GQ1005 / GeneQuantum Healthcare, Fosun Pharma, Shanghai Henlius Biotech - LARVOL DELTA

Preliminary results of GQ1005 in metastatic HER2-low expressing breast cancer and HER2 positive gastric cancer (ESMO 2024) - P1 | "Background: GQ1005 is an innovative anti-HER2 antibody-drug conjugate (ADC) processed through a novel, integrated and stable enzyme conjugation links DXd to engineered trastuzumab, the drug-to-antibody ratio is 4. In the FIH phase 1a/1b study, patients(pts) of HER2 expressing/mutated metastatic solid tumors progressed from the standard of care were included. GQ1005 demonstrates excellent safety profile and encouraging antitumor activity in HER2 expressing tumors, including heavily treated HER2 low BC and HER2 positive GC. Given the wider therapeutic window and the safer profile of GQ1005, a superior survival benefit could be expected from the patients treated with GQ1005. (Sponsored by GeneQuantum Healthcare (Suzhou) Co., Ltd.)."

Metastases • Breast Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Oncology • Solid Tumor • HER-2

Preliminary Results from a FIH Study of GQ1005, A Novel HER2-ADC, in Patients with Advanced HER2-Expressing Solid Tumors and HER2-Mutated NSCLC (IASLC-WCLC 2024) - P1 | "Preclinical studies have shown that GQ1005 exhibits similar antitumor efficacy to Enhertu and better stability than Enhertu, with a notable absence of toxicity, suggesting a superior therapeutic profile. The phase Ib trial in four cohorts with a dose of 7.2 mg/kg is ongoing. (NCT06154343)"

Clinical • Metastases • Anemia • Dry Eye Disease • Fatigue • Hematological Disorders • Interstitial Lung Disease • Leukopenia • Lung Cancer • Neutropenia • Non Small Cell Lung Cancer • Oncology • Ophthalmology • Pulmonary Disease • Renal Disease • Respiratory Diseases • Solid Tumor • Thrombocytopenia • HER-2

A Trial Comparing GQ1005 and T-DM1 in Patients With HER2-Positive Unresectable or Metastatic Breast Cancer (clinicaltrials.gov) - P3 | N=228 | Recruiting | Sponsor: GeneQuantum Healthcare (Suzhou) Co., Ltd.

New P3 trial • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

…HLX22 (anti-HER2 monoclonal antibody) entered phase II clinical trials for the first-line treatment of HER2-positive recurrent or metastatic breast cancer in combination with HLX87 (The Manila Times)

Trial status • HER2 Positive Breast Cancer

Phase I study of GQ1005, a new generation HER2-ADC, in patients with HER2-expressing and HER2 mutated advanced solid tumors (AACR 2024) - P1 | "In preclinical studies, GQ1005 demonstrated comparable antitumor activity compared to Enhertu in multiple tumor cell line xenograft models with no noticeable toxicity, indicating higher therapeutic index. GQ1005 demonstrated a promising antitumor activity in HER2-expressing/mutated advanced solid tumors patients previously heavily treated, and showed a good tolerance and manageable safety profile. The dose expansion study is on-going at 7.2 mg/kg to establish the RP2D in four cohorts."

ADC • Clinical • Metastases • P1 data • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Lung Cancer • Oncology • Solid Tumor • HER-2

A Study to Evaluate HLX22 in Combination With HLX87 in Patients With HER2-Positive Recurrent or Metastatic Breast Cancer (clinicaltrials.gov) - P2/3 | N=706 | Recruiting | Sponsor: Shanghai Henlius Biotech | Not yet recruiting ➔ Recruiting

Enrollment open • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • ER • HER-2 • PGR

…The first patient has been dosed in a phase 2/3 clinical study of HLX22 (recombinant humanised anti-HER2 monoclonal antibody injection) ('HLX22') in combination with HLX87 for injection (antibody-drug conjugate targeting HER2) ('HLX87') for first-line treatment of patients with HER2-positive recurrent or metastatic breast cancer (BC) in Chinese Mainland… (HKEXnews) - "This study is an open-label, randomised, multicenter phase 2/3 clinical study to evaluate HLX22 in combination with HLX87 for the first-line treatment of patients with HER2-positive recurrent or metastatic breast cancer."

