A Phase Ib/II , Multicenter, Open-Label Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Preliminary Anti-Tumor Effects of SC0245 in Combination With Irinotecan in Patients With ES-SCLC

This study is a single arm, multi-center, open label phase Ib/II study of SC0245 and Irinotecan combination therapy in subjects with extensive-stage small cell lung cancer (ES-SCLC) as a second therapy. This study will have three parts, phase 1 dose escalation (Part 1), phase 1 dose expansion (Part 2), and phase 2 combination therapy (Part 3).

Start Date23 Feb 2023

Sponsor / Collaborator

Wuxi Zhikang Hongyi Biological Technology Co Ltd

CTR20223363 / RecruitingPhase 1/2

SC0245片联合伊立替康在复发难治的广泛期小细胞肺癌患者中的一项开放性、多中心Ib/II期临床研究

[Translation] An open-label, multicenter phase Ib/II clinical study of SC0245 tablets combined with irinotecan in patients with relapsed or refractory extensive-stage small cell lung cancer

Ib递增阶段主要目的：评估SC0245联合伊立替康在经标准治疗失败，或无标准治疗方案，或现阶段不适用标准治疗，或不能耐受标准治疗的晚期恶性实体瘤患者中的安全性和耐受性，确定联合治疗中SC0245的MTD及RP2D。次要目的：PK特征，初步抗肿瘤活性。Ib扩展阶段主要目的：评估SC0245联合伊立替康在一线含铂化疗（联合或不联合免疫治疗）失败或不耐受的广泛期SCLC患者中的安全性和耐受性；次要目的：PK特征，初步抗肿瘤活性。II期阶段主要目的：评估SC0245联合伊立替康在一线含铂化疗（联合或不联合免疫治疗）失败或不耐受的广泛期SCLC中的初步抗肿瘤活性。次要目的：安全性和耐受性。

[Translation]

The main purpose of the Ib escalation phase is to evaluate the safety and tolerability of SC0245 combined with irinotecan in patients with advanced malignant solid tumors who have failed standard treatment, or have no standard treatment options, or are not currently suitable for standard treatment, or cannot tolerate standard treatment, and to determine the MTD and RP2D of SC0245 in combination therapy. Secondary objectives: PK characteristics, preliminary anti-tumor activity. The main purpose of the Ib expansion phase is to evaluate the safety and tolerability of SC0245 combined with irinotecan in patients with extensive-stage SCLC who have failed or are intolerant to first-line platinum-containing chemotherapy (with or without immunotherapy); secondary objectives: PK characteristics, preliminary anti-tumor activity. The main purpose of the Phase II phase is to evaluate the preliminary anti-tumor activity of SC0245 combined with irinotecan in patients with extensive-stage SCLC who have failed or are intolerant to first-line platinum-containing chemotherapy (with or without immunotherapy). Secondary objectives: safety and tolerability.

Start Date01 Feb 2023

Sponsor / Collaborator

Wuxi Zhikang Hongyi Biological Technology Co Ltd

CTR20210769 / RecruitingPhase 1

一项开放、单臂的剂量递增和剂量扩展的临床研究，在晚期恶性实体瘤患者评估 SC0245 的安全性、耐受性、药代动力学特征与初步有效性

[Translation] An open-label, single-arm, dose-escalation and dose-expansion clinical study to evaluate the safety, tolerability, pharmacokinetic characteristics and preliminary efficacy of SC0245 in patients with advanced malignant solid tumors

第一阶段（剂量递增阶段）：主要目的： -评估 SC0245 单药在晚期恶性实体瘤患者的安全性和耐受性； -确定 SC0245 的剂量限制毒性（Dose-Limiting Toxicity， DLT）和最大耐受剂量（MTD）或 II 期推荐剂量（RP2D）。次要目的： - 评估 SC0245 单药在晚期恶性实体瘤患者中的药代动力学（PK）特征； -评估 SC0245 单药在晚期恶性实体瘤患者中的初步抗肿瘤活性。第二阶段（剂量扩展阶段）主要目的：进一步评估 SC0245 单药在晚期恶性实体瘤患者的安全性和耐受性。次要目的： -进一步在多种特定肿瘤类型中初步评价 SC0245 单药在晚期恶性实体瘤患者中的抗肿瘤活性。 -进一步探索生物标记物与临床疗效之间的关系。

