Famitinib

Famitinib
Legal status
Legal status	Investigational;
Identifiers
	IUPAC name 5-[2-(Diethylamino)ethyl]-2-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-3-methyl-6,7-dihydro-1H-pyrrolo[3,2-c]pyridin-4-one;
CAS Number	1044040-56-3;
PubChem CID	16662431;
IUPHAR/BPS	7886;
DrugBank	DB11741;
ChemSpider	17595500;
UNII	768FW21J3L;
ChEMBL	ChEMBL1278146;
CompTox Dashboard (EPA)	DTXSID301358976 ;
Chemical and physical data
Formula	C23H27FN4O2
Molar mass	410.493 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCN(CC)CCN1CCC2=C(C1=O)C(=C(N2)/C=C\3/C4=C(C=CC(=C4)F)NC3=O)C;
	InChI InChI=1S/C23H27FN4O2/c1-4-27(5-2)10-11-28-9-8-19-21(23(28)30)14(3)20(25-19)13-17-16-12-15(24)6-7-18(16)26-22(17)29/h6-7,12-13,25H,4-5,8-11H2,1-3H3,(H,26,29)/b17-13-; Key:GKEYKDOLBLYGRB-LGMDPLHJSA-N;

Famitinib is a tyrosine kinase receptor inhibitor developed by Jiangsu Hengrui for a variety of cancers.^[1]^[2]^[3]^[4]^[5]^[6]

References

^ Chen, Li; Jiang, Yi-Zhou; Wu, Song-Yang; Wu, Jiong; Di, Gen-Hong; Liu, Guang-Yu; Yu, Ke-Da; Fan, Lei; Li, Jun-Jie; Hou, Yi-Feng; Hu, Zhen; Chen, Can-Ming; Huang, Xiao-Yan; Cao, A-Yong; Hu, Xin; Zhao, Shen; Ma, Xiao-Yan; Xu, Ying; Sun, Xiang-Jie; Chai, Wen-Jun; Guo, Xiaomao; Chen, Xizi; Xu, Yanhui; Zhu, Xiao-Yu; Zou, Jian-Jun; Yang, Wen-Tao; Wang, Zhong-Hua; Shao, Zhi-Ming (1 July 2022). "Famitinib with Camrelizumab and Nab-Paclitaxel for Advanced Immunomodulatory Triple-Negative Breast Cancer (FUTURE-C-Plus): An Open-Label, Single-Arm, Phase II Trial". Clinical Cancer Research. 28 (13): 2807–2817. doi:10.1158/1078-0432.CCR-21-4313. PMC 9365373. PMID 35247906.
^ Xie, Cen; Zhou, Jialan; Guo, Zitao; Diao, Xingxing; Gao, Zhiwei; Zhong, Dafang; Jiang, Haoyuan; Zhang, Lijia; Chen, Xiaoyan (April 2013). "Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients". British Journal of Pharmacology. 168 (7): 1687–1706. doi:10.1111/bph.12047. PMC 3605876. PMID 23126373.
^ Qu, Yuan-Yuan; Zhang, Hai-Liang; Guo, Hongqian; Luo, Hong; Zou, Qing; Xing, Nianzeng; Xia, Shujie; Sun, Zhongquan; Zhang, Xuepei; He, Chaohong; Cai, Jinling; Zhang, Xiao; Wang, Quanren; Ye, Ding-Wei (1 November 2021). "Camrelizumab plus Famitinib in Patients with Advanced or Metastatic Renal Cell Carcinoma: Data from an Open-label, Multicenter Phase II Basket Study". Clinical Cancer Research. 27 (21): 5838–5846. doi:10.1158/1078-0432.CCR-21-1698. PMID 34400414. S2CID 237150083.
^ Zhou, Aiping; Zhang, Wen; Chang, Chunxiao; Chen, Xiaoyan; Zhong, Dafang; Qin, Qiong; Lou, Donghua; Jiang, Haoyuan; Wang, Jinwan (November 2013). "Phase I study of the safety, pharmacokinetics and antitumor activity of famitinib". Cancer Chemotherapy and Pharmacology. 72 (5): 1043–1053. doi:10.1007/s00280-013-2282-y. PMID 24043137. S2CID 22355164.
^ Xia, Lingfang; Zhou, Qi; Gao, Yunong; Hu, Wenjing; Lou, Ge; Sun, Hong; Zhu, Jianqing; Shu, Jin; Zhou, Xianfeng; Sun, Rong; Wu, Xiaohua (2022-12-08). "A multicenter phase 2 trial of camrelizumab plus famitinib for women with recurrent or metastatic cervical squamous cell carcinoma". Nature Communications. 13 (1). Springer Science and Business Media LLC: 7581. doi:10.1038/s41467-022-35133-4. ISSN 2041-1723. PMC 9732039. PMID 36481736.
^ Xu, Rui-Hua; Shen, Lin; Wang, Ke-Ming; Wu, Gang; Shi, Chun-Mei; Ding, Ke-Feng; Lin, Li-Zhu; Wang, Jin-Wan; Xiong, Jian-Ping; Wu, Chang-Ping; Li, Jin; Liu, Yun-Peng; Wang, Dong; Ba, Yi; Feng, Jue-Ping; Bai, Yu-Xian; Bi, Jing-Wang; Ma, Li-Wen; Lei, Jian; Yang, Qing; Yu, Hao (2017). "Famitinib versus placebo in the treatment of refractory metastatic colorectal cancer: a multicenter, randomized, double-blinded, placebo-controlled, phase II clinical trial". Chinese Journal of Cancer. 36 (1). Springer Science and Business Media LLC: 97. doi:10.1186/s40880-017-0263-y. ISSN 1944-446X. PMC 5741870. PMID 29273089.

