The Pharmaceutical Industry in 2019. An Analysis of FDA Drug Approvals from the Perspective of Molecules

Abstract

During 2019, the US Food and Drug Administration (FDA) approved 48 new drugs (38 New Chemical Entities and 10 Biologics). Although this figure is slightly lower than that registered in 2018 (59 divided between 42 New Chemical Entities and 17 Biologics), a year that broke a record with respect to new drugs approved by this agency, it builds on the trend initiated in 2017, when 46 drugs were approved. Of note, three antibody drug conjugates, three peptides, and two oligonucleotides were approved in 2019. This report analyzes the 48 new drugs of the class of 2019 from a strictly chemical perspective. The classification, which was carried out on the basis of chemical structure, includes the following: Biologics (antibody drug conjugates, antibodies, and proteins); TIDES (peptide and oligonucleotides); drug combinations; natural products; and small molecules.

Keywords: API; TIDES; antibodies; antibody drug conjugate; biologics; chemical entities; drug discovery; fluorine-based drugs; natural products; oligonucleotides; peptides; pyrazoles; small molecules.

Figure 1

New chemical entities and biologics approved by the FDA in the last two decades [1,6].

Figure 2

Structure of enfortumab vedotin and polatuzumab vedotin.

Figure 3

Structure of Fam-trastuzumab deruxtecan.

Figure 4

Structure of Ga 68 dodecanetetraacetic acid-Tyr3-octeotride (DOTA-TOC).

Figure 5

Structure of α-melanocyte-stimulating hormone (αMSH) vs. afamelanotide.

Figure 6

Structure of bremelanotide.

Figure 7

Comparison of the sequences of afamelanotide and bremelanotide (in pink, the common part).

Figure 8

Structure of Golodirseen.

Figure 9

Structure of givosiran.

Figure 10

Structure of Trikafta^TM, a drug combination (in green the structure of pyrazole, in blue the fluorine).

Figure 11

Structure of Recarbrio^TM, a combination drug.

Figure 12

Structure of the natural product-based drugs (in blue the fluorine).

Figure 13

Structure of drugs containing fluoroaryl moieties.

Figure 14

Structures of drugs containing trifluoromethyl groups.

Figure 15

Structure of pretomanid.

Figure 16

Structure of drugs, containing pyrazole/indazole moieties (* denotes a chiral center).

Figure 17

Structure of cenobamate, triclabendazole, and tafamidis.

Figure 18

Structure of tenapanor, trifarotene, and pitolisant.

Figure 19

Structure of ferric maltol and Tissue Blue.

Figure 20

Drugs approved by the FDA in 2019 and classified on the basis of their chemical structure (drugs could belong to two different classes).