Drug analysis Archives | Report Store

show blocks helper

Sort by Default Order
- Default Order
- Name
- Price
- Date
- Popularity

Click to order products descending

Display 15 Products per page

Delstrigo
Read More
Delstrigo ([doravirine + lamivudine + tenofovir disoproxil fumarate (TDF)]; Merck & Co) is a single-tablet regimen being developed for the treatment of HIV-1 infection. The drug is a co-formulation of the non-nucleoside reverse transcriptase inhibitor (NNRTI) doravirine and the two nucleos(t)ide reverse transcriptase inhibitors (NRTIs), lamivudine and TDF.
July 28, 2019
Find out more
Descovy
Read More
Descovy ([emtricitabine + tenofovir alafenamide (TAF)]; Gilead/Japan Tobacco) is a fixed-dose combination of two of Gilead’s nucleos(t)ide reverse transcriptase inhibitors, Emtriva (emtricitabine) and Vemlidy (tenofovir alafenamide [TAF]). The combination is currently approved in the US, Japan, and EU.
July 28, 2019
Find out more
Trogarzo
Read More
Trogarzo (ibalizumab; Theratechnologies/TaiMed Biologics) is a recombinant humanized monoclonal antibody approved for the treatment of HIV-1 infection. It targets the HIV-1 post-attachment process by binding one of the domains of the CD-4 protein, which inhibits a conformational change in CD-4 that is necessary to allow entry of HIV into T-cells.
July 28, 2019
Find out more
Cilofexor
Read More
Cilofexor (Gilead), a nonsteroidal FXR agonist, is a ligand-activated nuclear hormone receptor that is a key regulator of bile acid synthesis, conjugation, and excretion. It is abundant in the liver, gallbladder, intestines, and kidney. Stimulation of FXR in the intestine by bile acids or an FXR agonist results in the release of fibroblast growth factor 19 (FGF19).
July 22, 2019
Find out more
Cenicriviroc
Read More
Cenicriviroc (Allergan/Takeda) is a potent immunomodulator that blocks the chemokine receptors-2/5 (CCR-2/5). CCR-2/5 have been linked to the inflammatory and fibrogenic pathways in non-alcoholic steatohepatitis (NASH), and by inhibiting CCR-2/5 it is anticipated that cenicriviroc will reduce inflammation and fibrosis.
July 22, 2019
Find out more
VK2809
Read More
VK2809 (Viking Therapeutics) is a thyroid hormone receptor (THR) β-selective agonist which is selective to liver tissue. It is delivered as a prodrug. VK2809 selectively activates the cytochrome P450 isozyme 3A4 (CYP3A4), which is predominantly found in the liver. This allows increased hepatic exposure, which simultaneously reduces systemic exposure to other tissues such as skeletal muscle and the heart.
July 22, 2019
Find out more
Aramchol
Read More
Aramchol (arachidyl amido cholanoic acid; Galmed) is a conjugate of cholic acid and arachidic acid, and belongs to the synthetic fatty acid bile acid conjugates (FABACs) family. Aramchol inhibits the liver enzyme stearoyl-CoA desaturase 1 inhibitor (SCD1), and as a result fatty acid synthesis is reduced while fatty acid oxidation is increased. Additionally, Aramchol has hypocholesterolemic effects due to the upregulation of ATP-binding cassette transporter 1 (ABCA1). Ultimately, Aramchol causes incomplete SCD inhibition while also being anti-atherogenic.
July 22, 2019
Find out more
Ocaliva
Read More
Ocaliva (obeticholic acid; Intercept Pharmaceuticals) is a selective farnesoid X receptor (FXR) agonist. FXR is a nuclear bile acid receptor involved in the regulation of bile acids, lipids, and possibly glucose. Ocaliva is a derivative of chenodeoxycholic acid, the endogenous FXR agonist found naturally in human bile acid. By activating FXR, Ocaliva improves insulin sensitivity and inhibits lipogenesis, which reduces fat buildup in the liver and results in decreased inflammation. Ocaliva has also been linked to weight loss. Ocaliva is currently approved in the US and EU for primary biliary cholangitis (PBC) in combination with ursodeoxycholic acid (UDCA) in adults with an inadequate response to UDCA, or as monotherapy in adults unable to tolerate UDCA.
