特考韦瑞是什么药？

(tecovirimat, code-named ST-246) is a small molecule virus inhibitor. The drug has strong activity against viruses of the genus Orthopoxvirus, such as smallpox virus, monkeypox virus, cowpox virus, etc. It can inhibit 50% of monkeypox virus in vitro replication at a concentration of 0.01umol/L. More importantly, it has high tolerance to animals with complete or partial loss of immune function.

About Tecovir

Tecovir is an effective and specific orthopoxvirus replication inhibitor developed by SIGA Technologies. It has antiviral effects against a variety of orthopoxviruses, including cowpox, monkeypox, mousepox and smallpox viruses. Tecovirimat has been approved by the European Medicines Agency (EMA) and the U.S. Food and Drug Administration (FDA) for the treatment of smallpox. In addition, the EMA has also approved Tecovirimat for the treatment of monkeypox. The U.S. Centers for Disease Control and Prevention (CDC) has authorized the use of Tecovirimat for the treatment of monkeypox under the expanded access investigational new drug (IND) program.

The role of Tecovirimat

Tecovirimat is a highly active small molecule virus inhibitor. Only 0.01 μM Tecovirimat can inhibit 50% of the in vitro replication of monkeypox virus. Its mechanism of action is to achieve therapeutic purposes by combining with viral genes to prevent the virus from being released within cells. Therefore, Tecovirib plays a therapeutic role in two aspects: preventing the virus from multiplying in cells and reducing the fatality rate of smallpox; preventing the virus from falling off the carrier and reducing the infection rate of smallpox. In addition, the combined use of Tecovir and smallpox vaccine can prevent and treat adverse reactions caused by the latter, reduce the level of damage, and accelerate wound healing.

The efficacy of Tecovirib

In a prospective study, 25 patients with monkeypox received Tecovirimat (oral) for 2 weeks. The results showed that on the 7th day of treatment, 10 patients (40%) had complete regression of skin lesions, and on the 21st day of treatment, a total of 23 patients (92%) had skin lesions and pain subsided. In addition, a British retrospective study found that patients treated with Tecovirimat had shorter symptom duration and upper respiratory tract virus shedding time than patients treated with other treatments [1].

In addition, Tecovirimat has also shown good efficacy in immunosuppressed patients. Take an adult male monkeypox patient as an example. The man suffered from AIDS, Kaposi's sarcoma and secondary syphilis. After 2 weeks of treatment, he was given 600 mg Tecovirimat twice a day, along with doxycycline, ceftriaxone and valacyclovir. The patient's skin lesions recovered quickly.

Safety of Tecovirimat

Tecovirimat is generally well tolerated, with only minor side effects. According to a clinical study using Tecovirimat to treat monkeypox, the most commonly reported adverse events after 7 days of treatment included fatigue in 7 patients (28%), headache in 5 patients (20%), nausea in 4 patients (16%), pruritus in 2 patients (8%), and diarrhea in 2 patients (8%). However, Tecovirimat injection is contraindicated in patients with severe renal impairment (creatinine clearance less than 30 mL·min-1).

Summary

In January 2022, the EMA approved the listing of tecoririmat. Based on animal studies, tecoririmat is effective in reducing deaths caused by smallpox, monkeypox and cowpox. Although the drug safety was evaluated in non-infected people, the adverse drug reactions of tecovirimat in infected people are expected to be similar and acceptable.

Monkeypox and cowpox are rare but life-threatening diseases for which there are no other approved treatments. In addition, although smallpox has been eradicated, it is an extremely serious infection and there is no available treatment if it occurs. The EMA believes that the benefits of tecoririmat outweigh the risks, and approved its marketing under "exceptional circumstances" for the treatment of smallpox, monkeypox, and cowpox infections in adults and children over 13 kg. It is also suitable for the treatment of complications caused by vaccinia virus replication in adults and children over 13 kg after vaccination with smallpox vaccine.

References

[1] Gao Xu, Peng Jin'e, Li Xingwang, et al. Current status of research on monkeypox antiviral drugs and vaccines [J]. Chinese Pharmacovigilance, 2024, 21(01): 111-116.DOI: 10.19803/j.1672-8629.20230690.

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