NN3201 / 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

KOAS seeks to acquire antibody drug developer Novelty Nobility (Korea Biomedical Review) - "KOAS has decided to invest 50 billion won ($36 million) in Novelty Nobility through new funding from institutional investors....Novelty Nobility has two pipelines, NN3201 and NN3206, which apply unique next-generation payloads."

M&A • 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

A Study of the C-Kit Specific Antibody-Drug Conjugate NN3201 for Advanced And/or Metastatic Solid Tumors Known to Express C-Kit (clinicaltrials.gov) - P1 | N=67 | Recruiting | Sponsor: Novelty Nobility, Inc. | Not yet recruiting ➔ Recruiting

Enrollment open • Adenoid Cystic Carcinoma • Clear Cell Renal Cell Carcinoma • Endocrine Cancer • Eye Cancer • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Genito-urinary Cancer • Lung Cancer • Melanoma • Neuroendocrine Tumor • Oncology • Renal Cell Carcinoma • Sarcoma • Small Cell Lung Cancer • Solid Tumor • Uveal Melanoma • KIT

A Study of the C-Kit Specific Antibody-Drug Conjugate NN3201 for Advanced And/or Metastatic Solid Tumors Known to Express C-Kit (clinicaltrials.gov) - P1 | N=67 | Not yet recruiting | Sponsor: Novelty Nobility, Inc.

New P1 trial • Adenoid Cystic Carcinoma • Clear Cell Renal Cell Carcinoma • Endocrine Cancer • Eye Cancer • Gastrointestinal Cancer • Gastrointestinal Disorder • Gastrointestinal Stromal Tumor • Genito-urinary Cancer • Lung Cancer • Melanoma • Neuroendocrine Tumor • Oncology • Renal Cell Carcinoma • Sarcoma • Small Cell Lung Cancer • Solid Tumor • Uveal Melanoma • KIT

NoveltyNobility Selected for c-Kit Target ADC KDDF Project [Google translation] (Hankyung) - "Novelty Nobility announced on the 16th that it has been selected as a phase 1 clinical trial company for the 2nd Korea Drug Development Fund (KDDF) ​​in 2024. Novelty Nobility will receive research and development funding from KDDF for the next 24 months to conduct clinical development of NN3201, a c-Kit targeting antibody-drug conjugate (ADC). The target patients are cancer patients with c-Kit overexpression, such as small cell lung cancer (SCLC) and gastrointestinal stromal tumors (GIST)."

Commercial • Gastrointestinal Stromal Tumor • Lung Cancer • Small Cell Lung Cancer • Solid Tumor

Novelinobility, ADC anticancer drug candidate ’NN3201’ approved by FDA for Phase 1 [Google translation] (MedigateNews) - "Novelty Nobility announced on the 4th that it received approval for a phase 1 clinical trial (IND) for the antibody drug conjugate (ADC) anticancer drug candidate 'NN3201' from the U.S. Food and Drug Administration (FDA) on the 29th of last month (local time). This phase 1 trial was designed as a basket encompassing patients with solid tumors overexpressing c-Kit, including small cell lung cancer (SCLC), gastrointestinal tumor (GIST), neuroendocrine tumor (NET), and adenoid cystic carcinoma...It will be conducted in the United States starting in the second half of this year to confirm safety and tolerability."

IND • New P1 trial • Adenoid Cystic Carcinoma • Gastrointestinal Stromal Tumor • Lung Cancer • Neuroendocrine Tumor • Oncology • Small Cell Lung Cancer • Solid Tumor

NN3201, a novel c-Kit targeting ADC, exhibits robust preclinical anti-tumor efficacy in SCLC and GIST models (AACR 2024) - "While imatinib, a small molecule c-Kit inhibitor, has been a beneficial treatment for GIST, resistance eventually develops to the drug, moreover, shows limited efficacy in c-Kit overexpressing tumors such as SCLC...Enhanced anti-tumor activity and delayed tumor growth were observed in an SOC-treated (etoposide and carboplatin) SCLC xenograft model, by NN3201 in comparison to second line SOC (topotecan or irinotecan)...We confirmed HNSTD (Highest Non-Severely Toxic Dose) of NN3201 to be 2 mg/kg through exploratory and GLP repeat dose toxicity studies as no serious irreversible toxicity was observed. Accumulating data suggest that NN3201 is a promising therapeutic alternative for the treatment of SCLC and GIST regardless of wild-type or activating mutations in c-Kit."

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

In vivo efficacy and preclinical safety profile of NN3201, an anti-cKIT antibody-drug conjugate, for treating SCLC and AML (AACR 2023) - "Since small molecule inhibitors including imatinib frequently have a limited therapeutic application due to eventual drug resistance and severe adverse events, we developed the cKIT-directed antibody-drug conjugate (ADC), NN3201, for the treatment of wild-type and mutant cKIT-positive cancers. Even though a decrease in reticulocyte, red cell mass (hemoglobin and red blood cell), neutrophil, and monocyte counts, along with bone marrow recovery and reticulocyte compensatory mechanism, red blood cell and white blood cell recovery were observed from day 14 in the low and medium dose groups and day 21 in the high dose group, dose-dependently. These preclinical results suggest that NN3201 is a potential therapeutic agent for the treatment of cKIT-positive cancers and support the further clinical evaluation in SCLC and AML."

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

An optimized preclinical antibody-drug conjugate against cancers with cKIT overexpression or activating mutations (AACR 2022) - "This linker-payload system is the same used in ado-trastuzumab emtansine, an approved ADC for HER2-positive breast cancer. There were no significant toxicities detected at doses up to 60 mg/kg in normal mice, suggesting a therapeutic index greater than 20 times. In conclusion, NN3201 showed potent anti-tumor activity and was selected as preclinical candidate."

Preclinical • Acute Myelogenous Leukemia • Breast Cancer • Gastrointestinal Cancer • Gastrointestinal Stromal Tumor • Hematological Malignancies • HER2 Breast Cancer • HER2 Positive Breast Cancer • Leukemia • Lung Cancer • Neuroendocrine Tumor • Oncology • Sarcoma • Small Cell Lung Cancer • Solid Tumor • HER-2