Hernix Tablet
Neratinib
40mg
Beacon Pharmaceuticals Ltd.
| Pack size | 180's pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 56.99 AED |
Indications
Hernix Tablet is used for:
As a single agent in early-stage HER2-positive breast cancer, In combination with Capecitabine in advanced or metastatic HER2-positive, breast cancer
Adult Dose
Breast Cancer
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.
240 mg (6 tablets) given orally once daily, with food, continuously until disease recurrence for up to 1 year.
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.
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.
Consider a two-week dose escalation instead of starting at the 240-mg daily dose to minimize severe diarrhea if not using antidiarrheal prophylaxis
Dose escalation regimen
Days 1 to 7: 120 mg PO once Daily
Days 8 to 14: 160 mg PO once Daily
Day 15 and thereafter: 240 mg PO once Daily; continue for up to 1 year
If diarrhea occurs, treat with antidiarrheal medications, fluids, and electrolytes as clinically warranted
Antidiarrheal prophylaxis
When not using dose escalation, administer loperamide prophylaxis during the first 2 cycles (56 days) of treatment and initiate with the first neratinib dose
Titrate dose to 1-2 bowels/day
Weeks 1-2 (days 1-14): 4 mg PO TID
Weeks 3-8 (days 15-56): 4 mg PO BID
Weeks 9-52 (days 57-365): 4 mg PO PRN; not to exceed 16 mg/day
If diarrhea occurs despite prophylaxis, treat with additional antidiarrheals, fluids and electrolytes as clinically indicated
Dose interruptions and reductions may also be required to manage diarrhea
Hepatic impairment
Severe (Child-Pugh C): Reduce starting dose to 80 mg
Mild-moderate (Child-Pugh A or B): No dose modifications are required
Child Dose
Renal Dose
Renal impairment
No clinical significant effect on pharmacokinetics
Administration
Take with food at approximately the same time each day
Contra Indications
It is contraindicated in patients with known hypersensitivity to Neratinib or any other components of this product.
Precautions
Diarrhea: Diarrhea should be managed through either Neratinib dose escalation or loperamide prophylaxis. If diarrhea occurs despite recommended prophylaxis, treat with additional
antidiarrheals, fluids, and electrolytes as clinically indicated. Withhold Neratinib in patients experiencing severe and/or persistent diarrhea. Neratinib should be Permanently
discontinued in patients experiencing Grade 4 diarrhea or Grade ≥2 diarrhea that occurs after maximal dose reduction.
Hepatotoxicity: Neratinib should be Withheld in patients experiencing Grade 3 liver abnormalities and permanently discontinued Neratinib in patients experiencing Grade 4 liver
abnormalities.
Embryo-Fetal Toxicity: Neratinib can cause fetal harm. Should Advise patients of potential risks to a fetus and to use effective contraception
Pregnancy-Lactation
Pregnancy
Based on findings from animal studies and its mechanism of action, can cause fetal harm when administered to pregnant women; females of reproductive potential should have a pregnancy test prior to starting treatment
If drug used during pregnancy, or if patient becomes pregnant while taking drug, patient should be apprised of potential hazard to fetus
Animal studies
Administration to pregnant rabbits during organogenesis caused abortions, embryo-fetal death, and fetal abnormalities in rabbits at maternal AUCs approximately 0.2 times the AUC in patients receiving the recommended dose
Contraception
Females of reproductive potential should use effective contraception during treatment and for at least 1 month after last dose of drug
Males with females of reproductive potential should use effective contraception during treatment and for 3 months after the last dose
Lactation
Unknown if distributed in human breast milk
Because of the potential for serious adverse reactions in breastfed infants, advise lactating women not to breastfeed while taking neratinib and for at least 1 month after the last dose
Interactions
Gastric acid reducing agents: Avoid concomitant use with proton pump inhibitors. Separate Neratinib by at least 2 hours before or 10 hours after H2-receptor antagonists. Or
separate Neratinib by at least 3 hours after antacids.
Strong CYP3A4 inhibitors: Should avoid concomitant use.
P-gp and moderate CYP3A4 dual inhibitors: Should avoid concomitant use.
Strong or moderate CYP3A4 inducers: Should avoid concomitant use.
Certain P-gp substrates: Should Monitor for adverse reactions of P-gp substrates for which minimal concentration change may lead to serious adverse reactions when used
concomitantly with Neratinib.
Adverse Effects
Side effects of Neratinib :
>10%
All grades
Diarrhea (95%)
Nausea (43%)
Abdominal pain (36%)
Fatigue (27%)
Vomiting (26%)
Rash (18%)
Stomatitis (14%)
Decreased appetite (12%)
Muscle spasms (11%)
Grade 3-4
Diarrhea (40%)
1-10%
All grades
Dyspepsia (10%)
ALT increased (9%)
Nail disorder (8%)
AST increased (7%)
Dry skin (6%)
Abdominal distension (5%)
Urinary tract infection (5%)
Decreased (5%)
Epistaxis (5%)
Dehydration (4%)
Dry mouth (3%)
Skin fissures (2%)
Grade 3-4
Vomiting (3%)
Nausea (2%)
Abdominal pain (2%)
Fatigue (2%)
ALT increased (1%)
<1%
Grade 3-4
Dehydration (0.9%)
Stomatitis (0.6%)
Rash (0.3%)
AST increased (0.5%)
Dyspepsia (0.4%)
Abdominal distension (0.3%)
Nail disorder (0.3%)
Decreased appetite (0.2%)
Skin fissures (0.1%)
Dry mouth (0.1%)
Urinary tract infection (0.1%)
Decreased weight (0.1%)
Muscle spasms (0.1%)
Mechanism of Action
Irreversible tyrosine kinase inhibitor (TKI) that blocks signal transduction through the epidermal growth factor receptors (EGFRs), human epidermal growth factor receptor 2 (HER2), and HER4
In vitro, inhibition reduces EGFR and HER2 autophosphorylation, subsequently inhibits signal transduction pathways, and demonstrates antitumor activity in overexpressed EGFR and/or HER2 carcinoma cells; neratinib human metabolites (M3, M6, M7, and M11) inhibit EGFR, HER2, and HER4 activity
Note
Hernix 40mg Tablet manufactured by Beacon Pharmaceuticals Ltd.. Its generic name is Neratinib. Hernix is availble in Bangladesh.
Farmaco BD drug index information on Hernix Tablet is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.