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Antiviral API
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Cytomegalovirus (CMV)
CAS No. | Product Name | Inquiry |
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160369-77-7 |
Fomivirsen sodiumFomivirsen sodium, an antisense 21 mer phosphorothioate oligonucleotide, is an antiviral drug used in cytomegalovirus retinitis (CMV) studies, including AIDS. It binds to and degrades mRNAs encoding the CMV immediate early 2 protein (required for viral replication), thereby providing biological activity for CMV retinitis by inhibiting viral proliferation. |
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175865-60-8 |
ValganciclovirIn cell culture model systems using Caco-2 cells for PEPT1 and SKPT cells for PEPT2, valganciclovir inhibited glycylsarcosine transport mediated by PEPT1 and PEPT2 with K(i) values (inhibition constant) of 1.68+/-0.30 and 0.043+/- 0.005 mM, respectively. The inhibition by valganciclovir was competitive in both cases.37 patients were enrolled; 19 patients received treatment with VGV and 18 patients received treatment with GCV. The VGV was not inferior in efficacy to GCV as pre-emptive therapy, with rates of viral clearance at 28 days of 89.5% and 83%, respectively (P-value for non-inferiority = 0.030). Toxicities were similar between the 2 arms. No patients developed CMV disease. Patients being treated with an alemtuzumab-containing regimen received prophylaxis with either valaciclovir 500 mg orally daily orvalganciclovir 450 mg orally twice daily. None of the 20 patients randomized to valganciclovir experienced CMV reactivation (P = .004). |
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176161-24-3 |
Maribavir1263W94 inhibited viral replication in a dose-dependent manner, with a mean 50% inhibitory concentration (IC50) of 0.12 ± 0.01 μM compared to a mean IC50 for GCV of 0.53 ± 0.04 μM, as measured by a multicycle DNA hybridization assay. Maribavir inhibits viral genome copy numbers and infectivity to levels similar to and exceeding levels produced by BGLF4 knockout virus. Introduction of 1.0 or 10 nM maribavir, a known pUL97 inhibitor, and subsequent Lineweaver-Burk analysis demonstrated competitive inhibition of CPV phosphorylation, with a Ki of 3.0+/-0.3 nM. Maribavir has significant activity against both human cytomegalovirus (CMV) and Epstein-Barr virus, but not other herpesviruses. Unlike ganciclovir, which needs to be phosphorylated by UL 97 kinase to become an active inhibitor of DNA polymerase, maribavir directly inhibits UL 97 kinase. |
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207226-35-5 |
Calcium trinatrium diethylenetriaminepentaacetic acid hydrateCalcium trinatrium diethylenetriaminepentaacetic acid hydrate is a metal chelator and useful antidote (such as acute cadmium intoxication), as well as a non-toxic CMV replication inhibitor. |
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233254-24-5 |
TomeglovirTomeglovir is a potent and selective inhibitor of cytomegalovirus (CMV) replication. |
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233255-39-5 |
BAY-43-9695 |
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2467411-25-0 |
Fiztasovimab |
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255730-18-8 |
ArtemifoneArtemifone is a potent and semi-synthetic antimalarial agent that can inhibit p. falciparum with an average IC50 value of 0.83 nM. It is also a potent human CMV inhibitor. |
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351351-75-2 |
Braco-19Braco-19 is a potent telomerase/telomere inhibitor that prevents telomerase catalysis. Braco-19, as a G-quadruplex (GQ) binding ligand, stabilizes GQ formation at 3V telomeric DNA overhang and produces rapid senescence or selective cell death. It is also an HAdV virus replication inhibitor. |
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352554-02-0 |
SIRT1-IN-1SIRT1-IN-1 is an inhibitor of cytomegalovirus (CMV) with antiviral activity. SIRT1-IN-1 is a selective SIRT1 inhibitor with an IC50 of 0.205 μM. It inhibits SIRT2 with an IC50 of 11.5 μM. |
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391680-92-5 |
5,6-Dihydroxy-2-thiophen-2-yl-pyrimidine-4-carboxylic acid methyl esterpUL89 Endonuclease-IN-1 (Compound 13d) is a potent inhibitor of human cytomegalovirus (HCMV) pUL89 endonuclease with the IC50 value of 0.88 μM and has antiviral activitiy. |
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50-91-9 |
FloxuridineFloxuridine is an antineoplastic antimetabolite, used in the treatment of colon carcinoma and colorectal cancer that has metastasized to the liver. |
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519021-48-8 |
pUL89-Endonuclease-IN-2pUL89 Endonuclease-IN-2 (Compound 15k) is a potent inhibitor of human cytomegalovirus (HCMV) pUL89 endonuclease with the IC50 of 3.0 μM. |
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520-32-1 |
