^
    1d
    Design and synthesis of new nicotinamides as immunomodulatory VEGFR-2 inhibitors and apoptosis inducers. (PubMed, Future Med Chem)
    Compound 16c boosted the level of the apoptotic caspase-3 and inhibited the level of TNF-α and IL-6 in tumor cells. Molecular docking and molecular dynamics (MD) simulations indicated the outstanding binding potential of compound 16c against VEGFR-2. Compound 16c is a good candidate for the creation of a novel antiangiogenic lead anticancer medication.
    Journal • Immunomodulating
    |
    IL6 (Interleukin 6) • TNFA (Tumor Necrosis Factor-Alpha) • CASP3 (Caspase 3)
    4d
    A Phase 3 Study of AK112 Plus AK117 Versus Pembrolizumab in Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma (R/M HNSCC) (clinicaltrials.gov)
    P3, N=510, Recruiting, Akeso | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Keytruda (pembrolizumab) • Yidafan (ivonescimab) • ligufalimab (AK117)
    5d
    An Exploratory, Multi-cohort Phase II Study of Combination Therapy of AK112 With Chemotherapy and/or Olaparib in Platinum-sensitive Ovarian Cancer (clinicaltrials.gov)
    P2, N=150, Not yet recruiting, Akeso
    New P2 trial
    |
    Lynparza (olaparib) • Yidafan (ivonescimab)
    6d
    A Multicenter, Single-arm, Open-label Study Evaluating the Safety and Efficacy of AK112 Combined With Chemotherapy as First-line Treatment for Non-squamous NSCLC Patients With BRAIN Metastases and Negative Driver Genes (IVO BRAIN) (clinicaltrials.gov)
    P2, N=55, Not yet recruiting, Sun Yat-sen University
    New P2 trial
    |
    Yidafan (ivonescimab)
    8d
    RE-SHINE: Clinical effectiveness of remote management in patients with diabetic macular edema receiving long-term intravitreal anti-VEGF therapywith Diabetes Macular Edem (ChiCTR2400090348)
    P=N/A, N=900, Completed, Shanghai General Hospital; Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine
    New trial
    8d
    the effect of Xuefuzhuyu Decoction on the blood flow density and FAZ of RVO-ME after receiving anti-VEGF with OCTA (ChiCTR2400089976)
    P=N/A, N=60, Recruiting, Guangdong Provincial Hospital of Chinese Medicine; Guangdong Provincial Hospital of Chinese Medicine
    New trial
    8d
    Anti-vegf factor for rhegmatogenous retinal detachment after scleral buckling repair Effect of macular epiretinal membrane formation (ChiCTR2400088902)
    P4, N=120, Completed, The Second Affiliated Hospital of Harbin Medical University; The Second Affiliated Hospital of Harbin Medical University
    New P4 trial
    8d
    DME HOME: Home- vs Hospital-based Care of Anti-VEGF Treatment for Diabetic Macular Edema: Non-inferiority RCT (ChiCTR2400090425)
    P4, N=308, Not yet recruiting, Zhongshan Ophthalmic Center, Sun Yat-sen University; Zhongshan Ophthalmic Center, Sun Yat-sen University
    New P4 trial • Head-to-Head
    8d
    A Single-Arm, Single-Center, Phase II Clinical Study of Neoadjuvant Treatment of Resectable EGFR-Sensitive Mutant Non-Small Cell Lung Cancer with Ivonescimab (Anti-PD-1 and VEGF Bispecific Antibody) Combination with Chemotherapy (ChiCTR2400089410)
    P2, N=25, Recruiting, Cancer Hospital Affiliated of Shandong First Medical University; Cancer Hospital Affiliated of Shandong First Medical University
    New P2 trial • IO biomarker
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • EGFR L858R • EGFR exon 19 deletion
    |
    Yidafan (ivonescimab)
    8d
    AK104 in combination with AK112 in an exploratory, multi-cohort stage II treatment of recurrent ovarian cancer study (ChiCTR2400090899)
    P2, N=172, Not yet recruiting, Fudan University Shanghai Cancer Center; Fudan University Shanghai Cancer Center
    New P2 trial • Combination therapy • IO biomarker
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    Kaitanni (cadonilimab) • Yidafan (ivonescimab)
    8d
    A Prospective, Multicenter Clinical Study of the Efficacy and Safety of First-Line Treatment with Ivonescimab in Combination with XELOX for Unresectable Advanced Gastric/Gastroesophageal Junction Adenocarcinoma (ChiCTR2400089954)
