Piqray

Last updated on RxList: 7/29/2021
Piqray Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

What Is Piqray?

Piqray (alpelisib) is a kinase inhibitor indicated in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer as detected by an FDA-approved test following progression on or after an endocrine-based regimen.

What Are Side Effects of Piqray?

Common side effects of Piqray include:

  • diarrhea
  • rash
  • nausea
  • fatigue
  • decreased appetite
  • inflammation of the mouth and lips
  • vomiting
  • weight loss
  • hair loss
  • abdominal pain
  • indigestion
  • swelling of extremities
  • fever
  • dry nose
  • urinary tract infection (UTI)
  • changes in taste
  • headache
  • itching
  • dry skin
  • prolonged aPTT
  • and laboratory abnormalities (increased or decreased blood sugar
  • increased creatinine
  • decreased lymphocyte count
  • increased GGT
  • increased ALT
  • decreased hemoglobin
  • increased lipase
  • and decreased calcium)

Dosage for Piqray

The recommended dose of Piqray is 300 mg (two 15 0 mg tablets) taken orally once daily with food.

What Drugs, Substances, or Supplements Interact with Piqray?

Piqray may interact with CYP3A4 inducers, BCRP inhibitors, warfarin, and acid reducing agents. Tell your doctor all medications and supplements you use.

Piqray During Pregnancy and Breastfeeding

Piqray is not recommended for use during pregnancy; it may harm a fetus. Piqray is used in combination with fulvestrant, which may also harm a fetus. It is unknown if Piqray passes into breast milk. Because of the potential for serious adverse reactions in the breastfed child, breastfeeding is not recommended during treatment with Piqray and for 1 week after the last dose.

Additional Information

Our Piqray (alpelisib) Tablets, for Oral Use Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

QUESTION

A lump in the breast is almost always cancer. See Answer
Piqray Consumer Information

Get emergency medical help if you have signs of an allergic reaction (hives, warmth or tingling, difficult breathing, fast heartbeats, swelling in your face or throat) or a severe skin reaction (fever, sore throat, burning eyes, skin pain, red or purple skin rash with blistering and peeling).

Seek medical treatment if you have a serious drug reaction that can affect many parts of your body. Symptoms may include: skin rash, fever, swollen glands, muscle aches, severe weakness, unusual bruising, or yellowing of your skin or eyes.

Call your doctor at once if you have:

  • chest pain, cough, feeling short of breath;
  • severe or ongoing diarrhea;
  • blisters or ulcers in your mouth, red or swollen gums, trouble swallowing;
  • pale skin, unusual tiredness, cold hands and feet;
  • little or no urination; or
  • high blood sugar--increased thirst, increased urination, dry mouth, fruity breath odor, confusion, hunger, weight loss;

Your cancer treatments may be delayed or permanently discontinued if you have certain side effects.

Common side effects may include:

  • nausea, vomiting;
  • loss of appetite, weight loss;
  • feeling weak or tired;
  • mouth sores;
  • rash;
  • hair loss; or
  • abnormal blood tests.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the entire detailed patient monograph for Piqray (Alpelisib Tablets)

SLIDESHOW

Breast Cancer Awareness: Symptoms, Diagnosis, and Treatment See Slideshow
Piqray Professional Information

SIDE EFFECTS

The following adverse reactions are discussed in greater detail in other sections of the labeling:

  • Severe Hypersensitivity [see WARNINGS AND PRECAUTIONS]
  • Severe Cutaneous Adverse Reactions [see WARNINGS AND PRECAUTIONS]
  • Hyperglycemia [see WARNINGS AND PRECAUTIONS]
  • Pneumonitis [see WARNINGS AND PRECAUTIONS]
  • Diarrhea [see WARNINGS AND PRECAUTIONS]

Clinical Trial Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

The safety of PIQRAY was evaluated in a randomized, double-blind, placebo-controlled trial (SOLAR-1) in 571 patients with HR-positive, HER2-negative, advanced or metastatic breast cancer enrolled into two cohorts, with or without a PIK3CA mutation [see Clinical Studies].

