MP2021
MP2021
TM4SF19 – Novel Target for Bone Health & inflammatory diseases
First-in-class bone diseases therapy
TM4SF19
MP2021 : Competitive Inhibitor for TM4SF19
Significantly inhibits bone-loss and restores bone balance (Rheumatoid Arthritis, Osteoporosis)
Inhibition of bone metastasis (anticancer)
Inhibition of muscle loss
Reduction of visceral white fat (fatty liver prevention)
Efficacy study for IND completed
Significantly inhibits bone-loss and restores bone balance in osteoporotic model.
Confirmed improvement in BMD, BV/TV, Tb.N, and Tb.Sp.
Suppresses adipocyte differentiation and inflammation, prevent obesity and bone loss, and promote browning of white adipose tissue to enhance thermogenesis.
TOX study for IND completed
Highest dose selected as the NOAEL
Safe due to distinctive MoA of TM4SF19.
Mar, 2025
Tm4sf19 inhibition ameliorates inflammation and bone destruction in collagen-induced arthritis by suppressing TLR4-mediated inflammatory signaling and abnormal osteoclast activation
Bone ResearchNov, 2024
MIMERET, a Novel Mitochondrial-Targeted Drug, Improves Hepatic Steatosis by Stimulating Mitochondrial Fatty Acid Beta-Oxidation to Prevent Lipid Accumulation
AASLD 2024Nov, 2024
Vactosertib, a TGF-β signaling inhibitor, in combination with Durvalumab increased mOS in ≥2L treatment of patients with PD-L1-positive advanced NSCLC
SITC 2024Aug, 2024
The TGFβ type I receptor kinase inhibitor vactosertib in combination with pomalidomide in relapsed/refractory multiple myeloma: a phase 1b trial
Nature CommunicationsJul, 2024
Oral transforming growth factor-beta receptor 1 inhibitor vactosertib promotes osteosarcoma regression by targeting tumor proliferation and enhancing anti-tumor immunity
Cancer CommunicationsNov, 2023
Tm4sf19 deficiency inhibits osteoclast multinucleation and prevents bone loss
Metabolism 151Apr, 2023
Vactosertib combined treatment with T1-44, a PRMT5 activity inhibitor, improves the survival and inhibits tumor invasion of murine pancreatic cancer model
American Association for Cancer Research 2023(AACR 2023)Feb, 2023
Combination treatment of T1-44, a PRMT5 inhibitor with Vactosertib, an inhibitor of TGF-β signaling, inhibits invasion and prolongs survival in a mouse model of pancreatic tumors
Cell Death and Disease (2023)Jan, 2023
Discovery of TRD-93 as a novel DRAK2 inhibitor
BULLETIN OF THE KOREAN CHEMICAL SOCIETYDec, 2022
MAST4 controls cell cycle in spermatogonial stem cells
Cell proliferation(IF : 8.755)Dec, 2022
Therapeutic Implications of TGF-β Pathway in Desmoid Tumor Based on Comprehensive Molecular Profiling and Clinicopathological Properties
CancersOct, 2022
ESRP1-regulated isoform switching of LRRFIP2 determines metastasis of gastric cancer
Nature communicationSep, 2022
Phase 1b Study of Vactosertib in Combination with FOLFOX in Patients with Metastatic Pancreatic Ductal Adenocarcinoma who have Failed First-Line Gemcitabine/nab-Paclitaxel
AACR Special Conference on Pancreatic Cancer 2022Jan, 2022
Phase 1b Study of Vactosertib in Combination with nal-IRI plus 5FU/LV in Patients with Metastatic Pancreatic Ductal Adenocarcinoma who Failed First-Line Gemcitabine/nab-Paclitaxel
ASCO GI 2022Nov, 2021
Tumor Microenvironment based on PD-L1 and CD8 T-cell infiltration correlated with the survival of MSS mCRC patients treated vactosertib in combination with pembrolizumab
SITC 2021Nov, 2021
Spatial analysis of tumor-infiltrating lymphocytes correlates with the response of metastatic colorectal cancer patients treated with vactosertib in combination with pembrolizumab
SITC 2021Jun, 2021
Efficacy and Safety of Vactosertib and Pembrolizumab Combination in Patients with Previously Treated Microsatellite Stable Metastatic Colorectal Cancer
ASCO 2021Jun, 2021
Phase 1b trial of Vactosertib in Combination with Pomalidomide in Relapsed Multiple Myeloma: A Corticosteroid-Free Approach by Targeting TGF-β Signaling Pathway
ASCO 2021Apr, 2021
BAG2 Promotes Tumorigenesis and Metastasis by Regulating the Cathepsin B Cleavage in Triple Negative Breast Cancer Cells
AACR 2021Apr, 2021
DRAK1 suppresses inflammation induced cervical cancer progression by targeting TRAF6 protein
AACR 2021Apr, 2021
Beneficial effect of vactosertib combined with nal IRI5 FULV in pancreatic cancer treatment
AACR 2021Apr, 2021
Genomic and transcriptomic analyses of desmoid tumor reveals enrichment of transforming growth factor beta responsive signature
AACR 2021Nov, 2020
Vactosertib and Durvalumab as Second or Later Line Treatment for PD-L1 Positive Non-small Cell Lung Cancer: Interim Result
SITC 2020Sep, 2020
Safety and Efficacy of Vactosertib, a TGFBR1 Kinase Inhibitor, in Combination with Paclitaxel in Patients with Metastatic Gastric Adenocarcinoma
ESMO Congress 2020May, 2020
A Phase 1 study of TGF-β inhibitor, Vactosertib, in combination with Imatinib in patients with advanced desmoid tumor (aggressive fibromatosis)
ASCO 2020Nov, 2019
Safety and Preliminary clinical activity of Vactosertib, a selective TGF-β receptor I kinase inhibitor, in combination with Durvalumab in advanced Non-small cell lung cancer patients with low PD-L1 expression
SITC 2019Nov, 2019
Safety and preliminary clinical activity of Vactosertib, a selective TGF-β receptor I kinase inhibitor, in combination with Pembrolizumab in patients with metastatic colorectal or gastric cancer
SITC 2019Nov, 2019
TGF-β as a promising therapeutic target for treating Osteosarcoma
Innovation in AYA cancerJun, 2018
TGF-β Responsive signature is associated with anti-tumor effect of Vactosertib, a potent oral TGF-β receptor type1(TGFBRI) inhibitor in patients with advanced solid tumors
ASCO 2018