Simnotrelvir Ritonavir
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Simnotrelvir Ritonavir
Simnotrelvir/ritonavir (trade name Xiannuoxin) is a pharmaceutical drug used for the treatment of COVID-19. Simnotrelvir/ritonavir is a combination drug of simnotrelvir, an inhibitor of SARS-CoV-2 3CLpro, and ritonavir, a CYP3A inhibitor. It was developed by Simcere Pharmaceutical and conditionally approved in China by the National Medical Products Administration (NMPA) in January 2023. Results for the phase Ib trial are available. In a phase II/III trial, it reduced the duration of symptoms by a median of 36 hours compared to placebo. See also * Nirmatrelvir/ritonavir Nirmatrelvir/ritonavir, sold under the brand name Paxlovid, is a co-packaged medication used as a treatment for COVID19. It contains the antiviral medications nirmatrelvir and ritonavir and was developed by Pfizer. Nirmatrelvir inhibits ... References External links NHSA slideshow also shows adverse effect data from phase II/III {{RNA antivirals Antiviral drugs Combination antiviral ...
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3C-like Protease
The 3C-like protease (3CLpro) or main protease (Mpro), formally known as C30 endopeptidase or 3-chymotrypsin-like protease, is the main protease found in coronaviruses. It cleaves the coronavirus polyprotein at eleven conserved sites. It is a cysteine protease and a member of the PA clan of proteases. It has a cysteine-histidine catalytic dyad at its active site and cleaves a Gln–( Ser/ Ala/ Gly) peptide bond. The Enzyme Commission refers to this family as SARS coronavirus main proteinase (Mpro; ). The 3CL protease corresponds to coronavirus nonstructural protein 5 (nsp5). The "3C" in the common name refers to the 3C protease (3Cpro) which is a homologous protease found in picornaviruses. Function The 3C-like protease is able to catalytically cleave a peptide bond between a glutamine at position P1 and a small amino acid (serine, alanine, or glycine) at position P1'. The SARS coronavirus 3CLpro can for instance self-cleave the following peptides: The protease is ...
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Protease Inhibitor (pharmacology)
Protease inhibitors (PIs) are medications that act by interfering with enzymes that cleave proteins. Some of the most well known are antiviral drugs widely used to treat HIV/AIDS, hepatitis C and COVID-19. These protease inhibitors prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles. Protease inhibitors that have been developed and are currently used in clinical practice include: * Antiretroviral HIV-1 protease inhibitors—class stem ** Amprenavir ** Atazanavir ** Darunavir ** Fosamprenavir ** Indinavir ** Lopinavir ** Nelfinavir ** Ritonavir ** Saquinavir ** Tipranavir * Hepatitis C virus NS3/ 4A protease inhibitors—class stem ** Asunaprevir ** Boceprevir ** Grazoprevir ** Glecaprevir ** Paritaprevir ** Simeprevir ** Telaprevir ** Voxilaprevir * 3-chymotrypsin-like protease (including, but n ...
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COVID-19
Coronavirus disease 2019 (COVID-19) is a contagious disease caused by the coronavirus SARS-CoV-2. In January 2020, the disease spread worldwide, resulting in the COVID-19 pandemic. The symptoms of COVID‑19 can vary but often include fever, fatigue, cough, breathing difficulties, anosmia, loss of smell, and ageusia, loss of taste. Symptoms may begin one to fourteen days incubation period, after exposure to the virus. At least a third of people who are infected asymptomatic, do not develop noticeable symptoms. Of those who develop symptoms noticeable enough to be classified as patients, most (81%) develop mild to moderate symptoms (up to mild pneumonia), while 14% develop severe symptoms (dyspnea, hypoxia (medical), hypoxia, or more than 50% lung involvement on imaging), and 5% develop critical symptoms (respiratory failure, shock (circulatory), shock, or organ dysfunction, multiorgan dysfunction). Older people have a higher risk of developing severe symptoms. Some complicati ...
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Combination Drug
A combination drug is a combination of two or more pharmaceutical drugs as active ingredients combined into a single dosage form, typically as a ''fixed-dose combination'', with each constituent standardized to specifications of a fixed dose. Fixed-dose combinations are mass production, mass-produced and mass marketing, mass marketed, intended to serve as a near universal treatment for a large patient population with diverse medical histories, conditions, predisposition thereof, and treatment requirements. A ''polypill'' is a tablet (pharmacy), pharmacy or capsule (pharmacy), capsule containing four or more active ingredients, often needing to be Compounding, compounded at a specialized pharmacy in order to satisfy the specifications of a patient's personalized medical prescription, prescription and treatment plan, including dosage form, Dosage (pharmacology), medicinal dosing, and/or modified-release dosage, mechanism of release. Polypills encompass approved drug, approved prescr ...
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Enzyme Inhibitor
An enzyme inhibitor is a molecule that binds to an enzyme and blocks its Enzyme activity, activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which Substrate (biochemistry), substrate molecules are converted into Product (chemistry), products. An enzyme Enzyme catalysis, facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the Rate-determining step, most difficult step of the reaction. An enzyme inhibitor stops ("inhibits") this process, either by binding to the enzyme's active site (thus preventing the substrate itself from binding) or by binding to another site on the enzyme such that the enzyme's catalysis of the reaction is blocked. Enzyme inhibitors may bind Reversible reaction, reversibly or irreversibly. Irreversible inhibitors form a Covalent bond, chemical bond with the enzyme such that the enzyme is inhibited until the chemical bond is broken. By cont ...
