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Brand Name :
Piqray
(United States) [Available] ,Vijoice
(United States) [Available]Synonyms :
Alpelisib
Class :
Antineoplastics and PI3K Inhibitors
Brand Name :
Piqray
(United States) [Available] ,Vijoice
(United States) [Available]Synonyms :
Alpelisib
Class :
Antineoplastics and PI3K Inhibitors
Dosage Forms & Strengths
Tablet-Piqray
50mg
150mg
200mg
Tablet-Vijoice
50mg
125mg
200mg
300
mg
Orally
once a day
;Treatment continued until the disease progression, or unacceptable toxicity occurs
The dose recommended for fulvestrant is 500 mg given orally on days 1, 15, and 29, and once monthly thereafter
Note:
Alpelisib with fulvestrant combination used for the treatment of PIK3CAmutated, postmenopausal women, and men, human epidermal growth factor receptor 2 (HER2)-negative, advanced or metastatic breast cancer and recommended by FDA
PIK CA Related Overgrowth Spectrum
250
mg
Orally
once a day
Treatment continued until the disease progression, or unacceptable toxicity occurs
Dose Adjustments
Renal Dose Adjustments:
no adjustment recommended for mild and moderate renal impairment
data is not available for severe renal impairment
Liver Dose Adjustments:
no adjustment recommended
Dosage Forms & Strengths
Tablet-Vijoice
50mg
125mg
PIK CA Related Overgrowth Spectrum
For patients<2 years, the safety and efficacy are not established
For patients ≥2 years with PROS who require systemic therapy
For 2 to < 6 years
50 mg taken orally once a day
treatment continued until the disease progression or unacceptable toxicity occurs
For 6 to <18 years
The Initial dose is 50 mg, taken orally once a day
later after 24 weeks, start increasing the dose up to 125 mg once a day for response optimization
Treatment continued until the disease progression, or unacceptable toxicity occurs
For ≥18 years
consider a gradually increasing dose up to 250 mg taken orally once a day
alpelisib: it may increase the risk of CNS depression
alpelisib: it may increase the risk of CNS depression
alpelisib: it may increase the risk of CNS depression
alpelisib: it may increase the risk of CNS depression
alpelisib: it may increase the risk of CNS depression
when both drugs are combined, there may be an increase in the serum concentration of alpelisib
may enhance the serum concentration of BCRP/ABCG2 inhibitors
may enhance the serum concentration of P-glycoprotein/ABCB1 Inhibitors
may increase the serum concentration
may enhance the serum concentration of BCRP/ABCG2 inhibitors
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
may enhance the serum concentration of BCRP/ABCG2 inhibitors
may enhance the serum concentration of BCRP/ABCG2 inhibitors
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
may enhance the serum concentration of P-glycoprotein/ABCB1 Inhibitors
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
may enhance the serum concentration of BCRP/ABCG2 Inhibitors
when both drugs are combined, there may be an increasing effect of alpelisib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased metabolism of acalabrutinib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be a reduced level of the serum concentration of atazanavir
when both drugs are combined, there may be a decreased level of serum concentration of bosentan
when both drugs are combined, there may be an increasing effect of alpelisib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
when both drugs are combined, there may be an increased metabolism of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased metabolism of erdafitinib
when both drugs are combined, there may be a decreased levels of serum concentration of etravirine
when both drugs are combined, there may be a decreased metabolism of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased metabolism of ivosidenib
when both drugs are combined, there may be a decreased metabolism of alpelisib
when both drugs are combined, there may be a decreased metabolism of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased metabolism of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of lonafarnib
when both drugs are combined, there may be a decreased metabolism of alpelisib
when both drugs are combined, there may be an increased metabolism of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
may diminish the serum concentration of CYP3A4 inducers
may diminish the serum concentration of CYP3A4 inducers
may diminish the serum concentration of CYP3A4 inducers
may diminish the serum concentration of CYP3A4 inducers
may diminish the serum concentration of CYP3A4 inducers
It may enhance the effect when combined with tafamidis meglumine
nafcillin will decrease the effect of action of alpelisib by synergism.
