Hertinib

Niratinib instructions

Common name: Neratinib

Trade name: Hernix

Full names: Niratinib, Niratinib, Nerlynx, Hernix, Neratinib

Niratinib is an oral, irreversible tyrosine kinase inhibitor. It is the only product in the world approved for intensive adjuvant treatment after trastuzumab (Herceptin) is used to treat HER2-positive breast cancer to reduce the risk of disease recurrence. The applicable population is patients whose disease has not progressed after completing standard trastuzumab adjuvant therapy but who have high-risk factors.

Additional extended adjuvant treatment with neratinib after chemotherapy and trastuzumab significantly reduces the proportion of clinically significant breast cancer recurrences—recurrences that may lead to death, such as distant and local recurrences outside of the breast-sparing breast—without increasing the risk of long-term toxicity.

Currently, in the treatment of HER2-positive breast cancer, chemotherapy combined with or sequential trastuzumab adjuvant therapy is the standard therapy. However, after stopping trastuzumab treatment, there are still patients who relapse. The highest probability of recurrence is from the last 6 months of one-year trastuzumab treatment to 1 year after the completion of trastuzumab. Neratinib, which was approved by the US FDA in July 2017, is an urgently needed new treatment to reduce the risk of recurrence of early-stage HER2-positive breast cancer.

Neratinib has a broad and specific target, and can target HER1/HER2/HER4. It is currently the most widely targeted class of drugs among HER2 drugs. Neratinib-based treatment can still be considered after resistance to trastuzumab, pertuzumab, T-DM1, and lapatinib.

Even when there is a point mutation in HER2, neratinib can still achieve good efficacy. In addition to amplification of HER2, its gene can also undergo primary mutations, which is consistent with secondary mutations. The HER2 point mutations that have been discovered so far include: G309A, L755S, del755–759, D769H, D769Y, V777L, P780ins, V842I and R896C. Cell line experiments have proven that the above mutations are sensitive to the clinical trial drug neratinib.

In terms of safety, gastrointestinal toxicity such as diarrhea is still the most common adverse reaction of neratinib, but the adverse reactions caused by neratinib treatment can be managed. Diarrhea is not severe and reversible. Severe diarrhea occurs early, is of short duration, does not lead to serious complications, and pretreatment can improve tolerance and reduce the incidence and duration of severe diarrhea.

The research results also show that: in addition to breast cancer, neratinib has a significant effect in non-small cell lung cancer, cervical cancer, biliary system tumors and salivary gland tumors with HER2 mutations. In all patients, the tumors shrank by more than 30%, and some patients even experienced complete tumor remission.

Neratinib indications:

It is used for breast cancer patients who have completed standard trastuzumab (Herceptin) adjuvant treatment and whose disease has not progressed but who have high-risk factors.

Neratinib usage and dosage:

The recommended dose is 240 mg (6 tablets), taken orally once a day with food for 1 year.

Loperamide should be given 56 days in advance before the first treatment with neratinib to prevent severe diarrhea.

Use of Neratinib in Special Populations:

Women who are breastfeeding or breastfeeding should stop taking Neratinib.

Common side effects of neratinib:

Diarrhea is a common side effect of neratinib. Other common side effects include diarrhea, nausea, abdominal pain, fatigue, vomiting, rash, swelling and stomatitis (stomatitis), decreased appetite, muscle cramps, indigestion, etc.

Loperamide treatment should be started 56 days before receiving neratinib treatment to prevent or slow down diarrhea. Additional antidiarrheal medications, fluids, and electrolytes may be given clinically to help treat diarrhea.