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Grazoprevir
Grazoprevir is a drug approved for the treatment of hepatitis C. It was developed by Merck and completed Phase III trials, used in combination with the NS5A replication complex inhibitor elbasvir under the trade name ''Zepatier'', either with or without ribavirin. Grazoprevir is a second generation hepatitis C virus protease inhibitor acting at the NS3/ 4A protease targets. It has good activity against a range of HCV genotype variants, including some that are resistant to most currently used antiviral medications. Side effects Side effects have only been assessed in the combination with elbasvir. Common side effects of the combination include feeling tired, nausea, reduced appetite, and headache. Low red blood cell count has occurred when co-administered with ribavirin in some cases. The most important risks are alanine transaminase elevation, hyperbilirubinemia, drug resistance development and drug interactions. Interactions Grazoprevir is transported by the solu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Zepatier
Elbasvir/grazoprevir (trade name Zepatier ) is a fixed-dose combination for the treatment of hepatitis C, containing elbasvir (an inhibitor of hepatitis C virus's NS5A protein) and grazoprevir (an NS3 (HCV), NS3/NS4A, 4A inhibitor). It is used to treat chronic hepatitis C virus (HCV) genotypes 1 or 4 infection in both treatment-naïve and treatment-experienced patients. Both elbasvir and grazoprevir were developed by Merck & Co. The US Food and Drug Administration (FDA) approved the drug on 28 January 2016. Medical uses Elbasvir/grazoprevir received FDA approval in January 2016. Its indication is for treatment of chronic hepatitis C of the genotypes 1 and 4 for adults. Hepatitis C is a global disease that infects upwards of 150 million people worldwide, especially in older generations. Hepatitis C causes inflammation of the liver that eventually leads to diminished liver function or even failure. Zepatier is indicated for treatment with or without use of ribavirin, as well. Zepa ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 and hepatitis C. 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 * Severe acute respiratory syndrome coronavirus 2 3-chymotrypsin-like protease inhibitors ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Elbasvir
Elbasvir is a drug approved by the FDA in January 2016 for the treatment of hepatitis C. It was developed by Merck and completed Phase III trials, used in combination with the NS3/ 4A protease inhibitor grazoprevir under the trade name ''Zepatier'', either with or without ribavirin. Elbasvir is a highly potent and selective NS5A inhibitor of the hepatitis C virus NS5A replication complex. It has only been investigated as a combination product with other complementary hepatitis C antiviral drugs such as grazoprevir and MK-3682, and it is unclear whether elbasvir would show robust antiviral activity if it was administered by itself. Nevertheless, combination products of this type represent the most successful approach yet developed for actually curing hepatitis C, rather than merely slowing the progression of the disease. Side effects Side effects have only been assessed in the combination with grazoprevir; see Elbasvir/grazoprevir#Side effects. Interactions Elbasvir is d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bilirubin
Bilirubin (BR) (Latin for "red bile") is a red-orange compound that occurs in the normal catabolic pathway that breaks down heme in vertebrates. This catabolism is a necessary process in the body's clearance of waste products that arise from the destruction of aged or abnormal red blood cells. In the first step of bilirubin synthesis, the heme molecule is stripped from the hemoglobin molecule. Heme then passes through various processes of porphyrin catabolism, which varies according to the region of the body in which the breakdown occurs. For example, the molecules excreted in the urine differ from those in the feces. The production of biliverdin from heme is the first major step in the catabolic pathway, after which the enzyme biliverdin reductase performs the second step, producing bilirubin from biliverdin.Boron W, Boulpaep E. Medical Physiology: a cellular and molecular approach, 2005. 984–986. Elsevier Saunders, United States. Ultimately, bilirubin is broken down within ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tipranavir
Tipranavir (TPV), or tipranavir disodium, is a nonpeptidic protease inhibitor (PI) manufactured by Boehringer Ingelheim under the trade name Aptivus . It is administered with ritonavir in combination therapy to treat HIV infection. Tipranavir has the ability to inhibit the replication of viruses that are resistant to other protease inhibitors and is recommended for patients who are resistant to other treatments. Resistance to tipranavir itself seems to require multiple mutations. Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008. Tipranavir should only be taken in combination with ritonavir and other antiretroviral drugs, and is not approved for treatment-naïve patients. Like lopinavir and atazanavir, it is very potent and is effective in ''salvage'' therapy for patients with drug resistance. However, side effects of tipranavir may be more severe than those of other antiretrovirals. Some side ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Saquinavir
Saquinavir (SQV), sold under the brand names Invirase and Fortovase, is an antiretroviral drug used together with other medications to treat or prevent HIV/AIDS. Typically it is used with ritonavir or lopinavir/ritonavir to increase its effect. It is taken by mouth. Common side effects include nausea, vomiting, diarrhea, and feeling tired. More serious side effects include problems with QT prolongation, heart block, high blood lipids, and liver problems. It appears to be safe in pregnancy. It is in the protease inhibitor class and works by blocking the HIV protease. Saquinavir was patented in 1988 and first sold in 1995. Medical uses Saquinavir is used together with other medications to treat or prevent HIV/AIDS. Typically it is used with ritonavir or lopinavir/ritonavir to increase its effect. Side effects The most frequent adverse events with saquinavir in either formulation are mild gastrointestinal symptoms, including diarrhoea, nausea, loose stools and abdominal dis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lopinavir