Patients received either PIQRAY 300 mg plus fulvestrant (n = 284) or placebo plus fulvestrant (n = 287). Fulvestrant 500 mg was administered intramuscularly on Cycle 1, Day 1 and 15, and then at Day 1 of each 28-day cycle during treatment phase.

Two patients (0.7%) died while on treatment with PIQRAY plus fulvestrant due to causes other than the underlying malignancy. Causes of death included one cardio-respiratory arrest and one second primary malignancy. Neither was suspected to be related to study treatment.

Serious adverse reactions occurred in 35% of patients receiving PIQRAY plus fulvestrant. Serious adverse reactions in > 2% of patients receiving PIQRAY plus fulvestrant included hyperglycemia (10%), rash (3.5%), diarrhea (2.8%), acute kidney injury (2.5%), abdominal pain (2.1%), and anemia (2.1%).

Osteonecrosis of the jaw (ONJ) was reported in 4.2% of patients (12/284) in the PIQRAY plus fulvestrant arm compared to 1.4% of patients (4/287) in the placebo arm. All patients experiencing ONJ had prior or concomitant bisphosphonates or RANK-ligand inhibitor administration.

Among patients receiving PIQRAY plus fulvestrant, 4.6% permanently discontinued both PIQRAY and fulvestrant and 21% permanently discontinued PIQRAY alone, due to ARs. The most frequent ARs leading to treatment discontinuation of PIQRAY in > 2% patients receiving PIQRAY plus fulvestrant were hyperglycemia (6%), rash (4.2%), diarrhea (2.8%), and fatigue (2.5%).

Dose reductions due to ARs occurred in 55% of patients receiving PIQRAY plus fulvestrant. The most frequent ARs leading to dose reduction in > 2% patients receiving PIQRAY plus fulvestrant were hyperglycemia (29%), rash (9%), diarrhea (6%), stomatitis (3.5%), and mucosal inflammation (2.1%).

The most common adverse reactions, including laboratory abnormalities (all grades, incidence ≥ 20%) were glucose increased, creatinine increased, diarrhea, rash, lymphocyte count decreased, gamma glutamyl transferase (GGT) increased, nausea, alanine aminotransferase (ALT) increased, fatigue, hemoglobin decreased, lipase increased, decreased appetite, stomatitis, vomiting, weight decreased, calcium decreased, glucose decreased, activated partial thromboplastin time (aPTT) prolonged, and alopecia.

Adverse reactions and laboratory abnormalities are listed in Table 6 and Table 7, respectively.

Table 6: Adverse Reactions Occurring in ≥ 10% and ≥ 2% Higher than Placebo Arm in SOLAR-1 (All Grades)

Adverse reactions PIQRAY plus fulvestrant
N = 284
Placebo plus fulvestrant
N = 287
All Grades % Grade 3-4 % All Grades % Grade 3-4 %
Gastrointestinal disorders
Diarrhea 58 7* 16 0.3*
Nausea 45 2.5* 22 0.3*
Stomatitis1 30 2.5* 6 0*
Vomiting 27 0.7* 10 0.3*
Abdominal pain2 17 1.4* 11 1*
Dyspepsia 11 0* 6 0*
General disorders and administration site conditions
Fatigue3 42 5* 29 1*
Mucosal inflammation 19 2.1* 1 0*
Edema peripheral 15 0* 5 0.3*
Pyrexia 14 0.7 4.9 0.3*
Mucosal dryness4 12 0.4* 4.2 0*
Infections and infestations
Urinary tract infection5 10 0.7* 5 1*
Investigations
Weight decreased 27 3.9* 2.1 0*
Metabolism and nutrition disorders
Decreased appetite 36 0.7* 10 0.3*
Nervous system disorders
Dysgeusia6 18 0.4* 3.5 0*
Headache 18 0.7* 13 0*
Skin and subcutaneous tissue disorders
Rash7 52 20* 7 0.3*
Alopecia 20 0* 2.4 0*
Pruritus 18 0.7* 6 0*
Dry skin8 18 0.4* 3.8 0*
Grading according to CTCAE Version 4.03
1 Stomatitis: including stomatitis, aphthous ulcer and mouth ulceration
2 Abdominal pain: abdominal pain, abdominal pain upper, abdominal pain lower
3 Fatigue: including fatigue, asthenia
4 Mucosal dryness: including dry mouth, mucosal dryness, vulvovaginal dryness
5 Urinary tract infection: including UTI and single case of urosepsis
6 Dysgeusia: including dysgeusia, ageusia, hypogeusia
7 Rash: including rash, rash maculo-papular, rash macular, rash generalized, rash papular, rash pruritic
8 Dry skin: including dry skin, skin fissures, xerosis, xeroderma
* No Grade 4 adverse reactions were reported.

