Idelalisib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Idelalisib is an ofp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2014. Its mechanism of action is classified as Cytochrome P450 3A Inhibitors and Kinase Inhibitors. DrugCentral lists 7 molecular targets, including PIK3CD, PIK3CG and PIK3CB. Recorded indications include Chronic lymphoid leukemia, disease, Follicular non-Hodgkin's lymphoma and Malignant lymphoma - small lymphocytic.

• Approval status: ofp (first approved 2014 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Cytochrome P450 3A Inhibitors; Kinase Inhibitors.
• Molecular targets: PIK3CD, PIK3CG, PIK3CB and PIK3CA (7 listed in DrugCentral).
• Indications: Chronic lymphoid leukemia, disease, Follicular non-Hodgkin's lymphoma and Malignant lymphoma - small lymphocytic.
• ATC code: L01EM01 (Phosphatidylinositol-3-kinase (Pi3K) inhibitors).
• Molecular formula: C22H18FN7O; molecular weight 415.43 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Chronic lymphoid leukemia, disease
• Follicular non-Hodgkin's lymphoma
• Malignant lymphoma - small lymphocytic

Contraindications (1)

• Toxic epidermal necrolysis due to drug

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A Inhibitors; Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (7)

Target	Gene	Action	Activity
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	PIK3CD	inhibitor	IC50 8.60
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	PIK3CG	unknown	IC50 7.05
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform	PIK3CB	unknown	IC50 6.25
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform	PIK3CA	unknown	IC50 6.09
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform	Pik3cg	unknown	IC50 5.88
Phosphatidylinositol 3-kinase catalytic subunit type 3	PIK3C3	unknown	IC50 5.36
DNA-dependent protein kinase catalytic subunit	PRKDC	unknown	IC50 5.17

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2014-07-25	EMA	—	—
2014-07-23	FDA	—	GILEAD SCIENCES INC

ATC classification

ATC code	Therapeutic hierarchy
L01EM01	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Phosphatidylinositol-3-kinase (Pi3K) inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Disease progression	2878.0
Pneumonitis	351.0
Diarrhoea	313.8
Colitis	302.5
Death	226.7
Chronic lymphocytic leukaemia recurrent	177.1
Pneumonia	172.8
Neutropenia	166.5
Febrile neutropenia	112.7
Off label use	110.2
Dehydration	104.7
Cytomegalovirus infection	101.1

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Idelalisib is on its molecule page.

• Molecular formula: C₂₂H₁₈FN₇O
• Molecular weight: 415.43 g/mol
• CAS number: —
• InChIKey: IFSDAJWBUCMOAH-HNNXBMFYSA-N
• PubChem CID: 11625818

CC[C@H](NC1=NC=NC2=C1NC=N2)C1=NC2=C(C(F)=CC=C2)C(=O)N1C1=CC=CC=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Idelalisib used for?

DrugCentral lists the following indications for Idelalisib: Chronic lymphoid leukemia, disease, Follicular non-Hodgkin's lymphoma and Malignant lymphoma - small lymphocytic.

How does Idelalisib work?

Idelalisib is classified as Cytochrome P450 3A Inhibitors and Kinase Inhibitors; its molecular targets in DrugCentral include PIK3CD (inhibitor), PIK3CG, PIK3CB and PIK3CA.

When was Idelalisib first approved?

Idelalisib was first approved by the FDA in 2014.

What drug class does Idelalisib belong to?

Idelalisib is in the Kinase Inhibitor class.

What is the chemical formula of Idelalisib?

Idelalisib has the molecular formula C22H18FN7O and a molecular weight of 415.43 g/mol.

Sources

• DrugCentral drug card 4878 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2216870 — compound record and bioactivity
• PubChem CID 11625818 — chemical identifiers
• DrugBank DB09054 — drug record
• FDA UNII YG57I8T5M0 — substance identity
• DailyMed: FDA labels for Idelalisib — current prescribing information (label search)
• UniProt O00329 (PIK3CD) — target protein
• UniProt P48736 (PIK3CG) — target protein
• UniProt P42338 (PIK3CB) — target protein
• UniProt P42336 (PIK3CA) — target protein
• UniProt Q8NEB9 (PIK3C3) — target protein
• UniProt P78527 (PRKDC) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.