Highlights on US FDA-approved fluorinated drugs over the past five years (2018-2022)

被引：65

作者：

Ali, Saghir ^{[1
]}

Zhou, Jia ^{[1
]}

机构：

[1] Univ Texas Med Branch UTMB, Dept Pharmacol & Toxicol, Chem Biol Program, Galveston, TX 77555 USA

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2023年 / 256卷

基金：

美国国家卫生研究院;

关键词：

Fluorinated drugs; Fluorine; FDA-approved drugs; Drug development; Cancer; CNS disorders; Infectious diseases; PET imaging; Diagnosis; Therapeutics; Drug discovery; SELECTIVE NONSTEROIDAL INHIBITORS; RHEUMATOLOGY; 1990; CRITERIA; PEPTIDASE-IV INHIBITORS; CYSTIC-FIBROSIS; JANUVIA(TM) SITAGLIPTIN; BIOLOGICAL EVALUATION; CARBOXYLIC-ACID; HIGHLY POTENT; DOUBLE-BLIND; AMINO-ACIDS;

D O I：

10.1016/j.ejmech.2023.115476

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The objective of this review is to provide an update on the fluorine-containing drugs approved by U.S. Food and Drug Administration in the span of past five years (2018-2022). The agency accepted a total of fifty-eight fluorinated entities to diagnose, mitigate and treat a plethora of diseases. Among them, thirty drugs are for therapy of various types of cancers, twelve for infectious diseases, eleven for CNS disorders, and six for some other diseases. These are categorized and briefly discussed based on their therapeutic areas. In addition, this review gives a glimpse about their trade name, date of approval, active ingredients, company developers, in-dications, and drug mechanisms. We anticipate that this review may inspire the drug discovery and medicinal chemistry community in both industrial and academic settings to explore the fluorinated molecules leading to the discovery of new drugs in the near future.

引用

页数：12

共 125 条

[1] In vivo MRI cell tracking using perfluorocarbon probes and fluorine-19 detection [J].

Ahrens, Eric T. ;

Zhong, Jia .

NMR IN BIOMEDICINE, 2013, 26 (07) :860-871

[2] A Review of 177Lutetium-PSMA and 225Actinium-PSMA as Emerging Theranostic Agents in Prostate Cancer [J].

Alam, Mohammad R. ;

Singh, Shashi B. ;

Thapaliya, Shreeya ;

Shrestha, Shreeya ;

Deo, Sulav ;

Khanal, Kishor .

CUREUS JOURNAL OF MEDICAL SCIENCE, 2022, 14 (09)

[3] A Diverse Series of Substituted Benzenesulfonamides as Aldose Reductase Inhibitors with Antioxidant Activity: Design, Synthesis, and in Vitro Activity [J].

Alexiou, Polyxeni ;

Demopoulos, Vassilis J. .

JOURNAL OF MEDICINAL CHEMISTRY, 2010, 53 (21) :7756-7766

[4] I. Novel HCV NS5B polymerase inhibitors: Discovery of indole 2-carboxylic acids with C3-heterocycles [J].

Anilkumar, Gopinadhan N. ;

Lesburg, Charles A. ;

Selyutin, Oleg ;

Rosenblum, Stuart B. ;

Zeng, Qingbei ;

Jiang, Yueheng ;

Chan, Tin-Yau ;

Pu, Haiyan ;

Vaccaro, Henry ;

Wang, Li ;

Bennett, Frank ;

Chen, Kevin X. ;

Duca, Jose ;

Gavalas, Stephen ;

Huang, Yuhua ;

Pinto, Patrick ;

Sannigrahi, Mousumi ;

Velazquez, Francisco ;

Venkatraman, Srikanth ;

Vibulbhan, Bancha ;

Agrawal, Sony ;

Butkiewicz, Nancy ;

Feld, Boris ;

Ferrari, Eric ;

He, Zhiqing ;

Jiang, Chuan-kui ;

Palermo, Robert E. ;

Mcmonagle, Patricia ;

Huang, H. -C. ;

Shih, Neng-Yang ;

Njoroge, George ;

Kozlowski, Joseph A. .

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2011, 21 (18) :5336-5341

[5]

[Anonymous], 2020, MED LETT DRUGS THER, V62, P5

[6]

[Anonymous], 2018, MED LETT DRUGS THER, V60, P174

[7]

[Anonymous], 2018, MED LETT DRUGS THER, V60, P158

[8] Design, Synthesis, Biological Evaluation and Pharmacokinetics of Bis(hydroxyphenyl) substituted Azoles, Thiophenes, Benzenes, and Aza-Benzenes as Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) [J].

Bey, Emmanuel ;

Marchais-Oberwinkler, Sandrine ;

Werth, Ruth ;

Al-Soud, Yaseen A. ;

Kruchten, Patricia ;

Oster, Alexander ;

Frotscher, Martin ;

Birk, Barbara ;

Hartmann, Rolf W. .

JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (21) :6725-6739

[9] Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases [J].

Bey, Emmanuel ;

Marchais-Oberwinkler, Sandrine ;

Kruchten, Patricia ;

Frotscher, Martin ;

Werth, Ruth ;

Oster, Alexander ;

Alguel, Oztekin ;

Neugebauer, Alexander ;

Hartmann, Rolf W. .

BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (12) :6423-6435

[10] New Insights into the SAR and Binding Modes of Bis(hydroxyphenyl)thiophenes and -benzenes: Influence of Additional Substituents on 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) Inhibitory Activity and Selectivity [J].

Bey, Emmanuel ;

Marchais-Oberwinkler, Sandrine ;

Negri, Matthias ;

Kruchten, Patricia ;

Oster, Alexander ;

Klein, Tobias ;

Spadaro, Alessandro ;

Werth, Ruth ;

Frotscher, Martin ;

Birk, Barbara ;

Hartmann, Rolf W. .

JOURNAL OF MEDICINAL CHEMISTRY, 2009, 52 (21) :6724-6743

← 1 2 3 4 5 6 7 8 9 10 →