    P2, N=30, Not yet recruiting, Renji Hospital affiliated to Shanghai Jiaotong University School of Medicine; Renji Hospital affiliated to Shanghai Jiaotong University School of Medi
    New P2 trial • Combination therapy • Metastases
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 negative
    |
    capecitabine • oxaliplatin • Yidafan (ivonescimab)
    8d
    Ivonescimab (AK112) plus paclitaxel and carboplatin in frontline neoadjuvant therapy of advanced ovarian cancer, fallopian tube cancer, or primary peritoneal cancer: a phase II trial (ChiCTR2400090496)
    P2, N=132, Recruiting, Sun Yat-sen University Cancer Center; Sun Yat-sen University Cancer Center
    New P2 trial • Metastases
    |
    carboplatin • paclitaxel • Yidafan (ivonescimab)
    8d
    ICONIC trial: Ivonescimab (AK112) combination with radiochemotherapy in the first-line treatment of small cell lung cancer patients, a single arm, multicenter, phase Ib clinical study. (ChiCTR2400089992)
    P1, N=48, Not yet recruiting, Taizhou People's Hospital; Taizhou People's Hospital
    New P1 trial
    |
    Yidafan (ivonescimab)
    8d
    A study of the safety, efficacy, and cost-effectiveness of using non-vitrectomised subretinal anti-VEGF injections to treat neovascular age-related macular degeneration (ChiCTR2400090827)
    P1, N=80, Not yet recruiting, Department of Ophthalmology and Visual Sciences, CUHK; Department of Ophthalmology and Visual Sciences, The Chinese University of Hong Kong
    New P1 trial • HEOR • Cost effectiveness
    10d
    Multicentre, randomized trial of immunotherapy prior to surgical resection for early-stage hepatocellular carcinoma (ACTRN12624001345572)
    P2, N=208, Not yet recruiting, Western Sydney Local Health District
    New P2 trial
    |
    Avastin (bevacizumab) • Tecentriq (atezolizumab)
    11d
    Design, synthesis, and evaluation of novel thiadiazole derivatives as potent VEGFR-2 inhibitors: a comprehensive in vitro and in silico study. (PubMed, RSC Adv)
    Compound 20b presents as a promising anti-proliferative agent targeting VEGFR-2. Also, this comprehensive investigation underscores the potential of 2,3-dihydro-1,3,4-thiadiazole derivatives as promising candidates for further development in anti-cancer research.
    Preclinical • Journal
    |
    CASP8 (Caspase 8) • CASP9 (Caspase 9)
    |
    sorafenib
    12d
    Comprehensive analysis of VEGF/VEGFR inhibitor-induced immune-mediated hypertension: integrating pharmacovigilance, clinical data, and preclinical models. (PubMed, Front Immunol)
    The temporal dynamics of these effects demonstrated greater significance than dose-dependent responses. Both VEGFi and VEGFRi significantly augmented the risk of immune-mediated, blood pressure-related adverse events, with VEGFRi inducing a more rapid and pronounced onset of blood pressure elevation and a higher incidence of immune-related, blood pressure-associated adverse events compared to VEGFi.
    Clinical data • Preclinical • Journal • Adverse events
    |
    NOS3 (Nitric oxide synthase 3)
    14d
    A Phase I/II Study of IVONESCIMAB in Recurrent Glioblastoma (clinicaltrials.gov)
    P1/2, N=45, Not yet recruiting, M.D. Anderson Cancer Center
    New P1/2 trial
    |
    Yidafan (ivonescimab)
    19d
    AK112-102: A Study of AK112, a PD-1/VEGF Bispecific Antibody, for Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=59, Completed, Akeso | Active, not recruiting --> Completed | Trial completion date: May 2023 --> Jul 2024
    Trial completion • Trial completion date • Metastases
    |
    Yidafan (ivonescimab)
    26d
    Novel quinazolin-4-one based derivatives bearing 1,2,3-triazole and glycoside moieties as potential cytotoxic agents through dual EGFR and VEGFR-2 inhibitory activity. (PubMed, Sci Rep)
