efdelikofusp alfa (GI-101) / GI Innovation, Simcere - LARVOL DELTA

GI Innovation's Urothelial Carcinoma Treatment 'GI-101A' Designated for US FDA Fast Track [Google translation] (BioTimes) - "In a Phase 1 combination therapy clinical trial involving four patients with advanced or metastatic urothelial carcinoma who had previously received immunotherapy, early clinical results showed an objective response rate (ORR) of 50% and a disease control rate (DCR) of 75%. These results were presented orally at the 2026 American Society of Clinical Oncology (ASCO)."

Fast track • Urothelial Cancer

KEYNOTE-B59: An open-label, multicenter, phase 1/2 study of efdelikofusp alfa (GI-101A; CD80-IgG4 Fc-IL2v2) in advanced solid tumors (part E & F of GII-101-P101). (ASCO 2026) - P1/2 | "Funded by GI Innovation, Inc., Korea Drug Development Fund Clinical Trial Registration Number: NCT04977453 Background: Efdelikofusp alfa is a novel immunocytokine consisting of CD80 fused to an engineered IL-2 variant (IL-2v2) optimized to reduce IL-2Rα affinity. Efdelikofusp alfa was well tolerated as a monotherapy and in combination with pembrolizumab. Antitumor activity was observed with a favorable benefit–risk profile, supporting continued development in selected tumors, including ccRCC."

Clinical • Metastases • P1/2 data • Bladder Cancer • Cervical Cancer • Clear Cell Renal Cell Carcinoma • Genito-urinary Cancer • Hypertension • Lung Cancer • Lung Non-Small Cell Squamous Cancer • Mesothelioma • Non Small Cell Lung Cancer • Non-melanoma Skin Cancer • Oncology • Pancreatic Adenocarcinoma • Pancreatic Cancer • Solid Tumor • Squamous Cell Carcinoma • Squamous Cell Skin Cancer • Urothelial Cancer • CD8 • CD80 • IL2

GI Innovation will give an oral presentation on GI-101A (efdelikofusp alfa) as monotherapy and in combination with pembrolizumab. (Korea Biomedical Review) - "In the phase 1/2 study, GI-101A monotherapy induced a complete response in a patient with immunotherapy-refractory bladder cancer and a partial response in a malignant mesothelioma patient. In the pembrolizumab combination arm, antitumor activity was observed across multiple cancer types, including renal cell carcinoma, urothelial cancer, squamous non-small cell lung cancer, pancreatic cancer and cervical cancer."

P1/2 data • Bladder Cancer • Cervical Cancer • Lung Non-Small Cell Squamous Cancer • Mesothelioma • Pancreatic Cancer • Renal Cell Carcinoma • Urothelial Cancer

KEYNOTE-B59: GI-101/GI-101A as a Single Agent or in Combination With Pembrolizumab or Lenvatinib in Advanced Solid Tumors (clinicaltrials.gov) - P1/2 | N=317 | Recruiting | Sponsor: GI Innovation, Inc. | Trial completion date: Dec 2026 ➔ Jun 2028 | Trial primary completion date: Oct 2026 ➔ Jun 2028

Trial completion date • Trial primary completion date • Cervical Cancer • Clear Cell Renal Cell Carcinoma • Genito-urinary Cancer • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • Urothelial Cancer

At the Advancing Oncology Innovation Workshop held on March 2 at SKV1 Tower in Seongnam, Gyeonggi Province, Yun Nari, Executive Vice President of GI Innovation, underlined the value of the company's pipeline by disclosing partial clinical data on GI-101A in combination with Keytruda... (BioNews) - "The clinical findings presented by Yun, including data on the combination therapy of GI-101A and Keytruda...drew particular attention at the event. One notable case involved a patient with advanced gastric neuroendocrine carcinoma who failed to respond to prior third-line chemotherapy. Following administration of the GI-101A + Keytruda combination therapy, the patient exhibited a marked reduction of hepatic metastases by approximately 50%. Overall tumor size decreased by 50.3% and progression-free survival (PFS) exceeded 5.3 months."

