主要目的：在经标准治疗失败（疾病进展或无法耐受）或缺乏标准治疗的晚期实体肿瘤患者中确定注射用BGC0222的最大耐受剂量（MTD）或II期推荐剂量（RP2D）及安全性。次要目的：探索注射用BGC0222单药治疗在单次和多次给药条件下在晚期实体肿瘤患者中的药代动力学（PK）特征；初步评价注射用BGC0222单药治疗晚期实体肿瘤（如结直肠癌、胰腺癌、胃癌、食管癌、乳腺癌、非小/小细胞肺癌等）患者的临床疗效。

[Translation]

Primary objective: To determine the maximum tolerated dose (MTD) or phase II recommended dose (RP2D) and safety of BGC0222 for injection in patients with advanced solid tumors who have failed standard treatment (disease progression or intolerance) or lack standard treatment. Secondary objective: To explore the pharmacokinetic (PK) characteristics of BGC0222 for injection monotherapy in patients with advanced solid tumors under single and multiple dosing conditions; to preliminarily evaluate the clinical efficacy of BGC0222 for injection monotherapy in patients with advanced solid tumors (such as colorectal cancer, pancreatic cancer, gastric cancer, esophageal cancer, breast cancer, non-small/small cell lung cancer, etc.).

Start Date19 Jul 2022

Sponsor / Collaborator

Gaorui Yaoye (Beijing) Technologies Co Ltd

100 Clinical Results associated with BGC-0222

100 Translational Medicine associated with BGC-0222

100 Patents (Medical) associated with BGC-0222

Literatures (Medical) associated with BGC-0222

01 Jan 2020·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Design, synthesis and antitumor activity of a novel PEG-A6-conjugated irinotecan derivative

Q4 · MEDICINE

Article

Author: Zhang, Ye ; Ding, Hai-Feng ; Song, Yun-Song ; Huang, Yang-Qing ; Yuan, Jian-Dong ; Wang, Jia-Li ; Qian, Gang ; Ji, Min

A novel PEG-A6-conjugated irinotecan derivative 8 was designed and synthesized as antitumor agent by the PEGylation and A6-peptide modification of irinotecan. In vivo antitumor activity screening assay revealed that 8 exhibited better in vivo antiproliferation activity than irinotecan and its previous PEG-cRGD-conjugated derivative BGC0222 in MIA PaCa-2, NCI-H446, MDA-MB-231, HT-29 and NCI-N87 xenograft models, while the tumor of one in six mice in NCI-H446 assay and the tumors of two in six mice in MIA PaCa-2 assay completely subsided and disappeared within the 21-day period of 8-treatment, indicating that 8 should be a potential antitumor agent.

01 Oct 2018·European Journal of Medicinal ChemistryQ1 · MEDICINE

Design, synthesis and pharmacological evaluation of a novel PEG-cRGD-conjugated irinotecan derivative as potential antitumor agent

Q1 · MEDICINE

Article

Author: Yang-Qing Huang ; Jian-Dong Yuan ; Jia-Li Wang ; Hai-Feng Ding ; Yun-Song Song ; Gang Qian ; Min Ji ; Ye Zhang

A novel PEG-cRGD-conjugated irinotecan derivative BGC0222 was designed and synthesized as antitumor agent. Antitumor activity screening assay indicated that BGC0222 exhibited better in vitro antiproliferation activity than irinotecan and NKTR-102 against HT29, MIA PaCa-2 and MCF-7 tumor cell lines, with IC₅₀ of 1.83 ± 0.09 μM, 3.95 ± 0.16 μM and 0.68 ± 0.04 μM, respectively, while it displayed better in vivo antiproliferation activity than irinotecan and NKTR-102 in HT-29, MIA PaCa-2, NCI-H446, U-87 MG and MDA-MB-231 xenograft models. The action mechanism of BGC0222 was then investigated by integrin-binding competition (IBC) and chick chorioallantoic membrane (CAM) angiogenesis assays, which indicated that BGC0222 may exert antitumor activity by binding to α_vβ₃ target and consequently inducing neovascularization effect. Pharmacokinetic analysis showed that BGC0222 could slowly and steadily release irinotecan, which was subsequently metabolized into 7-ethyl-10-hydroxycamptothecin (SN-38) in the whole blood.

Bioconjugate Chemistry

A pH-Sensitive cRGD-PEG-siRNA Conjugated Compound Targeting Glioblastoma

Article

Author: He, Shuai ; Liu, Ziyuan ; Chen, Junxiao ; Fan, Yiqi ; Su, Qing

Glioblastoma ranks among the most prevalent primary intracranial tumors, characterized by high mortality and poor prognosis. Chemotherapy remains a key treatment strategy for gliomas, though most current drugs suffer from limited efficacy and significant toxicity. This study focuses on a cRGD-siEGFR coupling compound synthesized in a previous stage. Prior research indicated that cRGD-siEGFR molecules exhibited certain targeting and antitumor properties but faced issues of inadequate targeting, low efficacy, and high renal toxicity. To enhance antitumor efficacy and mitigate side effects, a pH-responsive, long-circulating, and highly targeted siRNA delivery system, the cRGD-PEG-siEGFR conjugate, was developed. The targeting, antitumor effects, and biological distribution of cRGD-PEG-siEGFR were examined. The results demonstrated that cRGD-PEG-siEGFR was effectively taken up by αvβ3-positive U87MG cells, specifically silenced EGFR gene expression, and exhibited antitumor effects. In normal physiological conditions, it avoided uptake by normal cells, thereby reducing side effects. Furthermore, in vivo biodistribution experiments revealed that cRGD-PEG-siEGFR, compared to cRGD-siEGFR, significantly decreased renal accumulation and exhibited prolonged circulation. Consequently, cRGD-PEG-siRNA emerges as a promising drug candidate with attributes of long circulation, high targeting, pH responsiveness, and substantial antitumor efficacy.

100 Deals associated with BGC-0222

R&D Status

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Indication	Highest Phase	Country/Location	Organization	Date
Advanced Malignant Solid Neoplasm	Phase 1	CN	Gaorui Yaoye (Beijing) Technologies Co Ltd	19 Jul 2022
Breast Cancer	IND Approval	CN	Suzhou Tianmayiyao Group Tianji Biology Pharmacy Co. Ltd.	12 Jun 2023
Colonic Cancer	IND Approval	CN	Suzhou Tianmayiyao Group Tianji Biology Pharmacy Co. Ltd.	12 Jun 2023
Glioma	IND Approval	CN	Suzhou Tianmayiyao Group Tianji Biology Pharmacy Co. Ltd.	12 Jun 2023
Pancreatic Cancer	IND Approval	CN	Suzhou Tianmayiyao Group Tianji Biology Pharmacy Co. Ltd.	12 Jun 2023
Small Cell Lung Cancer	IND Approval	CN	Suzhou Tianmayiyao Group Tianji Biology Pharmacy Co. Ltd.	12 Jun 2023
Stomach Cancer	IND Approval	CN	Suzhou Tianmayiyao Group Tianji Biology Pharmacy Co. Ltd.	12 Jun 2023
Neoplasms	Preclinical	CN	BrightGene Pharmaceutical Co., Ltd.	01 Oct 2018

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