deulorlatinib (TGRX-326) / Shenzhen TargetRx, Simcere - LARVOL DELTA

TGRX-326-1004: TGRX-326 Pharmacokinetic Mass Balance (clinicaltrials.gov) - P1 | N=6 | Completed | Sponsor: Shenzhen TargetRx, Inc. | Not yet recruiting ➔ Completed

Trial completion • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Safety, efficacy and biomarker analysis of deulorlatinib (TGRX-326) in ALK-positive non-small-cell lung cancer: a multicentre, open-label, phase 1/1b trial. (PubMed, J Thorac Oncol) - P1 | "Deulorlatinib showed desirable tolerability and efficacy in ALK-positive NSCLC, demonstrating the potential to become a new treatment option in this population."

Biomarker • Journal • P1 data • Dyslipidemia • Hypertriglyceridemia • Lung Cancer • Metabolic Disorders • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK

TGRX-326 Phase I Oral Pharmacokinetic Study (clinicaltrials.gov) - P1 | N=72 | Not yet recruiting | Sponsor: Shenzhen TargetRx, Inc.

New P1 trial • Chronic Myeloid Leukemia • Hematological Malignancies • Leukemia • Oncology

Deulorlatinib (TGRX-326)in Patients with ALK Fusion-Positive NSCLC: Update from the Phase 1 Trial (IASLC-WCLC 2024) - P1, P2, P3 | "Cohort-expansion stage enrolled ALK-positive patients with disease progression after crizotinib with or without chemotherapy (EXP-A1), ALK-positive patients with disease progression after at least one second-generation ALK inhibitors (EXP-A2) and TKI-naïve ALK-positive patients (EXP-C). Based on these findings, 2 pivotal studies (NCT05955391/NCT06082635) are currently ongoing. Efficacy of deulorlatinib Cohort A1 n=14 Cohort A2 n=97 Cohort C n=33 ORR, % (95% CI) 71.4 (41.9-91.6) 39.2 (29.4-49.6) 87.9 (71.8-96.6) DCR, % (95% CI) 100 (79.8-100) 82.5 (73.4-89.5) 97.0 (84.2-99.9) Median DOR, months (95% CI) NA (11.8-NA) 18.0 (15.1-NA) NA (NA-NA) 12-month DOR estimate, % (95% CI) 90.0 (73.2-100) 73.3 (60.4-89.0) 88.9 (77.8-100) Median PFS, months (95% CI) NA (9.7-NA) 9.0 (5.7-16.8) NA (NA-NA) 12-month PFS estimate, % (95% CI) 74.1 (51.3-99.5) 47.5 (38.1-59.1) 78.5 (65.5-94.0) Median OS, months (95% CI) NA (NA-NA) NA (22.4-NA) NA (NA-NA) 12-month OS estimate, %..."

Clinical • P1 data • Dyslipidemia • Hypertriglyceridemia • Lung Cancer • Metabolic Disorders • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK

Simcere Zaiming collaborates with TargetRx to introduce a third-generation ALK inhibitor (PRNewswire) - "On September 02, 2024, Simcere Zaiming...announced a collaboration agreement with Shenzhen TargetRx Inc. The partnership focuses on the ALK/ROS1 dual receptor tyrosine kinase inhibitor TGRX-326, a clinical-stage anti-tumor candidate. According to the terms of the agreement, Simcere Zaiming will acquire exclusive commercial rights to TGRX-326 in Mainland China. These rights encompass but are not limited to marketing promotion, strategy formulation and adjustment, and the right to obtain relevant benefits from TGRX-326. TargetRx will receive an initial payment exceeding $20 million. Additionally, TargetRx will compensate Simcere Zaiming for promotional services....This inhibitor holds significant therapeutic potential for ALK/ROS1 fusion gene-positive non-small cell lung cancer (NSCLC) patients, especially those with multiple ALK-resistant mutations, including G1202R."

