Progress and potential impact of RET kinase targeting in cancer

Mulligan, Lois M.

doi:10.1080/14789450.2016.1205491

Cited by 7 publications

(6 citation statements)

References 21 publications

(48 reference statements)

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“…Rearranged during transfection (RET) is a developmentally important receptor tyrosine kinase, which function as an oncogenic driver in thyroid and lung cancer. In addition, it also contributes to tumor diffusion and drug resistance to treatment in a large number of human cancers (Mulligan, 2016). RET fusions, identified in 1–2% of nonsmall‐cell lung cancers (NSCLCs), are actionable oncogenic drivers (Aisner et al, 2018; Drilon, Hu, Lai, & Tan, 2018).…”

Section: Introductionmentioning

confidence: 99%

Determination of selpercatinib, a RET kinase inhibitor, in rat plasma and its application to a pharmacokinetic study

Wang

Shi

Jin

et al. 2020

Biomedical Chromatography

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Selpercatinib (LOXO‐292) is a selective and potent RET inhibitor. A highly sensitive, rapid and specific high‐performance liquid chromatography with tandem mass spectrometry (LC–MS/MS) method for quantification of selpercatinib in rat plasma is reported. The method was validated in terms of selectivity, linearity, accuracy and precision, extraction recovery and matrix effect, stability and carryover as per the US Food and Drug Administration guidelines for bioanalytical method validation. Selpercatinib was detected by an electrospray ionization interface under selective reaction monitoring conditions in the positive ion mode. The calibration curve was linear over the concentration range from 1 to 2000 ng/ml with r2 = 0.9951. The intra‐ and inter‐batch accuracy values ranged from 97.45 to 100.97% and from 98.70 to 100.74% with coefficients of variation of 2.45–6.99% and 5.89–7.99%, respectively. The extraction recovery and IS‐normalized matrix factor were acceptable for the bioanalysis of selpercatinib. Additionally, selpercatinib was found to be stable under the detected conditions. It showed linear pharmacokinetic characteristics following oral administration to rats at 2.0–18.0 mg/kg. The results showed that the novel method for detecting selpercatinib in rat plasma could be successfully applied for quantification of selpercatinib in biosamples from nonclinical studies.

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Section: Introductionmentioning

confidence: 99%

Determination of selpercatinib, a RET kinase inhibitor, in rat plasma and its application to a pharmacokinetic study

Wang

Shi

Jin

et al. 2020

Biomedical Chromatography

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“…El conocimiento sobre los cambios genéticos de cada persona tiene como objetivo ayudar a decidir cuál tratamiento será el adecuado o puede tener mayor probabilidad de funcionar en un paciente específico. 38,39…”

Section: Conclusionesunclassified

Diagnóstico mutacional del gen <i>RET</i> y la medicina de precisión en México

Martínez-Castillo¹,

Zárate²,

Valenzuela-Pérez³

et al. 2022

GMM

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La medicina de precisión en algunas enfermedades es una realidad; respalda el desarrollo de métodos diagnósticos certeros y específicos, de nuevas drogas y moléculas. Nuestro equipo de investigación en México, conformado por investigadores clínicos y biomédicos, desde hace 20 años realiza de forma gratuita el diagnóstico mutacional del gen RET y su relación con el cáncer medular de tiroides y la neoplasia endocrina múltiple (NEM) 2 y 3. Las variantes patogénicas de RET en la población mexicana coinciden con los datos reportados: la mayoría con 634/NEM2 y 918/NEM3. Actualmente se están desarrollando nuevos métodos de nanobiotecnología para este tipo de determinaciones, de tal forma que puedan obtenerse resultados más rápidos, simples, sensibles y específicos aplicables en todo tipo de laboratorio.

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“…The RET proto-oncogene encodes a receptor tyrosine kinase which is activated by gene fusion in 1-2% of NSCLC and rarely in many other tumor types. RET gene fusions are bona fide cancer drivers and they display the key characteristics of oncogene addiction preclinically 9 .…”

Section: Introductionmentioning

confidence: 99%

Overcoming MET-Dependent Resistance to Selective RET Inhibition in Patients with RET Fusion–Positive Lung Cancer by Combining Selpercatinib with Crizotinib

Rosen

Johnson

Clifford

et al. 2021

Clinical Cancer Research

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and Company. L.M.S. reports consulting fees from EMD Serono, scientific advisory board roles for Loxo Oncology and Foghorn Therapeutics, and honorarium from Astra Zeneca. B.S.T. reports honoraria and research funding from Genentech and discovery board activities for Boehringer Ingelheim and Loxo Oncology; all stated activities were outside of the work described herein. M. Ladanyi reports ad hoc advisory board roles for

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Progress and potential impact of RET kinase targeting in cancer

Cited by 7 publications

References 21 publications

Determination of selpercatinib, a RET kinase inhibitor, in rat plasma and its application to a pharmacokinetic study

Determination of selpercatinib, a RET kinase inhibitor, in rat plasma and its application to a pharmacokinetic study

Diagnóstico mutacional del gen <i>RET</i> y la medicina de precisión en México

Overcoming MET-Dependent Resistance to Selective RET Inhibition in Patients with RET Fusion–Positive Lung Cancer by Combining Selpercatinib with Crizotinib

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