Avapritinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Avapritinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2020. Its mechanism of action is classified as Bile Salt Export Pump Inhibitors, Breast Cancer Resistance Protein Inhibitors and Cytochrome P450 2C9 Inhibitors. DrugCentral lists 4 molecular targets, including PDGFRA, KIT and ABCG2. Recorded indications include Gastrointestinal stromal tumor and Systemic mast cell disease.

• Approval status: onp (first approved 2020 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Bile Salt Export Pump Inhibitors; Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2C9 Inhibitors.
• Molecular targets: PDGFRA, KIT, ABCG2 and Kit (4 listed in DrugCentral).
• Indications: Gastrointestinal stromal tumor and Systemic mast cell disease.
• ATC code: L01EX18 (Other protein kinase inhibitors).
• Molecular formula: C26H27FN10; molecular weight 498.57 g/mol.

Indications & contraindications

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

Indications (2)

• Gastrointestinal stromal tumor
• Systemic mast cell disease

Mechanism & targets

• Mechanism of action (MoA): Bile Salt Export Pump Inhibitors; Breast Cancer Resistance Protein Inhibitors; Cytochrome P450 2C9 Inhibitors; Multidrug and Toxin Extrusion Transporter 1 Inhibitors; Multidrug and Toxin Extrusion Transporter 2 K Inhibitors; P-Glycoprotein Inhibitors; Tyrosine Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (4)

Target	Gene	Action	Activity
Platelet-derived growth factor receptor alpha	PDGFRA	inhibitor	IC50 9.62
Mast/stem cell growth factor receptor Kit	KIT	inhibitor	IC50 9.57
ATP-binding cassette sub-family G member 2	ABCG2	unknown	IC50 8.82
Mast/stem cell growth factor receptor Kit	Kit	inhibitor	IC50 7.66

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2020-09-24	EMA	—	Blueprint Medicines (Netherlands) B.V.	Yes
2020-01-09	FDA	—	BLUEPRINT MEDICINES	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EX18	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: PDGFRA · Testing Required
• FDA label: PDGFRA · Testing Required
• HCSC label: KIT, PDGFRA

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
Off label use	443.9
Periorbital oedema	319.4
Hair colour changes	196.7
Tryptase increased	172.2
Disease progression	165.0
Face oedema	144.2
Periorbital swelling	106.4
Cognitive disorder	76.6
Swelling face	68.2
Lacrimation increased	59.8
Oedema	54.6
Platelet count decreased	46.6

Chemical structure

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

• Molecular formula: C₂₆H₂₇FN₁₀
• Molecular weight: 498.57 g/mol
• CAS number: 1703793-34-3
• InChIKey: DWYRIWUZIJHQKQ-SANMLTNESA-N
• PubChem CID: 118023034

CN1C=C(C=N1)C1=CN2N=CN=C(N3CCN(CC3)C3=NC=C(C=N3)[C@@](C)(N)C3=CC=C(F)C=C3)C2=C1

Frequently asked questions

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

What is Avapritinib used for?

DrugCentral lists the following indications for Avapritinib: Gastrointestinal stromal tumor and Systemic mast cell disease.

How does Avapritinib work?

Avapritinib is classified as Bile Salt Export Pump Inhibitors, Breast Cancer Resistance Protein Inhibitors and Cytochrome P450 2C9 Inhibitors; its molecular targets in DrugCentral include PDGFRA (inhibitor), KIT (inhibitor), ABCG2 and Kit (inhibitor).

When was Avapritinib first approved?

Avapritinib was first approved by the FDA in 2020.

What drug class does Avapritinib belong to?

Avapritinib is in the Kinase Inhibitor class.

What is the chemical formula of Avapritinib?

Avapritinib has the molecular formula C26H27FN10 and a molecular weight of 498.57 g/mol.

Sources

• DrugCentral drug card 5379 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4204794 — compound record and bioactivity
• PubChem CID 118023034 — chemical identifiers
• DrugBank DB15233 — drug record
• FDA UNII 513P80B4YJ — substance identity
• DailyMed: FDA labels for Avapritinib — current prescribing information (label search)
• UniProt P16234 (PDGFRA) — target protein
• UniProt P10721 (KIT) — target protein
• UniProt Q9UNQ0 (ABCG2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

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