Synlett
DOI: 10.1055/a-2564-4559
perspectives
Small Molecules in Medicinal Chemistry

Quinoline-Based FDA-Approved Drugs: Synthetic Route and Clinical Uses

Devesh Chandra
a   C–H Activation & Phytochemistry Lab, Chemical Technology Division, CSIR-IHBT, Palampur-176061, India
,
Sachin Sachin
a   C–H Activation & Phytochemistry Lab, Chemical Technology Division, CSIR-IHBT, Palampur-176061, India
b   Academy of Scientific and Innovative Research (AcSIR), Ghaziabad-201002, India
,
Shourabh Rav
a   C–H Activation & Phytochemistry Lab, Chemical Technology Division, CSIR-IHBT, Palampur-176061, India
,
Upendra Sharma
a   C–H Activation & Phytochemistry Lab, Chemical Technology Division, CSIR-IHBT, Palampur-176061, India
b   Academy of Scientific and Innovative Research (AcSIR), Ghaziabad-201002, India
› Author Affiliations
This work is funded by the Council of Scientific and Industrial Research, India (CSIR, FTT020503 and MMP035201).


Abstract

In the last 25 years, the U.S. Food and Drug Administration (FDA) approved 11 new molecular entities (NMEs) comprising quinoline as core moiety. These drugs are primarily used for the treatment of anemia, malaria, hepatitis, and various types of cancer, i.e., lung, breast, kidney, blood, and thyroid. Based on their approval date, a chronological discussion on these marketed drugs is provided. This Perspective summarizes the industrial synthesis, mechanism of action, and clinical uses of the quinoline-based FDA-approved NMEs of the 21st century.

1 Introduction

2 Quinoline-Based FDA-Approved Drugs

2.1 Mitapivat (2022)

2.2 Tivozanib (2021)

2.3 Capmatinib (2020)

2.4 Tafenoquine (2018)

2.5 Neratinib (2017)

2.6 Lenvatinib (2015)

2.7 Simeprevir (2013)

2.8 Bosutinib (2012)

2.9 Cabozantinib (2012)

2.10 Bedaquiline (2012)

2.11 Pitavastatin (2009)

3 Conclusion

4 Abbreviations



Publication History

Received: 22 January 2025

Accepted after revision: 21 March 2025

Accepted Manuscript online:
21 March 2025

Article published online:
20 May 2025

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