The 2023 Top-Selling Drugs
Here we investigate the top 200 drugs by retail sales in 2023, we extract some insightful statistics, and we highlight the uses of the top 10 drugs that are deposited in the Cambridge Structural Database (CSD).
The statistics quoted are correct at the time of writing, September 2024. The structures available in the CSD are constantly updated, so this may change.
The Origins and the Statistics
In 2010 the Njarðarson research group (University of Arizona) published a graphical representation of the top selling drugs in 2008 [1]. They wanted to inspire students and researchers by showing the importance and real-life use of these products. Since then, the team have created yearly posters that highlight the top 200 drugs by retail sales, which can be easily accessed by the public and downloaded.
Inspired by this work, our CCDC Scientific Editor Philip Andrews created a modified version of the 2023 poster that highlights the structures found in the CSD (colour coded in green) and in the Protein Data Bank, PDB (colour coded in grey).
Download here the high-resolution file of the poster that includes the top-selling drugs in the CSD.
Looking at the poster we can see that 53% are small molecule drugs, while 47% are biological molecules. 79 drugs out of the 200 top-selling drugs in 2023 (39.5%) have at least one component included in the CSD, while 94 out of the 200 drugs (47%) are included in the PDB.
The remaining 27 drugs (13.5%, colour coded in white) are small molecules that have not been deposited in the CSD yet. These pharmaceutical compounds are most likely included in patents, and hence protected by intellectual property. Our editorial team at the CCDC works constantly to reduce the number of published compounds with no crystal structure deposited in the CSD. They search for patents and publications, and contact the pharmaceutical companies involved, aiming to add the missing compounds to the CSD and further enrich the database and the learnings which can be drawn from it.
Diving Deeper Into the 2023 Top-Selling Drugs
Valuable knowledge can be extracted from the poster shown above.
Starting by looking at the top 10 drugs from the 200 top-selling drugs in 2023, we can see that these are used in the following therapeutic areas: oncology, cardiology and vascular diseases, diabetes, immunology, and infectious diseases (Table 1).
The retail sales from each of the top 10 ranking drugs can be also seen in Table 1, as well as their ranking in the year 2020. A comparison of the latter to that of year 2023 shows a significative jump to higher positions for drugs used in the treatment of diabetes, such as Ozempic and Jardiance, which gained respectively 33 and 18 places. A minor loss in ranking was seen instead for Humira, Stelara and Opdivo of respectively -3, -1 and -2 places from year 2020.
| 2023 Rank | Brand Name | Sales | Therapeutic Area | 2020 Rank |
| 1 | Keytruda | $25.011 Billion | Oncology | 2 |
| 2 | Eliquis | $18.953 Billion | Cardiology/ Vascular Diseases | 3 |
| 3 | Ozempic | $18.468 Billion | Diabetes | 36 |
| 4 | Humira | $14.494 Billion | Immunology | 1 |
| 5 | Biktarvy | $11.850 Billion | Infectious Diseases | 11 |
| 6 | Dupixent | $11.565 Billion | Immunology | 10 |
| 7 | Stelara | $11.297 Billion | Immunology | 6 |
| 8 | Comirnaty | $11.220 Billion | Infectious Diseases | N/A |
| 9 | Jardiance | $10.600 Billion | Diabetes | 27 |
| 10 | Opdivo | $10.010 Billion | Oncology | 8 |
Looking instead at the therapeutic areas of the 200 top-selling drugs in 2023 (Figure 1), it can be seen that 52 out of 200 are used in oncology (26%), 27 are used in immunology (13.5%), 24 are used in infectious diseases (12%), 23 are used in neurology (11.5%) and 17 are used for the treatment of diabetes (8.5%). The remaining 28.5% is split between 14 different therapeutic areas that are less populated. In Figure 1 it is possible to also see how many drugs are in the CSD, PDB or Not Deposited in the CSD for each of the most popular therapeutic areas.
