Delving into the Latest Updates on BN-104 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

(2-(6-(2-(4-cyclopropylpyrimidin-5-yl)-4-fluorophenoxy)-1,2,4-triazin-5-yl)-2,7-diazaspiro[3.5]nonan-7-yl)((1S,3aR,6aS)-octahydrocyclopenta[c]pyrrol-1-yl)methanone

Target

menin

Mechanism

menin inhibitors(Menin inhibitors)

Therapeutic Areas

NeoplasmsImmune System DiseasesHemic and Lymphatic Diseases

Active Indication

acute leukemiaAdult Acute Lymphocytic LeukemiaAdult Acute Myeloblastic Leukemia+ [3]

Inactive Indication-

Originator Organization

BioNova Pharmaceuticals (Shanghai) Ltd.Startup

Active Organization

BioNova Pharmaceuticals (Shanghai) Ltd.Startup

Inactive Organization-

Drug Highest PhasePhase 1/2

First Approval Date-

RegulationFast Track (US), Orphan Drug (US)

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I期剂量递增阶段主要目的：1. 评价BN104治疗复发/难治性急性白血病患者的安全性和耐受性；2. 确定BN104治疗复发/难治性急性白血病患者的MTD和/或RP2D II期剂量扩展阶段主要目的：1. 评价BN104治疗复发/难治性伴有特定突变（KMT2A基因重排或NPM1基因突变）的急性白血病患者的疗效

[Translation]

The main objectives of the Phase I dose escalation phase are: 1. To evaluate the safety and tolerability of BN104 in the treatment of patients with relapsed/refractory acute leukemia; 2. To determine the MTD and/or RP2D of BN104 in the treatment of patients with relapsed/refractory acute leukemia. The main objectives of the Phase II dose expansion phase are: 1. To evaluate the efficacy of BN104 in the treatment of patients with relapsed/refractory acute leukemia with specific mutations (KMT2A gene rearrangement or NPM1 gene mutation).

Start Date16 Oct 2023

Sponsor / Collaborator

BioNova Pharmaceuticals (Shanghai) Ltd.Startup

NCT06052813 / RecruitingPhase 1/2

A PhaseI/II, Multicenter, Open-label Clinical Study to Evaluate the Safety, Pharmacokinetics, and Efficacy of the Menin Inhibitor BN104 in the Treatment of Patients With Relapsed/Refractory Acute Leukemia

The Phase I/II trial is to learn the safety, pharmacokinetics, and preliminary efficacy of BN104 taken once daily or twice daily in patients with acute lymphocytic leukemia or acute myeloblastic leukemia.

Start Date16 Sep 2023

Sponsor / Collaborator

BioNova Pharmaceuticals (Shanghai) Ltd.Startup

100 Clinical Results associated with BN-104

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100 Translational Medicine associated with BN-104

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100 Patents (Medical) associated with BN-104

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9

Literatures (Medical) associated with BN-104

01 Apr 2022·Journal of Chromatography AQ2 · CHEMISTRY

Rapid separation of americium from complex matrices using solvent impregnated triazine extraction chromatography resins

Q2 · CHEMISTRY

Article

Author: Heath, Scott L ; Gilligan, Christopher ; Livens, Francis ; Thompson, Paul ; Mahmoud, Joe ; Higginson, Matthew

Several novel extraction chromatography resins (EXC) have been synthesised by solvent impregnation of the triazine ligands 6,6'-bis(5,5,8,8-tetramethyl-5,6,7,8-tetrahydrobenzo[1,2,4]triazin-3-yl)-2,2'-bipyridine (CyMe₄BTBP) and 2,9-bis(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-benzo[1,2,4]triazin-3-yl)-1,10-phenanthroline (CyMe₄BTPhen) into Amberlite XAD7 and Amberchrom CG300 polymer supports. The resins have been physically characterised by a suite of spectroscopic, analytical and imaging techniques. The resins have also been evaluated in terms of their ability to selectively extract americium from complex matrices intended to simulate those typical of spent nuclear fuel raffinate, environmental samples and nuclear forensics samples. The resins have been compared with previously reported attempts to generate EXC resins based on CyMe₄BTBP and CyMe₄BTPhen. Previously reported resins all rely on complex synthesis for the formation of a covalent bond between extractant and support by contrast with the simpler solvent impregnation method reported here. The Amberchrom supported CyMe₄BTBP resin achieved a weight distribution ration (D_Am) of 170 within 60 min and a decontamination factor (DF) of >1000 for americium over lanthanides by column chromatography. The Amberchrom CyMe₄BTPhen resin achieved a D_Am of 540 within 30 min and a DF for americium from lanthanides of 60-160.

