5.6 , 8.1 , 8.3) Alcohol Content: The alcohol content in a dose of IXEMPRA may affect the central nervous system. This may include impairment of a patient's ability to drive or use machines immediately after infusion. ( 5.7 ).

The following adverse reactions are discussed in greater detail in other sections. Peripheral neuropathy [see Warnings and Precautions ( 5.1 )] Myelosuppression [see Warnings and Precautions ( 5.2 )] Hypersensitivity reactions [see Warnings and Precautions ( 5.4 )] Cardiac Adverse reactions [see Warnings and Precautions ( 5.5) ] The most common adverse reactions (≥20%) are peripheral sensory neuropathy, fatigue/asthenia, myalgia/arthralgia, alopecia, nausea, vomiting, stomatitis/mucositis, diarrhea, and musculoskeletal pain. Additional reactions occurred in ≥20% in combination treatment: palmar-plantar erythrodysesthesia syndrome, anorexia, abdominal pain, nail disorder, and constipation ( 6 ). Hematologic laboratory abnormalities (>40%) include neutropenia, leukopenia, anemia, and thrombocytopenia ( 6 ). To report SUSPECTED ADVERSE REACTIONS, contact R-Pharm US at 1-844-586-8953 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, the adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in other clinical trials and may not reflect the rates observed in clinical practice. Unless otherwise specified, assessment of adverse reactions is based on one randomized study (Study 046) and one single-arm study (Study 081).

Lactation: Advise not to breastfeed ( 8.2 ). Hepatic Impairment: Reduce the dosage in patients with elevated AST, ALT, or bilirubin ( 2.4 , 8.6 ). 8.1 Pregnancy Risk Summary Based on findings in animals and its mechanism of action, IXEMPRA can cause fetal harm when administered to a pregnant woman [see Clinical Pharmacology ( 12.1 )] . There are no available data on the use of IXEMPRA in pregnant women to inform the drug-associated risk. IXEMPRA contains alcohol which can interfere with neurobehavioral development [see Clinical Considerations]. In animal reproduction studies, intravenous administration of ixabepilone to pregnant rats and rabbits during the period of organogenesis caused maternal toxicity, embryo-fetal lethality, and fetal abnormalities at maternal exposures below the human clinical exposure based on AUC (see Data). Advise females of reproductive potential and pregnant women of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Clinical Considerations IXEMPRA contains alcohol [see Warnings and Precautions ( 5.7 )] .

Metabolism

Following administration of a single 40 mg/m 2 dose of IXEMPRA, the mean (% coefficient of variation) maximum plasma concentration (Cmax) was 252 ng/mL (56%), and the mean (%CV) area under the curve (AUC) was 2,143 ng·hr/mL (48%). The pharmacokinetics of ixabepilone were linear at doses of 15 (0.375 times the approved recommended dosage) to 57 mg/m 2 (1.425 times the approved recommended dosage).

In patients who received an overdosage of IXEMPRA of up to 100 mg/m 2 (approximately 2.5 times the recommended dosage), peripheral neuropathy, fatigue, musculoskeletal pain/myalgia, and gastrointestinal symptoms (nausea, anorexia, diarrhea, abdominal pain, stomatitis) occurred. There is no known antidote for overdosage of IXEMPRA. In case of overdosage, closely monitor patients for adverse reactions and provide supportive treatment as clinically indicated.

• Oct 16, 2007NDANDA022065R-pharm Us Llc

1. 1Death10610%
2. 2Vomiting949.0%
3. 3Nausea938.9%
4. 4Anaemia918.7%
5. 5Fatigue898.5%
6. 6Diarrhoea767.2%
7. 7Malignant Neoplasm Progression706.7%
8. 8White Blood Cell Count Decreased696.6%
9. 9Neutropenia686.5%
10. 10Neutrophil Count Decreased676.4%
11. 11Dyspnoea605.7%
12. 12Dehydration575.4%
13. 13Neuropathy Peripheral525.0%
14. 14Febrile Neutropenia494.7%
15. 15Disease Progression454.3%

