Development of treatment
for patients

Vactosertib

MOA of Vactosertib

Vactosertib can be combined with all existing cancer treatment

TGF-β1 acts on stromal cells around cancerous tissues to produce large quantities of extracellular matrix, creating a barrier surrounding the tumor

- prevent anticancer drugs and immune cells from attacking cancer tissue

Vactosertib, a TGF-β1 signaling inhibitor, prevents the formation of matrix walls around cancerous tissues

- Various cancer therapies help attack cancer cells

Without Vactosertib
ICI, Chemo mono

Impossible to penetrate tumor stroma, Low responses to anticancer drugs,
Development of drug resistance

With Vactosertib
Anticancer drug in combination

Inhibit Cancer Growth

Collaboration with Blockbuster Immuno-oncology Drugs

Ongoing clinical trials combining vactosertib, a well-tolerated and effective compound, with leading IO drugs developed by global pharma

Metastatic Colorectal Cancer(MSS type) Clinical Trial Results Overview

MP-VAC-204 vs MSS type standard therapy

MP-VAC-204 vs MSS type standard therapy
Category MP-VAC
-204
(Vactosertib
+
Pembroli
-zumab)
Regorafenib
-mono
CORRECT
Lonsurf
-mono
mOS
(Median
Overall
Survival)
15.8 months 6.4 months 7.1 months
ORR
(Overall
Response
Rate)
16.0% (8/50) 1% (5/505) 1.6% (9/534)

* mOS = Median Overall Survival
* ORR = Overall Response Rate

Colorectal Cancer(MSS type) Clinical Trial Results

Colorectal Cancer(MSS type) Clinical Trial Results
Atezoli
-zumab
+
cobimetinib
Pembroli
-zumab
-mono
M-7824 Lonsurf
+
Nivolumab
Regorafenib
+
Avelumab
Pembroli
-zumab
+
Lenvatinib
Atezoli
-zumab
+
Imprime
PGG
+
bevaci
-zumab
Regorafenib
+
Nivolumab
8.9 months 5.0 months - - 10.8 months 7.5 months 5.7 months 11.9 months
2.7% (5/183) 0.0% (0/18) 3.4% (1/29) 0% (0/35) 0% (0/43) 22% (7/32) 0% (0/15) 7.1% (5/70)

US Phase 1 Results

Advanced solid tumors

Vactosertib is safe and well-tolerated as a monotherapy

  • - Mild adverse events seen even in high dose groups
  • - Stability confirmed in ongoing combination trials

Ongoing Clinical Collaborations

Ongoing combination therapy trials with blockbuster IO drugs

  • Free supply of Keytruda & Imfinzi by MSD & AZ
  • Co-development of clinical trial strategy and design
  • Keytruda* (anti-PD-1) Colorectal
  • Keytruda (anti-PD-1) NSCLC 1L
  • Among all IO drugs, obtained the greatest number of FDA approvals – more than 20 indications
  • Forecasted to be global top-selling drug by revenue by 2021
  • Imfinzi* (anti-PD-L1) NSCLC 2L
  • Imfinzi (anti-PD-L1) Bladder cancer
  • AstraZeneca’s main immunooncology product
  • Forecasted to be a blockbuster drug in the near future

* Keytruda (pembrolizumab), Imfinzi (durvalumab)

Ongoing Trials with Leading Combination Agents

Clinical trials will demonstrate the combination potential
with existing anticancer therapies to maximize Vactosertib’s commercial value

  • SIT

  • IIT

Clinical Development Status
Category Cancer Type [Country] Regimen Clinical Development Status Clinical information
Preclinical Phase 1 Phase 2 Phase 3
Solid Cancer Monotherapy Osteosarcoma [US]Vactosertib Monotherapy
Chemo-therapy combination Gastric Cancer [KR]+ Paclitaxel
[KR]+ Paclitaxel +Ramucirumab
Pancreatic Cancer [KR]+ FOLFOX
[KR]+ 5FU/LV/Onivyde삼성
NK cell therapy combination colorectal/blood tumor cancer [US]+ NK Cell Therapy + Interleukin(IL-2)
Immuno-therapy combination Colorectal Cancer [KR]+ Keytruda (anti-PD-1)MSD
Colorectal Cancer (Neoadjuvant) [US]+ Keytruda (anti-PD-1)
NSCLC 1L [KR]+ Keytruda (anti-PD-1)MSD
NSCLC 2L [KR]+ Imfinzi (anti-PD-L1)AstraZeneca
Bladder Cancer [US]+ Imfinzi (anti-PD-L1)AstraZeneca
Gastric Cancer [KR]+ Imfinzi (anti-PD-L1)
  • [US]Monotherapy

