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@pushingarrows
Linagliptin - an inhibitor of dipeptidyl peptidase-4 (DPP-4) which prevent the hormone incretin from being degraded thus allowing the pancreas is stimulated to produce more insulin. It can potentially be used for the treatment of type 2 diabetes and may protect vascular health by reducing arterial stiffness.
Rivoglitazone - a thiazolidinedione derivative which is an agonist of the protein receptor PPARgamma found in fat tissue. Activation of PPARgamma lowers blood sugar by increasing sensitivity to insulin and changing the metabolism of fat and sugar. It can potentially be used for the treatment of type-2 diabetes.
Capecitabine - a prodrug which is metabolised by enzymes in the body to 5-fluorouracil (5-FU). 5-FU is a thymidylate synthase inhibitor, hence inhibiting the synthesis of thymidine monophosphate which is essential for DNA synthesis.
Talazoparib - an inhibitor of poly ADP ribose polymerase (PARP) for the treatment of advanced breast cancer with germline BRCA mutation and is similar to olaparib.
Edaravone - an antioxidant and it is used for the treatment of amyotrophic lateral sclerosis (ALS) and help the recovery of stroke.
Ixazomib - a selective and reversible inhibitor of the protein proteasome subunit beta type-5 (PSMB5) similar to bortezomib. It contains leucine derivative with the carboxylate acid replaced by a boronic acid. It is used for the treatment of multiple myeloma together with daratumumab and elotuzumab.
Bictegravir - an integrate inhibitor used in combination with tenofovir alafenamide and emtricitabine for the treatment of HIV-1 infection. It has less negative side effects on the bones and kidneys.
Pemetrexed - a folate antimetabolites chemotherapy medication which inhibits thymidylate synthase, dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT) enzymes used in purine and pyrimidine synthesis, hence formation of RNA and DNA. It is used for the treatment of non-small cell lung carcinoma, and pleural mesothelioma.
Varenicline - a partial agonist of various subtypes of nicotinic acetylcholine receptors used for the treatment of nicotine addiction. It produces less effect of dopamine release than nicotine and its competitive binding reduces the ability of nicotine to bind, therefore reduces craving and pleasurable effect of nicotine. A report suggest it does not increase side effects such as higher risk to heart attack, or risk of depression or self-harm.
DSM265 - a potential antimalarial medication for the treatment of malaria.
Canagliflozin - an inhibitor of subtype 2 sodium-glucose transport (SGLT-2) proteins of the gliflozin class. It is used as an anti-diabetic drug for the treatment of type 2 diabetes either as monotherapy or in combination with other medications such as metformin, sulfonylurea, and pioglitazone. SGLT-2 is responsible for at least 90% of renal glucose reabsorption and blocking this transporter causes blood glucose to be eliminated through urine. It may have positive effects on cardiometabolic health by improving adipose tissue function in patients with type 2 diabetes mellitus (T2DM). Treatment with canagliflozin cause a reduction in serum leptin and IL-6 levels as well as an increase in adiponectin and TNFa levels compared to glimepiride.
Midostaurin - a multi-target protein kinase inhibitor for the treatment of acute myeloid leukaemia with an FLT3 mutation. It is being investigated for other cancers such as myelodysplastic syndrone, and systemic mastocytosis. It is a semi-synthetic derivative of staurosporine.
Enzalutamide - an androgen receptor signalling inhibitor and antagonist for the treatment of metastatic castration-resistant prostate cancer. It is a synthetic non-steroidal antiandrogen (NSAA) which is more effective and with less hepatotoxicity side effect compared to first generation NSAA like flutamide, nilutamide, and bicalutamide.
Regorafenib - an inhibitor of tyrosine kinase (VEGFR - TIE2) for the treatment of metastatic colorectal cancer, unresectable hepatocellular carcinoma, and gastrointestinal stromal tumours. Its structure is closely related sorafenib with a Florine replacement.
Bryostatin 1 - is a macrolide isolated from the bryozoan marine organism, Bugula neritina, and is a potent modulator of protein kinase C (PKC). It has been investigated for the treatment of cancer and AIDS/HIV. There is some evidence that it improves cognition and ability activities in patients with moderate to severe Alzheimer’s disease.
ABX464 - has shown potential in reduction of HIV reservoirs as demonstrated by a small scale study measuring total HIV DNA in peripheral blood mononuclear cells (PBMCs).
Tofacitinib - an inhibitor of the enzyme Janus kinase (JAK1 & JAK3) and interferes with the JAK-STAT signalling pathway which transmits extra cellular information into the cell nucleus hence influencing DNA transcription. It is used for the treatment for rheumatoid arthritis and have potential for treating psoriasis and ulcerative colitis (an inflammatory bowel disease).