Tucaxen 150 mg (Tablet)

Indications

• Treatment of advanced unresectable or metastatic HER2-positive breast cancer
• Treatment of patients with brain metastases
• Combination therapy with trastuzumab and capecitabine
• For adult patients who have received prior anti-HER2-based regimens

Pharmacology

• Tyrosine kinase inhibitor of HER2
• Inhibition of downstream MAPK and AKT signaling
• Cell proliferation inhibition
• Anti-tumor activity in HER2 expressing tumor cells
• Inhibition of tumor growth

Exposure Response Relationship

Not fully characterized

Cardiac Electrophysiology

No large mean increase in QTc detected following treatment

Pharmacokinetics

• AUC0-INF and Cmax increase proportionally over a dosage range
• 1.7-fold accumulation for AUC
• 1.5-fold accumulation for Cmax following administration of 300 mg twice daily for 14 days
• Time to steady state approximately 4 days

Absorption

Median time to peak plasma concentration approximately 2 hours

Distribution

• Geometric mean apparent volume of distribution approximately 1670 L
• Plasma protein binding at 97.1%

Elimination

• Geometric mean half-life approximately 8.5 hours
• Apparent clearance 148 L/h

Metabolism

• Primarily metabolized by CYP2C8
• Metabolized to a lesser extent via CYP3A

Excretion

• Approximately 86% of radiolabeled dose recovered in feces
• 4.1% recovered in urine
• Overall total recovery of 90% within 13 days post-dose

Dosage & Administration

• Recommended dosage of 300 mg orally twice daily
• Tablets to be swallowed whole
• Patients advised to take approximately 12 hours apart and at the same time each day
• Recommended dosage of capecitabine is 1000 mg/m2 orally twice daily
• Dosage modifications for severe hepatic impairment
• Dosage modifications for concomitant use with strong CYP2C8 inhibitors

Side Effects

• Diarrhea
• Palmar-plantar erythrodysesthesia
• Nausea
• Fatigue
• Hepatotoxicity
• Vomiting
• Stomatitis
• Decreased appetite
• Abdominal pain
• Headache
• Anemia
• Rash

Pregnancy & Lactation

• Potential fetal harm
• No available human data on use in pregnant women
• Advised not to breastfeed during treatment and for at least 1 week after last dose

Precautions & Warnings

• Severe diarrhea including dehydration and hypotension
• Severe hepatotoxicity
• Embryo-fetal toxicity
• Use of effective contraception during treatment

Use in Special Populations

• Safety and effectiveness not established in pediatric patients
• Use not recommended in severe renal impairment
• No dose adjustment recommended for mild or moderate renal impairment
• Tucaxen exposure increased in severe hepatic impairment

Overdose Effects

No specific antidote, general supportive measures recommended

Therapeutic Class

Cytotoxic Chemotherapy

Storage Conditions

Store below 25°C, in a cool and dry place, keep away from light, keep out of the reach of children

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