the effect of alpelisib is decreased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
when both drugs are combined, there may be an increased risk of adverse effects
when both drugs are combined, there may be a decreased effect of alpelisib by affecting hepatic or intestinal enzyme cyp3a4 metabolism
alpelisib and lapatinib will increase the effect of each other when used simultaneously
CYP3A strong enhancers of the small intestine may reduce the the bioavailability of alpelisib
both the drugs, when used in combination, increase the effect of one another
regorafenib, when used in combination with alpelisib, increases the impact or level of each other
It may diminish the level when combined with efavirenz by affecting CYP3A4 metabolism
by affecting intestinal metabolism, the effect of alpelisib may be increased
when both drugs are combined, there may be an increased metabolism of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of bexarotene
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased levels of serum concentration of celecoxib
when both drugs are combined, there may be a decreased level of serum concentration of chlorpropamide
when both drugs are combined, there may be a decreased level of serum concentration of diclofenac
when both drugs are combined, there may be a decreased level of serum concentration of dronabinol
when both drugs are combined, there may be a decreased metabolism of elagolix
when both drugs are combined, there may be a decreased level of serum concentration of glipizide
when both drugs are combined, there may be a decreased level of serum concentration of glyburide
when both drugs are combined, there may be an increased level of serum concentration of alpelisib
when both drugs are combined, there may be a decreased level of serum concentration of ketamine
when both drugs are combined, there may be a decreased level of serum concentration of lacosamide
when both drugs are combined, there may be a decreased level of serum concentration of lesinurad
when both drugs are combined, there may be a decreased level of serum concentration of losartan
when both drugs are combined, there may be a decreased level of serum concentration of warfarin
when both drugs are combined, there may be a decreased level of the serum concentration of zafirlukast
Combining tegafur with alpelisib can reduce tegafur’s metabolism
When alprazolam and alpelisib is used together, this leads to reduction in the alprazolam’s metabolism
When dexrabeprazole and alpelisib is used together, this leads to reduction in the dexrabeprazole’s metabolism
When domeperidone and alpelisib is used together, this leads to reduction in the domeperidone’s metabolism
When alpelisib is used together with fluconazole, this leads to reduction in the alpelisib metabolism
When alpelisib is used together with norelgestromin, this leads to a rise in norelgestromin’s metabolism
When alpelisib is used together with allylestrenol, this leads to a reduction in the alpelisib metabolism
When alpelisib is used together with oleandomycin, this leads to enhanced concentration serum of alpelisib
When alpelisib is used together with ridaforolimus, this leads to enhanced concentration serum of alpelisib
alpelisib: it may increase the metabolism of gestodene
when both drugs are combined, there may be an increased metabolism of etoposide
when both drugs are combined, there may be an increased metabolism of vincristine
when both drugs are combined, there may be an increased metabolism of paclitaxel
may decrease the level by affecting hepatic enzyme CYP2C9 metabolism
may decrease the serum concentration
It may diminish the metabolism when combined with nilvadipine
the serum levels of alpelisib may be increased
the serum levels of alpelisib may be increased
the serum levels of alpelisib may be increased
the serum concentration of alpelisib can be increased when it is combined with fostamatinib
when both drugs are combined, there may be an increased metabolism of alpelisib
when both drugs are combined, there may be a decreased level of the serum concentration of dapsone
Actions and spectrum:
Actions:
The growth factor-tyrosine kinase pathway activates. It triggers cell growth by phosphorylation. A PI3Kα subunit mutates in some cancers. Alpelisib targets and prevents this process. It blocks the PI3Kα catalytic subunit specifically.
Spectrum:
Alpelisib impacts many conditions. CLOVES syndrome, CLAPO syndrome, Facial infiltrating lipomatosis (FIL), Lipomatosis of the nerve (LON), Muscular hemihyperplasia (HH), and Hemimegalencephaly (HMEG). It has a wide effect on these disorders.
Adverse drug reactions:
Frequency defined
>10%
Lymphocyte count decreased
Hemoglobin decreased
Activated partial thromboplastin time prolonged
Platelet count decreased
Glucose increased
Hyperglycemia
Weight loss
Calcium (corrected) decreased
Glucose decreased
Potassium decreased
Albumin decreased
Magnesium decreased
Urinary tract infection
0.1-1%
Anaphylaxis
Anaphylactic shock
Dyspnea
Flushing
Rash
Fever
Tachycardia
Osteonecrosis of the jaw
Alpelisib does not carry a U.S. FDA Black Box Warning. However, it is associated with serious adverse effects that require close monitoring, particularly hyperglycemia, severe cutaneous reactions, and pneumonitis.
Alpelisib is contraindicated in patients with known hypersensitivity to alpelisib or any of its components. Reported hypersensitivity reactions include severe cutaneous adverse reactions and anaphylaxis.
Caution is advised in patients with or at risk for severe hyperglycemia, as alpelisib commonly induces elevated blood glucose levels. Patients with a history of diabetes or glucose intolerance should be closely monitored. Use should also be approached carefully in individuals with a history of pneumonitis or interstitial lung disease, as rare but serious cases have occurred during treatment. Additionally, patients with renal or hepatic impairment may require closer monitoring due to altered drug metabolism and clearance. Concomitant use of drugs that interact with CYP3A4 may affect alpelisib levels and increase the risk of toxicity. Regular monitoring of blood glucose, liver enzymes, and renal function is recommended throughout therapy.
Pregnancy warnings:
Breastfeeding warnings:
Pregnancy Categories:
Pharmacology:
Alpelisib stops cancer cells from growing. It is taken by mouth with food. The medicine works better with higher doses. Most of it leaves the body in poop and pee. It doesn’t make the heart beat funny. Taking alpelisib twice a day may work best for people who need a small dose.
Pharmacodynamics:
Alpelisib does not increase the QTcF interval’s duration. Treatment with alpelisib works better when higher doses are given. A dose of 200 mg each day is 51% more effective than 100 mg. Taking 300 mg once daily provides a 22% advantage over 150 mg taken twice daily. Patients needing a lower dose may benefit from splitting it into two smaller doses.
Pharmacokinetics:
Absorption
Alpelisib gets absorbed quickly. Its peak concentration in blood happens 2-4 hours after taking it. When the levels are steady, its peak concentration is 2480 ng/ml.
Distribution
Around 89% of alpelisib binds to proteins in the body. It has a very large distribution volume of 114L.
Metabolism
Metabolism occurs mainly through enzymatic and chemical hydrolysis. This leads to the formation of its main metabolite, BZG791.
Elimination and excretion
Most of the drug gets eliminated via feces (81%). 36% is unchanged, and 32% is as its metabolite. 14% gets excreted in urine. Alpelisib has a half-life ranging from 8 to 9 hours.
Administration:
Eating meals is crucial when taking alpelisib. You must swallow the tablet whole, without crushing or chewing it. And you should take alpelisib around the same time daily. By doing this, you’ll ensure proper absorption and consistent dosing.
Patient Information Leaflet
Alpelisib fights cancer when used with fulvestrant. Together, they block the growth of certain hormone-positive, HER2-negative metastatic cancer types. Alpelisib interferes with cancer cell growth, but can affect healthy cells too, causing side effects. It’s crucial to follow your doctor’s advice closely, especially if you have other medical issues. Potential side effects include changes in blood sugar levels, diarrhea, and dehydration – stay hydrated during treatment. Proper storage of Alpelisib is essential.
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