- March 15, 2022
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Brand Name :
Rydapt
Synonyms :
midostaurin
Class :
Antineoplastic agent and Tyrosinase Kinase Inhibitor
Dosage forms & Strengths:
Capsule
25mg
50 mg orally twice daily from the 8th to the 21st day of the cycle
Use the drug in combination with standard daunorubicin and cytarabine
The dose should be taken with food
midostaurin is indicated for patients having aggressive systemic mastocytosis, mast cell leukemia, or neoplasm-associated systemic mastocytosis
100 mg of the drug is given orally twice daily with meals
Note:
Before initiating the medication, administer antiemetics to prevent the risk of vomiting and nausea
Dose Adjustments
When the platelet count <50 x 10^9/L
Interrupt the dosing until platelet count reaches more than 50 x 10^9/L, later resume at 50 mg twice daily; if tolerated, increase the dose to 100 mg twice daily
Discontinue if decreased platelet count persists for more than 21 days and is suspected to be related to midostaurin
When hemoglobin <8 g/L
Interrupt the dosing until hemoglobin reaches more than 8 g/L, later resume at 50 mg twice daily; if tolerated, increase the dose to 100 mg twice daily
Discontinue the dose if the lower platelet count persists for more than 21 days and is related to midostaurin
Safety and efficacy of midostaurin are not found for pediatric dosing
Refer to the adult dosing
midostaurin is contraindicated in the patients who are hypersensitive to any of the excipients in the formulation
midostaurin: they may increase the QTc-prolonging effect of QTc-prolonging Agents
midostaurin: they may increase the QTc-prolonging effect of QTc-prolonging Agents
midostaurin: they may increase the QTc-prolonging effect of QTc-prolonging Agents
midostaurin: they may increase the QTc-prolonging effect of QTc-prolonging Agents
midostaurin: they may increase the QTc-prolonging effect of QTc-prolonging Agents
midostaurin is contraindicated in the patients who are hypersensitive to any of the excipients in the formulation
abametapir increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
atazanavir increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
bosentan decreases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
midostaurin and ceritinib, when used simultaneously, increase the QTc level
midostaurin and crizotinib, when used simultaneously, increase the QTc level
midostaurin and desflurane, when used simultaneously, increase the QTc level
midostaurin and entrecitinib, when used simultaneously, increase the QTc level
midostaurin and fingolimod, when used simultaneously, increase the QTc level
midostaurin and gilteritinib, when used simultaneously, increase the QTc level
idelalisib increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
ketoconazole increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
nelfinavir increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
oxcarbazepine decreases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
phenytoin decreases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
ritonavir increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
voriconazole increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of midostaurin
when used together, entrectinib and midostaurin both increase the QTc interval
when used together, encorafenib and midostaurin both increase the QTc interval
midostaurin and gilteritinib, when used in combination, increase the QTc interval
midostaurin and arformoterol, when used simultaneously, increase the QTc level
duvelisib increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
fedratinib increases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
lorlatinib decreases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
stiripentol decreases the effect or level of midostaurin by altering the CYP3A4 enzyme metabolism
midostaurin: they may diminish the serum concentration of CYP3A4 Inducers
midostaurin: they may diminish the serum concentration of CYP3A4 Inducers
midostaurin: they may diminish the serum concentration of CYP3A4 Inducers
midostaurin: they may diminish the serum concentration of CYP3A4 Inducers
midostaurin: they may diminish the serum concentration of CYP3A4 Inducers
when both drugs are combined, there may be a decreased metabolism of vinblastine
the effect of midostaurin is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
may increase the arrhythmogenic effect of Inhalational Anaesthetics
It may diminish the metabolism when combined with Melatonin
It may diminish the metabolism when combined with Melatonin
It may diminish the metabolism when combined with Melatonin
It may diminish the metabolism when combined with Melatonin
Actions and Spectrum:
Frequency defined:
>10%
Nausea
Febrile neutropenia
Hypocalcemia
Increased ALT
Mucositis
Vomiting
Headache
Petechiae
Musculoskeletal pain
Epistaxis
Device-related infection
Hypernatremia
Upper respiratory tract infection
Hyperglycemia
Increased ALT
Hemorrhoids
Arthralgia
Hyperhidrosis
Prolonged aPTT
Renal insufficiency
Insomnia
1-10%
Hyperuricemia
Hypertension
Cellulitis
Fungal infection
Dry skin
Weight increased
Pleural effusion
Thrombosis
Tremor
Pericardial effusion
Hypercalcemia
Eyelid edema
Minor:
Pneumonitis
Contraindication/Caution:
Pregnancy consideration: The drug is toxic and unsafe for pregnant women and the developing fetus. It may cause fetal death or lower birth weight.
Breastfeeding warnings: No data available regarding the excretion of midostaurin in breast milk. Due to the possibility of serious adverse effects, women are advised to breastfeed one month after the last dose of midostaurin.
Pregnancy category:
Pharmacology:
midostaurin inhibits the activity of multiple receptor tyrosine kinases by binding to their ATP-binding sites, preventing their autophosphorylation and downstream signaling pathways. This leads to decreased cell proliferation, induction of apoptosis, and inhibition of angiogenesis.
Pharmacodynamics:
The pharmacodynamics of midostaurin refers to the drug’s effects on the body and its mechanism of action. midostaurin is a small molecule inhibitor that selectively inhibits multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3), KIT, and platelet-derived growth factor receptor (PDGFR).
Pharmacokinetics:
Absorption
The peak plasma is achieved in 1-3 hours (single fasting dose) and 2.5-3 hours (with food)
Distribution
Protein-bound is more than 99.8%
The volume of distribution is 95.2 L
Metabolism
midostaurin undergoes primary metabolism by CYP3A4
Elimination and Excretion
The half-life is 21 hours for midostaurin; 32 hours (CGP62221) and 482 hours (CGP52421)
The systemic clearance rate is 14.9 L/hr
The drug is excreted 95% in feces and 4% in urine
Administration:
midostaurin is available in the form of oral capsules, and it is usually taken with food to enhance its absorption. The recommended dose and duration of treatment depend on the specific indication and the patient’s medical condition, as determined by their healthcare provider.
Here are some general guidelines for the administration of midostaurin:
Patient information leaflet
Generic Name: midostaurin (Rx)
Pronounced: MYE-doe-STAW-rin
Why do we use midostaurin?
midostaurin is an anti-cancer agent of the tyrosinase kinase inhibitor class. It is used for the treatment of several types of cancers, including advanced systemic mastocytosis (ASM) and acute myeloid leukemia (AML).
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