P1/2 data • Bladder Cancer • Colorectal Cancer • Esophageal Squamous Cell Carcinoma • Merkel Cell Carcinoma • Non Small Cell Lung Cancer • Renal Cell Carcinoma • Sarcoma • Squamous Cell Carcinoma of Head and Neck • Vaginal Cancer • Vulvar Cancer

Novel immunocytokine CD80/IL2v synergizes with α-PD-1 for treatment of preclinical murine glioblastoma models (SNO 2025) - "GI-101 and GI-102 are novel CD80/IL-2v immunocytokines designed to selectively activate immune cells by targeting IL-2Rβγ while minimizing IL-2Rα binding. Furthermore, through immune depletion strategies, we determined that both CD4+ T cells and CD8+ T cells were the critical immune cell type required for these therapeutic effects. These findings imply that anti-PD-1 checkpoint blockade supplemented with fusion protein that includes CD80, and engineered IL-2 cytokine could be effective in treating human GBM."

Preclinical • Brain Cancer • Glioblastoma • Glioma • Solid Tumor • CD4 • CD8 • CD80 • IL2 • TRB

Novel immunocytokine CD80/IL2v synergizes with α-PD-1 for treatment of preclinical murine glioblastoma models (WFNOS 2025) - "GI-101 and GI-102 are novel CD80/IL-2v immunocytokines designed to selectively activate immune cells by targeting IL-2Rβγ while minimizing IL-2Rα binding. Furthermore, through immune depletion strategies, we determined that both CD4+ T cells and CD8+ T cells were the critical immune cell type required for these therapeutic effects. These findings imply that anti-PD-1 checkpoint blockade supplemented with fusion protein that includes CD80, and engineered IL-2 cytokine could be effective in treating human GBM."

Preclinical • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • Oncology • Solid Tumor • CD4 • CD8 • CD80 • IL2 • TRB

GI Innovation announced on the 9th that the formulation patent for its immuno-oncology drug ’GI-101A’ has been registered in Europe. [Google translation] (BioTimes)

Patent • Oncology

GI Innovation "Participating in US JPM to Promote Technology Transfers including GI-102" [Google translation] (Hankyung) - "GI Innovation will be participating in the JP Morgan Healthcare Conference held in San Francisco, USA from the 13th to the 16th (local time)....At this event, GI Innovation will discuss the transfer of blood cancer technology through the combination of T cell-based treatment with the company's main pipeline 'GI-101A/GI-102', and solid cancer technology transfer following the acquisition of clinical results for the subcutaneous injection (SC) formulation."

Commercial • Hematological Malignancies • Solid Tumor

GI Innovation decides to increase capital by allocating 80 billion won to shareholders [Google translation] (Hankyung) - "GI Innovation is conducting a paid-in capital increase with shareholder allocation of 80 billion won...The new share allocation base date is February 12, 2025, the listing date is April 10, 2025, and Korea Investment & Securities will be the lead manager for the paid-in capital increase....The company plans to use the raised funds for Korean/US phase 1/2 clinical trials of immunotherapy drugs GI-101A and GI-102, clinical trials of metabolism-modulating anticancer drug GI-108, R&D of new pipelines such as GI-305, GI-213, and GI-128 other operating funds, etc."

Financing • Solid Tumor

GI-101A, a novel CD80-IgG4-IL2v2 fusion protein, promotes CAR-T expansion and enhances anticancer potential by increasing memory T cell population in a lymphoma model (SITC 2024) - "These findings suggest that GI-101A can potentiate the antitumor efficacy of CAR-T cell therapy, offering a promising strategy to improve clinical outcomes for patients with lymphoid malignancies. Furthermore, GI-101A showed potential as a maintenance therapy following CAR-T treatment."

Clinical • Hematological Malignancies • Lymphoma • Oncology • CD4 • CD8 • CD80 • IL2

[SITC 2024] GI Innovation, 2 research results including 'GI-108' solid cancer clinical design, "announced at SITC" [Google translation] (eDaily) - "GI Innovation will disclose the mechanism of action and clinical design of GI-108, which is scheduled to proceed with phase 1/2a clinical trials for solid tumors, at the Society for Immuno-Oncology Conference (SITC 2024)...The clinical trial targets patients with advanced or metastatic solid cancer. The main clinical objectives are to evaluate the safety, tolerability, pharmacodynamics, and antitumor effects of GI-108 monotherapy....In addition, GI Innovation plans to present the preclinical study results of GI-101A in a lymphoma model as a poster."

Clinical protocol • Preclinical • Hematological Malignancies • Lymphoma • Oncology • Solid Tumor

GI Innovation, which increased capital by 20 bi llion won, is likely to raise additional funds [Google translation] (Pharm E Daily) - "Nevertheless there is an analysis, that is important to keep an eye on it, as operating expenses are expected to decrease in the future and there is a possibility that technology transfer will be successful in the second half of the year...The company is currently pursuing a global technology transfer for 'GI-101A' and 'GI-102', which are currently under development as immune-oncology drugs....The company plan to submit a domestic phase 1 clinical trial plan (IND) for the 4th generation immunotherapy drug 'GI-108' this month."

