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. 2021 Dec 24;14(1):87. doi: 10.3390/cancers14010087

Table 3.

Features of the phosphatidylinositol-3 kinase (PI3K) inhibitors approved by the Food and Drug Administration (FDA) from 2011 to 2021. The order of drugs is tabulated in order of most recent to oldest registration date.

No. Generic Name of Drug Brand Name
and Company
First FDA/EMA Approved Date Structure Molecular
Target
Route of
Administration
Indication Adverse Effects Reference
1 Duvelisib COPIKTRA Verastem, Inc. Needham, MA, USA FDA:
24 September 2018
EMA:
19 May 2021
graphic file with name cancers-14-00087-i010.jpg PI3K-δ 1, PI3K-γ 2 Oral Chronic Lymphocytic Leukemia, Follicular Lymphoma Neutropenia,
thrombocytopenia, anemia, diarrhea, pyrexia, nausea, vomiting,
anorexia
[84,85]
2 Copanlisib ALIQOPA
Bayer HealthCare Pharmaceuticals Inc., HanoverWhippany, NJ, USA
FDA:
14 September 2017
EMA:
Not approved
graphic file with name cancers-14-00087-i011.jpg PI3K-α 3, PI3K-δ 1 Intravenous infusion Follicular
Lymphoma
Hyperglycemia,
hypertension,
infections, neutropenia
[86,87]
3 Idelalisib ZYDELIG
Gilead Sciences, Inc., Foster City, CA, USA
FDA:
23 July 2014
EMA:
18 September 2014
graphic file with name cancers-14-00087-i012.jpg PI3K-δ 1 Oral Chronic Lymphocytic Leukemia, Follicular Lymphoma Diarrhea, nausea,
vomiting, fatigue, headache, pneumonia, chill, dyspnea, rash,
neutropenia, pyrexia, sepsis, decreased
neutrophil count,
hypertriglyceridemia, hyperglycemia, elevated alanine and aspartate transaminases
[88,89]

1 PI3K-δ: phosphatidylinositol 3-kinase delta. 2 PI3K-γ: phosphatidylinositol 3-kinase gamma. 3 PI3K-α: phosphatidylinositol 3-kinase alpha.