GV101 / Sino Biopharm, Graviton Biosci, Ovid Therapeutics - LARVOL DELTA

A Phase I Clinical Trial Protocol to Evaluate the Safety and Efficacy of TDI01 Suspension in Subjects with Radiation-Induced Pulmonary Fibrosis (ChiCTR) - P1 | N=6 | Not yet recruiting | Sponsor: West China Hospital, Sichuan University; West China Hospital, Sichuan University

New P1 trial • Breast Cancer • Immunology • Pulmonary Disease • Respiratory Diseases

Graviton BioScience Corporation Announces Publication of Positive Ph1b Trial Results for GV101 (TDI01) in Chronic Graft versus Host Disease in Signal Transduction and Targeted Therapy, by Beijing Tide Pharmaceutical (Yahoo Finance) - "At 24-weeks, GV101 yielded a bORR of 86.2% (95% CI: 68.3 to 96.1) at 400 mg and 67.9% (95% CI: 47.6 to 84.1) at 200 mg; FFS was 89.4% at 400 mg and 78.6% at 200 mg. Median FFS was not met at the time of analysis. OS was 96.6% at 400 mg and 100% at 200 mg; a single participant died, attributed to COVID-19 pneumonia. Median time to first response was 30.0 days (range 28-115 days) at 400 mg and 44.5 days (range 28-284 days) at 200 mg, consistent with a rapid onset. Median time to first response was 30.0 days (range 28-115 days) at 400 mg and 44.5 days (range 28-284 days) at 200 mg, consistent with a rapid onset...There was no grade ≥3 leukopenia, thrombocytopenia, or anemia, and only one grade 3 neutropenia. There were no CMV infections....Next: Graviton is currently in Phase III RCT planning for GV101 in cGvHD and plans to carry the high dose forward."

P1 data • Chronic Graft versus Host Disease

Novel highly selective ROCK2 inhibitor (TDI01) for the treatment of chronic graft-versus-host disease: a multicenter, open-label phase Ib/II study. (PubMed, Signal Transduct Target Ther) - P1/2 | "The most common adverse events ( ≥ 20% of patients) were transient bilirubin elevation (total bilirubin elevation 81.7%, unconjugated 56.7%, conjugated 45.0%) and headache (23.3%), without significant increases in liver enzymes. Thus, TDI01, particularly at the 400 mg QD dose, demonstrated promising efficacy and safety in moderate-to-severe cGVHD, which will be confirmed in a forthcoming phase III randomized controlled trial."

Journal • P1/2 data • Bone Marrow Transplantation • Chronic Graft versus Host Disease • Graft versus Host Disease • Immunology • Pain • Transplantation

ROCK2 inhibitor targets vascular niche angiocrine signaling in liver fibrosis. (PubMed, Trends Pharmacol Sci) - "identifies that Rho-associated coiled-coil containing kinase 2 (ROCK2) upregulation in sinusoidal endothelial and perivascular cells drives liver fibrosis via pro-fibrotic angiocrine signaling. The selective ROCK2 inhibitor TDI01 reverses fibrosis preclinically and demonstrates safety and target engagement in patients, highlighting vascular niche targeting as a therapeutic strategy."

Journal • Fibrosis • Hepatology • Immunology • Liver Cirrhosis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis

A Adaptive Design Clinical Trial to Evaluate the Efficacy and Safety of TDI01 Suspension in the Treatment of Idiopathic Pulmonary Fibrosis (IPF) (clinicaltrials.gov) - P3 | N=508 | Recruiting | Sponsor: Beijing Tide Pharmaceutical Co., Ltd

New P3 trial • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Selective targeting of endothelial and perivascular angiocrine ROCK2 treats liver fibrosis. (PubMed, Cell) - P=N/A, P1 | "An extended clinical trial (ChiCTR2400082056) showed a trend toward reducing liver fibrosis in five of six patients after TDI01 treatment. Thus, we discover vascular ROCK2 as a pro-fibrotic target, and development of an inhibitor selectively targeting angiocrine ROCK2 may provide a treatment of liver fibrosis in human patients."

Journal • Fibrosis • Hepatology • Immunology • Liver Cirrhosis • Metabolic Disorders • Metabolic Dysfunction-Associated Steatohepatitis

…Sino Biopharmaceutical Limited…announces that the enrollment of the first patient in the Phase III clinical trial for TDI01 'ROCK2 inhibitor' independently developed by the Group for the treatment of idiopathic pulmonary fibrosis (IPF) has been completed… (HKEXnews)

Trial status • Idiopathic Pulmonary Fibrosis

TDI01 in the treatment of moderate to severe chronic graft-versus-host disease: Updated results from a multicenter, OPEN-label phase IB/II study (An Update) (ASH 2025) - P1/2 | "Median follow-up was 48.1 (95% CI, 48.0, 48.3) weeks and 72% (41/57) of evaluable patients had been previously treatedwith ruxolitinib. TDI01 demonstrated durable responses in moderate-to-severe cGVHD. The 400mg cohort showed ahigher ORR, a longer DOR, and a favorable FFS/OS than that of 200mg cohort. Safety was manageablewith primarily reversible hyperbilirubinemia."

