预约演示
更新于：2026-08-22
Risovalisib Mesilate Hydrate
更新于：2026-08-22
概要
基本信息
原研机构- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2026-03-23), |
最高研发阶段(中国)临床2期 |
特殊审评- |
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结构/序列
分子式C25H33F3N8O8S2 |
InChIKeyCYWUJTNXNJVGLY-UHFFFAOYSA-N |
CAS号1494684-33-1 |
关联
9
项与 Risovalisib Mesilate Hydrate 相关的临床试验JPRN-jRCT2041250168
A Phase I/II, multicenter study to evaluate the safety, tolerability, pharmacokinetics characteristics, and efficacy of CYH33 in patinets with PIK3CA related overgrowth spectrum (PROS) and PIK3CA related vascular malformations (PRVM) (A Phase I/II study of CYH33 in Patients with PROS and PRVM)
NCT06975618
A Phase I/II, Multicenter Study to Evaluate the Safety, Tolerability, Pharmacokinetic Characteristics, and Efficacy of CYH33 (a Selective PI3Kα Inhibitor) in Patients With PIK3CA-related Overgrowth Spectrum (PROS) and PIK3CA-related Vascular Malformations (PRVM)
CTR20223417
[14C]CYH33在中国成年男性健康受试者体内的物质平衡临床试验
100 项与 Risovalisib Mesilate Hydrate 相关的临床结果
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100 项与 Risovalisib Mesilate Hydrate 相关的转化医学
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100 项与 Risovalisib Mesilate Hydrate 相关的专利（医药）
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18
项与 Risovalisib Mesilate Hydrate 相关的文献（医药）2026-06-01International Journal of Clinical Oncology
PMDA regulatory update on approval and revision of the precautions for use of anticancer drugs in Japan; trastuzumab deruxtecan for solid tumors, talazoparib for prostate cancer, sacituzumab govitecan for breast cancer, darolutamide for salivary gland cancer, risovalisib for ovarian cancer, and mosunetuzumab plus polatuzumab vedotin for lymphoma
作者: Matsumura, Noriomi
2026-05-01ACTA PHARMACOLOGICA SINICA
Targeting intrinsic and CAF-mediated signaling by PI3Kα inhibitor CYH33 attenuated metastasis in lung squamous cell carcinoma
Article
作者: Xu, Lan ; Cao, Zhe-Rui ; Ding, Jian ; Meng, Ling-Hua ; Ma, Xiao-Yu ; Deng, Jie-Ting
Aberrant activation of PI3K signaling is frequently observed in lung squamous cell carcinoma (LUSC) and is strongly associated with metastasis in advanced-stage patients, but the therapeutic efficacy of PI3K inhibitors and underlying mechanisms in LUSC remain poorly defined. CYH33 is a highly selective PI3Kα inhibitor, which is in phase I/II clinical trials for the therapy of advanced solid tumors including LUSC. In this study, we investigated the efficacy of CYH33 against metastatic LUSC. We showed that CYH33 dose-dependently suppressed the motility of LUSC cells by blocking PI3K signaling and disrupting cytoskeletal structure. Oral administration of CYH33 significantly attenuated the metastasis of orthotopically implanted xenografts derived from LUSC SK-MES-1 cells. RNA-seq and GO enrichment analysis revealed that CYH33 treatment resulted in decreased infiltration of cancer-associated fibroblasts (CAFs) in primary tumors. We demonstrated that CAFs promoted the migration of SK-MES-1 cells by secreting the pro-migratory factors and activating PI3K signaling in tumor cells, which was blocked by CYH33. Moreover, CYH33 concurrently suppressed the trans-differentiation and proliferation of CAFs, thereby reducing the secretion of hepatocyte growth factor (HGF), which likely contributed to its anti-metastatic effect. Consistently, co-inoculation of SK-MES-1 cells with fibroblasts significantly potentiated tumor metastasis in nude mice, whereas CYH33 treatment robustly suppressed this process, accompanied with reduced expression of α-SMA and HGF as well as epithelial-mesenchymal transition (EMT) signature in primary tumor. Furthermore, CYH33 possessed potent activity against the growth of LUSC with hyperactivated PI3K signaling. Collectively, the dual-targeting of CYH33 that directly blocked PI3Kα in tumor cells and disrupted CAF-mediated pro-metastatic signaling supported PI3Kα inhibitors as a potential therapeutic approach for advanced LUSC.