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Ritonavir
Ritonavir, sold under the brand name Norvir, is an antiretroviral medication used along with other medications to treat HIV/AIDS. This combination treatment is known as highly active antiretroviral therapy (HAART). Ritonavir is a protease inhibitor, though it now mainly serves to boost the potency of other protease inhibitor (pharmacology), protease inhibitors. It may also be used in combination with other medications to treat hepatitis C and COVID-19. It is taken Oral administration, by mouth. Common side effects of ritonavir include nausea, vomiting, loss of appetite, diarrhea, and numbness of the hands and feet. Serious side effects include liver complications, pancreatitis, allergic reactions, and arrhythmias. Serious interactions may occur with a number of other medications including amiodarone and simvastatin. At low doses, it is considered to be acceptable for use during pregnancy. Ritonavir is of the protease inhibitor class. However, it is also commonly used to inhibi ...
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CYP3A Inhibitor
Cytochrome P450 3A4 (abbreviated CYP3A4) () is an important enzyme in the body, mainly found in the liver and in the intestine, which in humans is encoded by ''CYP3A4'' gene. It oxidizes small foreign organic molecules (xenobiotics), such as toxins or drugs, so that they can be removed from the body. It is highly homologous to CYP3A5, another important CYP3A enzyme. While many drugs are deactivated by CYP3A4, there are also some drugs that are ''activated'' by the enzyme. Some substances, such as some drugs and furanocoumarins present in grapefruit juice, interfere with the action of CYP3A4. These substances will, therefore, either amplify or weaken the action of those drugs that are modified by CYP3A4. CYP3A4 is a member of the cytochrome P450 family of oxidizing enzymes. Several other members of this family are also involved in drug metabolism, but CYP3A4 is the most common and the most versatile one. Like all members of this family, it is a hemoprotein, i.e. a protein conta ...
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National Medical Products Administration
The National Medical Products Administration (NMPA; ) is a national bureau responsible for drug supervision under the State Council of China and is managed by the State Administration for Market Regulation. History The agency had multiple former names, including China Food and Drug Administration and State Food and Drug Administration. The National Medical Products Administration was founded on the basis of the former State Food and Drug Administration (SFDA). In March 2013, the former regulatory body was rebranded and restructured as the China Food and Drug Administration, elevating it to a ministerial-level agency. In 2018, as part of China's 2018 government administration overhaul, the name was changed to 'National Medical Products Administration' and merged into the newly created State Administration for Market Regulation. The headquarters are in Xicheng, Beijing. In its first incarnation as the CFDA, the NMPA replaced a large group of overlapping regulators with an ent ...
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Median
The median of a set of numbers is the value separating the higher half from the lower half of a Sample (statistics), data sample, a statistical population, population, or a probability distribution. For a data set, it may be thought of as the “middle" value. The basic feature of the median in describing data compared to the Arithmetic mean, mean (often simply described as the "average") is that it is not Skewness, skewed by a small proportion of extremely large or small values, and therefore provides a better representation of the center. Median income, for example, may be a better way to describe the center of the income distribution because increases in the largest incomes alone have no effect on the median. For this reason, the median is of central importance in robust statistics. Median is a 2-quantile; it is the value that partitions a set into two equal parts. Finite set of numbers The median of a finite list of numbers is the "middle" number, when those numbers are liste ...
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Nirmatrelvir/ritonavir
Nirmatrelvir/ritonavir, sold under the brand name Paxlovid, is a co-packaged medication used as a treatment for COVID19. It contains the antiviral medications nirmatrelvir and ritonavir and was developed by Pfizer. Nirmatrelvir inhibits SARS-CoV-2 main protease, while ritonavir is a strong CYP3A inhibitor, slowing down nirmatrelvir metabolism and therefore boosting its effect. It is taken by mouth. In unvaccinated high-risk people with COVID19, nirmatrelvir/ritonavir can reduce the risk of hospitalization or death by 88% if taken within five days of symptom onset. People who take nirmatrelvir/ritonavir also test negative for COVID19 about two and a half days earlier than people who do not. Side effects of nirmatrelvir/ritonavir include changes in sense of taste ( dysgeusia), diarrhea, high blood pressure (hypertension), and muscle pain (myalgia). In December 2021, the United States Food and Drug Administration (FDA) granted nirmatrelvir/ritonavir emergency use autho ...
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Antiviral Drugs
Antiviral drugs are a class of medication used for treating viral infections. Most antivirals target specific viruses, while a broad-spectrum antiviral is effective against a wide range of viruses. Antiviral drugs are a class of antimicrobials, a larger group which also includes antibiotic (also termed antibacterial), antifungal and antiparasitic drugs, or antiviral drugs based on monoclonal antibodies. Most antivirals are considered relatively harmless to the host, and therefore can be used to treat infections. They should be distinguished from virucides, which are not medication but deactivate or destroy virus particles, either inside or outside the body. Natural virucides are produced by some plants such as eucalyptus and Australian tea trees. Medical uses Most of the antiviral drugs now available are designed to help deal with HIV, herpes viruses, the hepatitis B and C viruses, and influenza A and B viruses. Viruses use the host's cells to replicate and this makes i ...
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Combination Antiviral Drugs
In mathematics, a combination is a selection of items from a set that has distinct members, such that the order of selection does not matter (unlike permutations). For example, given three fruits, say an apple, an orange and a pear, there are three combinations of two that can be drawn from this set: an apple and a pear; an apple and an orange; or a pear and an orange. More formally, a ''k''-combination of a set ''S'' is a subset of ''k'' distinct elements of ''S''. So, two combinations are identical if and only if each combination has the same members. (The arrangement of the members in each set does not matter.) If the set has ''n'' elements, the number of ''k''-combinations, denoted by C(n,k) or C^n_k, is equal to the binomial coefficient \binom nk = \frac, which can be written using factorials as \textstyle\frac whenever k\leq n, and which is zero when k>n. This formula can be derived from the fact that each ''k''-combination of a set ''S'' of ''n'' members has k! permutati ...
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