    The quinazoline based glycosyl-1,2,3-triazoles 10-13 with free hydroxy sugar moiety revealed excellent potency against (IC50 range = 5.70-8.10 µM, IC50 Doxorubicin = 5.6 ± 0.30 µM, IC50 Erlotinib = 4.3 ± 0.1 µM)...The hydroxylated glycosides incorporating triazole and quinazoline system 11 and 13 with N-methyl substitution of quinazolinone, gave excellent potency against EGFR (IC50 = 0.35 ± 0.11 and 0.31 ± 0.06 µM, correspondingly) since glycoside 13 revealed comparable IC50 (3.20 ± 0.15 µM) to sorafenib against VEGFR-2...Additionally, the latter derivative may trigger apoptosis, as indicated by a significant increase in apoptotic cells. Furthermore, molecular docking was simulated to make an obvious validation and comprehension acquirement of the binding's characteristics also attractions among the most forceful compounds side by side with their aimed enzymes.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • BCL2 (B-cell CLL/lymphoma 2) • KDR (Kinase insert domain receptor) • BAX (BCL2-associated X protein)
    |
    erlotinib • sorafenib • doxorubicin hydrochloride
    26d
    A Study of TAVO412 in Patients with Cancer (clinicaltrials.gov)
    P1, N=50, Active, not recruiting, Tavotek Biotherapeutics | Recruiting --> Active, not recruiting | Trial completion date: Dec 2025 --> Jun 2026 | Trial primary completion date: Jun 2024 --> Dec 2025
    Enrollment closed • Trial completion date • Trial primary completion date • Metastases
    |
    EGFR (Epidermal growth factor receptor) • MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    EGFR mutation • EGFR expression • EGFR overexpression • MET overexpression • MET mutation
    |
    TAVO412
    28d
    A Study to Evaluate SSGJ-707 in Advanced Gynecologic Cancer Patients (clinicaltrials.gov)
    P2, N=80, Recruiting, Sunshine Guojian Pharmaceutical (Shanghai) Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    carboplatin • paclitaxel
    29d
    Study of LM-299 in Subjects Advanced Malignant Tumors (clinicaltrials.gov)
    P1/2, N=230, Recruiting, LaNova Medicines Limited
    New P1/2 trial • Combination therapy • Metastases
    |
    carboplatin
    1m
    AK112 and Cadonilimab Combined With Chemotherapy for 1L Treatment of Metastatic Pancreatic Cancer (clinicaltrials.gov)
    P1/2, N=110, Not yet recruiting, Akeso
    New P1/2 trial • Metastases
    |
    gemcitabine • albumin-bound paclitaxel • Kaitanni (cadonilimab) • Yidafan (ivonescimab)
    1m
    ASCENT: Pivotal 2 Study of RGX-314 Gene Therapy in Participants With nAMD (clinicaltrials.gov)
    P3, N=660, Recruiting, AbbVie | N=465 --> 660 | Trial completion date: Dec 2025 --> Nov 2026 | Trial primary completion date: Feb 2025 --> Nov 2025
    Enrollment change • Trial completion date • Trial primary completion date • Gene therapy
    |
    Eylea (aflibercept intravitreal)
    1m
    Efficacy and Safety Study of Disitamab Vedotin + RC148 vs. Albumin-Paclitaxone ± Toripalimab in HR-/HER2-low Breast Cancer (clinicaltrials.gov)
    P2, N=40, Not yet recruiting, RemeGen Co., Ltd.
    New P2 trial • Combination therapy • Metastases
    |
    Loqtorzi (toripalimab-tpzi) • Aidixi (disitamab vedotin)
    1m
    Phase II Clinical Trial of Chidamide Combined With AK112 for Second-line and Advanced Bone and Soft Tissue Sarcoma (clinicaltrials.gov)
    P2, N=30, Recruiting, Shanxi Province Cancer Hospital
    New P2 trial • Metastases
    |
    Epidaza (chidamide) • Yidafan (ivonescimab)
    1m
    Safety, Pharmacokinetics, and Efficacy of AI-081, a Bispecific Antibody for PD-1 And VEGF in Advanced Solid Tumors (clinicaltrials.gov)
    P1/2, N=204, Not yet recruiting, OncoC4, Inc.
    New P1/2 trial
    2ms
    Retrospective study assessing the role of the androgen receptor in clear cell renal cell cancer patients treated with VEGFR inhibitors in monotherapy. (PubMed, Clin Transl Oncol)
    AR-overexpression and its association with other genes could favor a transcriptomic signature set to aid in identifying patients suitable for TKI in monotherapy, rather than aggressive combinations, enhancing thus, precision and personalized therapeutic decisions.