TricinTricin, a natural flavonoid isolated from the herb of Avena sativa, exhibits potential activity of anti-inflammatory, and has diverse biological activities including antigrowth activity in several human cancer cell lines and cancer chemopreventive effects in the gastrointestinal tract of mice, might be beneficial in HSC-targeting therapeutic or chemopreventive applications for hepatic fibrosis.Tricin exerts potential role as a chemopreventive and anticancer agent, which indicates the compound is a potential multifunctional nutraceutical. |
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55726-47-1 |
EnocitabineEnocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator. Enocitabine inhibits the replication of human cytomegalovirus. Enocitabine has antileukemic and antiviral activities. |
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607368-97-8 |
SB-734117SB-734117 is a human cytomegalovirus (HCMV) replication inhibitor that blocks CREB and histone H3 post-translational modifications. SB-734117 has a variety of pharmacological effects and is an inhibitor of several proteins in the AGC and CMCG kinase groups. |
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632325-71-4 |
FilociclovirFilociclovir is a broad-spectrum anti-herpesvirus compound with good antiviral activity against cytomegalovirus (CMV), herpes simplex virus (HHV)-6 and HHV-8, with EC50 values ranging from 0.7 μM to 8 μM. |
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69304-47-8 |
BrivudineBrivudine, also known as bromovinyl-deoxyuridine, is a uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator of transcription 3), which may result in the downregulation of vascular endothelial growth factor (VEGF). BVDU has also been found to inhibit the upregulation of chemoresistance genes (Mdr1 and DHFR) during chemotherapy. Overall, the gene expression changes associated with BVDU treatment result in the decrease or prevention of chemoresistance. In addition, this agent has been shown to enhance the cytolytic activity of NK-92 natural killer cells towards a pancreatic cancer cell line in vitro. |
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82410-32-0 |
GanciclovirGanciclovir is an antiviral drug for feline herpesvirus type-1 with IC50 of 5.2 μM. |
|
86357-14-4 |
Triacetyl-ganciclovir |
What is Cytomegalovirus?
Cytomegalovirus (CMV) is a DNA virus of the herpesvirus group, also known as cell inclusion body virus, which is called cytomegalovirus because the infected cells are enlarged and have large intranuclear inclusion bodies. CMV is widespread and can be infected in humans and other animals. The one that infects humans is called human cytomegalovirus (HCMV), officially known as human herpesvirus 5 (HHV-5).
Cytomegalovirus belongs to the herpesvirus subfamily, which is the largest genome member of the herpesvirus family, with a diameter of about 120~200nm, double-stranded DNA, which can encode more than 200 proteins. CMV is mostly a latent infection, most people are infected with latent infection, usually do not develop the disease, but when the body is immunodeficient or the immune system is in a suppressed state, it will be very susceptible to CMV infection, such as patients receiving immunosuppressive therapy after organ transplantation, patients after chemotherapy or radiotherapy for malignant tumors, AIDS patients, etc. Infection in these patients often leads to high mortality and severe illness.
Cytomegalovirus infection process
The pathological mechanism of cytomegalovirus (CMV) infection is complex, including viral invasion, replication, latent and reactivation. CMV first enters the body through contact with body fluids (e.g., saliva, urine, blood, etc.) of an infected person and infects host cells. The DNA of the virus enters the nucleus, where it begins to replicate and assemble new viral particles, causing the cell to expand and inclusions appear within the nucleus.
CMV can replicate in various cells of the human body, mainly infecting macrophages, endothelial cells, and monocytes. Myeloid cells may be the latent site of CMV, which maintains a long-term latent equilibrium state through intermittent activation under the surveillance of the immune system. CMV is weak in pathogenicity, mostly asymptomatic infection, and generally has little impact on healthy people, but can cause serious health hazards to newborns and special populations with suppressed or immunocompromised immune function. The pathogenic mechanism of CMV is not fully understood, and it may be related to the replication of CMV in target cells and the production of inclusions that cause cell lysis and death.
CMV-related diseases
Cytomegalovirus (CMV) infection can lead to a variety of diseases, especially in patients with compromised immune systems. In healthy individuals, CMV infection is usually asymptomatic or presents with only mild flu-like symptoms. However, in neonates, AIDS patients, organ transplant recipients, and cancer patients, CMV infection can cause serious complications.