Licensing / partnership • New P1 trial • Oncology • Solid Tumor

GI Innovation decides to issue 20 billion won worth of CB and CPS… First fundraising after listing [Google translation] (HIT News) - "GI Innovation announced on the 30th that it had decided to raise a total of KRW 20 billion through KRW 10 billion in convertible stocks (CPS) and KRW 10 billion in convertible bonds (CB). This is the first capital infusion since its listing in March 2023....The company plans to use the funds for the subcutaneous injection (SC) monoclinical clinical trials of the immunotherapy anticancer drugs 'GI-101A' and 'GI-102' and combination clinical trials with Enhertu and Keytruda, the metabolic anticancer drug 'GI-108'..."

Financing • Oncology • Sarcoma • Solid Tumor

'Cancer vaccine + immunotherapy' combined clinical trial begins… 'Maximizing synergy' (Daily Pharm) - "The three companies will begin phase 2 clinical trials of a combination therapy of GI-101A and the DNA vaccine treatment 'PG-101' targeting prostate cancer patients...and has obtained investigator-led clinical approval from the Korean Cancer Study Group (KCSG)."

New trial • Prostate Cancer

GI Innovation, Registers Material Patent for Immune Anticancer Drugs 'GI-101A·GI-102' in China [Google translation] (HIT News) - "Innovative new drug development company GI Innovation...announced on the 3rd that the material patent for the immune anticancer drug 'GI-101A·GI-102' has been registered in China...Following the US, Europe, and Japan, the company has successfully registered a material patent for GI-101A/GI-102 in China, securing exclusive rights in major countries in the global biopharmaceutical market....'Since patent registration is proceeding smoothly in other countries where we have applied, such as Russia and Australia, we expect successful registration in other countries where the patent is currently in the review stage. This will be advantageous in future licensing agreement negotiations.'" "

Patent • Oncology • Solid Tumor

GI Innovation, GI-101 and Keytruda combination clinical trial demonstrates partial remission [Google translation] (Global Economics) - P1/2 | N=430 | KEYNOTE-B59 (NCT04977453) | Sponsor: GI Innovation, Inc. | "PR results confirmed in pancreatic cancer, kidney cancer, and bladder cancer....GI Innovation announced on the 15th that it confirmed three partial remissions (PR) in the dose escalation phase of the phase 1/2 clinical trial of the combination of the immunotherapy anticancer drug GI-101A and Keytruda....Compared to other cancers, pancreatic cancer has few early symptoms or is difficult to detect early, so the 5-year survival rate is less than about 10%. Even if approved chemotherapy is administered, the survival period is less than a year....'We are putting all our efforts into technology transfer and plan to directly receive FDA approval for specific cancer types.'"

P1/2 data • Bladder Cancer • Kidney Cancer • Pancreatic Cancer

[KOSDAQ CEO Interview] GI Innovation President Jang Myeong-ho: "Immuno-oncology drug, following US FDA, completes Chinese material patent… technology transfer possible within the year" [Google translation] (Nate) - "President Jang expressed confidence in the technology transfer within the year...'We are discussing technology transfer for GI-101 and GI-102 with four of the top 10 global pharmaceutical companies.'....'We are also discussing with several domestic and foreign pharmaceutical companies about the new drug candidate GI-108, which is in the preclinical stage.'"

Licensing / partnership • Preclinical • Oncology • Solid Tumor

The promising feeder-free allogenic NK cell therapy: Clinical outcomes of GIC-102 monotherapy (GIC-102101) and synergistic potential with GI-101 (CD80-IgG4 Fc-IL2v) in advanced solid tumors and hematologic malignancies. (ASCO 2024) - P1, P1/2 | "A lympho-conditioning strategy using cyclophosphamide (300 mg/m2) and fludarabine (30 mg/m2) was implemented every two cycles before GIC-102 treatment. The GIC-102, feeder-free allogeneic NK cell, was well tolerated without DLTs and demonstrated early promise in efficacy in patients for advanced solid tumors and hematologic malignancy. Further clinical investigation of GIC-102 in combination with GI-101, bi-specific Fc fusion protein, is currently ongoing. Clinical trial information: NCT05880043."