Lopinavir is an antiretroviral of the protease inhibitor class. It is used against HIV infections as a fixed-dose combination with another protease inhibitor, ritonavir (lopinavir/ritonavir). It was patented in 1995 and approved for medical use in 2000. Side effects Side effects, interactions, and contraindications have only been evaluated in the drug combination lopinavir/ritonavir. Pharmacology Lopinavir is highly bound to plasma proteins (98–99%). Reports are contradictory regarding lopinavir penetration into the cerebrospinal fluid (CSF). Anecdotal reports state that lopinavir cannot be detected in the CSF; however, a study of paired CSF-plasma samples from 26 patients receiving lopinavir/ritonavir found lopinavir CSF levels above the IC50 in 77% of samples. Research A 2014 study indicates that lopinavir is effective against the human papilloma virus (HPV). The study used the equivalent of one tablet twice a day applied topically to the cervices of women with high- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Darunavir
Darunavir (DRV), sold under the brand name Prezista among others, is an antiretroviral medication used to treat and prevent HIV/AIDS. It is generally recommended for use with other antiretrovirals. It is often used with low doses of ritonavir or cobicistat to increase darunavir levels. It may be used for prevention after a needlestick injury or other potential exposure. It is taken by mouth once to twice a day. Common side effects include diarrhea, nausea, abdominal pain, headache, rash and vomiting. Severe side effects include allergic reactions, liver problems, and skin rashes such as toxic epidermal necrolysis. While poorly studied in pregnancy it appears to be safe for the baby. It is of the protease inhibitor (PI) class and works by blocking HIV protease. Developed by pharmaceutical company Tibotec, darunavir is named after Arun K. Ghosh, the chemistry professor who discovered the molecule at the University of Illinois at Chicago. It was approved by the Food and Drug Adm ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Atazanavir
Atazanavir, sold under the brand name Reyataz among others, is an antiretroviral medication used to treat HIV/AIDS. It is generally recommended for use with other antiretrovirals. It may be used for prevention after a needlestick injury or other potential exposure (postexposure prophylaxis (PEP)). It is taken by mouth once a day. Common side effects include headache, nausea, yellowish skin, abdominal pain, trouble sleeping, and fever. Severe side effects include rashes such as erythema multiforme and high blood sugar. Atazanavir appears to be safe to use during pregnancy. It is of the protease inhibitor (PI) class and works by blocking HIV protease. Atazanavir was approved for medical use in the United States in 2003. It is on the World Health Organization's List of Essential Medicines. As of 2017 there is a generic version available in the United States manufactured by Teva Pharmaceuticals Medical uses Atazanavir is used in the treatment of HIV. The efficacy of atazanavir ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ciclosporin
Ciclosporin, also spelled cyclosporine and cyclosporin, is a calcineurin inhibitor, used as an immunosuppressant medication. It is a natural product. It is taken orally or intravenously for rheumatoid arthritis, psoriasis, Crohn's disease, nephrotic syndrome, and in organ transplants to prevent rejection. It is also used as eye drops for keratoconjunctivitis sicca (dry eyes). Common side effects include high blood pressure, headache, kidney problems, increased hair growth, and vomiting. Other severe side effects include an increased risk of infection, liver problems, and an increased risk of lymphoma. Blood levels of the medication should be checked to decrease the risk of side effects. Use during pregnancy may result in preterm birth; however, ciclosporin does not appear to cause birth defects. Ciclosporin is believed to work by decreasing the function of lymphocytes. It does this by forming a complex with cyclophilin to block the phosphatase activity of calcineurin, w ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Rifampicin
Rifampicin, also known as rifampin, is an ansamycin antibiotic used to treat several types of bacterial infections, including tuberculosis (TB), mycobacterium avium complex, ''Mycobacterium avium'' complex, leprosy, and Legionnaires’ disease. It is almost always used together with other antibiotics with two notable exceptions: when given as a "preferred treatment that is strongly recommended" for latent TB infection; and when used as post-exposure prophylaxis to prevent Haemophilus influenzae type b, ''Haemophilus influenzae'' type b and meningococcal disease in people who have been exposed to those bacteria. Before treating a person for a long period of time, measurements of liver enzymes and blood counts are recommended. Rifampicin may be given either Oral administration, by mouth or intravenously. Common side effects include nausea, vomiting, diarrhea, and loss of appetite. It often turns urine, sweat, and tears a red or orange color. Liver problems or allergic reactions ma ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SLCO1B3
Solute carrier organic anion transporter family member 1B3 (SLCO1B3) also known as organic anion-transporting polypeptide 1B3 (OATP1B3) is a protein that in humans is encoded by the ''SLCO1B3'' gene. OATP1B3 is a 12-transmembrane domain influx transporter. Normally expressed in the liver, the transporter functions to uptake large, non-polar drugs and hormones from the portal vein. Clinical significance OATP1B3 has also been identified as a transporter aberrantly expressed in prostate cancer and implicated in prostate cancer progression. Increasing mRNA expression of OATP1B3 was also correlated to prostate cancer Gleason score. In addition, lower expression of OATP1B3 mRNA was also detected in testicular cancer. Substrates Small molecules that are transported by SLCO1B3 include: * Amanitin * Atrasentan * Bilirubin * Bosentan * BQ-123 * Bromsulphthalein (BSP) * CDCA-NBD * Cholate (CA) * Cholecystokinin octapeptide (CCK-8) * Dehydroepiandroserone-3-sulfate (DHEAS) * Deltorphin I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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