Alpelisib Brand Name– PIQRAY
What is Alpelisib
Alpelisib is an oral phosphatidylinositol 3-kinase (PI3K) inhibitor.
It is indicated in combination with fulvestrant for the treatment of men and postmenopausal women with HR-positive, HER2-negative, PIK3CA-mutated, advanced or metastatic breast cancer following progression on or after an endocrine-based regimen.
PI3K inhibition by alpelisib treatment has been shown to induce an increase in estrogen receptor (ER) transcription in breast cancer cells.
The combination of alpelisib and fulvestrant demonstrated increased anti-tumor activity compared to either treatment alone in xenograft models derived from ER-positive, PIK3CA-mutated breast cancer cell lines.
Hyperglycemia is an expected laboratory abnormality related to PI3K inhibition; the safety of alpelisib in patients with Type 1 and uncontrolled Type 2 diabetes has not been established as these patients were excluded from clinical trials.
Indications
- breast cancer
Side Effects
- abdominal pain
- alopecia
- anaphylactic shock
- anaphylactoid reactions
- anemia
- anorexia
- asthenia
- dehydration
- diabetic ketoacidosis
- diarrhea
- dysgeusia
- dyspepsia
- dyspnea
- elevated hepatic enzymes
- erythema multiforme
- fatigue
- fever
- flushing
- headache
- hyperglycemia
- hypoalbuminemia
- hypocalcemia
- hypoglycemia
- hypokalemia
- hypomagnesemia
- infection
- interstitial lung disease
- lymphopenia
- maculopapular rash
- nausea
- osteonecrosis
- pancreatitis
- peripheral edema
- pneumonitis
- prolonged bleeding time
- pruritus
- rash
- renal failure (unspecified)
- Stevens-Johnson syndrome
- stomatitis
- thrombocytopenia
- vomiting
- weight loss
- xerosis
- xerostomia
Monitoring Parameters
- blood glucose
- glycosylated hemoglobin A1c (HbA1c)
- pregnancy testing
Contraindications
- breast-feeding
- chronic lung disease (CLD)
- contraception requirements
- diabetes mellitus
- diarrhea
- hyperglycemia
- infertility
- interstitial lung disease
- male-mediated teratogenicity
- pneumonitis
- pregnancy
- pregnancy testing
- reproductive risk
- serious rash
- type 1 diabetes mellitus
Interactions
- Acalabrutinib
- Amlodipine; Celecoxib
- Apalutamide
- Atazanavir; Cobicistat
- Atropine; Hyoscyamine; Phenobarbital; Scopolamine
- Belladonna Alkaloids; Ergotamine; Phenobarbital
- Brigatinib
- Carbamazepine
- Celecoxib
- Cobicistat
- Cyclosporine
- Daclatasvir
- Darolutamide
- Darunavir; Cobicistat
- Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
- Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
- Elbasvir; Grazoprevir
- Eltrombopag
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
- Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
- Enzalutamide
- Fosphenytoin
- Fostamatinib
- Glecaprevir; Pibrentasvir
- Glimepiride
- Glimepiride; Pioglitazone
- Glimepiride; Rosiglitazone
- Ibrutinib
- Isoniazid, INH; Pyrazinamide, PZA; Rifampin
- Isoniazid, INH; Rifampin
- Itraconazole
- Ledipasvir; Sofosbuvir
- Leflunomide
- Lumacaftor; Ivacaftor
- Lumacaftor; Ivacaftor
- Mitotane
- Ombitasvir; Paritaprevir; Ritonavir
- Osimertinib
- Phenobarbital
- Phenytoin
- Ponatinib
- Primidone
- Regorafenib
- Rifampin
- Rolapitant
- Safinamide
- Sapropterin
- Simeprevir
- Sirolimus
- Sofosbuvir; Velpatasvir
- Sofosbuvir; Velpatasvir; Voxilaprevir
- St. John’s Wort, Hypericum perforatum
- Sulfasalazine
- Tacrolimus
- Tafamidis
- Tedizolid
- Teriflunomide
- Tolbutamide
- Vemurafenib
- Warfarin