R & D Pipeline

TT-00420：

TT-00420 is a Phase II clinical-stage, internally discovered and developed, potential first-in-class, unique spectrum-selective kinase inhibitor targeting drug-resistant, relapsed or refractory cancers. It combines with the target in a unique way, and has unique advantages in drug resistance mutation after some targeted drug therapy. At the same time, combination of target profile and mechanism of action can effectively treat highly heterogeneous tumors, such as TNBC and CCA without clear biomarkers. At present, the project has completed the clinical trials of dose escalation phase, and the expansion or Phase II clinical trial in different tumor species has begun.

TT-00434：

TT-00434 has improved target selectivity, robust antitumor efficacy,and high potential in combination therapy with other small moleculetargeted therapies or chemotherapies. We aim to complete the Phase I clinical trials in the second half of 2022.

TT-01488：

TT-01488 is a potential best-in-class, internally developed, novel non-covalent, reversible BTK inhibitor to overcome acquired resistance developed from marketed covalent BTKinhibitors in various types of relapsed or refractory hematological malignancies. In a head-to-head kinase panel screening, in addition to its higher potency, TT-01488 demonstrated better kinase selectivity than ARQ-531 (the frontrunner non-covalent reversible BTK inhibitor currently in Phase II trial) on EGFR and TEC, indicating its fewer off-target side effects and a better safety profile. In the DLBCL CDX model, TT-01488 showed a superior antitumor effect compared to ARQ-531. We plan to submit IND application to the FDA in the second half of 2021 and to the NMPA in the first half of 2022. Upon IND clearance, we will initiate clinical trials on hematological malignancies worldwide.

TT-00973：

TT-00973 is a novel, internally discovered and developed AXL/FLT3 dual inhibitor.TT-00973 has high activity in abrogating AXL phosphorylation and activation in tumor cells,which makes it effective in treating relapsed or refractory hematological malignancies as wellas solid tumor with AXL overexpression. In addition, it potently inhibits the growth of tumorcells harboring the FLT3-ITD-F691L gate keeper mutation and is expected to overcome theacquired resistance of AML patients who have been treated with first- and second-generationFLT3-ITD kinase inhibitors. We plan to submit IND application for TT-00973 to the FDA andthe NMPA in the first half of 2022.

TT-ROMI：

Undisclosed

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-01688：

TT-01688 is a clinically advanced, highly selective S1P1 modulator with potential low cardiovascular side effects. S1P1 is a promising autoimmunological disease target with a favorable target safety profile. It shows promise for the treatment of UC, which has been clinically validated by a S1P1 modulator ozanimod. Accumulating clinical evidence also supports S1P1 modulators in a variety of other immunological indications, including AD and CD. TT-01688 has proven its high selectivity for the S1P1 target and excellent mechanistic PK/PD profiles in preclinicaland Phase I clinical studies. We expect to file IND application for TT-01688 in China in August 2021. Subject to the CDE's consent, we plan to initiate a Phase II clinical trial of TT-01688 for the treatment of UC in China in the first half of 2022.

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 and aim to complete the subject enrollment in the first half of 2022.

TT-RIAN：

Undisclosed

Drug Candidate	Target/ Mechanism （MOA）	Indication	Mono/ Combo	Status Preclinical IND Enabling Phase I Phase II	Commercial rights	Partner
TT-00420	Unique MTK(FGFR mut ,Aurora A/B,VEGFRs,JAK1/2,CSF1R)	CCA⁽¹⁾ FGFR2 acquired resistance	Mono	US	Global	N/A
		CCA⁽¹⁾ FGFR2 primary resistanc	Mono	US
		CCA⁽¹⁾ Non-FGFR	Mono	US
		TNBC⁽²⁾	Mono	US/China	Global	N/A
		TNBC⁽²⁾	Combo with Chemo	US/China	Global	N/A
		BTC	Combo with PD-L1	China	Global	Roche Collaboration
		Solid tumors⁽⁷⁾	Mono	US/China	Global	N/A
TT-00434	FGFR1/2/3	Gastric Cancers FGFR2 amplification	Mono	US/China	Global	N/A
TT-01488	Reversible BTK	CLL/MCL/WM Acquired mutation	Mono		Global	N/A
TT-00973	AXL/FLT	R/R AML	Mono		Global	N/A
TT-00973	AXL/FLT	Solid tumors	Mono		Global	N/A
TT-ROMI	Undisclosed	Cancer	Mono		Global	Co-develop
TT-00920	PDE9	HF	Mono	US/China	Global	N/A
TT-00920	PDE9	SCD	Mono		Global	N/A
TT-01688	S1P1	UC/AD	Mono	China	China	In-license
TT-01688	S1P1	UC/AD	Mono	Partner’s global tria	China	In-license
TT-01025	VAP-1	NASH	Mono	China	China Japan	Out-license
TT-01025	VAP-1	NASH	Mono	Partner’s global tria	China Japan	Out-license
TT-RIAN	Undisclosed	Inflammation	Mono		Global	Co-develop
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Department Introduction

We are committed to developing global first-in-class and best-in-class therapies

and serving the urgent unmet medical needs of patients worldwide with innovative and highly differentiated small molecule drugs.

Transformative Therapy！TransThera