01 Nov 2021·Bioorganic & Medicinal ChemistryQ3 · MEDICINE

Synthesis of PF-6870961, a major hydroxy metabolite of the novel ghrelin receptor inverse agonist PF-5190457

Q3 · MEDICINE

Article

Author: Kenner C. Rice ; Fatemeh Akhlaghi ; Agnieszka Sulima ; Lorenzo Leggio

Preclinical and human studies have indicated involvement of the ghrelin system in alcohol-related behaviors illuminating the possibility of using ghrelin receptor blockers as a pharmacological intervention for alcohol use disorder (AUD). Preliminary data from a recently conducted phase 1b human study with a ghrelin receptor inverse agonist, PF-5190457 (2-(2-methylimidazo[2,1-b][1,3thiazol-6-yl)-1-{2-(1R)-5-(6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl]-2,7-diazaspiro[3.5]non-7-ylethanone), provided evidence on the safety and tolerability of this compound when co-administered with alcohol. Furthermore, the study revealed important information on the biotransformation pathways for this compound and prompted the discovery and then synthesis of a newly identified major metabolite, PF-6870961 ((R)-1-(2-(5-(2-hydroxy-6-methylpyrimidin-4-yl)-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro[3.5]nonan-7-yl)-2-(2-methylimidazo[2,1-b]thiazol-6-yl)ethan-1-one). The metabolite was synthesized and fully characterized through a design that enabled it to be prepared in useful quantities. The synthesis provided direct access to the recently discovered PF-6870961 and is allowing researchers to conduct additional and deeper evaluation of its in vitro and in vivo properties.

01 Apr 2021·European Journal of Medicinal ChemistryQ1 · MEDICINE

Developing novel classes of protein kinase CK1δ inhibitors by fusing [1,2,4]triazole with different bicyclic heteroaromatic systems

Q1 · MEDICINE

Article

Author: Spalluto, Giampiero ; Viola, Giampietro ; Cozza, Giorgio ; Perez, Daniel I ; Redenti, Sara ; Perez, Conception ; Bortolozzi, Roberta ; Federico, Stephanie ; Martinez, Ana ; Mariotto, Elena ; Moro, Stefano ; Tiz, Davide Benedetto ; Grieco, Ilenia ; Bissaro, Maicol

Protein kinase CK1δ expression and activity is involved in different pathological situations that include neuroinflammatory and neurodegenerative diseases. For this reason, protein kinase CK1δ has become a possible therapeutic target for these conditions. 5,6-fused bicyclic heteroaromatic systems that resemble adenine of ATP represent optimal scaffolds for the development of a new class of ATP competitive CK1δ inhibitors. In particular, a new series of [1,2,4]triazolo[1,5-c]pyrimidines and [1,2,4]triazolo[1,5-a][1,3,5]triazines was developed. Some crucial interactors have been identified, such as the presence of a free amino group able to interact with the residues of the hinge region at the 5- and 7- positions of the [1,2,4]triazolo[1,5-c]pyrimidine and [1,2,4]triazolo[1,5-a][1,3,5]triazine scaffolds, respectively; or the presence of a 3-hydroxyphenyl or 3,5-dihydroxyphenyl moiety at the 2- position of both nuclei. Molecular modeling studies identified the key interactions involved in the inhibitor-protein recognition process that appropriately fit with the outlined structure-activity relationship. Considering the fact that the CK1 protein kinase is involved in various pathologies in particular of the central nervous system, the interest in the development of new inhibitors permeable to the blood-brain barrier represents today an important goal in the pharmaceutical field. The best potent compound of the series is the 5-(7-amino-5-(benzylamino)-[1,2,4]triazolo[1,5-a][1,3,5]triazin-2-yl)benzen-1,3-diol (compound 51, IC₅₀ = 0.18 μM) that was predicted to have an intermediate ability to cross the membrane in our in vitro assay and represents an optimal starting point to both studies the therapeutic value of protein kinase CK1δ inhibition and to develop new more potent derivatives.

100 Deals associated with BN-104

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
acute leukemia	Phase 2	CN	BioNova Pharmaceuticals (Shanghai) Ltd.Startup	16 Oct 2023
Adult Acute Lymphocytic Leukemia	Phase 2	CN	BioNova Pharmaceuticals (Shanghai) Ltd.Startup	16 Sep 2023
Adult Acute Myeloblastic Leukemia	Phase 2	CN	BioNova Pharmaceuticals (Shanghai) Ltd.Startup	16 Sep 2023
Recurrent Acute Leukemia	IND Approval	US	BioNova Pharmaceuticals (Shanghai) Ltd.Startup	21 Sep 2023
Refractory Acute Leukemia	IND Approval	US	BioNova Pharmaceuticals (Shanghai) Ltd.Startup	21 Sep 2023
Acute Myeloid Leukemia	Preclinical	US	BioNova Pharmaceuticals (Shanghai) Ltd.Startup	17 Apr 2023