Trial status • HER2 Positive Breast Cancer

A Hase II/III Clinical Study to Evaluate HLX22 in Combination With HLX87 as First-Line Treatment in Patients With HER2-Positive Recurrent or Metastatic Breast Cancer (clinicaltrials.gov) - P2/3 | N=706 | Not yet recruiting | Sponsor: Shanghai Henlius Biotech

New P2/3 trial • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor

A Phase II/III Clinical Study to Evaluate the Efficacy and Safety of HLX87in Combination With HLX22 or Pertuzumab in the Neoadjuvant Therapy of HER2-Positive Bresat Cancer (clinicaltrials.gov) - P2/3 | N=817 | Not yet recruiting | Sponsor: Shanghai Henlius Biotech

New P2/3 trial • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor

Shanghai Henlius Biotech…is pleased to announce that, recently, the applications for phase 2/3 clinical trials of HLX22…in combination with HLX87 for injection…(1) for first-line treatment of HER2-positive breast cancer (BC); and (2) for neoadjuvant treatment for HER2-positive breast cancer (BC neo) have been approved by the National Medical Products Administration (NMPA), respectively (HKEXnews)

New P2/3 trial • HER2 Positive Breast Cancer

Site-specific ligase-dependent conjugation with ring-opening linker improves safety and stability of HER2-targeting ADCs. (PubMed, Nat Commun) - "GQ1001 exhibits HER2 expression-dependent activity (contrary to T-DM1), indicating decreased off-target toxicity. GQ1001 is efficacious in cancers resistant to T-DXd due to high ABCG2 expression. Together, the LDC technology and ring-opening linker improve the stability and safety in GQ1001 and GQ1005 for treating refractory HER2-positive cancers."

Journal • Oncology • ABCG2 • HER-2

Site-specific ligase-dependent conjugation with ring-opening linker improves safety and stability of HER2-targeting ADCs (Nat Commun, Nature) - "GQ1001 and GQ1005 are effective in animal models against pretreated HER2-positive cancers insensitive to HER2-targeting and/or chemotherapeutic drugs. The efficacy of GQ1001 is supra-additively enhanced by tyrosine-kinase inhibitors or chemotherapy, with manageable toxicity. GQ1001 is efficacious in cancers resistant to T-DXd due to high ABCG2 expression."

Preclinical • Breast Cancer • Gastric Cancer

Site-specific ligase-dependent conjugation with ring-opening linker improves safety and stability of HER2-targeting ADCs (Nat Commun, Nature) - "GQ1001 and GQ1005 are effective in animal models against pretreated HER2-positive cancers insensitive to HER2-targeting and/or chemotherapeutic drugs. The efficacy of GQ1001 is supra-additively enhanced by tyrosine-kinase inhibitors or chemotherapy, with manageable toxicity. GQ1001 is efficacious in cancers resistant to T-DXd due to high ABCG2 expression."

Preclinical • Breast Cancer • Gastric Cancer

Henlius Licenses Phase 3 Innovative HER2 ADC from GeneQuantum (Henlius Press Release) - "As agreed, Henlius will obtain the development and exclusive commercialization rights for the innovative HER2-targeted...ADC GQ1005 in China and certain overseas markets. The drug candidate...is being evaluated for HER2-positive breast cancer."

Licensing / partnership • HER2 Positive Breast Cancer

Efficacy and Safety of GQ1005, a Promising HER2-ADC, in Patients with Metastatic HER2-Positive Breast Cancer. (SABCS 2024) - P1 | "All participants had received chemotherapy, 93.3% had received trastuzumab, 86.7% had received HER2 TKIs (nearly all received pyrotinib), and 63.2% had received other HER2 ADCs (including TDM1, FS-1502, A-166, etc.). GQ1005 demonstrates robust anti-tumor activity and a favorable safety profile in patients with heavily pretreated HER2-positive MBC. Notably, GQ1005 exhibits significantly superior safety profiles, attributable to its higher linker stability and minimal payload shedding in circulation. These promising results warrant further investigation in randomized, controlled phase III studies."

Clinical • Metastases • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor • HER-2

Qide Pharmaceutical Technology (Suzhou) Co., Ltd.'s application for implied clinical trial approval for its drug has been accepted [Google translation] (163.com) - "On October 11, according to the official website of CDE, Qide Pharmaceutical Technology (Suzhou) Co., Ltd. jointly applied for the drug 'GQ1005 Injection' and obtained implicit clinical trial approval, acceptance number CXSL2400522....Public information shows that the drug 'GQ1005 Injection' is indicated for use in combination with carboplatin to treat patients with advanced or metastatic non-small cell lung cancer with HER2 exon 19 or 20 mutations."

