Overview

NCI Definition [1]:
An orally bioavailable inhibitor of the serine/threonine kinase, transforming growth factor (TGF)-beta receptor type 1 (TGFBR1), also known as activin receptor-like kinase 5 (ALK5), with potential antineoplastic activity. Upon oral administration, ALK5 inhibitor TEW-7197 inhibits the activity of TGFBR1 and prevents TGF-beta/TGFBR1-mediated signaling. This suppresses tumor growth in TGFBR1-overexpressing tumor cells. TGFBR1, which is overexpressed in a variety of tumor cell types, plays a key role in tumor cell proliferation. Expression of TGF-beta promotes tumor cell proliferation, enhances the migration of tumor cells and suppresses the response of the host immune system to tumor cells.

Vactosertib has been investigated in 6 clinical trials, of which 5 are open and 1 is closed. Of the trials investigating vactosertib, 2 are phase 1 (1 open), 2 are phase 1/phase 2 (2 open), and 2 are phase 2 (2 open).

Complex karyotype, Loss of Y, and Monosomy 7 are the most frequent biomarker inclusion criteria for vactosertib clinical trials.

Non-small cell lung carcinoma, bladder urothelial carcinoma, and malignant solid tumor are the most common diseases being investigated in vactosertib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Vactosertib
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Vactosertib
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating vactosertib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
tgfbr1 inhibitor tew-7197, tgfbr1 inhibitor tew-7197, tew7197, alk5 inhibitor tew-7197, tew-7197, tew 7197
Drug Categories [2]:
Serine/threonine kinase inhibitors, TGFBR1 inhibitors
Drug Target(s) [2]:
TGFBR1
NCIT ID [1]:
C116357

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.