MARQIBO KIT
Clinical safety rating
cautionComprehensive clinical and safety monograph for MARQIBO KIT (MARQIBO KIT).
Comprehensive clinical and safety monograph for MARQIBO KIT (MARQIBO KIT).
Treatment of adult patients with Philadelphia chromosome-negative (Ph-) acute lymphoblastic leukemia (ALL) in second or greater relapse or whose disease has progressed after two or more anti-leukemia therapies
Vinca alkaloid that binds to tubulin, inhibiting microtubule assembly and mitotic spindle formation, causing metaphase arrest in dividing cells.
| Metabolism | Primarily hepatic metabolism via CYP3A4; also undergoes biliary excretion. |
| Excretion | Primarily hepatobiliary excretion; approximately 5-16% of the dose is excreted unchanged in the urine over 72 hours. Fecal excretion accounts for about 10% of the administered dose, with the remainder undergoing extensive hepatic metabolism and biliary elimination. |
| Half-life | Terminal elimination half-life ranges from 19 to 40 hours (mean 23 hours) in adults. The prolonged half-life in Marqibo (liposomal vincristine) is due to the sustained release from the liposomal formulation, allowing once-weekly dosing. |
| Protein binding | Approximately 75% bound to plasma proteins, primarily to albumin and beta-globulins. |
| Volume of Distribution | Volume of distribution (Vd) is 4.0-7.9 L/kg (mean 5.6 L/kg), indicating extensive tissue binding and distribution into tissues, consistent with its lipophilic nature. |
| Bioavailability | Not applicable; Marqibo is administered intravenously only. Oral bioavailability is negligible (<5%) due to extensive first-pass metabolism and P-glycoprotein efflux. |
| Onset of Action | Onset of clinical effect (antitumor activity) is typically observed within 1-2 weeks of initiating therapy, corresponding to the time required for vincristine to reach therapeutic concentrations in tumor tissues. |
| Duration of Action | Duration of clinical effect after a single dose is approximately 2-3 weeks, allowing for every-2-week dosing schedule. The prolonged duration is attributed to the sustained release from liposomes and the long half-life. |
| Molecular Weight | 924.99 |
2.25 mg/m2 intravenously over 1 hour every 7 days. Maximum dose per administration is 3.6 mg.
| Dosage form | INJECTABLE, LIPOSOMAL |
| Renal impairment | No specific dose adjustment guidelines. Use caution in patients with creatinine clearance <50 mL/min due to potential for increased exposure. |
| Liver impairment | Contraindicated in patients with severe hepatic impairment (Child-Pugh class C). For moderate impairment (Child-Pugh B), reduce dose to 1.8 mg/m2 every 7 days. Mild impairment (Child-Pugh A): no adjustment necessary. |
| Pediatric use | Safety and efficacy not established in patients <18 years. Data limited to case reports; no standard dosing guidelines available. |
| Geriatric use | No specific dose adjustment based on age alone. Monitor closely for increased toxicity (e.g., neurotoxicity, myelosuppression) due to potential for decreased organ function and comorbidities. |
| 1st trimester | Contraindicated due to embryotoxicity; avoid pregnancy. Animal studies show teratogenicity. |
| 2nd trimester | Contraindicated; may cause fetal harm. Use only if benefit outweighs risk. |
| 3rd trimester | Contraindicated; may cause fetal harm. Use only if benefit outweighs risk. |
Clinical note
Comprehensive clinical and safety monograph for MARQIBO KIT (MARQIBO KIT).
| Placental transfer | Yes; vincristine crosses placenta; fetal malformations reported in animals. |
| Breastfeeding | Excreted in human milk; potential for serious adverse reactions in nursing infants. Discontinue breastfeeding or drug, considering importance of drug to mother. |
| Lactation Rating | L5 |
| Teratogenic Risk | Pregnancy Category D. First trimester: high risk of embryofetal toxicity including malformations (neural tube, cardiac, skeletal defects) and spontaneous abortion. Second and third trimesters: risk of fetal growth restriction, oligohydramnios, and preterm birth. Avoid in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor complete blood counts (CBC), hepatic function, and renal function. During pregnancy, perform fetal ultrasound for growth and anatomy, and monitor amniotic fluid volume. Assess for signs of tumor lysis syndrome and neuropathy. |
| Fertility Effects | May cause ovarian failure and testicular dysfunction. Reversible or permanent infertility possible. Advise fertility preservation before treatment. Men may experience azoospermia, women amenorrhea and premature menopause. |
■ FDA Black Box Warning
MARQIBO is for intravenous use only. Fatal if given intrathecally. Use only with a medical provider experienced in the administration of chemotherapeutic agents. Contains vincristine sulfate, a vesicant. Ensure proper administration technique.
| Serious Effects |
Hypersensitivity to vincristine or any componentIntrathecal administrationPatients with demyelinating conditions (e.g., Charcot-Marie-Tooth syndrome)
| Precautions | Extensive extravasation precautions required; neurotoxicity (peripheral neuropathy, autonomic neuropathy); hematologic toxicity (myelosuppression); gastrointestinal toxicity (constipation, ileus); hepatic impairment; monitor serum uric acid levels; embryo-fetal toxicity. |
| Food/Dietary | Avoid grapefruit and grapefruit juice as they may inhibit CYP3A4 and alter drug levels. Avoid St. John's wort as it may induce CYP3A4 and reduce efficacy. No specific food restrictions other than these. Maintain adequate hydration to prevent tumor lysis syndrome. |
| Clinical Pearls | MARQIBO KIT (vincristine sulfate liposome injection) is indicated for adult patients with Philadelphia chromosome-negative (Ph-) relapsed or refractory acute lymphoblastic leukemia (ALL). It is a liposomal formulation of vincristine that prolongs drug exposure and enhances tumor delivery. Administer intravenously over 1 hour at a dose of 2.25 mg/m² without a maximum dose cap, unlike standard vincristine. Do not substitute for other vincristine formulations. Monitor for neurotoxicity, including peripheral neuropathy, autonomic neuropathy (constipation, ileus), and cranial nerve palsies. Premedicate with corticosteroids and antiemetics. Avoid concomitant use of strong CYP3A4 inducers or inhibitors due to altered metabolism. Neurotoxicity is dose-limiting and may require dose reduction or discontinuation. Tumor lysis syndrome may occur; ensure adequate hydration and allopurinol. Pregnancy category D; verify pregnancy status. Extravasation management is similar to other vinca alkaloids (apply heat, hyaluronidase). |
| Patient Advice | This medication is a form of chemotherapy given intravenously for a type of leukemia. · It may cause nerve damage; report numbness, tingling, pain, weakness, or constipation immediately. · Do not receive any live vaccines during treatment and for 6 months after. · Use effective contraception during treatment and for at least 1 month after the last dose. · Avoid grapefruit juice and St. John's wort while on this medication. · Drink plenty of fluids to prevent tumor lysis syndrome. · Report any signs of infection (fever, chills) or bleeding (easy bruising, black stools). |
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