LOXO-101 1223403-58-4

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Ngaran API Indikasi Inovator Tanggal Kadaluarsa Patén (AS)
LOXO-101 1223403-58-4 Obat onkologi Onkologi Loxo 21 Okt.2029

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IC50: kisaran nanomolar anu handap pikeun ngahambat sadaya anggota kulawarga TRK

LOXO-101 mangrupikeun panghambat reséptor kinases (TRK) tropomyosin.

Kulawarga TRK reséptor neurotrofin sareng ligand neurotrofinna ngatur kamekaran neuron, diferensiasi sareng salamet.

Dina vitro: Dina panilitian samemehna, LOXO-101 dievaluasi pikeun sambatan énzim kinase kaluar-target ngalawan panel kinase non-TRK dina konsentrasi 1.000 nM sareng ATP konsentrasi di sakitar Km. Hasilna nunjukkeun yén LOXO-101 ngagaduhan panghambat langkung ageung ti 50% pikeun ngan ukur hiji non-TRK kinase, nyaéta TNK2 kalayan IC50 tina 576 nM. Sumawona, teu aya hambatan hERG anu aya hubunganana ogé panjagaan QT anu berkepanjangan [1].

In vivo: Panilitian sato mendakan yén LOXO-101 sanggup ngahambat pertumbuhan tumor vivo. Beurit buligir Athymic nyuntik sél KM12 dirawat sacara lisan ku LOXO-101 unggal dinten salami 2 minggu, sareng résistansi tumor gumantung dosis dititénan, nunjukkeun kamampuan LOXO-101 ngahambat pertumbuhan tumor in-vivo [1].

Sidang klinis: Tahap multicenter I diajar dosis-eskalasi dina pasién anu tumors padet anu maju (ClinicalTrials.gov no. NCT02122913) dilaksanakeun di 2014 pikeun ngaevaluasi kasalametan sareng PK of LOXO-101. Pasien dosed sakali atanapi dua kali unggal dinten salami 28 dinten dosis teras-terasan dina cohorts anu ningkat. Data awal PK sareng kaamanan nunjukkeun yén kadar plasma gratis LOXO-101 aya dina konsentrasi anu biologis pikeun ngahambat onkogén TRK. Dina pangajaran ieu, anu sabar anu munggaran sareng ngan ukur nunjukkeun TRK fusi sareng régrési tumor klinis gancang ditingali kalayan perlakuan LOXO-101 [1].

Rujukan:
[1] Doebele RC dkk. Fusi Ontrogenik NTRK dina Pasién sareng Sarcoma Lemes-jaringan sareng réspon kana Penghambat Kinase Terkait Tropomyosin LOXO-101. Kanker Discov. 2015 Okt; 5 (10): 1049-57.

 

Katerangan

 

Larotrectinib (LOXO-101) mangrupikeun panghambat ATP-kompetitif oral, selektif sambetan reséptor kulawarga kinase (TRK) anu aya hubunganana sareng tropomyosin, sareng konsentrasi hambatan nanomolar 50% ngalawan sadayana tilu isoforms (TRKA, B, sareng C).

 

Sidang Klinis

Nomer NCT Sponsor Kaayaan Tanggal mimiti

Tahap

NCT03025360 Bayer Tumor Harbour NTRK Fusion  

NCT02637687 Bayer Tumor Padet Harbour NTRK Fusion 16 Désémber 2015

Fase 1 | Fase 2

NCT02122913 Bayer Tumor Padet Harbour NTRK Fusion 4 Méi 2014

Fase 1

NCT03213704 Institut Kanker Nasional (NCI) Neoplasma Padet Malignant Canggih | Ependymoma Berulang | Tumiba Ewing Sarcoma + Peripheral Primitive Neuroectodermal Tumor | Glioma Recurrent | Hepatoblastoma Recurrent | Recurrent Langerhans Cell Histiocytosis | Recurrent Malignant Germ Cell Tumor | Recurrent Gignan Recurrent | Recopent Non-Hodgkin Lymphoma | Osteosarcoma Recurrent | Tumor Rhabdoid Recurrent | Rhabdomyosarcoma Recurrent | Lemes jaringan Tissue Sarcoma | Refractory Ependymoma | Refractory Ewing Sarcoma + Peripheral Primitive Neuroectodermal Tumor | Refractory Garnium Refractory Malignant Glioma | Refractory Malignant Solid Neoplasm | Refractory Neuroblastoma | Refractory Non-Hodgkin Lymphoma | Refractory Osteosarcoma | Refractory Central Nervous System Neoplasm | Refractory Rhabdoid Tumor | Refractory Rhabdomyosarcoma | Wilms Tumor 24 Juli 2017