Clinical • P1/2 data • Chronic Graft versus Host Disease • Cough • Gastrointestinal Disorder • Graft versus Host Disease • Hepatology • Immunology • Infectious Disease • Respiratory Diseases

TDI01 Suspension in the Treatment of Chronic Graft-versus-host Disease (cGVHD)) (clinicaltrials.gov) - P1/2 | N=60 | Active, not recruiting | Sponsor: Beijing Tide Pharmaceutical Co., Ltd | Recruiting ➔ Active, not recruiting | N=120 ➔ 60 | Trial primary completion date: Feb 2025 ➔ Feb 2026

Enrollment change • Enrollment closed • Trial primary completion date • Chronic Graft versus Host Disease • Graft versus Host Disease • Immunology

New molecules in the therapy of chronic graft-versus-host disease. (PubMed, Curr Opin Hematol) - "Expanding therapeutic options in cGvHD require decision-making based on organ involvement, prior therapy, and tolerability. Emerging compounds offer the potential to modulate chronic inflammation and fibrosis more precisely, supporting a move toward personalized and combinatorial approaches in advanced-line settings."

Journal • Chronic Graft versus Host Disease • Fibrosis • Graft versus Host Disease • Immunology • Inflammation • Transplantation

Taide Pharmaceuticals' TDI01 suspension starts Phase III clinical trial for graft-versus-host disease [Google translation] (Sina Corp) - "Data from the Drug Clinical Trial Registration and Information Disclosure Platform show that a multicenter, randomized, open-label, positive-controlled Phase III clinical study of Beijing Taide Pharmaceutical Co., Ltd.'s TDI01 suspension versus the investigator's selected regimen for the treatment of moderate to severe chronic graft-versus-host disease (cGVHD) who have previously received 2 lines of systemic treatment but no more than 5 lines has been launched. The clinical trial registration number is CTR20252713, and the first public information date is July 9, 2025.The primary endpoint of this trial includes the overall response rate at week 24; secondary endpoints include effectiveness indicators such as the best overall response rate at week 24, overall response rate at different times, and duration of remission, as well as safety indicators such as the incidence of adverse events and pharmacokinetic parameters....Currently, the experiment is in progress..."

Trial status • Chronic Graft versus Host Disease

NEW INDICATION OF TDI01 SUSPENSION (“ROCK2 INHIBITOR”) INCLUDED IN BREAKTHROUGH THERAPY DESIGNATION PROCESS BY CDE (HKEXnews) - "The board of directors (the 'Board') of Sino Biopharmaceutical Limited (the 'Company', together with its subsidiaries, the 'Group') announces that the Group’s self-developed Class 1 innovative drug TDI01 suspension, a 'ROCK2 inhibitor', has been included in the Breakthrough Therapy Designation (BTD) process by the Center for Drug Evaluation (CDE) of the National Medical Products Administration of China. The drug is used for the treatment of moderate to severe chronic graft-versus-host disease (cGVHD) in patients who have received at least 1 prior line but no more than five prior lines of systemic therapy.... Results from a Phase Ib/II clinical study demonstrated that TDI01 exhibited significant efficacy potential and good safety in patients with moderate to severe cGVHD who had received 1-5 prior lines of treatment."

Breakthrough therapy • Chronic Graft versus Host Disease

TDI-01 IN THE TREATMENT OF MODERATE TO SEVERE CHRONIC GRAFT-VERSUS-HOST DISEASE: INTERIM RESULTS FROM A MULTICENTER, OPEN-LABEL PHASE IB/II STUDY (EBMT 2025) - P1/2 | "TDI-01 showed promising efficacy and acceptable safety in patients with moderate to severe cGVHD after 1 to 5 lines of prior therapies, which may offer a new therapeutic option for cGVHD patients. Further follow-up will provide more information on durability and long-term outcomes. Clinical Trial Registry: NCT06169722; Study Details; TDI01 Suspension in the Treatment of Chronic Graft-versus-host Disease (cGVHD)); ClinicalTrials.gov"

Clinical • P1/2 data • Bone Marrow Transplantation • Chronic Graft versus Host Disease • Graft versus Host Disease • Immunology • Pain

