Delving into the Latest Updates on B-013 with Synapse

Overview

Basic Info

Drug Type

Monoclonal antibody

Synonyms

Target-

Mechanism-

Therapeutic Areas

NeoplasmsSkin and Musculoskeletal DiseasesDigestive System Disorders+ [2]

Active Indication

Triple Negative Breast CancerFallopian Tube CarcinomaPlatinum-Resistant Ovarian Carcinoma+ [6]

Inactive Indication-

Originator Organization

Shanghai Pharmaceuticals Holding Co., Ltd.

Active Organization

Shanghai Jiaolian Drug Development Co. Ltd.

Shanghai Pharmaceuticals Holding Co., Ltd.

Inactive Organization-

Drug Highest PhasePhase 2/3

First Approval Date-

Regulation-

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This Phase II/III study assessed the efficacy, safety, pharmacokinetics, and immunogenicity of B013 administered with nab-paclitaxel in participants with locally advanced or metastatic triple negative breast cancer (TNBC) who have not received prior systemic therapy for metastatic breast cancer (mBC).

Start Date06 Dec 2022

Sponsor / Collaborator

Shanghai Jiaolian Drug Development Co. Ltd.

[+1]

100 Clinical Results associated with B-013

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100 Translational Medicine associated with B-013

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100 Patents (Medical) associated with B-013

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83

Literatures (Medical) associated with B-013

17 Oct 2023·ChemMedChem

Synthesis of Quinazolin‐2,4,6‐triamine Derivatives as Non‐purine Xanthine Oxidase Inhibitors and Exploration of Their Toxicological Potential**

Article

Author: Lopez-Sanchez, Marcela A ; Aguayo-Ortiz, Rodrigo ; Figueroa-Figueroa, Diego I ; Hernandez-Cruz, Estefani ; Hernandez-Luis, Francisco ; Del Carmen Garcia-Rodriguez, María

AbstractIn this work, a new set of quinazolin‐2,4,6‐triamine derivatives were synthesized to explore their potential biological activity as xanthine oxidase (XO) inhibitors, superoxide scavengers and screening of their toxicological profile. Among all the synthesized compounds, B1 exhibited better inhibitory activity against bovine xanthine oxidase (bXO) than allopurinol (IC50=1.56 μM and IC50=6.99 μM, respectively). As superoxide scavengers, B1, B2 and B13 exhibited a better effect than allopurinol (97.3 %, 82.1 %, 87.4 % and 69.4 %, respectively). Regarding the toxicological profile, B1 was less cytotoxic than methotrexate on HCT‐15 cancer cells. Apoptosis results obtained in cells of female and male mice, showed that B1 and B2 presented a similar behaviour to CrO3 (positive control) with respect to the average frequency to induce apoptosis; while B13 apoptosis induced effect was similar to DMSO and control group. Finally, B1, B2, B13 did not induce genotoxicity in a micronuclei murine model compared to CrO3.

18 Jul 2023·Natural Product ResearchQ3 · CHEMISTRY

Synthesis and antifungal activity of novel chiral indole analogues

Q3 · CHEMISTRY

Article

Author: Zheng, Shaojun ; Tang, Bing ; Tan, Yi ; Dai, Huihui ; Lin, Chuansong ; Jiang, Qiaoju ; Fang, Yue ; Wu, Wenbin

Starting from L-tryptophan, 19 new N-substituted chiral indole analogs were synthesized. The prepared compounds were evaluated for biological activity against Sclerotinia sclerotiorum, Alternaria solani, Verticillium dahliae, Colletotrichum orbiculare, Cytospora juglandis and Curvularia lunata. The preliminary bioassays showed that most of the synthesized compounds exhibited fungicidal activity. Compound b13 in particular exhibited significant antifungal activity against Verticillium dahliae and Sclerotinia sclerotiorum, with the MIC value of 1.95 µg mL^-1. Compound b13 also showed excellent activity against six plant pathogen fungi, and was identified as the most active on the biological assays, and will be studied further.