[Translation]

Phase I (Dose Escalation Phase): Primary Objectives: - To evaluate the safety and tolerability of SC0245 monotherapy in patients with advanced malignant solid tumors; - To determine the dose-limiting toxicity (DLT) and maximum tolerated dose (MTD) or Phase II recommended dose (RP2D) of SC0245. Secondary Objectives: - To evaluate the pharmacokinetic (PK) characteristics of SC0245 monotherapy in patients with advanced malignant solid tumors; - To evaluate the preliminary anti-tumor activity of SC0245 monotherapy in patients with advanced malignant solid tumors. Phase II (Dose Expansion Phase) Primary Objectives: To further evaluate the safety and tolerability of SC0245 monotherapy in patients with advanced malignant solid tumors. Secondary Objectives: - To further preliminarily evaluate the anti-tumor activity of SC0245 monotherapy in patients with advanced malignant solid tumors in multiple specific tumor types. - To further explore the relationship between biomarkers and clinical efficacy.

Start Date29 Jun 2021

Sponsor / Collaborator

Shijiazhuang Zhikang Hongren New Drug Development Co., Ltd.

100 Clinical Results associated with SC-0245

100 Translational Medicine associated with SC-0245

100 Patents (Medical) associated with SC-0245

Literatures (Medical) associated with SC-0245

01 Apr 2014·Investigational New DrugsQ3 · MEDICINE

Synthesis and in vitro characterization of ionone-based compounds as dual inhibitors of the androgen receptor and NF-κB

Q3 · MEDICINE

Article

Author: Jinming Zhou ; Jian Hui Wu ; Rongtuan Lin ; Weiguo Liu ; Guoyan Geng

Current therapeutic strategy for advanced prostate cancer is to suppress the androgen receptor (AR) signaling. However, lethal castration-resistant prostate cancer (CRPC) arises due to AR reactivation via multiple mechanisms, including mutations in the AR and cross-talk with other pathways such as NF-κB. We have previously identified two ionone-based antiandrogens (SC97 and SC245), which are full antagonists of the wild type and the clinically-relevant T877A, W741C and H874Y mutated ARs. Here, we discovered SC97 and SC245 also inhibit NF-κB. By synthesizing a series of derivatives of these two compounds, we have discovered a novel compound 3b that potently inhibits both AR and NF-κB signalling, including the AR F876L mutant. Compound 3b showed low micromolar antiproliferative activites in C4-2B and 22Rv1 cells, which express mutated ARs and are androgen-independent, as well as DU-145 and PC-3 cells, which exhibit constitutively activated NF-κB signalling. Our studies indicate 3b is effective against the CRPC cells.

01 Jan 2005·Journal of ImmunotoxicologyQ4 · MEDICINE

Screening New Drugs for Immunotoxic Potential: II. Assessment of the Effects of Selective and Nonselective COX-2 Inhibitors on Complement Activation, Superoxide Anion Production and Leukocyte Chemotaxis and Migration Through Endothelial Cells

Q4 · MEDICINE

ArticleOA

Author: John Mennear ; Sylvia M. Furst ; K. Nasir Khan ; Lian Fan ; Wendy J. Komocsar

