Lapacent

- Tablet

Generic name: Lapatinib

250 mg

Manufactured by: Incepta Pharmaceuticals Ltd.

Unit Price: ৳ 300.00, (12's pack: ৳ 3, 600.00)
Unit Price: ৳ 300.00, (30's pack: ৳ 9, 000.00)

Indication

Carcinoma

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, 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.

Dosage & Administration

Interaction

May increase the serum levels of CYP3A4, CYP2C8 and P-glycoprotein substrates. Increased exposure with CYP3A4 inhibitors (e.g. ketoconazole, clarithromycin, atazanavir, ritonavir). CYP3A4 inducers (e.g. carbamazepine, rifampicin) may reduce exposure to lapatinib. Increased risk of QT prolongation with drugs known to prolong QT intervals (e.g. antiarrythmic agents, cumulative high-dose anthracycline therapy). May increase serum levels of digoxin.

Side 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.

Pregnancy & Lactation

Pregnancy category D. There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Precautions & Warnings

Patient with hypokalaemia or hypomagnesaemia, congenital QT prolongation. Severe hepatic impairment. Pregnancy and lactation.

Use in Special Populations

Patient on potent CYP3A4 inhibitor-

HER2 overexpressing advanced or metastatic breast cancer: Increase gradually from 1.25 g daily up to 4.5 g daily.
HER2 overexpressing hormone receptor positive metastatic breast cancer: Increase gradually from 1.5 g daily up to 5.5 g daily.

Hepatic Impairment (Severe)-

HER2 overexpressing advanced or metastatic breast cancer: 750 mg once daily.
HER2 overexpressing hormone receptor positive metastatic breast cancer: 1 g once daily.

Therapeutic Class

Cytotoxic Chemotherapy

Overdose Effects

Storage Conditions

Store between 15-30° C.