Licensing / partnership • Non Small Cell Lung Cancer

TGRX-326 Pharmacokinetic Drug Interaction (clinicaltrials.gov) - P1 | N=34 | Completed | Sponsor: Shenzhen TargetRx, Inc. | Recruiting ➔ Completed

Trial completion • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TGRX-326 Pharmacokinetic Mass Balance (clinicaltrials.gov) - P1 | N=6 | Not yet recruiting | Sponsor: Shenzhen TargetRx, Inc.

New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TGRX-326 Chinese Phase I for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov) - P1 | N=198 | Active, not recruiting | Sponsor: Shenzhen TargetRx, Inc. | Recruiting ➔ Active, not recruiting | N=100 ➔ 198 | Trial completion date: Jun 2024 ➔ Oct 2025 | Trial primary completion date: Dec 2023 ➔ Aug 2025

Enrollment change • Enrollment closed • Metastases • Monotherapy • Trial completion date • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK

TGRX-326 Food Effect Pharmacokinetic Study (clinicaltrials.gov) - P1 | N=24 | Completed | Sponsor: Shenzhen TargetRx, Inc.

New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TGRX-326 Pharmacokinetic Drug Interaction (clinicaltrials.gov) - P1 | N=32 | Recruiting | Sponsor: Shenzhen TargetRx, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TGRX-326 Drug-Drug Interaction Pharmacokinetic Study (clinicaltrials.gov) - P1 | N=32 | Not yet recruiting | Sponsor: Shenzhen TargetRx, Inc.

New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TGRX-326 Chinese Phase III for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov) - P3 | N=297 | Recruiting | Sponsor: Shenzhen TargetRx, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Metastases • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TGRX-326 Chinese Phase III for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov) - P3 | N=297 | Not yet recruiting | Sponsor: Shenzhen TargetRx, Inc.

Metastases • New P3 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

TGRX-326 Chinese Phase II for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov) - P2 | N=157 | Recruiting | Sponsor: Shenzhen TargetRx, Inc.

New P2 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

First-in-human, multicenter phase Ⅰ study of TGRX-326 in patients with advanced ALK-positive non-small cell lung cancer. (ASCO 2023) - P1 | "Background: TGRX-326, a deuterated derivative of lorlatinib (LOR), is a potent 3rd generation ALK and ROS1 dual TKI with high potency against multiple ALK-resistant mutations...In D-ESCAL and D-EXP, ALK+ pts prior failed on 2nd gen ALK-TKIs or ROS1+ pts resistant to crizotinib (CRZ) were enrolled; in C-EXP, ALK+ pts progression after CRZ (C-EXP-A1),progression after ≥1 2nd gen TKIs (C-EXP A2), ROS1+progression after CRZ (C-EXP-B) and pts with ALK TKI naïve (C-EXP-C) were enrolled... TGRX-326 was well tolerated in pts with advanced ALK+NSCLC and showed promising clinical antitumor activity irrespectively of ALK+ resistance to CRZ and 2nd gen TKIs, especially among those with brain metastases. Impressive activity was seen in ALK TKI naïve NSCLC. TGRX-326 demonstrated antitumor activity against multiple ALK mutations including G1202R."

Clinical • Metastases • P1 data • Dyslipidemia • Hypertriglyceridemia • Lung Cancer • Metabolic Disorders • Non Small Cell Lung Cancer • Oncology • Pain • Solid Tumor • ALK • ROS1

TGRX-326 Chinese Phase I for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov) - P1 | N=100 | Recruiting | Sponsor: Shenzhen TargetRx, Inc. | Trial completion date: Mar 2023 ➔ Jun 2024 | Trial primary completion date: Dec 2022 ➔ Dec 2023

Metastases • Monotherapy • Trial completion date • Trial primary completion date • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK

TGRX-326 Chinese Phase I for Advanced Non-small Cell Lung Cancer (NSCLC) (clinicaltrials.gov) - P1 | N=100 | Recruiting | Sponsor: Shenzhen TargetRx, Inc.

Monotherapy • New P1 trial • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK