Larotinib/Larotinib efficacy, role and price

Larotrectinib, a novel inhibitor of tropomyosin receptor kinase (TRK)/Larotrectinib was obtained from the U.S. Food and Drug Administration (FDA)Approved to market as Vitrakvi, a first-in-class drug that has been specifically approved to treat patients with tumors characterized by neurotrophic receptor tyrosine kinase (NTRK) gene fusions.

Larotrectinib demonstrated significant efficacy in inhibitingTRKA, TRKB and TRKC kinases (IC50=6.5, 8.1, 10.6 nmol/L) while exhibiting significant selectivity for these specific targets compared to other kinases. Orally administered larotrectinib is a potent TRK inhibitor with well-established antitumor properties. After administration, larotrectinib binds to TRK, effectively blocking the interaction between neurotrophins and TRK receptors, thereby hindering TRK activation. Therefore, in malignant tumors characterized by TRK overexpression, this mechanism triggers apoptosis and inhibits tumor cell proliferation. Larotrectinib represents a significant milestone as the second drug approved for a tumor-agnostic indication.

The original drug larotrectinib has been launched in China, but it is not yet covered by medical insurance. Its 100mg 56-capsule capsules cost more than 70,000 yuan per box, while the 50ml:1.0g oral liquid version costs more than 20,000 yuan per bottle. The price of the Hong Kong version of capsules is slightly lower, at more than 20,000 yuan per box. The American, European and German versions of larotrectinib sold overseas cost approximately RMB 20,000 per box for capsules, and approximately RMB 10,000 per box for the oral liquid version. Prices may fluctuate due to exchange rate changes. In addition, there are also generic drugs available in overseas markets, such as capsules produced in Bangladesh and Laos, which are more economical at only more than 2,000 yuan per box, but they may also be affected by exchange rates.