A Phase 1/2, Open-Label, Multicenter, Dose-Finding Study of SKL27969 to Evaluate Safety, Tolerability, Pharmacokinetics, Pharmacodynamics, and Preliminary Efficacy in Patients With Advanced Solid Tumors

Primary Objective of Part 1 (Dose Escalation Phase): Evaluate the safety and tolerability of SKL27969, and determine the maximum tolerated dose (MTD) and/or recommended Phase 2 dose (RP2D) of SKL27969
Primary Objective of Part 2 (Dose Expansion Phase): Evaluate the preliminary anti-tumor activity of SKL27969

开始日期2022-09-12

申办/合作机构

SK Life Science, Inc.

100 项与 SKL-27969 相关的临床结果

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100 项与 SKL-27969 相关的转化医学

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100 项与 SKL-27969 相关的专利（医药）

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项与 SKL-27969 相关的文献（医药）

2022-06-14·Analytical chemistry

Calibration-free Solid-State Ion-Selective Electrode Based on a Polarized PEDOT/PEDOT-S-Doped Copolymer as Back Contact

Article

作者: Goswami, Subir ; Gernhart, Sarah ; Bahro, Christopher ; Koley, Dipankar

Solid-contact ion-selective electrodes (ISEs) have the inherent advantage of being miniaturized in addition to maintaining high selectivity and sensitivity of the ionophore-based ISE. The major disadvantage of ISEs is the necessity of performing a calibration curve (varying the intercept in the linear calibration curve equation) each time before running experiments, which limits their application as one-time disposable sensors or for use in remote water sample analysis. To overcome these challenges, we designed a unique back contact made of 3,4-ethylenedioxythiophene (EDOT) and 4-(2,3-dihydrothieno[3,4-b][1,4]dioxin-2-yl-methoxy)-1-butanesulfonic acid, sodium salt (EDOT-S). The calibration-free ISEs showed near Nernstian responses of 57.2 ± 0.2 mV/log [K⁺] and 28.5 ± 0.3 mV/log [Ca²⁺], while maintaining their respective selectivity against major interfering ions. The detection limits for Ca²⁺ and K⁺ ISEs were 0.45 ± 0.01 and 1.68 ± 0.18 μM, respectively. The charging cycles of the PEDOT: PEDOT-S back contact allowed us to fix the background potential at a desired fixed intercept value across different ionophores (K⁺, Ca²⁺). This protocol was used to determine the K⁺ and Ca²⁺ contents in creek water samples. The activity and concentration of [Ca²⁺] and [K⁺] in a local creek was found to be 257 ± 7.3 and 28.1 ± 1.1 μM, respectively.

2021-06-01·Naunyn-Schmiedeberg's archives of pharmacology4区 · 医学

Effects of the monoamine stabilizer, (-)-OSU6162, on cocaine-induced locomotion and conditioned place preference in mice

4区 · 医学

Article

作者: Marçal, Anna P ; Moreira, Fabrício A ; Aguiar, Daniele C ; Soares, Nícia P ; Asth, Laila ; Briânis, Rayssa C ; Iglesias, Lia P

Cocaine addiction is a severe mental disorder for which few treatment options are available. The underlying mechanisms include facilitation of monoamine-neurotransmission, particularly dopamine. Here, we tested the hypothesis that the monoamine stabilizers, (-)-OSU6162 ((3S)-3-(3-methylsulfonylphenyl)-1-propylpiperidine) and aripiprazole (7-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy]-3,4-dihydro-1H-quinolin-2-one), prevent cocaine-induced behaviors. Male Swiss mice received injections of (-)-OSU6162 or aripiprazole and cocaine and were tested for cocaine-induced hyperlocomotion, locomotor sensitization, and acquisition and expression of conditioned place preference (CPP). The increase in the distance traveled induced by cocaine (20 mg/kg) was prevented by pretreatment with aripiprazole (1 and 10 mg/kg), whereas (-)-OSU6162 (3 mg/kg) exerted a minor effect. Aripiprazole, however, also impaired spontaneous locomotion. Neither (-)-OSU6162 nor aripiprazole interfered with the locomotor sensitization and expression of CPP induced by cocaine (15 mg/kg). (-)-OSU6162 (3 mg/kg), but not aripiprazole, prevented the acquisition of CPP induced by cocaine (15 mg/kg). (-)-OSU6162 exerts a minor effect in reducing cocaine-induced stimulatory activity and context-related memories, which are responsible for triggering drug seeking. Further studies are required to establish whether (-)-OSU6162 could be a candidate drug for the treatment of cocaine addiction.

2019-06-01·Bioorganic chemistry2区 · 化学

Synthesis of C C, C N coupled novel substituted dibutyl benzothiazepinone derivatives and evaluation of their thrombin inhibitory activity

2区 · 化学

Article

作者: Basappa ; Sannaningaiah Devaraja ; Naveen Shivalingegowda ; Peter E. Lobie ; C.P. Baburajeev ; Shobith Rangappa ; Vijay Pandey ; Chakrabhavi Dhananjaya Mohan ; Kanchugarakoppal S. Rangappa ; Andreas Bender ; Leen Kalash