01 Jun 2023·Bioorganic Chemistry

B13, a well-tolerated inhibitor of hedgehog pathway, exhibited potent anti-tumor effects against colorectal carcinoma in vitro and in vivo

Article

Author: Chen, Boyu ; Wu, Shaoyu ; Lv, Lin ; Chen, Qianqing ; Ai, Yangcheng ; Tian, Nannan ; Zhang, Jiajie ; Wu, Huanxian ; Tian, Yuanxin ; Ou, Baofang ; Zhang, Tingting ; Zhang, Lishun ; Yang, Danni ; Xu, Jiahuan ; Quan, Dongling

Abnormal activation of Hedgehog (Hh) signaling pathway mediates the genesis and progression of various tumors [1]. Currently, three drugs targeting the Hh signaling component Smoothened (Smo) have been marketed for the clinical treatment of basal cell tumors or acute myeloid leukemia. However, drug resistance is a common problem in those drugs, so the study of Smo inhibitors that can overcome drug resistance has important guiding significance for clinical adjuvant drugs. MTT assay, clone formation assay and EdU assay were used to detect the proliferation inhibitory activity of the drugs on tumor cells. The effect of B13 on cell cycle and apoptosis were detected by flow cytometry. An acute toxicity test was used to detect the toxicity of B13 in vivo, and xenograft tumor model was used to detect the efficacy of B13 in vivo. The binding of B13 to Smo was studied by BODIPY-cyclopamine competitive binding assay and molecular docking. The effect of B13 on the expression and localization of downstream target gene Gli1/2 of Smo was investigated by Western Blot and immunofluorescence assay. Smo^D473H mutant cell line was constructed to study the effect of B13 against drug resistance. (1) B13 had the strongest inhibitory activity against colorectal cancer cells. (2) B13 can effectively inhibit the clone formation and EdU positive rate of colon cancer cells. (3) B13 can block the cell cycle in the G2/M phase and cell apoptosis. (4) B13 has low toxicity in vivo, and its efficacy in vivo is better than that of the Vismodegib. (5) Molecular docking and BODIPY-cyclopamine experiments showed that B13 could bind to Smo protein. (6) B13 can inhibit the protein expression of Gli1, the downstream of Smo, and inhibit its entry into the nucleus. (7) B13 could inhibit the expression of Gli1 in the HEK293 cells with Smo^D473H, and the molecular docking results showed that B13 could bind Smo^D473H protein. B13 with the best anti-tumor activity was screened out by MTT assay. In vitro, pharmacodynamics experiments showed that B13 could effectively inhibit the proliferation and metastasis of colorectal cancer cells, induce cell cycle arrest, and induce cell apoptosis. In vivo pharmacodynamics experiments showed that B13 was superior to Vismodegib in antitumor activity and had low toxicity in vivo. Mechanism studies have shown that B13 can bind Smo protein, inhibit the expression of downstream Gli1 and its entry into the nucleus. Notably, B13 overcomes resistance caused by Smo^D473H mutations.

100 Deals associated with B-013

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Triple Negative Breast Cancer	Phase 3	-	Shanghai Pharmaceuticals Holding Co., Ltd.	23 Aug 2022
Fallopian Tube Carcinoma	Phase 2	CN	Shanghai Pharmaceuticals Holding Co., Ltd.	11 Jul 2024
Platinum-Resistant Ovarian Carcinoma	Phase 2	CN	Shanghai Pharmaceuticals Holding Co., Ltd.	11 Jul 2024
Platinum-Resistant Primary Peritoneal Carcinoma	Phase 2	CN	Shanghai Pharmaceuticals Holding Co., Ltd.	11 Jul 2024
Platinum-Resistant Fallopian Tube Carcinoma	Phase 2	CN	Shanghai Jiaolian Drug Development Co. Ltd.	20 Jun 2024
Neoplasms	Phase 2	US	Shanghai Pharmaceuticals Holding Co., Ltd.	21 Jul 2022
Recurrent Platinum-Resistant Fallopian Tube Carcinoma	IND Approval	CN	Shanghai Jiaolian Drug Development Co. Ltd.	30 Jan 2024
Recurrent Platinum-Resistant Ovarian Carcinoma	IND Approval	CN	Shanghai Jiaolian Drug Development Co. Ltd.	30 Jan 2024
Recurrent Platinum-Resistant Primary Peritoneal Carcinoma	IND Approval	CN	Shanghai Jiaolian Drug Development Co. Ltd.	30 Jan 2024