China LOXO-101 1223403-58-4 masana'anta da masu kaya

LOXO-101 1223403-58-4

Short Bayani:

Sunan API	Nuni	Mai kirkira	Kwanan wata Exparewar Patent (Amurka)
LOXO-101 1223403-58-4	Oncology magani	Loxo Oncology	Oktoba. 21,2029

Aika mana imel

Bayanin Samfura

Alamar samfur

CIKAKKEN BAYANI

Bayan Fage

IC50: ƙananan zangon nanomolar don hana duk membobin gidan TRK

LOXO-101 shine mai hana mai karɓa na kinomati (TRK).

Iyalin TRK na masu karɓar neurotrophin da layinsu na neurotrophin suna daidaita haɓakar neuron, bambance-bambancen rayuwa da rayuwa.

In vitro: A cikin binciken da ya gabata, LOXO-101 an kimanta shi ne don hana haɓakar enzyme na kinase a kan rukunin waɗanda ba TRK kinases ba a cikin nitsin 1,000 nM da ƙimar ATP a kusa da Km. Sakamako ya nuna cewa LOXO-101 ya fi 50% hanawa don guda ɗaya kawai wanda ba TRK kinase ba, wanda shine TNK2 tare da IC50 na 576 nM. Bugu da ƙari, babu mahimmancin hana hERG ko kuma dogon kallon QT [1].

A cikin rayuwa: Nazarin dabba ya gano cewa LOXO-101 ya sami ikon hana ci gaban ƙwayar tumo. An yi amfani da berayen tsirara na motsa jiki da aka yi wa allura tare da ƙwayoyin KM12 a baki tare da LOXO-101 kowace rana don makonni 2, kuma an lura da hana ƙwayar ƙwayar ƙwayar ƙwayar cuta, wanda ke nuna ikon LOXO-101 don hana haɓakar in-vivo [1].

Gwajin asibiti: An gudanar da bincike mai yawa a cikin marasa lafiya tare da ciwace-ciwacen ci gaba (ClinicalTrials.gov no. NCT02122913) a cikin 2014 don kimanta aminci da PK na LOXO-101. Ana amfani da marasa lafiya sau ɗaya ko sau biyu kowace rana don kwanaki 28 na ci gaba da yin allura a cikin haɓaka masu haɓaka. PK na farko da bayanan tsaro sun nuna cewa matakan plasma na kyauta na LOXO-101 suna cikin matakan dacewa da ilimin halittu don hana TRK oncogenes. A cikin wannan binciken, na farko kuma mai haƙuri kawai ya nuna haɗakar TRK da saurin ciwan ƙwayar asibiti da aka gani tare da maganin LOXO-101 [1].

Magana:
[1] Doebele RC et al. An Oncogenic NTRK Fusion a cikin Mai haƙuri tare da Soft-Tissue Sarcoma tare da Amsawa ga Tropomyosin-Related Kinase Inhibitor LOXO-101. Ciwon daji Canv.2015 Oktoba; 5 (10): 1049-57.

Bayani

Larotrectinib (LOXO-101) mai magana ne na ATP, mai zaɓaɓɓen mai hana karɓar dangi (TRK) masu karɓar raƙuman dangi, tare da ƙananan ƙwayoyin hana ƙarfi na 50% a kan dukkan abubuwa uku (TRKA, B, da C).