The formation of a thrombus is a key event in thromboembolic disorders, that contribute to high mortality and morbidity in affected patients. In the present study, we synthesized a library of novel substituted 3,3-dibutyl-8-methoxy-2,3-dihydrobenzo [b] [1,4] thiazepin-4(5H)-one derivatives which were tested for their platelet aggregation and thrombin inhibitory activity. Among the tested compounds, 3,3-dibutyl-7-(2-chlorophenyl)-8-methoxy-2,3-dihydrobenzo[b] [1,4]thiazepin-4(5H)-one (DCT) displayed the maximum thrombin inhibition with an IC₅₀ value of 3.85 μM and thus DCT was chosen for further studies. Next, the effect of DCT on primary hemostasis was evaluated using agonist-induced platelet aggregation model. The lead compound inhibited the collagen- or ADP- or thrombin-induced platelet aggregation in a dose-dependent manner. Furthermore, DCT prolonged the process of clot formation when evaluating plasma re-calcification time (320 ± 11 sec at 5 µg DCT), activated partial thromboplastin time (58.0 ± 0.01 sec at 2 µg), and prothrombin time (14.7 ± 0.01 sec at 5 µg). Molecular docking studies suggested that the benzothiazepinones evaluated here consistently display hydrogen bonding with Ser214 of thrombin, which is similar to that of the co-crystallized ligand (1-(2R)-2-amino-3-phenyl-propanoyl-N-(2,5dichlorophenyl)methylpyrrolidine-2-carboxamide). DCT displayed additional hydrogen bonding to Ser195 and π-π interactions between its methoxyphenyl groups and Trp60, thereby providing a structural rationale for the observed biological effect.

项与 SKL-27969 相关的新闻（医药）

2022-11-14

·PRNewswire

SK Biopharmaceuticals Receives Korea Drug Development Fund Investment Grant to Develop Novel Oncology Candidate, SKL27969

State-run financing to provide two-year support of Phase 1 research for oncology candidate, SKL27969, for the potential treatment of advanced solid tumors SK Biopharmaceuticals to present preclinical data on oncology candidate, SKL27969, at Society for Neuro-Oncology Conference PANGYO, South Korea, Nov. 13, 2022 /PRNewswire/ -- SK Biopharmaceuticals, a global innovative pharmaceutical company, announced that the state-run Korea Drug Development Fund (KDDF) has decided to support and finance the company's development of SKL27969, which is being evaluated as potential treatment for patients with advanced solid tumors, widening SK Biopharmaceuticals' area into oncology. The KDDF is a government fund that aims to support R&D for new drug development as part of efforts to advance Korea's pharmaceuticals and biotechnology sectors. A phase 1/2 clinical trial is being conducted under the US IND for SKL27969, a PRMT5 inhibitor, in adult patients with solid tumors for safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary efficacy. SK Biopharmaceuticals said the KDDF's two-year investment in the study will help the company and its U.S. subsidiary SK Life Science, Inc. to accelerate their clinical (Phase 1) and nonclinical trials, while expanding its oncology network. SK Biopharmaceuticals will present its preclinical data of SKL27969 at the annual Society for Neuro-Oncology (SNO) conference in Tampa Bay, Florida, November 16 - 20, 2022. About SKL27969 SKL27969 is a protein arginine methyltransferase 5 (PRMT5) inhibitor candidate that has shown activity in preclinical models of solid tumors, such as glioblastoma (GBM), non-small cell lung cancer (NSCLC), and triple negative breast cancer (TNBC). About SK Biopharmaceuticals Co., Ltd. and SK Life Science, Inc. SK Biopharmaceuticals and its U.S. subsidiary SK life science are pharmaceutical companies focused on the global research, development and commercialization of treatments for disorders of the central nervous system (CNS) and oncology. In 2017, SK Biopharmaceuticals established a research center to begin their expansion into oncology through research and development efforts. The companies have a pipeline of nine compounds in development in both CNS and oncology. For more information, visit SK Biopharmaceuticals' website at and SK life science's website at . Both SK Biopharmaceuticals and SK life science are part of SK Group, one of the largest conglomerates in Korea. SK Inc., the parent company of SK Biopharmaceuticals, continues to enhance its portfolio value by executing long-term investments with a number of competitive subsidiaries in various business areas, including pharmaceuticals and life science, energy and chemicals, information and telecommunication, and semiconductors. In addition, SK Inc. is focused on reinforcing its growth foundations through profitable and practical management based on financial stability, while raising its enterprise value by investing in new future growth businesses. For more information, please visit . Media Inquiries SK Biopharmaceuticals H. Park, Head of Communications Hyunkyung Cho, Deputy Communications Manager [email protected] SOURCE SK Biopharmaceuticals Co., Ltd

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适应症	最高研发状态	国家/地区	公司	日期
晚期恶性实体瘤	临床2期	美国	SK Life Science, Inc.	2022-09-12

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


EXTH-74 (SNO2023)	N/A	胶质母细胞瘤 SDMA \| phospho-Histone H3 \| pH2AX ... 更多	-	SKL27969 50 mg/kg (oral)	遞夢憲齋壓齋獵遞蓋網(鹹淵範網糧築鏇築齋製) = 獵鹽糧憲繭夢簾膚窪網襯淵繭積憲範襯獵願糧 (憲鏇鹹餘網選鬱鹹憲構 ) 更多	-	2023-11-10
				Placebo	遞夢憲齋壓齋獵遞蓋網(鹹淵範網糧築鏇築齋製) = 膚網繭醖齋餘構遞範網襯淵繭積憲範襯獵願糧 (憲鏇鹹餘網選鬱鹹憲構 ) 更多