    CategorySolid Cancer, Vactosertib Monotherapy

    Cancer TypeOsteosarcoma

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]Paclitaxel

    CategorySolid Cancer, Chemotherapy combination

    Cancer TypeGastric Cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]Paclitaxel +Ramucirumab

    CategorySolid Cancer, Chemotherapy combination

    Cancer TypeGastric Cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]FOLFOX

    CategorySolid Cancer, Chemotherapy combination

    Cancer TypePancreatic Cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]5FU/LV/Onivyde

    삼성

    CategorySolid Cancer, Chemotherapy combination

    Cancer TypePancreatic Cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [US]NK Cell Therapy + Interleukin(IL-2)

    CategorySolid Cancer, NK cell therapy combination

    Cancer Typecolorectal/blood tumor cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]Keytruda (anti-PD-1)

    MSD

    CategorySolid Cancer, Immunotherapy combination

    Cancer TypeColorectal Cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [US]Keytruda (anti-PD-1)

    CategorySolid Cancer, Immunotherapy combination

    Cancer TypeColorectal Cancer(Neoadjuvant)

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]Keytruda (anti-PD-1)

    MSD

    CategorySolid Cancer, Immunotherapy combination

    Cancer TypeNSCLC 1L

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]Imfinzi (anti-PD-L1)

    AstraZeneca

    CategorySolid Cancer, Immunotherapy combination

    Cancer TypeNSCLC 2L

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [US]Imfinzi (anti-PD-L1)

    AstraZeneca

    CategorySolid Cancer, Immunotherapy combination

    Cancer TypeBladder Cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

  • [KR]Imfinzi (anti-PD-L1)

    CategorySolid Cancer, Immunotherapy combination

    Cancer TypeGastric Cancer

    Clinical information

    Clinical
    Development Status

    Preclinical

    Phase 1

    Phase 2

    Phase 3

Presentations & Publications

Total 0

  • Nov, 2023

    Tm4sf19 deficiency inhibits osteoclast multinucleation and prevents bone loss

    Metabolism 151
  • Apr, 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 SOCIETY
  • Dec, 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

    Cancers
  • Oct, 2022

    ESRP1-regulated isoform switching of LRRFIP2 determines metastasis of gastric cancer

    Nature communication
  • Sep, 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 2022
  • Jan, 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 2022
  • Nov, 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 2021
  • Nov, 2021

    Spatial analysis of tumor-infiltrating lymphocytes correlates with the response of metastatic colorectal cancer patients treated with vactosertib in combination with pembrolizumab

    SITC 2021
  • Jun, 2021

    Efficacy and Safety of Vactosertib and Pembrolizumab Combination in Patients with Previously Treated Microsatellite Stable Metastatic Colorectal Cancer

    ASCO 2021
  • Jun, 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 2021
  • Apr, 2021

    BAG2 Promotes Tumorigenesis and Metastasis by Regulating the Cathepsin B Cleavage in Triple Negative Breast Cancer Cells

    AACR 2021
  • Apr, 2021

    DRAK1 suppresses inflammation induced cervical cancer progression by targeting TRAF6 protein

    AACR 2021
  • Apr, 2021

    Beneficial effect of vactosertib combined with nal IRI5 FULV in pancreatic cancer treatment

    AACR 2021
  • Apr, 2021

    Genomic and transcriptomic analyses of desmoid tumor reveals enrichment of transforming growth factor beta responsive signature

    AACR 2021
  • Nov, 2020

    Vactosertib and Durvalumab as Second or Later Line Treatment for PD-L1 Positive Non-small Cell Lung Cancer: Interim Result

    SITC 2020
  • Sep, 2020

    Safety and Efficacy of Vactosertib, a TGFBR1 Kinase Inhibitor, in Combination with Paclitaxel in Patients with Metastatic Gastric Adenocarcinoma

    ESMO Congress 2020
  • May, 2020

    A Phase 1 study of TGF-β inhibitor, Vactosertib, in combination with Imatinib in patients with advanced desmoid tumor (aggressive fibromatosis)

    ASCO 2020
  • Nov, 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 2019
  • Nov, 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 2019
  • Nov, 2019

    TGF-β as a promising therapeutic target for treating Osteosarcoma

    Innovation in AYA cancer
  • Jun, 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