- March 15, 2022
- Newsletter
- 617-430-5616
Menu
Menu
Menu
Menu
Menu
Menu
Brand Name :
Nerlynx
Synonyms :
neratinib
Class :
Antineoplastic agent and Tyrosinase Kinase Inhibitor/EFGR inhibitor
Dosage forms & Strengths
Tablet
40mg
Early-stage breast cancer
In the adults diagnosed with early-stage breast cancer, 240 mg of the drug in the form of tablets is administered orally each day for one year
In a cycle of 21 days
1-21 days- 240 mg orally each day, including
1-14 days- 750 mg/m2 capecitabine orally twice daily
Continue until unacceptable toxicities or disease progression
Dose Adjustments
In case of general toxicities and adverse reactions:
Monotherapy
1st dose reduction is 200 mg/day
2nd dose reduction is 160 mg/day
3rd dose reduction is 120 mg/day
When combined with capecitabine
1st dose reduction is 160 mg/day
2nd dose reduction is 120 mg/day
Renal impairment
No significant changes required
Hepatic impairment
Reduce the loading dose to 80 mg
The safety and efficacy of neratinib are not found for pediatric dosing
Refer to the adult dosing
neratinib: they may diminish the serum concentration of antacids
neratinib: they may diminish the serum concentration of antacids
neratinib: they may diminish the serum concentration of antacids
neratinib: they may diminish the serum concentration of antacids
neratinib: they may diminish the serum concentration of antacids
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
neratinib: they may diminish the serum concentration of CYP3A4 Inducers
neratinib: they may diminish the serum concentration of CYP3A4 Inducers
neratinib: they may diminish the serum concentration of CYP3A4 Inducers
neratinib: they may diminish the serum concentration of CYP3A4 Inducers
neratinib: they may diminish the serum concentration of CYP3A4 Inducers
neratinib increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of neratinib
CYP3A4 inducers decrease the concentration of neratinib in serum
metronidazole enhances the effect of neratinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
methimazole increases the effect of fedratinib when used simultaneously
may enhance the serum concentration of CYP3A4 inhibitors
it increases the gastric pH, thereby decreasing the effect or level of neratinib
it increases the gastric pH, thereby decreasing the effect or level of neratinib
it increases the gastric pH, thereby decreasing the effect or level of neratinib
in combination with the dengue vaccine, neratinib decreases its effect by immunosuppression
it increases the gastric pH, thereby decreasing the effect or level of neratinib
neratinib and siponimod, when used simultaneously, increase the effect of immunosuppression
sodium zirconium cyclosilicate
it increases the gastric pH, thereby decreasing the effect or level of neratinib
when both drugs are combined, there may be an increased level of serum concentration of etoposide
when both drugs are combined, there may be a decreased excretion rate of vincristine
when both drugs are combined, there may be an increased level of serum concentration of vinblastine
when both drugs are combined, there may be an increased metabolism of neratinib
when both drugs are combined, there may be a reduced excretion rate of topotecan and result in an elevated level of serum concentration
aluminum hydroxide/magnesium hydroxide
may diminish the serum concentration of Antacids
Actions and Spectrum:
Actions:
Spectrum:
Frequency defined:
>10%
Diarrhea
Nausea
Abdominal pain
Fatigue
Vomiting
Rash
Stomatitis
Decreased appetite
Muscle spasms
1-10%
Dyspepsia
ALT increased
Nail disorder
AST increased
Dry skin
Abdominal distension
Urinary tract infection
Decreased
Epistaxis
Dehydration
Dry mouth
Skin fissures
Minor:
Dehydration
Stomatitis
Rash
AST increased
Dyspepsia
Abdominal distension
Nail disorder
Decreased appetite
Skin fissures
Dry mouth
Urinary tract infection
Decreased weight
Muscle spasms
Contraindication/Caution:
Contraindications:
Cautions:
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 on the excretion of neratinib in breast milk is available. Due to the possibility of serious adverse effects, women are advised to breastfeed one month after the last dose of neratinib.
Pregnancy category:
Pharmacology:
neratinib is a tyrosine kinase inhibitor that works by blocking multiple signaling pathways involved in cell growth and division, which are often dysregulated in cancer cells. Specifically, it irreversibly binds to the intracellular domain of the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and HER4, preventing them from activating downstream signaling pathways.
Pharmacodynamics:
The pharmacodynamics of neratinib involve its effects on various signaling pathways that are involved in cell growth and division. Neratinib irreversibly binds to the intracellular domain of the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and HER4, which prevents these receptors from activating downstream signaling pathways.
Pharmacokinetics:
Absorption
The peak plasma is achieved in 2-8 hours (for active metabolites M3/M6/M7)
The peak plasma concentration is 1.7-times (for high fat); 1.2-times (for standard breakfast)
The area under the curve is 2.2-times (for high fat); and 1.1 times (for standard breakfast)
Distribution
The volume of distribution is 6433 L (for steady state)
The in-vitro protein-bound is more than 99%
Metabolism
Primarily metabolized by CYP3A4
Metabolites (active): M3, M6, M7, and M11
Elimination and Excretion
The half-life is 7-17 hours (for a single dose)
The drug is excreted 97.1% in feces and 1.13% in urine
Administration:
neratinib is an oral medication usually taken once daily, preferably at the same time every day, with a full glass of water. It should be taken on an empty stomach, either one hour before or two hours after a meal. Food can increase the absorption of neratinib, but it can also increase the risk of gastrointestinal side effects, so it is essential to follow specific instructions from the prescribing healthcare provider.
neratinib tablets should be swallowed whole and not crushed, broken, or chewed. If a dose is missed, it should be taken as soon as possible unless it is within 12 hours of the next scheduled dose. The missed dose should be skipped in that case, and the regular dosing schedule should be resumed.
Patient information leaflet
Generic Name: neratinib (Rx)
Pronounced: neh-RA-tih-nib
Why do we use neratinib?
neratinib is approved for use in several different settings of HER2-positive breast cancer, including:
ADVERTISEMENT
Founded in 2014, medtigo is committed to providing high-quality, friendly physicians, transparent pricing, and a focus on building relationships and a lifestyle brand for medical professionals nationwide.
