Our R&D is Focusing On TMERs for Innovative Medicine to Tackle Tumor Immune Escape
Tumor generates a unique microenvironment (TME) niche to escape body's immune attack.
TME factors engage receptors (TMERs) expressed on the cells of the immune system to evade anti-tumor immune surveillance.
Both Hippo-YAP and cAMP are immuno-suppressive signal transduction pathways in the immune cells, and linked to cell surface G-protein coupled receptor (GPCR) family members.
GPCR - An important class of TMERs, plays an important role in various diseases incl. cancer.
Depending on the subtypes & differential intracellular signal transduction pathways, a GPCR, upon engagement by a TME factor;
Inhibit tumor-killing immune cells such as CTL and NK cells.
Induce the formation of immune suppressive cells (iTreg, MDSC, Reg-DC), or cause chemotactic migration and
Redistribution of immune cells in favor of tumor survival and growth in a patient body.
Hippo-YAP is a major pathway driving tumorigenesis, particularly in tumors of epithelium origin, and is essential for tumor to escape immune attack by promoting Treg function and suppressing CTL function.
By selectively blocking YAP in immune cells and in cancer cells, a TMER inhibitor is expected to (1) inhibit tumor growth, and (2) activate anti-tumor immunity.
Bring breakthrough therapies to cancer patients through innovation and discovery of whole new generation small molecule I-O drugs
R & D Pipeline
program
target
indication
moa
development stage
CT3001
TMER1-i
Small molecule
GPR35
a.k.a.
Kynurenic Acid Receptor
IO, first-in-class
GPR35+ IDO1+ Tumors:
Colon, Pdac, Gastric, NSCLC
Hippo-YAP regulator
Block IDO-mediated tumor immune escape
Block tumor growth
CT3021
TMER2-i
Small molecule
Adenosine Receptors
A2a, A2b, A1
IO, Best-in-class
A1+ CD73+ Tumors
Highly potent triple antagonist
(Ki = 0.37 nM [A2a], 1.76 nM [A2b], 1.26 nM [A1]
Full antagonism in high adenosine TME
TMER3-i
Small molecule
Undisclosed
IO, first-in-class
Solid Tumors
Hippo-YAP regulator
Block tumor immune escape
Block tumor growth
Candidate Nomination
TMER4-i
Small molecule
Undisclosed
IO, first-in-class
Solid Tumors
Hippo-YAP regulator
Block tumor growth
“Hit” to “Lead”
PD1/PD-L1 Blocker
Small molecule
IO
mono/combo with other TMER-i
“Hit” to “Lead”