TDI01 Demonstrates Preliminary Efficacy and Tolerability in Moderate-to-Severe cGVHD (OncLive) - P1b/2 | N=120 | NCT06169722 | Sponsor: Beijing Tide Pharmaceutical Co., Ltd | "Treatment with TDI01-an oral, highly selective ROCK2 inhibitor-led to clinical activity and tolerability in patients with moderate-to-severe chronic graft-vs-host disease (cGVHD), according to findings from a phase 1b/2 study (NCT06169722) presented at the 51st Annual EBMT Meeting. Findings showed that at week 24, the best overall response rate (ORR) was 67.9% (95% CI, 47.6%-84.1%) in patients treated with TDI01 at 200 mg once daily (n = 30) and 86.2% (95% CI, 68.3%-96.1%) in those treated at 400 mg once per day (n = 30). The 24-week ORR was 50.0% (95% CI, 30.6%-69.4%) and 55.2% (95% CI, 35.7%-73.6%) in the 200-mg and 400-mg groups, respectively. The median time to response was 44.0 days (range, 29-169) and 31.0 days (range, 28-115) in the 200-mg and 400-mg arms, respectively. Across both arms, 67.4% of responders achieved a response within 8 weeks of treatment initiation."

P1 data • Chronic Graft versus Host Disease

Model-informed drug development of novel ROCK2 inhibitor TDI01: population pharmacokinetic study and simulation. (PubMed, Front Pharmacol) - "Results from the simulation show that the drug accumulation observed after multiple doses would not affect the safety of TID01 usage under the tested dosage regimen. The established model and simulation provide a useful approach to maximize the clinical medication safety and therapeutic efficacy of TDI01."

Journal • PK/PD data • Acute Respiratory Distress Syndrome • Infectious Disease • Novel Coronavirus Disease

An exploratory clinical trial to evaluate the safety and efficacy of TDI01 suspension in the patients with hepatic fibrosis (ChiCTR) - P=N/A | N=12 | Recruiting | Sponsor: West China Hospital, Sichuan University; West China Hospital, Sichuan University | Not yet recruiting ➔ Recruiting

Enrollment open • Fibrosis • Hepatology • Immunology

TDI01 Suspension in the Treatment of Chronic Graft-versus-host Disease (cGVHD)) (clinicaltrials.gov) - P1/2 | N=120 | Recruiting | Sponsor: Beijing Tide Pharmaceutical Co., Ltd | Not yet recruiting ➔ Recruiting

Enrollment open • Chronic Graft versus Host Disease • Graft versus Host Disease • Immunology

TDI01 Suspension in the Treatment of Chronic Graft-versus-host Disease (cGVHD)) (clinicaltrials.gov) - P1/2 | N=120 | Not yet recruiting | Sponsor: Beijing Tide Pharmaceutical Co., Ltd

New P1/2 trial • Chronic Graft versus Host Disease • Graft versus Host Disease • Immunology

A Clinical Trial on the Treatment of Idiopathic Pulmonary Fibrosis (clinicaltrials.gov) - P2 | N=120 | Not yet recruiting | Sponsor: Beijing Tide Pharmaceutical Co., Ltd

New P2 trial • Fibrosis • Idiopathic Pulmonary Fibrosis • Immunology • Pulmonary Disease • Respiratory Diseases

Zhongsheng Pharmaceutical's first-class innovative drug TDI01 is about to start phase II clinical trials [Google translation] (Shanghai Securities News) - "Shanghai Securities News China Securities Net News (Reporter Li Yuan) Beijing Tide Pharmaceuticals...held a National Investigator Meeting on Phase II clinical trials of the original innovative drug TDI01 in patients with idiopathic pulmonary fibrosis (IPF) in Beijing on April 28 , marking that this class of innovative drug independently developed by Chinese pharmaceutical companies is about to start II clinical trial enrollment, which is expected to bring good news to 3 million idiopathic pulmonary fibrosis patients worldwide."

New P2 trial • Idiopathic Pulmonary Fibrosis

Deficiency of endothelial FGFR1 signaling via upregulation of ROCK2 activity aggravated ALI/ARDS. (PubMed, Front Immunol) - "These data demonstrated that the loss of endothelial FGFR1 signaling mediated an increase in ROCK2 activity, which led to an inflammatory response and vascular leakage in vivo and in vitro. Moreover, inhibition of ROCK2 activity by TDI01 provided great value and shed light on clinical translation."

Journal • Acute Lung Injury • Acute Respiratory Distress Syndrome • Inflammation • Pulmonary Disease • Respiratory Diseases • FGFR1 • TNFA

TDI01, a selective ROCK2 inhibitor, alleviates inflammation and vascular permeability in mouse model of ALI/ARDS. (APSR 2022) - No abstract available

Preclinical • Immunology • Inflammation