Clinical • Clinical data • Metastases • Monotherapy • Anemia • Cardiovascular • Colorectal Cancer • Gastrointestinal Cancer • Heart Failure • Hematological Disorders • Hematological Malignancies • Lymphoma • Neutropenia • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor • CD80

GI Innovation announces clinical results of single-use 'GI-102' at 'ASCO' [Google translation] (Yakup Shinmoon) - P1 | N=9 | NCT05880043 | Sponsor: GI Cell, Inc. | "GI Cell also announced clinical results of ‘GIC-102’...According to the abstract, the best response overall was a complete response (CR) in 1/6 patients (NHL) and stable disease (SD) in 4/6 patients (3 CRC, 1 NHL), with CR (NHL) and SD (CRC). Treatment is ongoing (215+ days for NHL/160+ days and 153+ days for CRC)....In vivo studies combining GIC-102 and GI-101 demonstrated antitumor activity lasting up to 4 weeks and enhanced NK cell proliferation in vivo."

P1 data • Preclinical • Colorectal Cancer • Gastrointestinal Cancer • Hematological Malignancies • Lymphoma • Non-Hodgkin’s Lymphoma • Oncology • Solid Tumor

GI Innovation registers European substance patent for immunotherapy drugs ‘GI-101A·102’ [Google translation] (HIT News) - P1/2a | N=92 | NCT05824975 | Sponsor: GI Innovation, Inc. | "GI Innovation...announced on the 14th that material patents for immune anti-cancer drugs GI-101A and GI-102 (development code names) have been registered in Europe...the company explains that European patent registration for GI-101A and GI-102 means strong protection for all commercialization areas of the materials, and will greatly improve the technology's attractiveness in the global market....Meanwhile, clinical trials for both GI-101A (phase 1/2 clinical trial) and GI-102 (phase 1/2a clinical trial) are progressing smoothly. In particular, in the case of GI-102, partial responses (PRs) have been confirmed in five patients without serious toxicity so far in monotherapy dose-escalation clinical trials."

P1/2 data • Patent • Trial status • Oncology • Solid Tumor

GI Cell, GI Innovation to collaborate on cancer treatment development (Korea Biomedical Review) - "GI Cell, an affiliate of GI Innovation, has submitted an application to the Ministry of Food and Drug Safety for phase 1/2a clinical trials to evaluate the safety and efficacy of a combination therapy between GI Cell's allogeneic NK cell therapy, T.O.P. NK and GI-101A, in patients with recurrent and refractory solid tumors...,The companies plan to extend their collaboration to include clinical trials for a combination therapy involving T.O.P. NK and another drug, GI-102, in the future."

Licensing / partnership • New P1/2 trial • Oncology • Solid Tumor

GI Innovation decides to register U.S. patent for GI-101·GI-102 blockbuster anticancer drug combination [Google translation] (Hankyung) - "GI Innovation announced on the 15th that a U.S. patent has been registered for combination therapy with immunotherapy drugs GI-101 and GI-102 and various anticancer treatments...In particular, this patent registered a wide range of global blockbuster anticancer drugs such as PARP inhibitors, CDK4/6 inhibitors, and VEGFR inhibitors. It is now possible to enjoy exclusive rights to combination therapy with various anticancer drugs....The patent duration for GI-101, GI-102 and combination therapy with these anticancer drugs has been secured until 2041."

Patent • Oncology • Solid Tumor

Keynote-B59: dose escalation of a phase 1/2 first-in-human, open-label study of GI-101, a novel immunocytokine combining CD80-IL2v, in combination with pembrolizumab in advanced solid tumors (SITC 2023) - P1/2 | "GI-101 plus pembrolizumab demonstrated anti-tumor activity in a heavily pre-treated patient population, with prior anti-PD(L)1 therapies. The dose expansion phase of the study is currently ongoing."

Clinical • Combination therapy • Metastases • P1/2 data • Clear Cell Renal Cell Carcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • CD8 • CD80

Population pharmacokinetic-pharmacodynamic modeling to inform optimal dosing strategies for GI-101, a novel fusion protein, targeting IL2βγR and CTLA4 (ESMO 2023) - P1/2 | "Conclusions Our findings underscore the value of translational mathematical modeling for informing optimal dosing strategies in novel immunotherapies targeting IL2βγR and CTLA4. The identified OBD merits further investigation in clinical trials to validate its potential for enhancing patient outcomes."

Clinical • PK/PD data • Oncology • CD8