HIGHLIGHTS OF PRESCRIBING INFORMATION

These highlights do not include all the information needed to use LuciNera safely and effectively. See full prescribing information for LuciNera.

INDICATIONS AND USAGE

LuciNera 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 trastuzumabbased 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 AND ADMINISTRATION

• Premedication for diarrhea: When not using dose escalation, initiate loperamide with the first dose of LuciNera 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 LuciNera may also be initiated.

• Dose interruptions and/or dose reductions are recommended based on individual safety and tolerability.

• Hepatic impairment: Reduce starting dose to 80 mg in patients with severe hepatic impairment.  

DOSAGE FORMS AND STRENGTHS

Tablets: 40 mg×180 tablets

CONTRAINDICATIONS

None.

WARNINGS AND PRECAUTIONS

• Diarrhea: Manage diarrhea through either LuciNera dose escalation or loperamide prophylaxis. If diarrhea occurs despite recommended prophylaxis, treat with additional antidiarrheals, fluids, and electrolytes as clinically indicated. Withhold LuciNera in patients experiencing severe and/or persistent diarrhea. Permanently discontinue LuciNera in patients experiencing Grade 4 diarrhea or Grade ≥2 diarrhea that occurs after maximal dose reduction.

• Hepatotoxicity: Monitor liver function tests monthly for the first 3 months of treatment, then every 3 months while on treatment and as clinically indicated. Withhold LuciNera in patients experiencing Grade 3 liver abnormalities and permanently discontinue LuciNera in patients experiencing Grade 4 liver abnormalities.

• Embryo-Fetal Toxicity: LuciNera can cause fetal harm. Advise patients of potential risk to a fetus and to use effective contraception.

ADVERSE REACTIONS

The most common adverse reactions (reported in ≥5% of patients) were:

• LuciNera 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.

• LuciNera 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.

DRUG INTERACTIONS

• Gastric acid reducing agents: Avoid concomitant use with proton pump inhibitors. Separate LuciNera by at least 2 hours before or 10 hours after H2-receptor antagonists. Or separate LuciNera by at least 3 hours after antacids.

• Strong CYP3A4 inhibitors: Avoid concomitant use.

• P-gp and moderate CYP3A4 dual inhibitors: Avoid concomitant use.

• Strong or moderate CYP3A4 inducers: Avoid concomitant use.

• Certain P-gp substrates: Monitor for adverse reactions of P-gp substrates for which minimal concentration change may lead to serious adverse reactions when used concomitantly with LuciNera.

USE IN SPECIFIC POPULATIONS

Lactation: Advise women not to breastfeed.

Storage

Store at 20℃ to 25℃ (68℉ to 77℉), excursions permitted between 15℃ and 30℃ (59℉ and 86℉) [see USP Controlled Room Temperature]. Protect from moisture.