[1] Chen, Li; Jiang, Yi-Zhou; Wu, Song-Yang; Wu, Jiong; Di, Gen-Hong; Liu, Guang-Yu; Yu, Ke-Da; Fan, Lei; Li, Jun-Jie; Hou, Yi-Feng; Hu, Zhen; Chen, Can-Ming; Huang, Xiao-Yan; Cao, A-Yong; Hu, Xin; Zhao, Shen; Ma, Xiao-Yan; Xu, Ying; Sun, Xiang-Jie; Chai, Wen-Jun; Guo, Xiaomao; Chen, Xizi; Xu, Yanhui; Zhu, Xiao-Yu; Zou, Jian-Jun; Yang, Wen-Tao; Wang, Zhong-Hua; Shao, Zhi-Ming (1 July 2022). "Famitinib with Camrelizumab and Nab-Paclitaxel for Advanced Immunomodulatory Triple-Negative Breast Cancer (FUTURE-C-Plus): An Open-Label, Single-Arm, Phase II Trial". Clinical Cancer Research. 28 (13): 2807–2817. doi:10.1158/1078-0432.CCR-21-4313. PMC 9365373. PMID 35247906.

[2] Xie, Cen; Zhou, Jialan; Guo, Zitao; Diao, Xingxing; Gao, Zhiwei; Zhong, Dafang; Jiang, Haoyuan; Zhang, Lijia; Chen, Xiaoyan (April 2013). "Metabolism and bioactivation of famitinib, a novel inhibitor of receptor tyrosine kinase, in cancer patients". British Journal of Pharmacology. 168 (7): 1687–1706. doi:10.1111/bph.12047. PMC 3605876. PMID 23126373.

[3] Qu, Yuan-Yuan; Zhang, Hai-Liang; Guo, Hongqian; Luo, Hong; Zou, Qing; Xing, Nianzeng; Xia, Shujie; Sun, Zhongquan; Zhang, Xuepei; He, Chaohong; Cai, Jinling; Zhang, Xiao; Wang, Quanren; Ye, Ding-Wei (1 November 2021). "Camrelizumab plus Famitinib in Patients with Advanced or Metastatic Renal Cell Carcinoma: Data from an Open-label, Multicenter Phase II Basket Study". Clinical Cancer Research. 27 (21): 5838–5846. doi:10.1158/1078-0432.CCR-21-1698. PMID 34400414. S2CID 237150083.

[4] Zhou, Aiping; Zhang, Wen; Chang, Chunxiao; Chen, Xiaoyan; Zhong, Dafang; Qin, Qiong; Lou, Donghua; Jiang, Haoyuan; Wang, Jinwan (November 2013). "Phase I study of the safety, pharmacokinetics and antitumor activity of famitinib". Cancer Chemotherapy and Pharmacology. 72 (5): 1043–1053. doi:10.1007/s00280-013-2282-y. PMID 24043137. S2CID 22355164.

[Xia_Zhou_Gao_Hu_2022_p.-5] Xia, Lingfang; Zhou, Qi; Gao, Yunong; Hu, Wenjing; Lou, Ge; Sun, Hong; Zhu, Jianqing; Shu, Jin; Zhou, Xianfeng; Sun, Rong; Wu, Xiaohua (2022-12-08). "A multicenter phase 2 trial of camrelizumab plus famitinib for women with recurrent or metastatic cervical squamous cell carcinoma". Nature Communications. 13 (1). Springer Science and Business Media LLC: 7581. doi:10.1038/s41467-022-35133-4. ISSN 2041-1723. PMC 9732039. PMID 36481736.

[Xu_Shen_Wang_Wu_2017_p.-6] Xu, Rui-Hua; Shen, Lin; Wang, Ke-Ming; Wu, Gang; Shi, Chun-Mei; Ding, Ke-Feng; Lin, Li-Zhu; Wang, Jin-Wan; Xiong, Jian-Ping; Wu, Chang-Ping; Li, Jin; Liu, Yun-Peng; Wang, Dong; Ba, Yi; Feng, Jue-Ping; Bai, Yu-Xian; Bi, Jing-Wang; Ma, Li-Wen; Lei, Jian; Yang, Qing; Yu, Hao (2017). "Famitinib versus placebo in the treatment of refractory metastatic colorectal cancer: a multicenter, randomized, double-blinded, placebo-controlled, phase II clinical trial". Chinese Journal of Cancer. 36 (1). Springer Science and Business Media LLC: 97. doi:10.1186/s40880-017-0263-y. ISSN 1944-446X. PMC 5741870. PMID 29273089.

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