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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

CT3001 Phase 1/2a(Click to See Clinical Trial Details)

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

CT3021 IND-Enabling(Click to See Details)

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”