A closer look at the 79 small molecule drugs currently in the CSD, shows that oncology is the most populated therapeutic area for small molecules as well, with a total of 18 drugs out of 79 (22.8%, Figure 2). Infectious diseases are at the second place, with 16 drugs (20.3%), followed by neurology with 12 (15.2%), and cardiology and vascular diseases with 11 (13.9%). The remaining 27.8% is split between 10 different therapeutic areas that are less populated (Figure 2).
Top 10 Small Molecule Drugs in the CSD
The top 10 ranking drugs from the 200 top-selling drugs in 2023 accounted for a total of $143.468 Billion in retail sales, a value that indicates their importance and the impact that these medicines have in the treatment of a variety of diseases.
Among these, 7 drugs can be found in the PDB, while 3 are deposited in the CSD. We will now outline the rankings of the latter, what they are used for, and some information about their crystal structures.
Jardiance (Brand Name) ‒ Empagliflozin (Component Drug Name)
Jardiance is a drug that contains empagliflozin as the active substance and is found at the ninth position of the ranking. The retail sales for Jardiance were $10.600 Billion in 2023.
Jardiance is used to treat type 2 diabetes, chronic (long-term) heart failure and chronic kidney disease [2].
Deposited as a CSD Communication in 2018 (CSD Entry: NIQBIB, Figure 3), the crystal structure of empagliflozin was further studied in 2023 (CSD Entry: NIQBIB01) by the scientists who also determined its absolute configuration (Journal of Molecular Structure 2024, 1301, 137331).
Biktarvy ‒ Bictegravir, Emtricitabine and Tenofovir Alafenamide
At the fifth position we find Biktarvy, a drug that contains bictegravir, emtricitabine and tenofovir alafenamide as the active substances. The retail sales for Biktarvy were $11.850 Billion in 2023.
Biktarvy is an antiviral medicine used to treat patients infected with human immunodeficiency virus 1 (HIV-1), a virus that causes acquired immune deficiency syndrome (AIDS) [3].
Among the three components that are included in Biktarvy, the structures of emtricitabine (CSD Entry: HAKJIM, Figure 4) and tenofovir alafenamide (CSD Entry: BUKQOQ, Figure 5) are deposited in the CSD. While the first dates back to 1994 (Antiviral Chemistry and Chemotherapy, 1993, 4, 369), the solid state properties of the latter were investigated more recently. In particular, novel polymorphs of tenofovir alafenamide fumarate were studied, and the possibility for these to exist as co-crystals, salts, or pure forms was investigated (Pharmaceutics, 2020, 12, 342).
Eliquis ‒ Apixaban
At the second position of the top 10 ranking drugs there is Eliquis, a drug that contains apixaban as the active substance. The retail sales for Eliquis were $18.953 Billion in 2023.
Eliquis is used to prevent venous thromboembolism (blood clots in the veins) in adults following a hip or knee replacement operation, to prevent and treat deep vein thrombosis and pulmonary embolism, to prevent stroke and blood clots in other organs in adults with atrial fibrillation [4].
The drug was developed by Bristol-Myers Squibb and Pfizer, and its crystal structure, CSD Entry: NUPQEW in Figure 6, is known since 2015, when scientists crystallized it and investigated its interactions with human serum albumin (HAS, a blood plasma protein), aiming to elucidate the binding mechanism and site (RSC Advances, 2015, 5, 81696).
Top Selling Drug of 2023; Keytruda ‒ Pembrolizumab
Finally, the leader of the 200 top-selling drugs in 2023 is a drug that can be found in the PDB (PDB Entry: 5DK3), Keytruda, which contains pembrolizumab as the active substance. The retail sales for Keytruda were $25.011 Billion in 2023.
In adults, Keytruda is mainly used to treat a variety of cancers that are advanced, have spread or returned, are not responding to other treatments or cannot be removed by surgery. In children, Keytruda is used to treat Hodgkin lymphoma [5].
References
[1] J. Chem. Ed. 2010, 87, 1348.
[2] Jardiance | European Medicines Agency (EMA).
[3] Biktarvy | European Medicines Agency (EMA).