Top 10 small molecule drugs in global sales

The diseases treated by top 200 small molecule drugs include tumors, immunity, diabetes, and cardiovascular diseases. The following introduces the top ten small molecule drugs in sales.

Top 1 ($14.117 billion): Apixaban (Eliquis, apixaban)

Apixaban is a coagulation factor Xa (Factor Xa) inhibitor, which was launched in Europe and the United States in 2011 and 2012, respectively, for the prevention of postoperative venous thromboembolism (VTE) in patients and the prevention of stroke in patients with atrial fibrillation.

Top 2 (US$12.106 billion): Lenalidomide (Revlimid, Lenalidomide)

Lenalidomide is a classic case of new use of old drugs, and its predecessor is the infamous "thalidomide" thalidomide. In the 1990s, scientists discovered that thalidomide has anti-cancer effects. After molecular modification of it, lenalidomide was obtained. The latter was approved for marketing in 2005 for the treatment of multiple myeloma (MM) and myeloma Diseases such as dysplastic syndrome (MDS). Later, scientists discovered that lenalidomide induced the E3 ligase Cereblon (CRBN) to degrade the target protein through the mechanism of molecular glue, and lenalidomide/lenalidomide was also reborn due to its wide application in the field of protac and molecular glue.

Top 3 ($9.442 billion): Ibruvica (Ibrutinib)

Ibrutinib was launched in the United States in 2013 and is the world's first BTK inhibitor for the treatment of hematological tumors such as mantle cell lymphoma, chronic lymphocytic leukemia/small lymphocytic lymphoma and Waldenstrom's macroglobulinemia.

Top 4 ($7.806 billion): Rivaroxaban (Xarelto, Rivaroxaban)

Rivaroxaban and apixaban are both Factor Xa inhibitors. Rivaroxaban is also the first drug to be marketed for this target (in Europe and the United States in 2008 and 2011, respectively).

Top 5 ($7.259 billion): Biktarvy

Biktarvy (bictegravir 50mg/EMTRICITABINE 200 mg/tenofovir alafenamide 25 mg, BIC/FTC/TAF) is a new three-in-one compound drug that was launched in 2018 for the treatment of HIV. Among them, bictegravir is an inhibitor of HIV-1 integrase, emtricitabine and tenofovir alafenamide are both nucleoside analogs and act as reverse transcriptase inhibitors.

Top 6 ($5.392 billion): Pabocini (Ibrance, Palbociclib)

Pabocinil was launched in the United States in 2015 and is the world's first cyclin-dependent kinase (CDK) 4/6 inhibitor. Its indications are: 1) First-line use in combination with aromatase inhibitors (such as letrozole) Treatment of ER+/HER2-type advanced breast cancer; 2) Combination with Fulvestrant to treat ER+/HER2-type advanced breast cancer that has progressed after previous endocrine therapy.

Top 7 ($5.1 billion): Enzalutamide (Xtandi, Enzalutamide)

Enzalutamide is an androgen receptor (AR) inhibitor, which was launched in 2012 for the treatment of castrated prostate cancer and metastatic hormone-sensitive prostate cancer.

Top 8 ($4.328 billion): Osimertinib (Tagrisso, Osimertinib)

Osimertinib is a third-generation EGFR inhibitor. It was approved by the FDA in November 2015 in just two and a half years. It was approved in China in March 2017, setting a record for the fastest import of new anti-cancer drugs into the country. Osimitinib is used in the first-line treatment of EGFR-positive NSCLC patients.

Top 9 (US$4.108 billion): Empagliflozin (Jardiance, Empagliflozin)

Enpagliflozin is a sodium-glucose cotransporter-2 (SGLT2) inhibitor, which was approved by the FDA in August 2014 to improve the blood sugar control of adult patients with type 2 diabetes (T2D) and reduce the heart of adult patients with T2D. Vascular risk.

Top 10 ($3.864 billion): Trikafta (Elexacaftor, Tezacaftor, Ivacaftor)

Trikafta was approved by the FDA in October 2019 for the treatment of cystic fibrosis (cystic fibrosis, cystic fibrosis, which has at least one F508del mutation or other effective mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene of 6 years and older). CF) patients.