ASCO first look | Data is dazzling: bispecific antibody AK112, the first new drug targeting IL1-RAP to enter advanced NSCLC

annual global oncology event—— The annual meeting of the American Society of Clinical Oncology (ASCO) will be held from June 3 to June 7, 2022 local time. Following the success of PD-L1 antibody, bispecific antibodies have made a breakthrough in various tumor types in recent years. At this year’s ASCO conference, a number of targeted therapies and bispecific antibody therapies for new targets were introduced. The results of clinical studies of novel therapeutic strategies are striking. Among them, two results in the poster discussion session showed that the ORR of the bispecific antibody AK112 and the first-in-class drug targeting IL1-RAP in advanced NSCLC was as high as 76.9% and 53%, respectively. The first study came from the team of Professor Zhao Yuanyuan from Sun Yat-Sen University Cancer Center. Before the ASCO Conference kicks off, let’s get a sneak peek!

PD-1/VEGF bispecific antibody AK112 had the highest ORR in patients with no driver gene or progression on immunotherapy and platinum-based chemotherapy Up to 76.9%[1] strong>

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background:

PD-L1+VEGF antibody showed efficacy in advanced non-squamous NSCLC. Based on the IMPOWER150 study, atezolizumab + bevacizumab + platinum-based chemotherapy has become the first-line treatment for driver-negative advanced non-squamous NSCLC. AK112 is a first-in-class bispecific antibody targeting PD-1/VEGF. Preclinical studies have shown that AK112 has potential antitumor activity in solid tumors. Therefore, the team of Professor Yuanyuan Zhao from Sun Yat-Sen University Cancer Center conducted a phase II study to explore the efficacy and safety of AK112 combined with chemotherapy in patients with advanced NSCLC.

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Method:

< span>This is an open-label, multicenter Phase II study to evaluate the efficacy and safety of AK112 combined with chemotherapy in patients with advanced NSCLC. The enrolled patients were divided into three cohorts: EGFR/ALK wild-type naïve advanced NSCLC patients (cohort 1), EGFR-mutant patients without T790M mutation or osimertinib treatment failure (cohort 2), PD -1/L1 and patients after progression on platinum-based chemotherapy (cohort 3). Enrolled patients received AK112 (10 mg/kg or 20 mg/kg every 3 weeks) in combination with carboplatin and pemetrexed or carboplatin and paclitaxel (cohort 1 and cohort 2), with docetaxel for cohort 3. The primary endpoint was investigator-assessed objective response rate (ORR).

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Results :

From February 3, 2021 to December 31, 2021, a total of 133 patients were enrolled and received AK112 combined with chemotherapy, with 44 and 89 patients, respectively Received 10 mg/kg AK112 and 20 mg/kg AK112 treatment. As of December 31, 2021, among 26 evaluable squamous cell carcinoma patients in cohort 1, 20 had partial response (PR), 6 had stable disease (SD), ORR was 76.9%, disease control rate (DCR) was 100.0%, median duration of response (DOR) and median progression-free (PFS) were not reached, and the 6-month PFS rate was 86.2%. In Cohort 2, of 19 evaluable patients, 13 achieved PR partial response and 5 achieved SD, ORR was 68.4%, DCR was 94.7%, median DOR was 5.5 months, and median PFS was 8.3 moon. In cohort 3, there were 20 evaluable patients, 8 achieved PR and 8 were SD, ORR was 40.0%, DCR was 80.0%, median DOR and median PFS were not reached, and 6-month PFS rate was 71.1 %. The incidence of treatment-emergent adverse events (TEAEs) was 86.5% (115/133), and the incidence of grade 3 and above adverse events (AEs) was 28.6% (38/133). The most common AEs (incidence ≥5%) included increased aspartate aminotransferase, epistaxis, anemia, vomiting, nausea, rash, leukopenia, thrombocytopenia, and neutropenia. 3.0% (4/133) of patients discontinued treatment due to AEs.