The 10 most recently updated of 120 ClinicalTrials.gov registrations naming Ixabepilone as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Paclitaxel, Carboplatin, and Bevacizumab or Paclitaxel, Carboplatin, and Temsirolimus or Ixabepilone, Carboplatin, and Bevacizumab in Treating Patients With Stage III, Stage IV, or Recurrent Endometrial Cancer
  Active not recruiting · Phase 2 · Interventional · 349 enrolled · National Cancer Institute (NCI)
  NCT00977574updated 2026-05-29
• Ixabepilone in Treating Participants With Significant Residual Disease of HER2/Neu Negative Invasive Breast Cancer After Systemic Therapy
  Active not recruiting · Phase 2 · Interventional · 116 enrolled · M.D. Anderson Cancer Center
  NCT00877500updated 2026-05-22
• Ixabepilone and Temsirolimus in Treating Patients With Solid Tumors That Are Metastatic or Cannot Be Removed by Surgery
  Active not recruiting · Phase 1 · Interventional · 22 enrolled · National Cancer Institute (NCI)
  NCT01375829updated 2026-04-13
• Anti-tumor Effect of Ixabepilone in Metastatic Breast Cancer (mBC) Selected by the Ixabepilone DRP.
  Terminated · Phase 2 · Interventional · 13 enrolled · Allarity Therapeutics
  NCT04796324updated 2026-03-12
• Investigational Drug in Combination With Two Chemotherapy Drugs in Women With Locally Recurrent or Metastatic Breast Cancer
  Withdrawn · Phase 1 · Phase 2 · Interventional · 0 enrolled · Sidney Kimmel Comprehensive Cancer Center at Thomas Jefferson University
  NCT01349088updated 2025-05-02
• Pharmacodynamic Biomarkers of Standard Anti-microtubule Drugs as Assessed by Early Tumor Biopsy
  Terminated · Observational · 5 enrolled · University of Wisconsin, Madison
  NCT03393741updated 2024-06-25
• Evaluation of Weekly Ixabepilone With or Without Biweekly Bevacizumab
  Completed · Phase 2 · Interventional · 78 enrolled · Yale University
  NCT03093155updated 2024-05-14
• BMS-247550 in Treating Patients With Cancers That Have Not Responded to Previous Therapy
  Completed · Phase 1 · Interventional · National Cancer Institute (NCI)
  NCT00020371updated 2024-03-04
• Safety and Efficacy Comparison of Docetaxel and Ixabepilone in Non Metastatic Poor Prognosis Breast Cancer
  Completed · Phase 3 · Interventional · 762 enrolled · UNICANCER
  NCT00630032updated 2024-02-21
• Ixabepilone and Hydroxychloroquine in Treating Patients With Metastatic Breast Cancer
  Terminated · Phase 1 · Phase 2 · Interventional · 6 enrolled · University of Medicine and Dentistry of New Jersey
  NCT00765765updated 2023-08-09

Frequently asked questions

How does Ixabepilone work?

Ixabepilone is a semi-synthetic analog of epothilone B. Ixabepilone binds directly to β-tubulin subunits on microtubules, leading to suppression of microtubule dynamics.

What is Ixabepilone used for?

According to FDA labeling, Ixabepilone carries indications including: IXEMPRA is indicated in combination with capecitabine for the treatment of patients with metastatic or locally advanced breast cancer resistant to treatment with an anthracycline and a taxane, or whose cancer is taxane resistant and for whom further anthracycline therapy is contraindicated. Anthracycline resistance is defined as progression while on therapy or within 6 months in the adjuvant setting or 3 months in the metastatic setting.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ixabepilone?

Ixabepilone is classified as Other cytotoxic antibiotics, Microtubule Inhibitor, Tubulin Interactions, Decreased Mitosis, Increased Cellular Death, Microtubule Inhibition.

What are the brand names for Ixabepilone?

Ixabepilone is marketed under brand names including IXEMPRA.

What are the contraindications for Ixabepilone?

Ixabepilone labeling lists contraindications including: IXEMPRA is contraindicated in patients who have: a neutrophil count <1500 cells/mm 3 or a platelet count <100,000 cells/mm 3 [see Warnings and Precautions ( 5.2 )]. a history of severe hypersensitivity to agents containing Cremophor ® EL or its derivatives (e.g., polyoxyethylated castor oil) [see Warnings and Precautions ( 5.4 )].. Always consult the full prescribing information and a clinician.