July 22, 2019
Find out more
Elafibranor
Read More
Elafibranor (Genfit) is an oral peroxisome proliferator-activated receptor (PPAR) alpha-delta dual agonist. The medication activates PPAR-alpha and PPAR-delta, which control gene expression. Stimulating these receptors increases insulin sensitivity and fatty acid oxidation, which results in a reduction of fat buildup in the liver and leads to a decrease in fibrosis and inflammation.
July 22, 2019
Find out more
Tropifexor
Read More
FXR is a nuclear receptor that regulates bile acid metabolism and signaling. Activation of the receptor inhibits bile acid synthesis from cholesterol via cytochrome P450 7A1 and increases bile acid conjugation, transport, and excretion. This protects the liver from the potentially harmful effects caused during bile acid accumulation. Tropifexor (Novartis/Pfizer) is a novel, highly potent, non-bile acid FXR agonist. It has demonstrated potent activity in rodent Parkinson’s disease models by measuring the induction of FXR target genes in tissues.
July 22, 2019
Find out more
Selonsertib
Read More
Selonsertib (Gilead) is a small molecule that inhibits apoptosis signal-regulating kinase 1 (ASK1). ASK1 has been shown to promote inflammation, apoptosis, and fibrosis in settings of oxidative stress. Non-alcoholic steatohepatitis (NASH) increases oxidative stress and ASK1 activation, so by inhibiting ASK1, selonsertib has been shown to decrease inflammation and fibrosis in patients with NASH.
July 22, 2019
Find out more
Resmetirom
Read More
Resmetirom (Madrigal Pharmaceuticals) is a thyroid hormone receptor (THR) β-selective agonist which selectively targets receptors in the liver. The THR is involved in the regulation of metabolism, cholesterol, and triglycerides, as well as the pathological buildup of fat in the liver. The high liver specificity of resmetirom aims to avoid adverse events associated with THR activation outside the liver.
July 22, 2019
Find out more
Firsocostat
Read More
Firsocostat (Gilead) is an acetyl-CoA carboxylase (ACC) allosteric inhibitor which binds to the biotin carboxylase domain of ACC with high potency and selectivity. Firsocostat inhibits both isoforms (ACC1 and ACC2) of ACC, which results in the reduction of the production of malonyl-CoA carboxylase, therefore reducing a key substrate for fatty acid synthesis. This also reduces the inhibitory effect of malonyl-CoA on the carnitine palmitoyltransferase 1 (CPT-1), which is the rate-limiting step in β-oxidation and leads to an increase in the breakdown of free fatty acids.
July 22, 2019
Find out more
Emricasan
Read More
Emricasan (Conatus/Novartis) is a small molecule which inhibits pan-caspases. These enzymes are key modulators of apoptosis and inflammation, and chronically elevated apoptosis is often present in liver disease, which leads to the accumulation of apoptotic cells and the release of apoptotic bodies. These end products of apoptosis are engulfed by surrounding tissues which promote disease pathology and inflammation.
July 22, 2019
Find out more
Dovato
Read More
Dovato ([dolutegravir + lamivudine]; ViiV Healthcare) is a single-tablet regimen approved in the US for the treatment of HIV-1 infection in patients who are treatment-naïve. It is also being developed in the EU for the treatment of HIV-1 infection in patients who are treatment-naïve (with an approval decision expected by Q3 2019), as well as for patients who are virologically suppressed (US/Japan/EU).
June 28, 2019
Find out more

Drug analysis

Drug analysis

Delstrigo

Descovy

Trogarzo

Cilofexor

Cenicriviroc

VK2809

Aramchol

Ocaliva

Elafibranor

Tropifexor

Selonsertib

Resmetirom

Firsocostat

Emricasan

Dovato