Neratinib Maleate

Hercent is a kinase inhibitor indicated:
As a single agent, for the extended adjuvant treatment of adult patients with early-stage HER2-positive breast cancer, to follow adjuvant Trastuzumab based therapy.
In combination with Capecitabine, for the treatment of adult patients with advanced or metastatic HER2-positive breast cancer who have received two or more prior anti-HER2 based regimens in the metastatic setting.

Dosage & Administration

Premedication for diarrhea
: When not using dose escalation, initiate loperamide with the first dose of Neratinib and continue during the first 56 days of treatment. After day 56, use loperamide to maintain 1–2 bowel movements per day.
Extended adjuvant treatment of early-stage breast cancer
: 240 mg (6 tablets) given orally once daily, with food, continuously until disease recurrence for up to one year.
Advanced or metastatic breast cancer
: 240 mg (6 tablets) given orally once daily with food on Days 1–21 of a 21-day cycle plus capecitabine (750 mg/m2 given orally twice daily) on Days 1–14 of a 21-day cycle until disease progression or unacceptable toxicities.
Dose escalation
: A two-week dose escalation for Neratinib may also be initiated.
Hepatic impairment
: Reduce starting dose to 80 mg in patients with severe hepatic impairment.
Dose Modifications-
Recommended starting dose: 240 mg daily
First dose reduction: 200 mg daily
Second dose reduction: 160 mg daily
Third dose reduction: 120 mg daily

The most common adverse reactions (reported in ≥5% of patients) were:
Hercent as a single agent
: diarrhea, nausea, abdominal pain, fatigue, vomiting, rash, stomatitis, decreased appetite, muscle spasms, dyspepsia, AST or ALT increased, nail disorder, dry skin, abdominal distention, epistaxis, weight decreased, and urinary tract infection.
Hercent in combination with capecitabine
: diarrhea, nausea, vomiting, decreased appetite, constipation, fatigue/asthenia, weight decreased, dizziness, back pain, arthralgia, urinary tract infection, upper respiratory tract infection, abdominal distention, renal impairment, and muscle spasms.

Neratinib is a kinase inhibitor that irreversibly binds to Epidermal Growth Factor Receptor (EGFR), Human Epidermal Growth Factor Receptor 2 (HER2), and HER4. Neratinib is a member of the 4-anilino quinolidine class of protein kinase inhibitors.