Pralsetinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Pralsetinib 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 Rearranged during Transfection (RET) Inhibitors. DrugCentral lists 10 molecular targets, including RET, DDR1 and JAK1. Recorded indications include Medullary thyroid carcinoma, Metastatic non-small cell lung cancer and Non-small cell lung cancer.

• Approval status: onp (first approved 2020 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Rearranged during Transfection (RET) Inhibitors.
• Molecular targets: RET, DDR1, JAK1 and NTRK3 (10 listed in DrugCentral).
• Indications: Medullary thyroid carcinoma, Metastatic non-small cell lung cancer and Non-small cell lung cancer.
• ATC code: L01EX23 (Other protein kinase inhibitors).
• Molecular formula: C27H32FN9O2; molecular weight 533.61 g/mol.

Indications & contraindications

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

Indications (3)

• Medullary thyroid carcinoma
• Metastatic non-small cell lung cancer
• Non-small cell lung cancer

Mechanism & targets

• Mechanism of action (MoA): Rearranged during Transfection (RET) Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (10)

Target	Gene	Action	Activity
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	inhibitor	IC50 9.39
Epithelial discoidin domain-containing receptor 1	DDR1	inhibitor	IC50 8.70
Tyrosine-protein kinase JAK1	JAK1	inhibitor	IC50 8.66
NT-3 growth factor receptor	NTRK3	inhibitor	IC50 8.05
Fibroblast growth factor receptor 1	FGFR1	inhibitor	IC50 7.96
Receptor-type tyrosine-protein kinase FLT3	FLT3	inhibitor	IC50 7.80
Tyrosine-protein kinase JAK2	JAK2	inhibitor	IC50 7.72
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 7.46
High affinity nerve growth factor receptor	NTRK1	inhibitor	IC50 7.24
Platelet-derived growth factor receptor beta	PDGFRB	inhibitor	IC50 7.00

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2021-11-18	EMA	—	ROCHE REGISTRATION GMBH
2020-09-04	FDA	—	BLUEPRINT MEDICINES	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EX23	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: RET · Testing Required
• FDA label: RET · Testing Required
• HCSC label: RET · Testing Required

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	111.4
No adverse event	86.9
Myelosuppression	75.8
Death	66.1
Pneumonitis	66.0

Chemical structure

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

• Molecular formula: C₂₇H₃₂FN₉O₂
• Molecular weight: 533.61 g/mol
• CAS number: 2097132-94-8
• InChIKey: GBLBJPZSROAGMF-SIYOEGHHSA-N
• PubChem CID: 129073603

CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)N[C@@H](C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC

Frequently asked questions

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

What is Pralsetinib used for?

DrugCentral lists the following indications for Pralsetinib: Medullary thyroid carcinoma, Metastatic non-small cell lung cancer and Non-small cell lung cancer.

How does Pralsetinib work?

Pralsetinib is classified as Rearranged during Transfection (RET) Inhibitors; its molecular targets in DrugCentral include RET (inhibitor), DDR1 (inhibitor), JAK1 (inhibitor) and NTRK3 (inhibitor).

When was Pralsetinib first approved?

Pralsetinib was first approved by the FDA in 2020.

What drug class does Pralsetinib belong to?

Pralsetinib is in the Kinase Inhibitor class.

What is the chemical formula of Pralsetinib?

Pralsetinib has the molecular formula C27H32FN9O2 and a molecular weight of 533.61 g/mol.

Sources

• DrugCentral drug card 5412 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4582651 — compound record and bioactivity
• PubChem CID 129073603 — chemical identifiers
• DrugBank DB15822 — drug record
• FDA UNII 1WPE73O1WV — substance identity
• DailyMed: FDA labels for Pralsetinib — current prescribing information (label search)
• UniProt P07949 (RET) — target protein
• UniProt Q08345 (DDR1) — target protein
• UniProt P23458 (JAK1) — target protein
• UniProt Q16288 (NTRK3) — target protein
• UniProt P11362 (FGFR1) — target protein
• UniProt P36888 (FLT3) — 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.