cabazitaxel

Contraindicated in:

Severe hypersensitivity to cabazitaxel or polysorbate 80;
Neutrophil count ≤1,500/mm³;
Hepatic impairment (total bilirubin ≥3× upper limit of normal [ULN]);
Concurrent use of strong CYP3A4 inhibitors or inducers.

Use Cautiously in:

Patients with neutropenia or a history of pelvic radiation, adhesions, ulceration, or GI bleeding (↑ risk of GI and urinary adverse reactions);
Concomitant use of steroids, NSAIDs, or antithrombotics (↑ risk of GI adverse reactions);
Severe renal impairment (CCr <30 mL/min) or end-stage renal disease;
Hemoglobin <10 g/dL;
Lung disease (↑ risk of pulmonary toxicity);
Mild or moderate hepatic impairment (dose ↓ required);
Poor performance status, previous episodes of febrile neutropenia, extensive prior radiation ports, or poor nutritional status (↑ risk of complications from prolonged neutropenia);
Rep: Men with female partners of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: ↑risk of adverse reactions in older adults (especially prolonged neutropenia and febrile neutropenia).

Adv. Reactions/Side Effects ⬆ ⬇

CV: arrhythmias, hypotension

F and E: electrolyte imbalance

GI: abdominal pain, abnormal taste, anorexia, constipation, diarrhea, gi bleed, gi perforation, nausea, vomiting, dyspepsia, ENTEROCOLITIS, ILEUS

GU: hematuria, cystitis, RENAL FAILURE

Hemat: anemia, leukopenia, neutropenia, thrombocytopenia

MS: arthralgia, back pain, muscle spasms

Neuro: peripheral neuropathy, weakness, fatigue

Resp: dyspnea, ACUTE RESPIRATORY DISTRESS SYNDROME, INTERSTITIAL LUNG DISEASE

Misc: fever, HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS)

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A inhibitors including ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, and voriconazole↑ levels and risk of toxicity; concurrent use contraindicated.
Strong CYP3A inducers including phenytoin, carbamazepine, rifampin, rifabutin, rifapentin, and phenobarbital may ↓ levels and effectiveness; concurrent use contraindicated.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness; concomitant use contraindicated.

Availability ⬆ ⬇

(Generic available)

Viscous solution for injection: 40 mg/mL (contains polysorbate 80); comes with diluent (5.7 mL of 13% [w/w] ethanol in water for injection)
Solution for injection: 10 mg/mL

Route/Dosage ⬆ ⬇

IV (Adults ): 20 mg/m² every 3 wk (with prednisone 10 mg PO daily). A dose of 25 mg/m² may be considered in select patients.

Hepatic Impairment

IV (Adults ): Mild hepatic impairment (total bilirubin >1× to ≤1.5× ULN or AST >1.5× ULN): 20 mg/m² every 3 wk (with prednisone 10 mg PO daily); Moderate hepatic impairment (total bilirubin >1.5× to ≤3× ULN): 15 mg/m² every 3 wk (with prednisone 10 mg PO daily); Severe hepatic impairment (total bilirubin >3× ULN): Contraindicated.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Binds to intracellular tubulin and promotes its assembly into microtubules while inhibiting disassembly. Result is inhibition of mitosis and interphase.

Therapeutic effects:

Death of rapidly replicating cells, particularly malignant ones, with ↓ spread of metastatic prostate cancer.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacologic Classification: taxoids

Pharmacokinetics ⬆ ⬇

Absorption: IV administration results in complete bioavailability.

Distribution: Equally distributed between blood and plasma.

Metabolism/Excretion: Extensively (>95%) metabolized by the liver, 80–90% by the CYP3A4/5 isoenzymes. Metabolites are excreted in urine and feces. Minimal renal excretion.

Half-Life: 95 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
IV	rapid	end of infusion	unknown

Patient/Family Teaching ⬆ ⬇

Instruct patient to take oral prednisone as prescribed and to notify health care professional if a dose is missed or not taken in time.
Advise patient to notify health care professional immediately if signs or symptoms of hypersensitivity reactions; fever; sore throat; signs of infection; lower back or side pain; difficult or painful urination; sores on the mouth or on the lips; bleeding gums; bruising; petechiae; blood in urine, stool, or emesis; unusual swelling, shortness of breath, trouble breathing, chest pain, cough, or fever occur. Caution patient to avoid crowds and persons with known infections. Instruct patient to use soft toothbrush and electric razor and to avoid falls. Patient should also be cautioned not to drink alcoholic beverages or to take products containing aspirin or NSAIDs; may precipitate GI hemorrhage.
May cause dizziness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially St. John's wort.
Instruct patient not to receive any vaccinations without advice of health care professional.
Rep: Advise male patients with female partners of reproductive potential to use effective contraception during and for at least 4 mo after last dose of cabazitaxel. May impair fertility in males.
Emphasize need for periodic lab tests to monitor for side effects. Advise patient to monitor temperature frequently.

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Indications ⬇

Contraind./Precautions ⬆ ⬇