Names and pronunciation
(al-peh-lih′-sib) Piqray
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Drug reference
(al-peh-lih′-sib) Piqray
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Func. class.: Antineoplastic
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Chem. class.: Small molecule antineoplastic phosphatidylinositol- 3-kinase (PI3K) inhibitors
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ACTION: In breast cancer cell lines, inhibits the phosphorylation of PI3K downstream targets, including Akt, and showed activity in cell lines harboring a PI3KCA mutation
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USES: Hormone receptor (HR)–posi- tive, HER2–negative, PIK3CA-mutated, advanced or metastatic breast cancer in men and postmenopausal women after progression on or after an endocrine-based regimen, in combination with fulvestrant
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CONTRAINDICATIONS: Hyper- sensitivity, pregnancy Precautions: Breastfeeding, chronic lung disorders, contraceptive requirement, dia- betes mellitus, diarrhea, hyperglycemia, infertility, interstitial lung disease, male- mediated teratogenicity
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SIDE EFFECTS CNS: Fever, headache ENDO: Hypoglycemia, hyperglycemia INTEG: Rash, pruritus GU: Renal dysfunction GI: Nausea, vomiting, diarrhea, abdominal pain, anorexia, weight loss SYST: Infection, anaphylaxis, Stevens- Johnson syndrome
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INTERACTIONS Avoid use with CYP3A4 inhibitors, induc- ers, substrates Drug/Lab Test Increase: LFTs
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DOSAGE AND ROUTES Males and postmenopausal females: PO 300 mg PO daily with food, in combination with fulvestrant (500 mg IM on days 1, 15, and 29 and monthly thereafter) until dis- ease progression or unacceptable toxicity
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Available forms: Tablets 200, 250, 300 mg
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Administer: • Give with food at approximately the same time each day • Do not crush, chew, or split; do not use any tablet that is broken, cracked, or otherwise not intact • If a dose is missed, it can be taken with food within 9 hr after the time it is usually taken. After more than 9 hr, skip the dose for that day and resume dosing on the following day at the usual time • If vomiting occurs, do not administer an additional dose on that day. Resume dosing the following day at the usual time
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Assess: • Diabetes mellitus: Fasting blood glu- cose and hemoglobin A1c (HbA1c) should be monitored before starting treatment and any antidiabetic treatment change; continue to monitor blood glu- cose weekly for the first 2 wk, then q4wk; monitor HbA1c q3mo • Severe diarrhea: May use with antidi- arrheal medication (loperamide). An interruption of therapy, dose reduction, or discontinuation of therapy may be necessary • Severe hypersensitivity reactions (ana- phylaxis and anaphylactic shock): Monitor for severe hypersensitivity reactions (dys- A pnea, flushing, rash, fever, or tachycardia); permanently discontinue if this occurs • Pregnancy/breastfeeding: Do not use in pregnancy/breastfeeding. Obtain pregnancy testing before use
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Evaluate: • Therapeutic response: Decreased dis- ease progression in breast cancer
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CLINICAL CONSIDERATIONS
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Patient and caregiver information: • Pregnancy/breastfeeding: To report planned or suspected pregnancy; to use effective contraception during treatment and for at least 1 mo after the last dose; to avoid breastfeeding • To report new or worsening side effects • To take tablets whole, not to crush or chew; to take with food • Preexisting chronic lung disease (CLD); severe pneumonitis/interstitial lung disease: Advise patients to immedi- ately report any new or worsening respi- ratory symptoms (hypoxia, cough, dys- pnea) • Diarrhea: Teach patients to begin an- tidiarrheal treatment, increase oral flu- ids, and notify their health care provider if diarrhea occurs HIGH ALERT
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PHARMACOKINETICS 89% protein binding, half-life 8-9 hr; 81% excreted in feces (36% unchanged, 32% as metabolite), 14% excreted in urine (2% unchanged, 7.1% metabolite); affected by CYP2C9, CYP3A4, BCRP; peak 2-4 hr
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