Fase 2

NCT02465060 Institut Kanker Nasional (NCI) Canggih Malignant Padet Neoplasma | Kandung Kangker | Kanker Payudara | Kanker serviks | Kolon Karsinoma | Karsinoma koloréktim | Malignant Uterine Neoplasm | Melanoma | Ovarian Carcinoma | Pankreatic Carcinoma | Plasma Cell Myeloma | Prostate Carcinoma | Rectal Carcinoma | Recurrent Kandungan Karsinoma | Kambek Payudara Karsinoma | Kénsér servis Kangker Karakoma | | Glioma Berulang | Sirah Kepala sareng Beuheung Karsinoma | Karsinoma Hati Kambuh | Kambek Paru-paru | Kambuh Lymphoma | Neoplasma Padet Malignan Berulang | Melanoma Kambuh | Karsinoma Ovarian Kambuh | Kanker Pankreas Kambuh | Kanker Kanker Barengan | Kangker Kulit Terulang | Kelenjar Tiroid Terulang Kankeroma | Kangker rahim Corpus Corpus | Refractory Lymphoma | Refractory Malignant Solid Neoplasm | Refractory Plasma Cell Myeloma | Kulit Karsinoma | Tiroid Kelenjar Karsinoma | Kanker Rahim Corpus 12 Agustus 2015

Fase 2

NCT03834961 Grup Onkologi Barudak | Institut Kanker Nasional (NCI) Neoplasma Sistem Saraf Pusat | Fibrosarcoma Orok | Leukemia Akut Berulang | Refractory Leukemia Akut | Neoplasma Padet 18 Séptémber 2019

Fase 2

NCT04142437 Bayer Lokal Canggih atanapi Metastatik Tumor Padet Harbouring NTRK Gene Fusion 3 April 2020

NCT03155620 Institut Kanker Nasional (NCI) Advanced Malignant Solid Neoplasm | Ann Arbor Stage III Non-Hodgkin Lymphoma | Ann Arbor Stage IV Non-Hodgkin Lymphoma | Histiocytic Sarcoma | Juvenile Xanthogranuloma | Langerhans Cell Histiocytosis | Malignant Glioma | Recurrent Childhood Rhabdomyosarcoma | Recurrent Ependym | Recurrent Ependym Hepatoblastoma kumat | Langerhans Cell Histiocytosis Recurrent | Malignant Germ Cell Tumor | Recurrent Malignant Solid Neoplasm | Recurrent Medulloblastoma | Neuroblastoma Recurrent | Lemes Tissue Sarcoma Lemes | Refractory Ewing Sarcoma | Refractory Glioma | Refractory Hepatoblastoma | Refractory Langerhans Cell Histiocytosis | Refractory Malignant Germ Cell Tumor | Refractory Malignant Solid Neoplasm | Refractory Medulloblastoma | Refractory Refractory CTory Peripheral Primitive Neuroectodermal Tumor | Refractory Central Nervous System Neoplasm | Refractory Rhabdoid Tumor | Refractory Rhabdomyosarcoma | Rhabdoid Tumor | Panggung III Osteosarcoma AJCC v7 | Panggung III Lemes Tissue Sarcoma AJCC v7 | Tahap IV Osteosaruea | Panggung IVA Osteosarcoma AJCC v7 | Panggung IVB Osteosarcoma AJCC v7 | Wilms Tumor 24 Juli 2017

Fase 2

Struktur kimia

LOXO-101 1223403-58-4

SERTIPIKAT

2018 GMP-2
原料药GMP证书201811(captopril ,thalidomide etc)
GMP-of-PMDA-in-Chanyoo-平成28年08月03日 Nantong-Chanyoo-Pharmatech-Co
FDA-EIR-Letter-201901

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