R & D Pipeline

TT-00420：

TT-00420 is an innovative, global phase III stage spectrum-selective kinase inhibitor that exerts antitumor effects by targeting tumor cells and improving the tumor microenvironment. Ongoing clinical trials in the US and China have revealed the potential of TT-00420 to be efficacious in various solid tumors. It was granted the Orphan-Drug Designation and Fast Track Designation by the FDA for the treatment of CCA. In July 2023, TT-00420 was granted the Breakthrough Therapy Designation (BTD) by NMPA in China.

TT-01488：

TT-01488 is a non-covalent, reversible BTK inhibitor for overcoming acquired resistance mutation developed from marketed covalent BTK inhibitors in various types of B-Cell lymphomas. In preclinical trials, TT-01488 showed potential advantages such as overcoming drug resistance, improved target selectivity, antitumor efficacy and favorable safety.

TT-00973：

TT-00973 is a novel AXL/FLT3 dual inhibitor discovered by TransThera. It has high activity in abrogating AXL phosphorylation and activation in tumor cells, making it potentially effective in addressing unmet clinical needs in solid tumors. In addition, TT-00973 potently inhibits the growth of tumor cells harboring the FLT3-ITD-F691L gate keeper mutation and is expected to overcome the acquired resistance of AML patients who have been treated with first- and second-generation FLT3-ITD kinase inhibitors. TT-00973 was granted IND clearance for advanced hematologic malignancies by the U.S. FDA on February 24, 2022.

TT-00434：

TT-00434 has improved target selectivity, robust antitumor efficacy, and high potential in combination therapy with other small molecule targeted therapies or chemotherapies.

TT-ROMI：

Undisclosed

TT-01688：

TT-01688 is a Phase II stage, oral S1P1 receptor modulator targeting autoimmune diseases. TT-01688 has proven its high selectivity for the S1P1 target and excellent mechanistic PK/PD profiles in preclinical and Phase I clinical study. We will research, develop, manufacture and commercialize TT-01688 to treat various autoimmune indications, including UC and AD in China.

TT-00920：

TT-00920 is an internally discovered and developed, potential first-in-class, highly selective oral PDE9 small molecule inhibitor for chronic heart failure with a novel biological mechanism and strong disease rationale. Clinical patient samples and mechanistic studies support the cardioprotective mechanism that PDE9 inhibition may restore dysfunction in patients with heart failure. Pre-clinical studies have shown that TT-00920 can activate myocardial endogenous protective signaling pathways, restores cardiac function and improves myocardial remodeling. At present, the project is in clinical Phase I in the United States, continuing with MAD study with the aim to complete enrollment in 2021.

TT-01025：

TT-01025 is an irreversible VAP-1 small molecule inhibitor, targeting at the chronic inflammatory diseases such as non-alcoholic steatohepatitis. TT-01025 has the advantage of high clinical differentiation, and its high selectivity and low brain pass rate avoid the safety risk caused by the off target effect of clinical compounds with the same target its high selectivity and low brain pass rate avoid the safety risk caused by the off target effect of the clinical compounds with the same target. We licensed-out TT-01025 to LG Chem and we retain the development and commercialization rights in Greater China and Japan. We have initiated a Phase I study of TT-01025 in healthy subjects in China.

TT-RIAN：

Undisclosed

Drug Candidate	Target/ Mechanism	Indication	Mono/ Combo	Clinical Stage Pre-clinical IND Enabling Phase I Phase II Pivotal Phase II /Phase III	Rights Region	Partners	Learn more clinical information
Tinengotinib (TT-00420)	Unique MTK(FGFR mut ,Aurora A/B,VEGFRs,JAK1/2, CSF1R)	CCA	Mono	China	Global		Click here
		CCA	Mono	MRCT in the US/EU/Asia
		mCRPC	Mono	US, China
		Pan-FGFR solid tumor	Mono	US, China
		Her2- breast cancer (including TNBC)	Mono	US, China
		BTC	Combo with PD - L1	China		Roche
TT-01488	Reversible BTK	CLL/MCL/WM	Mono	US, China	Global		Click here
TT-00973	AXL/FLT3	R/R AML myelodysplasia	Mono	China	Global		Click here
TT-00973	AXL/FLT3	Solid tumor	Mono	US	Global		Click here
TT-00434	FGFR1/2/3	Gastric cancer FGFR 2 amplification	Mono	China	Global		Click here
TT-ROMI	Undisclosed	Cancer	Mono		Global		Click here
TT-01688	S1P1	AD	Mono	China	China		Click here
TT-01688	S1P1	UC	Mono	China	China		Click here
TT-00920	PDE9	HF	Mono	US, China	Global		Click here
TT-01025	VAP-1	NASH	Mono	China	China Japan		Click here
TT-RIAN	Undisclosed	inflammation	Mono		Global		Click here
Notes: As of October 26, 2023 ; The target patients are patients with cholangiocarcinoma that has progressed on prior treatment with FGFR inhibitors; TT-01688 is licensed-in from LG Chem, TransThera owns the clinical development and commercialization rights in Greater China; TT-01025 is licensed-out to LG Chem, with TransThera retaining rights in China and Japan;