Among the patients with Grade 2 or 3 rash, the median time to first onset of Grade 2 or 3 rash was 12 days. A subgroup of 86 patients received prophylaxis, including antihistamines, prior to onset of rash. In these patients, rash was reported less frequently than in the overall population, for all grades rash (27% vs 54%), Grade 3 rash (12% vs 20%) and rash leading to permanent discontinuation of PIQRAY (3.5% vs 4.2%). Of the 153 patients who experienced rash, 141 had resolution of the rash.

Table 7: Laboratory Abnormalities Occurring in ≥ 10% of Patients in SOLAR-1

Laboratory Abnormality PIQRAY plus fulvestrant
N = 284
Placebo plus fulvestrant
N = 287
All Grades % Grade 3-4 % All Grades % Grade 3-4 %
Hematological parameters
Lymphocyte count decreased 52 8 40 4.5*
Hemoglobin decreased 42 4.2* 29 1*
Activated Partial Thromboplastin Time (aPTT) prolonged 21 0.7* 16 0.3*
Platelet count decreased 14 1.1 6 0*
Biochemical parameters
Glucose increased1 79 39 34 1
Creatinine increased 67 2.8* 25 0.7*
Gamma Glutamyl Transferase (GGT) increased 52 11 44 10
Alanine Aminotransferase (ALT) increased 44 3.5 34 2.4*
Lipase increased 42 7 25 6
Calcium (corrected) decreased 27 2.1 20 1.4
Glucose decreased 26 0.4 14 0*
Potassium decreased 14 6 2.8 0.7*
Albumin decreased 14 0* 8 0*
Magnesium decreased 11 0.4* 4.2 0*
1Glucose increase is an expected laboratory abnormality of PI3K inhibition.
*No Grade 4 laboratory abnormalities were reported.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of PIQRAY. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

Metabolism and nutrition disorders: Hyperglycemic hyperosmolar nonketotic syndrome (HHNKS).

Skin and sub-cutaneous tissue disorders: Drug reaction with eosinophilia and systemic symptoms (DRESS).

DRUG INTERACTIONS

Effect Of Other Drugs On PIQRAY

CYP3A4 Inducer

Coadministration of PIQRAY with a strong CYP3A4 inducer may decrease alpelisib concentration [see CLINICAL PHARMACOLOGY], which may decrease alpelisib activity. Avoid coadministration of PIQRAY with strong CYP3A4 inducers.

Breast Cancer Resistance Protein Inhibitors

Coadministration of PIQRAY with a breast cancer resistance protein (BCRP) inhibitor may increase alpelisib concentration [see CLINICAL PHARMACOLOGY], which may increase the risk of toxicities. Avoid the use of BCRP inhibitors in patients treated with PIQRAY. If unable to use alternative drugs, when PIQRAY is used in combination with BCRP inhibitors, closely monitor for increased adverse reactions.

Effect Of PIQRAY On Other Drugs

CYP2C9 Substrates

Coadministration of PIQRAY with CYP2C9 substrates (e.g., warfarin) may reduce plasma concentration of these drugs [see CLINICAL PHARMACOLOGY]. Closely monitor when PIQRAY is used in combination with CYP2C9 substrates where decreases in the plasma concentration of CYP2C9 substrates may reduce activity of these drugs.

Read the entire FDA prescribing information for Piqray (Alpelisib Tablets)

© Piqray Patient Information is supplied by Cerner Multum, Inc. and Piqray Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

Health Solutions From Our Sponsors