Repotrectinib CAS 1802220-02-5

Product Description:

Product Name: Repotrectinib CAS 1802220-02-5

Synonyms:

(3R,11S)-6-fluoro-3,11-dimethyl-10-oxa-2,13,17,18,21-pentazatetracyclo[13.5.2.0^4,9.0^18,22]docosa-1(21),4(9),5,7,15(22),16,19-heptaen-14-one;

Chemical & Physical Properties:

Appearance: white to off-white powder

Assay: ≥ 99.0%

Density: 1.46g/cm3

Solubility: DMSO:35.0(Max Conc. mg/mL);98.5(Max Conc. mM)

Ethanol:10.0(Max Conc. mg/mL);28.1(Max Conc. mM)

Uses

Repotrectinib is a brand-new tyrosine kinase inhibitor( TKI) made specifically to address resistance in the treatment of non-small cell lung cancer( NSCLC), which is caused by ROS1 gene mutations.

One of the defined oncogenic drives of NSCLC is ROS1 mutations, and the solvent-front mutation ROS1 G2032R accounts for 50 to 60% of cases of [crizotinib]-resistant. Repotrectinib has a compact macrocyclic structure that both prevents side effects from hotspots of resistance mutations and targets mutations in the solvent-front region.

There has n't been a case of repotrectinib resistance, despite reports of resistance to multiple TKI, including [crizotinib], [lorlatinib], [taletrectinib], and [entrectinib].

Repotrectinib was approved by the FDA on November 15, 2023, under the name Augtyro, for the treatment of locally advanced or metastatic ROS1-Positive NSCLC. Based on conclusive findings from the TRIDENT-1 study, which showed that, for example, 38% of TKI-pretreated patients and 39% of TKI-naive patients, respectively, had an objective response rate of 79% and 38%..

Adagrasib obtained accelerated clearance from the FDA in December 2022 to treat KRASG12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC) patients who have had at least one prior systemic therapy. Adagrasib is the second KRASG12C inhibitor that the FDA has approved, after sotorasib.

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