TEQ101 / Cureteq, EMD Serono - LARVOL DELTA

Novel Methionine Aminopeptidase 2 Inhibitor M8891 Synergizes with VEGF Receptor Inhibitors to Inhibit Tumor Growth of Renal Cell Carcinoma Models. (PubMed, Mol Cancer Ther) - "Robust angiogenesis and tumor growth inhibition was observed with M8891 monotherapy. In combination with VEGF receptor inhibitors, tumor stasis and regression occurred in patient-derived xenograft renal cell carcinoma (RCC) models, particularly those that were p53 wild-type, had Von Hippel-Landau gene (VHL) loss-of-function mutations, and a mid/high MetAP1/2 expression score."

Journal • Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • Von Hippel-Lindau Syndrome • EEF1A1 • TAP1 • TP53

Preclinical Pharmacokinetics and Translational Pharmacokinetic/Pharmacodynamic Modeling of M8891, a Potent and Reversible Inhibitor of Methionine Aminopeptidase 2. (PubMed, Pharm Res) - P1 | "The defined target PK and PD levels supported the design of the clinical Phase Ia dose escalation study of M8891 (NCT03138538) and selection of the recommended Phase II dose."

Journal • PK/PD data • Preclinical • Kidney Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

A First-in-human, Dose-escalation Study of the Methionine Aminopeptidase 2 Inhibitor M8891 in Patients with Advanced Solid Tumors. (PubMed, Cancer Res Commun) - P1 | "This dose-escalation study assessed M8891 treatment for patients with advanced solid tumors. M8891 demonstrated favorable pharmacokinetics, tumoral target engagement, and a manageable safety profile, and thus represents a novel antitumor strategy warranting further clinical studies."

Journal • Metastases • P1 data • Oncology • Solid Tumor

First Report of Take-All Root Rot Caused by Gaeumannomyces graminis on Hybrid Bermudagrass in China. (PubMed, Plant Dis) - "The sterilized tissues were rinsed, air dried on sterile filter paper for 5 min and placed on potato dextrose agar (PDA) amended with 50 mg L-1 each of ampicillin, streptomycin sulfate and tetracycline...PCR products were sequenced (deposited as MZ889119 and MZ889120 in GenBank), and showed 99.43 to 99.81% homology when compared with a known G. graminis isolate (accession no...graminis was consistently reisolated from symptomatic roots and stolons, and confirmed by sequencing the ITS region as mentioned above. To our knowledge, this is the first report of G. graminis causing take-all root rot of hybrid bermudagrass in China, which may influence the management of this important root disease."

Journal • Transplantation

[VIRTUAL] A multicenter, open-label, dose-escalation, first-in-man study of MetAP2 inhibitor M8891 in patients with advanced solid tumours (ESMO 2020) - P1 | "Funding: Merck KGaA, Darmstadt, Germany. Clinical trial identification: NCT03138538."

Clinical • Oncology • Solid Tumor

M8891 First in Human in Solid Tumors (clinicaltrials.gov) - P1; N=97; Active, not recruiting; Sponsor: EMD Serono Research & Development Institute, Inc.; Recruiting ➔ Active, not recruiting

Clinical • Enrollment closed • Clear Cell Renal Cell Carcinoma • Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

M8891 First in Human in Solid Tumors (clinicaltrials.gov) - P1; N=97; Recruiting; Sponsor: EMD Serono Research & Development Institute, Inc.; N=27 ➔ 97; Trial completion date: Jul 2020 ➔ Mar 2022; Trial primary completion date: Jul 2020 ➔ Mar 2022

Clinical • Enrollment change • Trial completion date • Trial primary completion date • Clear Cell Renal Cell Carcinoma • Genito-urinary Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor

Identification of Methionine Aminopeptidase-2 (MetAP-2) inhibitor M8891, a Clinical Compound for the Treatment of Cancer. (PubMed, J Med Chem) - "Orally bioavailable, potent, and reversible MetAP-2 inhibitors impede growth of primary endothelial cells and demonstrated antitumoral activity in mouse models. This assessment led to nomination of the clinical development compound M8891 which is currently in Phase I clinical testing in oncology patients."

Clinical • Journal • Oncology

M8891 First in Human in Solid Tumors (clinicaltrials.gov) - P1; N=24; Recruiting; Sponsor: EMD Serono Research & Development Institute, Inc.; Trial completion date: Feb 2020 ➔ Jul 2020; Trial primary completion date: Feb 2020 ➔ Jul 2020

Clinical • Trial completion date • Trial primary completion date

M8891 First in Human in Solid Tumors (clinicaltrials.gov) - P1; N=21; Recruiting; Sponsor: EMD Serono Research & Development Institute, Inc.; Trial completion date: Sep 2019 ➔ Feb 2020; Trial primary completion date: Sep 2019 ➔ Feb 2020

Clinical • Trial completion date • Trial primary completion date

Antitumor activity of M8891, a potent and reversible inhibitor of methionine aminopeptidase 2 (AACR 2019) - "In combination with sunitinib, M8891 demonstrated strong and durable antitumor activity in a cohort of patient-derived renal cancer xenografts at well-tolerated exposure levels. Predictive biomarker hypotheses generated from CRISPR sensitivity/resistance screens as well as analyses of molecular profiling data from PDX tumors are currently being evaluated in further nonclinical studies. A dose-escalation phase 1 study in patients with advanced solid tumors is currently ongoing."

M8891 First in Human in Solid Tumors (clinicaltrials.gov) - P1; N=21; Recruiting; Sponsor: EMD Serono Research & Development Institute, Inc.; Trial completion date: Jul 2019 ➔ Oct 2019; Trial primary completion date: Dec 2018 ➔ Oct 2019

Clinical • Trial completion date • Trial primary completion date