Top 10 Small Molecule Drugs: A Half were Oncology Drugs

Biological drugs have obtained unprecedented development in recent years with the rapid development of biotechnology, for example, the monoclonal antibody drug Humira has been the sales champion for years, and its sales even approached USD20 billion in 2018, however, owing to the long development history, small molecule drugs still have a huge share in the global market at present, and are the biggest source of drugs. Let’s check the top 10 small molecule drugs by sales in 2018 below.

Table I Top 10 Small Molecule Drugs by Sales in 2018

Table I shows the top 10 small molecule drugs by sales in 2018, and mainly displays the following highlights:

I. Total volume still big

Seen from Table I overall, sales of the top 10 small molecule drugs were considerable to reach over USD50 billion in 2018 (amount to more than RMB300 billion), showing a very huge volume.

II. The company with the most drugs listed—Pfizer

As one of the companies earliest in conducting small molecule drug R&D in the world, Pfizer had 3 drugs listed among the top 10, separately Lyrica (pregabalin) for epilepsy and neuropathy, Ibrance (palbociclib) for breast cancer, and Xtandi (enzalutamide) for prostatic cancer, followed by J & J with 2 drugs listed, separately Imbruvica (ibrutinib) for lymphoma and Zytiga (abiraterone acetate) for prostatic tumor.

III. The disease field involved by the most drugs listed—oncology

Studies on oncology drugs have been in full swing in recent years, and the oncology drug market has been extremely active. Not surprisingly, oncology drugs took 5 positions among the top 10 small molecule drugs by sales in 2018, making oncology the field involved by the most drugs listed.

The 5 listed oncology drugs were separately: Revlimid (lenalidomide) for multiple myeloma, Imbruvica (ibrutinib) for lymphoma, Ibrance (palbociclib) for breast cancer, Xtandi (enzalutamide) for prostatic cancer, and Zytiga (abiraterone acetate).

IV. Sales of two drugs approaching USD10 billion

From the perspective of individual drugs, sales of both the top 2 small molecule drugs approached USD10 billion, separately, the anticoagulant Eliquis with 2018 sales of USD9.872 billion and Revlimid (lenalidomide) for multiple myeloma with 2018 sales of USD9.685 billion. Let’s see details of the two drugs below. If you want to know more about pharma industry, Pharmasource, a professional platform for medical product suppliers, would be your best choice.

1. Anticoagulant Eliquis

Fig. II Structural Formula of Eliquis

As the small molecule drug with the highest sales in 2018, Eliquis achieved sales performance of USD9.872 billion in 2018. The important approval process of the drug jointly developed by Pfizer and BMS is as shown in Fig. III. The drug has now been indicated for the prevention of venous thromboembolism (VTE) in adult patients who have undergone hip or knee replacement surgery, prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation (NVAF), treatment of deep vein thrombosis (DVT) and pulmonary embolism (PE), and prevention of recurrence of DVT and PE, etc.

Fig. III Relevant Approvals of Eliquis

2. Revlimid (lenalidomide) for multiple myeloma

Fig. IV Structural Formula of Revlimid (Lenalidomide)

The structural formula of Revlimid (lenalidomide) is as shown in Fig. IV. It is an immunomodulator against tumors and used to control tumor cell proliferation, and is an oncology drug originally developed by the U.S. pharmaceutical giant Celgene. As shown in Fig. V, Revlimid (lenalidomide) was first marketed in the U.S. in 2005 for the treatment of myelodysplasia, then in 2006 was formally approved for multiple myeloma treatment, and was subsequently approved to treat tumors such as lymphoma and leukemia.

Fig. V Relevant Approvals of Revlimid (Lenalidomide)

The global pharmaceutical industry is rapidly growing at present, and the technical content of drugs becomes increasingly high especially with the improvement of the pharmaceutical development technology. Small molecule chemical drugs have been much impacted by biological drugs in recent years, creating the illusion that the drug world has been dominated by the biological drugs, however, it’s still difficult for biological drugs to replace chemical drugs in many fields, which can be seen from the above analysis.

About  the Author:    

Yuntian, Ph.D. in medicinal chemistry, is mainly engaged in small molecule drug research, especially good at small molecule drug synthesis process and later stage drug development research. He has completed the synthesis and activity evaluation of multiple anti-cancer drug molecules. 

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