Results from earlier experiments in our laboratories revealed that both selective and nonselective inhibitors of cyclooxygenase-2 possess little potential for decreasing in vitro phagocytosis by rat macrophages or canine neutrophils and no potential for decreasing in vivo phagocytosis by the intact murine immune system. We now report the results of studies to assess in vitro and ex vivo effects of the drugs on 1) canine complement activation, 2) generation of superoxide anion and hydrogen peroxide (oxidative burst) by canine neutrophils, and 3) leukocytic chemotaxis and transmigration through endothelial cell monolayers. In vitro concentrations of naproxen sodium, SC-236, SC-245, and SC-791 ranging from 0.1 to 10 muM were tested for their abilities to inhibit canine complement-mediated hemolysis of opsonized sheep erythrocytes and to block phorbol myristate acetate-induced oxidative burst in canine neutrophils. Both models responded to known inhibitory agents, leupeptin in the complement activation test and staurosporine in the superoxide anion assay. In contrast, tested nonsteroidal anti-inflammatory drugs produced only trivial changes in complement activation and superoxide anion production. Experiments on plasma and neutrophils isolated from dogs administered an experimental selective COX-2 inhibitor during a 28-day toxicology study revealed no evidence of drug-associated changes in complement activation or formation of superoxide anion. SC-791 reduced chemotaxis of canine leukocytes toward zymosan-activated dog plasma, but not toward leukotriene B(4). None of the other drugs tested significantly affected leukocytic chemotaxis. Ibuprofen, SC-245 and SC-791 but not SC-236, reduced transmigration of canine leukocytes through endothelial cell monolayers. Based on the results of these experiments and our earlier studies we have concluded that, although high (suprapharmacologic) concentrations of the drugs may induce in vitro evidence of apparent immunomodulation of the innate immune system, the findings are unlikely to represent a significant human health risk.

01 Jan 2005·Journal of ImmunotoxicologyQ4 · MEDICINE

Screening New Drugs for Immunotoxic Potential: I. Assessment of the Effects of Conventional Nonsteroidal Anti-Inflammatory Drugs and Selective COX-2 Inhibitors onIn VitroandIn VivoPhagocytic Activity

Q4 · MEDICINE

ArticleOA

Author: John H. Mennear ; K. Nasir Khan ; Kimber L. White ; Sylvia M. Furst ; Wendy J. Komocsar ; Vanessa L. Peachee

Although both experimental and clinical literature contain reports suggestive of associations between enhanced susceptibility to soft tissue infections and nonsteroidal anti-inflammatory drug (NSAID) use, the immunotoxicological potential of this class of therapeutic agents has not been thoroughly investigated. In consideration of the widespread clinical use of these agents, we have initiated studies of the interaction between NSAIDs (both nonselective and selective COX-2 inhibitors) and the immune system. This communication describes the conduct and results of assessments of the effects of NSAIDs on the in vitro phagocytic activity of rat macrophages and canine neutrophils and on the functional activity of the intact murine mononuclear phagocytic system. During in vitro experiments 0.1 to 10 muM concentrations of naproxen, indomethacin, and experimental selective COX-2 inhibitors, SC-236, SC-245 and SC-791, caused marginal, but statistically significant, reductions in phagocytic activity of resident rat peritoneal macrophages. The effects were consistently small and there was no evidence of concentration-response relationships. An in vitro concentration of 10 muM of either SC-236 or SC-791 was required to decrease phagocytosis by dog neutrophils. Repeated oral doses of either naproxen or SC-236 (3, 10, or 30 mg/kg twice daily for 3 days) were without effect on the intact phagocytic system of the mouse. A potential immunotoxicologic effect based on direct impairment of phagocytic processes seems an unlikely explanation for drug-induced susceptibility to infection reported earlier. However, the results of these experiments do not support an unequivocal conclusion relative to immunotoxicological potential of either conventional NSAIDs or selective COX-2 inhibitors. Further studies on other components of the immune system are needed to fully explore possible immunomodulatory effects of NSAIDs.

100 Deals associated with SC-0245

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Small cell lung cancer recurrent	Phase 2	CN	Wuxi Zhikang Hongyi Biological Technology Co Ltd	23 Feb 2023
Advanced Malignant Solid Neoplasm	Phase 1	CN	Shijiazhuang Zhikang Hongren New Drug Development Co., Ltd.	29 Jun 2021

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT05731518 (NCT05731518, ASCO2024)	Phase 1/2	Small cell lung cancer recurrent ATR	15	SC0245 80mg QD	(wbguhrswfe) = izgqkwbznb qkmjxzyole (vaubspwaei )	Positive	24 May 2024
				SC0245 120mg QD	(wbguhrswfe) = ceubkzoned qkmjxzyole (vaubspwaei )

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