NN2101 / Novelty Nobility - LARVOL DELTA

Preclinical Antitumor Efficacy of a Novel Anti-c-Kit Antibody-Drug Conjugate, NN3201, in c-Kit-Positive Tumors. (PubMed, Mol Cancer Ther) - "A fully human c-Kit antibody NN2101 was conjugated to monomethyl auristatin E with a Drug-to-Antibody Ratio (DAR) of 4 utilizing a ThioBridge linker to generate NN3201. NN3201 exhibited significant c-Kit-dependent antitumor efficacies in various tumor models, followed by favorable pharmacokinetic and toxicity profiles in cynomolgus monkeys. These data suggest that NN3201 is a promising therapeutic in small cell lung cancer and gastrointestinal stromal tumors and warrant evaluation in a phase I clinical study."

Journal • Preclinical • Acute Myelogenous Leukemia • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Hematological Malignancies • Leukemia • Lung Cancer • Oncology • Sarcoma • Small Cell Lung Cancer • Solid Tumor

Preclinical Anti-Tumor Efficacy of a Novel Anti-c-Kit Antibody Drug Conjugate, NN3201, in c-Kit Positive Tumors. (PubMed, Mol Cancer Ther) - "A fully human c-Kit antibody NN2101 was conjugated to monomethyl auristatin E (MMAE) as DAR of 4 utilizing ThioBridge linker to generate NN3201. NN3201 exhibited significant c-Kit-dependent anti-tumor efficacies in various tumor models, followed by favorable pharmacokinetic and toxicity profile in cynomolgus monkeys. These data suggest that NN3201 is a promising therapeutic in SCLC and GIST, and warrants evaluation in a phase 1 clinical study."

Journal • Preclinical • Acute Myelogenous Leukemia • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Hematological Malignancies • Leukemia • Lung Cancer • Oncology • Sarcoma • Small Cell Lung Cancer • Solid Tumor

The novel function of NN2101, an anti-c-kit antibody, as an inhibitor of HIF via c-kit regulation in ocular neovascular disease (ARVO 2022) - "HRMEC/RPE co-culture exhibited that HIF-1α inhibition by NN2101 effectively blocks VEGF secretion from RPE, similar to Eylea. We demonstrated that c-kit inhibition with NN2101 efficiently suppresses pathological vessels by reducing expression of multiple angiogenic cytokines via destabilization of HIF in the retina."

Age-related Macular Degeneration • Ocular Inflammation • Ophthalmology • HIF1A

A Fully Human Monoclonal Antibody Targeting cKIT Is a Potent Inhibitor of Pathological Choroidal Neovascularization in Mice. (PubMed, Pharmaceutics) - "Ocular pharmacokinetic analysis in rabbits indicated that NN2101 demonstrated a pharmacokinetic profile suitable for intravitreal injection. These findings provide the first evidence of the potential use of the anti-cKIT blocking antibody, NN2101, as an alternative or additive therapeutic for the treatment of neovascular AMD."

Journal • Preclinical • Age-related Macular Degeneration • Macular Degeneration • Ophthalmology • Retinal Disorders • Wet Age-related Macular Degeneration

A novel anti-c-Kit antibody-drug conjugate to treat wild-type and activating-mutant c-Kit-positive tumors. (PubMed, Mol Oncol) - "In addition, NN2101-DM1 exhibited a significantly higher anti-cancer effect than carboplatin/etoposide against SCLC cells where c-Kit does not mediate cancer pathogenesis. Furthermore, the combination of NN2101-DM1 with imatinib in imatinib-sensitive GIST cells induced complete remission compared to treatment with NN2101-DM1 or imatinib alone in mouse xenograft models. These results suggest that NN2101-DM1 is a potential therapeutic agent for wild-type and mutant c-Kit-positive cancers."

Journal • Acute Myelogenous Leukemia • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Hematological Malignancies • Leukemia • Lung Cancer • Melanoma • Neuroendocrine Tumor • Oncology • Sarcoma • Small Cell Lung Cancer • Solid Tumor

[VIRTUAL] A Fully Human Monoclonal Antibody Targeting c-KIT is a Potent Inhibitor of Choroidal Neovascularization in Murine Model of Neovascular Age-Related Macular Degeneration (ARVO 2021) - "NN2101, a fully human monoclonal antibody targeting cKIT, may be a novel promising therapeutic and can enhance the potency of existing anti-vascular endothelial growth factor agents for the treatment of nAMD."

Preclinical • Age-related Macular Degeneration • Macular Degeneration • Ophthalmology • Retinal Disorders • Wet Age-related Macular Degeneration • KIT

Development and characterization of a fully human antibody targeting SCF/c-kit signaling. (PubMed, Int J Biol Macromol) - "The immunogenicity of NN2101 was similar to that of bevacizumab. Collectively, we generated a c-kit neutralizing human antibody (NN2101) for the treatment of erythroleukemia and characterized its biophysical properties. NN2101 can potentially be used as a therapeutic antibody to treat different cancers."

Journal • Brain Cancer • Glioblastoma • Hematological Disorders • Hematological Malignancies • Leukemia • Oncology