VV116 is an oral nucleoside analog RNA-dependent RNA polymerase (RdRp) inhibitor with broad-spectrum antiviral potential. Its tablet formulation for the treatment of COVID-19 has been approved for marketing in China (brand name: 民得维^®) and Uzbekistan (brand name: Mindvy^®). 民得维^® is the first orally administered nucleoside anti-SARS-CoV-2 drug to receive full approval with no genotoxicity risk. It demonstrates significant clinical efficacy, favorable safety, minimal drug-drug interactions, and few contraindications for combination therapy.

VV116 showed the significant anti-SARS-CoV-2 activity in preclinical studies. At the cellular level, VV116 exhibited potent inhibitory activity against both the original SARS-CoV-2 strain and  major variants of concern. In mouse models infected with the original strain, VV116 reduced the lung viral load to below the detection limit and significantly ameliorated pulmonary pathology.

A Phase III clinical trial published in The Lancet Infectious Diseases demonstrated that oral VV116 tablets significantly shortened the time to clinical recovery and reduced viral load in patients, with an incidence of adverse events comparable to that of the placebo. Another Phase III trial published in The England Journal of Medicine showed that VV116 tablets were non-inferior in efficacy to Paxlovid^® and were associated with a lower incidence of adverse events. The clinical trial conducted in Uzbekistan showed that VV116 tablets significantly reduced the risk of disease progression to critical illness or death in patients with moderate to severe COVID-19.

Additionally, VV116 demonstrated no relevant toxicity risk in standardized genotoxicity assessments, indicating a favorable safety profile. In elderly patients and those with mild renal impairment or mild-to-moderate hepatic impairment, VV116 exhibited good safety and tolerability without requiring dose adjustment. Clinical pharmacological studies have also confirmed that VV116 has minimal drug-drug interactions, significantly reducing contraindications for concomitant medications and thereby providing patients with a safer and more flexible treatment option.

The safety and efficacy of VV116 tablets in treating COVID-19 have been validated through clinical and real-world studies, garnering broad recognition from authoritative experts both in China and internationally. Even prior to its conditional approval in China, the editors-in-chief of The New England Journal of Medicine publicly offered positive remarks on VV116. In light of its significant clinical benefits, the editor-in-chief of Trends in Antiviral Drug Development invited the R&D team to contribute a comprehensive review on the development of VV116, which was subsequently published as a dedicated chapter in the book.

VV261 is a novel nucleoside double prodrug with broad-spectrum antiviral potential. It has demonstrated inhibitory activity against a variety of RNA viruses, including bunyaviruses, chikungunya virus, SARS-CoV-2, influenza viruses, and arenaviruses. Currently, VV261 is being clinically developed for the treatment of Severe Fever with Thrombocytopenia Syndrome (SFTS) caused by the novel bunyavirus (SFTSV) infection and is in Phase I study. Preclinical studies indicate that VV261 potently inhibits SFTSV, with its inhibitory potency surpassing that of the positive control drug, favipiravir. In an SFTSV-infected Ifnar1 gene knockout mouse model, VV261 effectively suppressed viral replication in multiple tissues (including spleen, liver, heart, lungs, and kidneys), ameliorated virus-induced hematological abnormalities and splenic pathology, and exhibited a clear dose-response relationship. Notably, 100% survival was achieved in the mid- and high-dose groups, whereas all animals in the model control group succumbed.

LV232 is a novel investigational antidepressant that acts as a dual modulator of both the serotonin transporter (5-HTT) and the 5-HT₃ receptor. It is currently in Phase II study. Research indicates that inhibition of 5-HTT increases serotonin concentration in the synaptic cleft, thereby alleviating depressive symptoms. Antagonism of the 5-HT₃ receptor not only mitigates adverse effects such as nausea and vomiting—which are commonly associated with 5-HTT inhibition—but also elevates levels of norepinephrine and acetylcholine in the brain, contributing to improved emotional and cognitive symptoms. Compared to marketed selective serotonin reuptake inhibitor (SSRI) antidepressants, LV232 is anticipated to demonstrate a more favorable gastrointestinal tolerability profile and potentially better patient compliance in clinical practice.

Preclinical studies have shown that LV232 exhibits excellent blood-brain barrier permeability, with a brain-to-plasma ratio of approximately 15 in cynomolgus monkeys. It demonstrated significant antidepressant effects across multiple animal models of depression. Results from Phase I clinical trials indicate that LV232 has a favorable safety profile with a low incidence of adverse events, all of which were mild in severity. LV232 also displays excellent pharmacokinetic properties. Notably, oral administration of LV232 capsules in healthy adults achieved a level of 5-HTT occupancy in the brain comparable to that of the highest clinically recommended dose of escitalopram.