Gwajin Clinical

Lambar NCT	Tallafawa	Yanayi	Fara Kwanan wata	Lokaci
NCT03025360	Bayer	Tumors Harboring NTRK Fusion
NCT02637687	Bayer	M Tumors Harboring NTRK Fusion	Disamba 16, 2015	Lokaci 1 \| Lokaci 2
NCT02122913	Bayer	M Tumors Harboring NTRK Fusion	Mayu 4, 2014	Lokaci 1
NCT03213704	Cibiyar Cancer ta Kasa (NCI)	Ci Gaban Ciwon Neoplasm \| Maimaitawa Ependymoma \| Maimaita Ewing Sarcoma + Tsinkaya Na Farko Neuroectodermal Tumor \| Glioma Mai Maimaitawa \| Maimaitawa Hepatoblastoma \| Maimaita Langerhans Cell Histiocytosis \| Maimaitawa Ciwon Girman Kwayar Kwayar Jiki Non-Hodgkin Lymphoma \| Maimaitaccen Osteosarcoma \| Maimaita Rhabdoid Tumor \| Maimaita Rhabdomyosarcoma \| Maimaita Raunin Softarfin Sarcoma \| ractarfafawa Ependymoma \| Earƙwarar Ewing Sarcoma + iparƙashin Primarƙashin ewayar Neuroectodermal \| Refarƙashin Garƙashin parfin \| Cutar Glioma \| Matsanancin Matsalar Neoplasm \| Refractory Neuroblastoma \| Lymphoma mai ƙyamar No-Hodgkin \| Osteosarcoma mai ƙyama \| Tsarin Tsarin Tsarin Tsarin Tsarin Tsarin Tsarin Neoplasm \| Tashin Cutar Rhabdoid mai Raunin \| Rhabdomyosarcoma mai ƙyama \| Wilms Tumor	Yuli 24, 2017	Lokaci 2
NCT02465060	Cibiyar Cancer ta Kasa (NCI)	Cutar Ciwon Cutar Ciwon Cutar Ciwon Cutar Ciwon Cutar Mara \| Cutar Carcinoma Cervical \| Colon Carcinoma \| Carcinoma Mai Sauƙi \| Ciwon Cutar Endometrial \| Esophageal Carcinoma \| Carcinoma Na Gastoma \| Glioma \| Ciwon kansa da Ciwan kansa \| Ciwan Carcinoma koda \| Hanta da Ciwon Cutar Lura \| \| Ciwon Cutar Neoplasm \| Melanoma \| Carcinoma na Ovarian \| Carcinoma na Pancreatic \| Myeloma cell Plasma \| Ciwon ƙwayar Carcinoma \| Carcinoma na Rectal \| Mai fama da Ciwon Cutar baya \| Ciwan Carcinoma na Maimaitawa \| Cutar Carcinoma na Ciwon Mara \| Cutar Carcinoma na Maimaitawa \| Cutar Carcinoma na Sau da yawa \| Glioma mai saurin dawowa \| Ciwon kai da Ciwan Carcinoma \| Ciwon Cutar Ciwon Ciki \| Ciwon Cutar Loma Carcinoma \| Maimaita Lymphoma \| Maimaitawa mai laushi Solid Neoplasm \| Mai dawowa Melanoma \| Ciwon Ovarian Carcinoma \| Ciwon Pancreatic Carcinoma \| Kwayar Plasma Cell Myeloma \| Carcinoma mai saurin dawowa \| Ciwon Skin Carcinoma na Maimaitawa \| Ciwon ƙwayar cuta na thyroid Carcinoma \| Ciwon Uterine Corpus Cancer \| Lymphoma mai ƙyama \| Solananan Neoplasm mai ƙyama \| Myeloma Plasma na ƙyama \| Carcinoma na Fata \| Ciwon Gwanin Glandar thyroid \| Uterine Corpus Cancer	12 ga Agusta, 2015	Lokaci 2
NCT03834961	Onungiyar Ciwon Lafiyar Yara \| Cibiyar Cancer ta Kasa (NCI)	Tsarin Neoplasm na tsakiya \| Fibrosarcoma na yara \| Mai saurin cutar sankarar bargo \| Ciwon Cutar sankarar bargo \| Ciwon Neoplasm	Satumba 18, 2019	Lokaci 2
NCT04142437	Bayer	Ci gaba na Gida ko astarfin Tarfin astarfin astarfin astasa mai NTRK Gene Fusion	Afrilu 3, 2020
NCT03155620	Cibiyar Cancer ta Kasa (NCI)	Ci Gaban Cutar Neoplasm \| Ann Arbor Mataki na III Non-Hodgkin Lymphoma \| Ann Arbor Stage IV Non-Hodgkin Lymphoma \| Tarihin Tarihin Sarcoma \| Juvenile Xanthogranuloma \| Langerhans Cell Histiocytosis \| Glioma mai cutar \| Matashi mai saurin haihuwa Rhabdomyosarcoma \| Maimaitawa Ejen Maimaita Hepatoblastoma \| Maimaita Langerhans Cell Histiocytosis \| Maimaita mummunan ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar cuta \| Maimaita Muguwar Solid Neoplasm \| Maimaitawa Medulloblastoma \| Maimaita Neuroblastoma \| Maimaitawa Non-Hodgkin Lymphoma \| Maimaitawa Osteosarcoma \| urrentwayar Perwayar ipwayar ewayar ewayar \| \| Nama mai laushi Sarcoma \| Ewing Sarcoma mai ƙyama \| Glioma mai ƙyama \| Hepatoblastoma mai ƙyama \| Tarihin Langerhans na Tarihi \| Refarƙashin Gerwayar mwayar mwayar \|arya \| Refarƙashin Nearfin Neoplasm \| ractarfafa Medulloblastoma \| ractarfin Neuroblastoma \| Refractory \| ctory Peripheral Primitive Neuroectodermal Tumor \| Tsarin Tsarin Tsarin Tsarin Tsarin Tsarin Tsarin Neoplasm \| Tashin Cutar Rhabdoid \| Rhabdomyosarcoma mai ƙyama \| Ciwon Rhabdoid \| Mataki na III Osteosarcoma AJCC v7 \| Mataki na III Soft Nama Sarcoma AJCC v7 \| Mataki na III \| Mataki na IVA Osteosarcoma AJCC v7 \| Mataki na IVB Osteosarcoma AJCC v7 \| Wilms Tumor	Yuli 24, 2017	Lokaci 2