2024-11-01Molecular Oncology
Cell‐free DNA from ascites identifies clinically relevant variants and tumour evolution in patients with advanced ovarian cancer
Article
作者: Caroline E. Ford ; Kristina Warton ; Bonnita Werner ; Ramanand Athavale ; Yeh Chen Lee ; Marilisa Cortesi ; Jennifer Duggan ; Michael Dean ; Elyse Powell ; Vivek Arora
The emergence of targeted therapies has transformed ovarian cancer treatment. However, biomarker profiling for precision medicine is limited by access to quality, tumour‐enriched tissue samples. The use of cell‐free DNA (cfDNA) in ascites presents a potential solution to this challenge. In this study, next‐generation sequencing was performed on ascites‐derived cfDNA samples (26 samples from 15 human participants with ovarian cancer), with matched DNA from ascites‐derived tumour cells (n = 5) and archived formalin‐fixed paraffin‐embedded (FFPE) tissue (n = 5). Similar tumour purity and variant detection were achieved with cfDNA compared to FFPE and ascites cell DNA. Analysis of large‐scale genomic alterations, loss of heterozygosity and tumour mutation burden identified six cases of high genomic instability (including four with pathogenic BRCA1 and BRCA2 mutations). Copy number profiles and subclone prevalence changed between sequential ascites samples, particularly in a case where deletions and chromothripsis in Chr17p13.1 and Chr8q resulted in changes in clinically relevant TP53 and MYC variants over time. Ascites cfDNA identified clinically actionable information, concordant to tissue biopsies, enabling opportunistic molecular profiling. This advocates for analysis of ascites cfDNA in lieu of accessing tumour tissue via biopsy.
100 项与 Risovalisib Mesilate Hydrate 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 卵巢透明细胞癌 | 日本 | 2026-03-23 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| PIK3CA相关的过度生长现象 | 临床2期 | 中国 | 2023-08-10 | |
| PIK3CA相关脉管畸形 | 临床2期 | 中国 | 2023-08-10 | |
| 输卵管透明细胞腺癌 | 临床2期 | 中国 | 2022-07-12 | |
| 输卵管透明细胞腺癌 | 临床2期 | 中国 | 2022-07-12 | |
| 原发性腹膜透明细胞癌 | 临床2期 | 中国 | 2021-10-11 | |
| 原发性腹膜透明细胞癌 | 临床2期 | 日本 | 2021-10-11 | |
| PIK3CA突变/HR阳性/HER2阴性乳腺癌 | 临床1期 | 中国 | 2021-07-09 | |
| PIK3CA突变/HR阳性/HER2阴性乳腺癌 | 临床1期 | 澳大利亚 | 2021-07-09 | |
| 晚期乳腺癌 | 临床1期 | - | 2021-04-01 | |
| HR阳性/HER2阴性乳腺癌 | 临床1期 | - | 2021-04-01 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | - | 襯醖糧觸遞簾膚糧構遞(獵艱獵衊憲夢築壓夢簾) = 本次适应症的上市许可申请主要基于CYH33-G201关键II期研究的有效性和安全性数据。 網鬱夢網築簾鬱窪艱鏇 (遞顧醖築憲積選壓壓鏇 ) | 积极 | 2025-08-15 | |||
临床1期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 HER2 Negative | PIK3CA Mutation | HR Positive | 52 | 窪襯積醖廠齋顧蓋糧鹽(積襯繭壓餘網構鹹憲艱) = CYH33 30mg QD + Fulvestrant 500mg 願憲膚艱鏇簾鑰襯衊夢 (願壓壓鏇醖衊鹹網襯齋 ) 更多 | 积极 | 2024-05-24 | ||
(PIK3CA-mutations without prior fulvestrant treatment) | |||||||
临床1期 | PIK3CA H1047R突变的实体瘤 PIK3CA Mutation | 51 | (overall) | 鬱願襯鹹鏇壓鏇觸廠願(齋範構膚鬱築鬱鬱膚膚) = 觸繭構簾構襯獵鬱觸糧 積夢構鬱鬱襯顧鹹觸醖 (廠窪膚齋窪憲選繭觸繭 ) 更多 | 积极 | 2022-11-16 | |
(patients with PIK3CA mutations) | 構蓋鹽積蓋鏇鏇廠糧築(願鑰製夢艱選壓憲襯觸) = 鏇鹽憲餘選膚襯築製糧 齋憲範鑰廠鹹繭鬱糧製 (鹹餘齋壓積夢顧膚齋鬱 ) |
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