    Retrospective data • Journal
    |
    AR (Androgen receptor)
    |
    AR overexpression • AR expression
    2ms
    A Study to Test Different Doses of BI 836880 Combined With Ezabenlimab in Patients With Advanced Non-small Cell Lung Cancer Followed by Other Types of Advanced Solid Tumours (clinicaltrials.gov)
    P1, N=252, Completed, Boehringer Ingelheim | Active, not recruiting --> Completed
    Trial completion
    |
    PD-L1 (Programmed death ligand 1)
    |
    PD-L1 expression
    |
    ezabenlimab (BI 754091) • BI 836880
    2ms
    A Phase II Study of Ivonescimab Combined with Cadonilimab and Chemotherapy in Extensive-stage Small Cell Lung Cancer (clinicaltrials.gov)
    P2, N=70, Not yet recruiting, Shanghai Pulmonary Hospital, Shanghai, China
    New P2 trial
    |
    carboplatin • paclitaxel • Kaitanni (cadonilimab) • Yidafan (ivonescimab)
    2ms
    Local Injection and Systemic Therapy in the Treatment of NSCLC. (clinicaltrials.gov)
    P2, N=84, Not yet recruiting, Henan Cancer Hospital
    New P2 trial
    |
    docetaxel • Enweida (envafolimab) • Endostar (recombinant human endostatin)
    2ms
    BIOVAS: BIOmarker Driven Trial of VEGFR2 Inhibitor in Advanced Sarcoma (clinicaltrials.gov)
    P2, N=30, Recruiting, Ruijin Hospital | Trial completion date: May 2024 --> Sep 2027 | Trial primary completion date: Feb 2024 --> Oct 2026
    Trial completion date • Trial primary completion date
    |
    AiTan (rivoceranib)
    2ms
    Efficacy and safety of intra-arterial cisplatin plus anti-angiogenesis inhibitor rh-endostatin (Endostar) combined with systematic chemotherapy in osteosarcoma (ChiCTR2400088085)
    P=N/A, N=10, Not yet recruiting, Shanghai Sixth People's Hospital Affiliated to Shanghai Jiao Tong University School of Medicine; Shanghai Sixth People's Hospital Affiliated to Shangh
    New trial
    |
    cisplatin • doxorubicin hydrochloride • Endostar (recombinant human endostatin)
    2ms
    Single-arm, open, exploratory study of ivonescimab combined with chemotherapy and SBRT in patients with advanced cholangiocarcinoma (ChiCTR2400088480)
    P2, N=35, Recruiting, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology; Union Hospital, Tongji Medical College, Huazhong University o
    New P2 trial • Metastases
    |
    Yidafan (ivonescimab)
    2ms
    Phase II Clinical Study of Anti-PD-1 and VEGF Bispecific Antibody AK112 in Combination With Etoposide and Carboplatin for the First-line Treatment of Patients With Extensive Stage Small Cell Lung Cancer (ChiCTR2400087910)
    P2, N=12, Not yet recruiting, Jilin Cancer Hospital; Jilin Cancer Hospital
    New P2 trial • Combination therapy
    |
    carboplatin • etoposide IV • Yidafan (ivonescimab)
    2ms
    A Phase 3 Study of AK112 Plus AK117 Versus Pembrolizumab in Recurrent or Metastatic Head and Neck Squamous Cell Carcinoma (R/M HNSCC) (clinicaltrials.gov)
    P3, N=510, Not yet recruiting, Akeso
    New P3 trial • Combination therapy • Metastases
    |
    Keytruda (pembrolizumab) • Yidafan (ivonescimab) • ligufalimab (AK117)
    2ms
    A Phase 2 Study of SSGJ-707 in Metastatic Colorectal Cancer Patients (clinicaltrials.gov)
    P2, N=130, Recruiting, Sunshine Guojian Pharmaceutical (Shanghai) Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    Avastin (bevacizumab) • 5-fluorouracil • capecitabine • oxaliplatin • leucovorin calcium
    2ms
    AK112 Combined With Chemotherapy Versus Durvalumab Combined With Chemotherapy in Advanced Biliary Tract Cancer (clinicaltrials.gov)
    P3, N=682, Not yet recruiting, Akeso
    New P3 trial • Metastases
    |
    cisplatin • Imfinzi (durvalumab) • gemcitabine • Yidafan (ivonescimab)
    2ms
    PRO-VISION: Patient Reported Outcomes-Based Monitoring of VEGF-Inhibitor Side Effects in ONcology (clinicaltrials.gov)
    P=N/A, N=42, Active, not recruiting, UNC Lineberger Comprehensive Cancer Center | Recruiting --> Active, not recruiting | Trial primary completion date: Jan 2026 --> Jan 2027
    Enrollment closed • Trial primary completion date • Adverse events • Patient reported outcomes
    2ms
    Phase III Study of AK112 for NSCLC Patients (clinicaltrials.gov)
    P3, N=420, Active, not recruiting, Summit Therapeutics | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    carboplatin • pemetrexed • Yidafan (ivonescimab)
    2ms
    Miracle-03: Lvosidenib (AK112) Combined With CapeOX and Radiotherapy in Patients With Unresectable Metastatic MSS-type Colorectal Cancer (clinicaltrials.gov)
    P2, N=36, Not yet recruiting, Fudan University
    New P2 trial • Metastases
    |
    Tibsovo (ivosidenib) • Yidafan (ivonescimab)