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Pralsetinib

Pralsetinib structure

CAS No:
2097132-94-8
Formula:
C27H32FN9O2
Chemical Name:
Pralsetinib
Synonyms:
CPD2049;PRALSETINIB;(1r,4S)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexanecarboxamide;BLU-667 (Pralsetinib);BLU-667;BLU 667;BLU667;2097132-94-8;(1r,4S)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexane-1-carboxamide;PRALSETINIB (BLU667);(1s,4R)-N-((S)-1-(6-(4-fluoro-1H-pyrazol-1-yl)pyridin-3-yl)ethyl)-1-methoxy-4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl)amino)pyrimidin-2-yl)cyclohexanecarboxamide
Categories:
Organic Chemistry > Quinones

Description

Pralsetinib is a Kinase Inhibitor. The mechanism of action of pralsetinib is as a Rearranged during Transfection (RET) Inhibitor.|Pralsetinib is an orally bioavailable selective inhibitor of mutant forms of and fusion products involving the proto-oncogene receptor tyrosine kinase RET, with potential antineoplastic activity. Upon administration, pralsetinib binds to and targets various RET mutants and RET-containing fusion product. RET gene mutations and translocations result in the upregulation and/or activation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and regression of these cancers.

Pralsetinib is a potent, selective RET inhibitor, and was optimized from a hit compound identified from a compound library that included more than 60 chemical scaffolds. However, as of 2020, detailed medicinal chemistry on the optimization process has yet to be published. Pralsetinib proved to be more potent and selective than cabozantinib or vandertanib against both wild-type and abnormal RET. The agent also showed a level of selectivity against RET relative to VEGFR2, whereas previous agents showed very little selectivity. On September 4, 2020, the Food and Drug Administration granted accelerated approval to pralsetinib (GAVRETO®, Blueprint Medicines Corporation) for adult patients with metastatic RET fusion-positive non-small cell lung cancer (NSCLC) as detected by an FDA-approved test.

Class: receptor tyrosine kinase; Treatment: RET-altered lung, thyroid cancers; Other name: BLU-667; Elimination half-life = 22 h; Protein binding = 97%

Pralsetinib Basic Attributes

Molecular Weight：

533.6

Exact Mass：

533.26629946

UNII：

1WPE73O1WV

NCI Thesaurus Code：

C132295

Color/Form：

White to off-white

Characteristics

Density：

1.40±0.1 g/cm3(Predicted)

Boiling Point：

799.1±60.0 °C(Predicted)

PKA：

14.33±0.10(Predicted)

Critical Temperature & Pressure：

Store at 4°C

Drug Information

Drug Indication：

Treatment of lung cancer (small cell and non-small cell lung cancer)|Drug: Pralsetinib

MeSH：

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)

MeSH Entry Terms：

BLU-667

Pralsetinib Use and Manufacturing

Uses

Pralsetinib is a highly potent and selective RET inhibitor designed for RET-driven cancers.

Use Classification：

Human Drugs -> EU pediatric investigation plans|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Drug Function and Efficacy

Pratinib is a receptor tyrosine kinase RET (Rearranged during Transfection) inhibitor that can selectively inhibit RET kinase activity, dose-dependently inhibit the phosphorylation of RET and its downstream molecules, and effectively inhibit the proliferation of cells expressing RET (wild type and various mutant types).

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Pratinib Capsules
Ingredients	The main ingredient of this product is pralatinib. Chemical name: (0-5S) 1-(6-(4-fluoro-1H-pyrazol-1-yl) pyridin-3-yl) ethyl)-1-methoxy 4-(4-methyl-6-((5-methyl-1H-pyrazol-3-yl) amino) pyrimidin-2-yl) cyclohexanecarboxamide. Chemical structure: Molecular formula: C2rHzFNgO2 Molecular weight: 533.61g/mol Excipients: Hydroxypropyl methylcellulose, microcrystalline cellulose, sodium bicarbonate, anhydrous citric acid, magnesium stearate, pregelatinized starch, and hydroxypropyl methylcellulose empty capsules.
Indication	Strong CYP3A inhibitors Avoid co-administration with strong CYP3A inhibitors. Co-administration of this product with strong CYP3A inhibitors results in increased exposure to pralsetinib, which may increase the incidence and severity of adverse reactions of this product. Avoid co-administration of this product with P-gp and strong CYP3A co-inhibitors. If co-administration with P-gP and strong CYP3A co-inhibitors cannot be avoided, reduce the dose of this product (see [Dosage and Administration] and [Pharmacology and Toxicology]. Strong CYP3A inducers Co-administration of this product with strong CYP3A inducers results in decreased exposure to pralsetinib, which may reduce the effectiveness of this product. Avoid co-administration of this product with strong CYP3A inducers. If co-administration with strong CYP3A inducers cannot be avoided, increase the dose of this product (see [Dosage and Administration] and [Pharmacology and Toxicology]).
Specifications	100mg120 tablets1 bottle

Registered Holders

VALARY LAB PRIVATE LIMITED

India
Active
OLON S.P.A.

Italy
Active
Asymchem Laboratories (Tianjin) Co., Ltd.

China
Active

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