TPN102 is a novel investigational anti-seizure drug candidate currently in Phase I clinical studies. While its precise mechanism of action for seizure control is still under investigation, available data suggest that it may be related to the modulation of sodium and calcium ion channels.

Preclinical studies have demonstrated that TPN102 exhibits significant efficacy in multiple animal models of drug-resistant epilepsy, with a superior protective effect against seizures compared to the positive control drugs topiramate (TPM) and zonisamide (ZNS). Furthermore, in vitro study indicate that TPN102 shows a significantly lower inhibitory effect on carbonic anhydrase II (CA-II)—an enzyme related to childhood growth and development—than TPM and ZNS, suggesting its potential suitability for long-term treatment in pediatric and adolescent epilepsy patients. Phase I clinical studies reveal that TPN102 has a favorable safety profile, with an incidence of adverse events comparable to that of the placebo group. It also displays excellent pharmacokinetic properties; systemic exposure in healthy subjects increased proportionally with dose following single oral administration of TPN102 across different dose levels.

VV119 is a novel, multi-target investigational antipsychotic drug candidate. It exerts its therapeutic effects by modulating key targets including dopamine receptors and serotonin receptors, and is currently in Phase I clinical study.

In multiple animal models, VV119 has demonstrated significant improvements across the positive symptoms, negative symptoms, and cognitive impairments associated with schizophrenia. It is anticipated to provide therapeutic benefits for all three core symptom domains in clinical settings, with a potentially more favorable safety profile. Results from Phase I clinical trials show that VV119 has a good safety profile. In multiple-dose studies involving healthy subjects, it did not cause common antipsychotic-related adverse events such as elevated prolactin levels or extrapyramidal symptoms. With a long half-life, VV119 is suitable for development into a long-acting formulation, which is expected to enhance patient compliance.

TPN171 is a highly active and highly selective PDE5 inhibitor with a novel chemical structure. Its tablet formulation for the treatment of erectile dysfunction (ED) has been approved and marketed in China (brand name: 昂伟达^®) and Uzbekistan (brand name: Onvita^®). 昂伟达^® has demonstrated significant clinical efficacy and a favorable safety profile, offering broad applicability across diverse patient populations and usage scenarios. It possesses the potential to become a Best-in-Class therapy.

Preclinical studies have shown that TPN171 is a potent PDE5 inhibitor and can significantly enhance penile erectile function in SD rats, Beagle dogs, and rabbits. A Phase III clinical trial demonstrated the marked clinical efficacy of TPN171 tablets. The recommended clinical starting dose is lower than that of other approved PDE5 inhibitors. When taken on demand at doses of 2.5 mg, 5 mg, and 10 mg, the respective rates for successful vaginal penetration were as high as 88.67%, 90.33%, and 92.02% (representing increases of 40.58%, 42.43%, and 43.98%). The respective rates for successful intercourse completion were 70.52%, 72.09%, and 74.65% (increases of 61.91%, 63.70%, and 65.19%). The respective Erectile Function domain scores of the International Index of Erectile Function (IIEF-EF) reached 25.7, 25.6, and 26.1 points (increases of 12.3, 12.3, and 12.7 points), approaching the normal range (≥26 points is considered normal).

TPN171 tablets demonstrate a superior safety profile, with a lower overall incidence of clinical adverse events compared to other approved PDE5 inhibitors. The Phase III clinical trial showed that at doses of 2.5 mg, 5 mg, and 10 mg, TPN171 had a lower incidence of common adverse events such as headache (2.6%, 3.2%, and 3.7%, respectively) and dyspepsia (0%, 0.5%, and 0.5%, respectively). Due to its weaker inhibition of other PDE subtypes (which are associated with side effects), TPN171 has not shown or rarely causes related adverse events. For instance, no visual abnormalities (associated with PDE6 inhibition) or adverse events like back pain and myalgia (associated with PDE11 inhibition) were observed. Additionally, the incidence of flushing (associated with PDE1 inhibition) was lower than that reported for sildenafil.

TPN171 tablets offer rapid onset of action, becoming effective within 30 minutes after oral administration, making them suitable for on-demand use. Their duration of action is well-balanced, with a half-life of 8 to 11 hours, which aligns well with natural daily rhythms. The efficacy of TPN171 is not affected when taken with moderate amounts of alcoholic beverages. Furthermore, TPN171 tablets have broad applicability and can be used by special patient populations, including the elderly, and those with mild to moderate hepatic impairment or mild, moderate, to severe renal impairment.