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

The latest research results of GQ1005, a new generation of HER2 ADC from Genentech, are unveiled丨Member News [Google translation] (Sohu.com) - P1 | N=150 | NCT06154343 | Sponsor: GeneQuantum Healthcare (Suzhou) Co., Ltd. | "On September 10, 2024, Qide Pharmaceuticals announced the latest data of the first-in-human study (FIH) of the HER2-targeted innovative ADC drug GQ1005 in HER2-expressing or mutated advanced solid tumors in the form of an oral report at the World Lung Cancer Conference (WCLC)...As of May 10, 2024, a total of 188 patients with solid tumors were included in the analysis, including 50 patients with non-small cell lung cancer (NSCLC)...In the overall population, the objective response rate (ORR) of 154 evaluable patients was 40.9%, and the disease control rate (DCR) was 83.8%. In the NSCLC population, the ORR of 40 evaluable patients was 32.5%, and the DCR was 92.5%....The 12-month OS rates of the overall population and NSCLC population were both over 72%, at 72.6% and 73.4%, respectively."

P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • HER-2

Selected for oral presentation! The latest research results of GQ1005, a new generation HER2 ADC from Genentech, will be presented at WCLC 2024 [Google translation] (bydrug.pharmcube.com) - "Epigenetics, a leader in ADC new drug development committed to the research and development of disruptive innovative bioconjugate technology, announced that it will announce the first-in-human study (FIH) results of the HER2-targeted innovative ADC drug GQ1005 in patients with HER2-expressing advanced solid tumors and HER2-mutated advanced NSCLC in the form of an oral report at the 2024 World Lung Cancer Conference (WCLC)."

P1 data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Genentech's new generation HER2 ADC GQ1005 approved for Phase III clinical trial丨Member News [Google translation] (Sohu.com) - "On August 26, Qide Pharmaceuticals announced that its independently developed new generation HER2 ADC GQ1005 was approved by the CDE to conduct Phase III clinical studies for the treatment of HER2-positive unresectable/metastatic breast cancer."

New P3 trial • Breast Cancer • HER2 Breast Cancer • HER2 Positive Breast Cancer • Oncology • Solid Tumor

Weekly Medical Highlights (July 29 - August 4) [Google translation] (Sina Corp) - "The National Medical Products Administration released the delivery information of the third phase of drug approval certificates, including 124 acceptance numbers, involving companies such as Sanofi (China) Investment Co., Ltd. (as of August 4)....CDE accepted 52 new drug applications, including GQ1005 injection and other drugs (as of August 4)."

New trial • Breast Cancer • Gastric Cancer • Gastrointestinal Cancer • HER2 Breast Cancer • Oncology • Solid Tumor

The objective response rate of HER2 ADC anticancer drug GQ1005 is 45.5%, and gastric cancer patients can apply for enrollment [Google translation] (163.com) - P1 | N=150 | NCT06154343 | Sponsor: GeneQuantum Healthcare (Suzhou) Co., Ltd. | "At the 2024 American Association for Cancer Research (AACR)...announced the results of a Phase I clinical trial of its next-generation HER2 ADC drug GQ1005 in patients with advanced solid tumors expressing or mutated HER2...Among the 38 evaluable patients, 1 patient achieved complete remission, 18 patients had confirmed partial remission, and 11 patients had stable disease. The objective response rate (ORR) of all patients was 50% (19/38)...As of March 8, 2024, the objective response rate (ORR) was 43% and the disease control rate (DCR) was 82.5% among 114 patients who had undergone at least one tumor assessment....The CDE official website shows that a clinical trial of GQ1005 intravenous infusion in subjects with HER2-expressing advanced solid tumors is underway, and gastric cancer patients are being recruited to participate in the clinical study."

P1 data • Trial status • Gastric Cancer • Gastrointestinal Cancer • Oncology • Solid Tumor • HER-2

GQ1005, a Novel HER2 ADC With Expanded Therapeutic Window in Advanced Solid Tumours (ADC London 2024) - "Unpacking GQ1005’s Efficacy in preclinical studies • Sharing preliminary results of GQ1005 Phase1a • Laying out preliminary results of GQ1005 Phase1b"

Metastases • Oncology • Solid Tumor • HER-2

A Study of GQ1005 in Subjects With HER2-Expressing Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=150 | Recruiting | Sponsor: GeneQuantum Healthcare (Suzhou) Co., Ltd.

Metastases • New P1 trial • Oncology • Solid Tumor

GeneQuantum Healthcare’s Two Next Generation Bioconjugate Drugs, GQ1005 and GQ1007, Have Been Approved for Clinical Trials in Australia (PRNewswire) - "GeneQuantum Healthcare (Suzhou)...announced that two of the company's bioconjugate drug candidates have won the approval for clinical trials in Australia, further enhancing GeneQuantum's pipelines in the clinical stage. They are GQ1005, an ADC with an excellent bystander killing effect, and GQ1007, a first-in-class antibody-immune-agonist-conjugate (AIAC) both with global intellectual property rights."

New trial • Oncology