Congenital CMV infection: Congenital CMV infection is the first infection of CMV during pregnancy by a pregnant woman, and the virus is transmitted to the fetus through the placenta. Infected newborns may develop hearing loss, mental retardation, epilepsy, and other neurological problems.
CMV infection in immunosuppressed patients: Patients with compromised immune systems, such as AIDS patients and organ transplant recipients, are vulnerable to CMV infection. These patients may develop cytomegalovirus pneumonia, gastroenteritis, retinitis, and encephalitis. CMV pneumonia and gastroenteritis can cause severe respiratory and gastrointestinal symptoms, while retinitis can lead to vision loss.
Mononucleosis-like syndrome: Mononucleosis-like syndrome occasionally occurs in healthy adults following CMV infection, with symptoms including prolonged fever, fatigue, hepatosplenomegaly, and lymphadenopathy.
Cytomegalovirus test
Diagnostic methods for CMV infection include serologic testing, viral culture, and molecular biology techniques.
Serologic testing: CMV infection can be determined by measuring the levels of CMV antibodies (IgM and IgG) in the blood. IgM antibodies usually appear during the acute phase of infection, while IgG antibodies indicate past infection.
Viral culture: CMV can be detected directly by culturing the virus in body fluids (e.g., saliva, urine, blood) of infected patients. However, virus culture takes a long time and is technically complex.
Molecular biology techniques: Such as polymerase chain reaction (PCR), are one of the most commonly used methods for diagnosing CMV because they can detect CMV DNA quickly and sensitively.
Cytomegalovirus treatment
The main principle of treatment for CMV infection is antiviral therapy. Patients with CMV infection in immunocompromised people should be treated aggressively.
Ganciclovir/Valganciclovir: Ganciclovir (GCV) or its prodrug valganciclovir (VGCV) is an acyclic nucleoside analogue that is the antiviral drug of choice for the treatment of confirmed HCMV disease. Intravenous ganciclovir is preferred for initial treatment of congenital CMV infection, and after 2 to 6 weeks, when the patient is stable and oral agents are acceptable, switch to oral valganciclovir, which is recommended to be started within 1 month of life. Preterm infants with acquired CMV infection who are eligible for oral administration may be treated with valganciclovir as the first choice. Patients who initially receive intravenous ganciclovir can be switched to valganciclovir after they are stable and can tolerate oral feeding.
Foscarnet: An inorganic pyrophosphate with broad spectrum activity that is a second-line treatment for cytomegalovirus and is not recommended for prophylactic and preemptive treatment. Two important uses of foscarnet are early after hematopoietic stem cell transplantation and in the treatment of GCV-resistant HCMV infections in transplant recipients and in patients with HIV/AIDS. The main adverse effects of sodium fluorophosphonate were renal impairment and electrolyte imbalance.
Cidofovir: Among nucleotide analogues, intravenous Cidofovir (CDV) is the first drug to receive FDA approval for the treatment of HCMV infection in HIV patients and transplant recipients. Cidofovir has high inhibitory activity against cytomegalovirus and is widely used in the prevention and treatment of cytomegalovirus infection in immunocompromised patients. The most common adverse effect of cidofovir is dose-limiting nephrotoxicity, which can lead to irreversible nephrotoxicity in severe cases.
Letmovir: A new non-nucleoside anti-cytomegalovirus drug approved by the FDA for the prevention of HCMV infection and disease in adults with HCMV seropositive receptors. The drug can be made into intravenous preparations and oral preparations, mainly used to prevent CMV infection and the development of CMV disease after infection.
Maribavir: A novel anti-cytomegalovirus (CMV) drug that blocks viral replication by inhibiting the pUL97 protein kinase. The drug is approved by the FDA for the treatment of refractory cytomegalovirus (CMV) infection in adult or child patients over 12 years of age who have undergone hematopoietic stem cell transplantation (HSCT) or solid organ transplantation (SOT) and have not responded to other available CMV infection antiviral drugs. Common side effects of Maribavir include abnormal taste, nausea, diarrhea, vomiting and fatigue.
Cytomegalovirus (CMV) infection can be asymptomatic in healthy individuals, but can be life-threatening in immunocompromised patients. BOC Sciences offers innovative drugs for the prevention and control of CMV, providing a wider range of clinical prevention options and new strategies for the prevention and control of CMV.
Reference
- Farrell, Helen E., and Philip G. Stevenson. Cytomegalovirus host entry and spread. Journal of General Virology 100.4 (2019): 545-553.
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