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Conclusion :

AK112 combined with chemotherapy showed promising antitumor efficacy in all cohorts, compared with PD-(L)1 antibody combined with VEGFR antibody in advanced NSCLC, AK112 combined with chemotherapy has a potentially superior safety profile, and AK112 combined therapy also significantly improved PFS and ORR. Based on this, a phase III registration study of AK112 combined with chemotherapy in the treatment of advanced NSCLC will start in 2022. Clinical trial information: NCT04736823.

Nadunolimab, a first-in-class drug targeting IL1-RAP, is used for unresectable or locally advanced or advanced NSCLC, with ORR of 53% [2]

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Background:

Background: Interleukin 1 Receptor Accessory Protein (IL1RAP) Expressed in various solid tumor cells and stromal cells. The interleukin-1 (IL-1) signaling pathway is active in tumor cells and is upregulated in response to chemotherapy. IL1RAP interacts with IL-1 receptor 1 (IL-1R1) and regulates downstream factors (eg, IL-6, IL-8) and C-reactive protein (CRP) levels. Nadunolimab (CAN04) is a fully humanized antibody-dependent cell-mediated cytotoxicity (ADCC)-enhanced IgG1 antibody that targets IL1-RAP and blocks IL-1α and IL-1β signaling. At this ASCO meeting, the researchers announced the results of a phase I/IIa CANFOUR trial designed to evaluate the efficacy of nadunolimab combined with CG in NSCLC.

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Method: span>

Patients with unresectable, locally advanced or metastatic NSCLC who have progressed on pembrolizumab or on first-line therapy are eligible. Enrolled patients received nadunolimab at 1 mg/kg (n=17), 2.5 mg/kg (n=3), or 5 mg/kg (=13) in cycle 1 (Q1W), administered every two weeks starting in cycle 2 Once (Q2W), in combination with standard therapy CG. Due to the risk of infusion-related reactions, an initial dose of nadunolimab (0.5 mg/kg) was given one week before CG. The primary endpoint was safety, secondary endpoints included ORR, PFS, and OS, and exploratory endpoints included effects on serum and tumor tissue biomarkers.

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results: span>

A total of 33 patients were included, the median age was 64 years (39-77 years), 30% were female, 42% had an ECOG score of 0, and the proportion of patients with non-squamous histology 55%, 82% of stage IV patients, and 45% of patients who had previously received pembrolizumab monotherapy. Grade 3 or higher adverse events occurred in 73%, including neutropenia (58%), febrile neutropenia (9%), thrombocytopenia (30%), and anemia (18%) . Neutropenia can be controlled with G-CSF. Thirty patients received the combination therapy and were included in the efficacy analysis. Three patients did not receive chemotherapy due to clinical deterioration (n=2) or withdrawal of consent (n=1). ORR was 53% (95% CI 34-72%), DCR was 80% (61-92%), median DOR was 5.5 months (3.7-7.0), and 23% of patients were still on treatment at data cutoff. The ORR for patients with squamous and non-squamous histology was 46% and 56%, respectively. Median PFS was 6.7 months (5.5-7.3) and median OS was 13.7 months. The neutrophil-to-lymphocyte ratio decreased throughout the experiment due to a decrease in the number of circulating neutrophils. IL1RAP expression by tumor cells and stromal cells was confirmed in tumor biopsies.

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Conclusion: span>

Nadunolimab combined with CG showed controllable safety and promising efficacy in NSCLC patients with ORR of 53%. Several studies are currently evaluating nadunolimab in combination with chemotherapy or IO. Clinical trial data: NCT03267316.

References

1.A phase II study of AK112 (PD-1/VEGF bispecific) in combination with chemotherapy in patients with advanced non-small cell lung cancer.Poster Discussion Session. Abstract9019

2.Phase1/2 a trial of nadunolimab, afirst-in-class fully humanized monoclonal antibody against IL1 RAP , in combination with cisplatin and gemcitabine (CG) in patients with non-small cell lung cancer(NSCLC). PosterDiscussionSession. Abstract9020

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