Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Alpelisib
Drug ID BADD_D02500
Description Alpelisib is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potent antitumor activity. It works by selectively inhibiting class I PI3K p110α [A179203], which is the catalytic subunit of PI3K, a lipid kinase that plays a role in various biological processes, including proliferation, survival, differentiation, and metabolism. Alpelisib was designed to target this enzyme that appears to be mutated at a rate of nearly 30% in human cancers, leading to hyperactivation.[A179209] There are several isoform-specific PI3K inhibitors that are under clinical development or currently approved, such as [idelalisib] used for chronic lymphocytic leukemia (CLL).[A179209] Approved by the FDA in May 2019, alpelisib is the first approved PI3K inhibitor indicated for the treatment of hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, PIK3CA-mutated, advanced or metastatic breast cancer in combination with [fulvestrant] for postmenopausal women and male patients. To initiate alpelisib therapy, it is required that the presence of a PIK3CA mutation in the tissue and/or liquid biopsy sample collection should be confirmed via FDA-approved diagnostic tests. Alpelisib is marketed under the trade name Piqray and is available as oral tablets. Studies evaluating the therapeutic effectiveness of alpelisib in other cancers, such as ovarian cancer [A179200] and colorectal cancer [A179203], are under ongoing investigations. Alpelisib was granted FDA approval on 24 May 2019.[L6652]
Indications and Usage Alpelisib is indicated in combination with fulvestrant to treat postmenopausal women, and men, with advanced or metastatic breast cancer.[Label] This cancer must be hormone receptor (HR)-positive, human epidermal growth factor receptor 2 (HER2)-negative, and PIK3CA­ mutated.[Label] The cancer must be detected by an FDA-approved test following progression on or after an endocrine-based regimen.[Label]
Marketing Status approved; investigational
ATC Code L01EM03
DrugBank ID DB12015
KEGG ID D11011
MeSH ID C585539
PubChem ID 56649450
TTD Drug ID D0W7HE
NDC Product Code 0078-0701; 0078-1021; 0078-1028; 0078-1035; 0078-0708; 0078-0715
UNII 08W5N2C97Q
Synonyms Alpelisib | BYL719 | Piqray | NVP-BYL719
Chemical Information
Molecular Formula C19H22F3N5O2S
CAS Registry Number 1217486-61-7
SMILES CC1=C(SC(=N1)NC(=O)N2CCCC2C(=O)N)C3=CC(=NC=C3)C(C)(C)C(F)(F)F
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice..
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal distension07.01.04.0010.000739%
Anaphylactic reaction24.06.03.006; 10.01.07.0010.000728%
Ascites07.07.01.001; 02.05.04.002; 09.01.05.0030.000280%
Asthenia08.01.01.0010.002518%Not Available
Bone pain15.02.01.0010.000739%
Breast cancer21.05.01.003; 16.10.01.0010.000783%Not Available
Breast cancer stage IV16.10.01.003; 21.05.01.0100.000112%Not Available
Cervix carcinoma21.06.02.001; 16.12.01.0010.000112%Not Available
Cheilitis23.03.03.025; 07.05.01.0010.000112%
Chills15.05.03.016; 08.01.09.0010.001634%
Colitis07.08.01.0010.001791%
Death08.04.01.0010.010801%
Dehydration14.05.05.0010.002451%
Dermatitis allergic23.03.04.003; 10.01.03.0140.000112%Not Available
Diabetes mellitus05.06.01.001; 14.06.01.0010.001903%Not Available
Diabetes mellitus inadequate control14.06.01.004; 05.06.01.0040.000336%Not Available
Diabetic coma17.02.09.004; 14.07.04.002; 05.07.04.0020.000168%Not Available
Diabetic ketoacidosis14.07.03.001; 05.07.03.0010.002295%Not Available
Diarrhoea07.02.01.0010.021860%
Diplopia17.17.01.005; 06.02.06.0020.000246%Not Available
Drug ineffective08.06.01.006--Not Available
Dry eye06.08.02.0010.000571%
Dry mouth07.06.01.0020.001399%
Dry skin23.03.03.0010.000985%
Dysphagia07.01.06.0030.004220%
Eating disorder19.09.01.008; 14.03.01.0080.000492%Not Available
Electrolyte imbalance14.05.01.0020.000112%Not Available
Eye disorder06.08.03.0010.000246%Not Available
Eye inflammation06.04.05.0020.000168%Not Available
Face oedema23.04.01.004; 10.01.05.002; 08.01.07.0030.000302%
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