Lapacent

Lapatinib ·Incepta Pharmaceuticals Ltd.·Tablet

0 views 0 reviews

Administration

The recommended dosage of Lapatinib for advanced or metastatic breast cancer is 1,250 mg (5 tablets) given orally once daily on Days 1-21 continuously in combination with capecitabine 2,000 mg/m2/day (administered orally in 2 doses approximately 12 hours apart) on Days 1-14 in a repeating 21 day cycle.

The recommended dose of Lapatinib for hormone receptor positive, HER2 positive metastatic breast cancer is 1500 mg (6 tablets) given orally once daily continuously in combination with letrozole. When Lapatinib is coadministered with letrozole, the recommended dose of letrozole is 2.5 mg once daily.

Lapatinib should be taken at least one hour before or one hour after a meal. However, capecitabine should be taken with food or within 30 minutes after food.
Lapatinib should be taken once daily. Do not divide daily doses of Lapatinib.
Modify dose for cardiac and other toxicities, severe hepatic impairment, and CYP3A4 drug interactions.

Effects

GI disturbances, dermatological reactions (e.g. palmar-plantar erythrodysesthesia, rash), fatigue, decreases in LVEF, QT interval prolongation, stomatitis, mucosal inflammation, pain in extremities, back pain, dyspnoea, insomnia, epistaxis, alopecia, nail disorders (e.g. paronychia), interstitial lung disease, pneumonitis and hypersensitivity reactions including anaphylaxis.

Indications

Lapatinib, a kinase inhibitor, is indicated in combination with:

Capecitabine, for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress HER2 and who have received prior therapy including an anthracycline, a taxane, and trastuzumab.
Letrozole for the treatment of postmenopausal women with hormone receptor positive metastatic breast cancer that overexpresses the HER2 receptor for whom hormonal therapy is indicated.

Lapatinib in combination with an aromatase inhibitor has not been compared to a trastuzumab-containing chemotherapy regimen for the treatment of metastatic breast cancer.

Pharmacology

Lapatinib is a 4-anilinoquinazoline tyrosine kinase inhibitor of both Epidermal Growth Factor Receptor (EGFR [ErbB1]) and Human Epidermal Receptor Type 2 (HER2 [ErbB2]) receptors. It blocks the phosphorylation and activation of downstream 2nd messengers (Erk1/2 and Akt) which regulate cellular proliferation and survival of ErbB- and ErbB2-expressing tumours.