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Cilofexor
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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
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Cenicriviroc
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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
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VK2809
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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
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Aramchol
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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
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Travivo
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Travivo (gepirone ER; GlaxoSmithKline/Mission Pharmacal) is a pyridinyl piperazine 5-HT1A receptor agonist, and is distinct from available therapies as it is not a reuptake inhibitor and has no material norepinephrine or dopamine activity. Unlike tricyclic antidepressants or selective serotonin reuptake inhibitors that act on most or all of the 5-HT subtypes in the brain and may have several adverse effects, trials for Travivo have shown benign adverse effects without significant dopaminergic effects.
March 29, 2019
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SAGE-217
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SAGE-217 (oral brexanolone; SAGE Therapeutics/Shionogi) is a novel, next-generation positive allosteric modulator that selectively binds synaptic and extrasynaptic gamma-aminobutyric acid-A (GABA-A) receptors and shares similar pharmacology properties to brexanolone.
March 29, 2019
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Zulresso
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Zulresso is SAGE Therapeutics’ proprietary intravenous formulation of brexanolone, which is an allosteric modulator of both synaptic and extra-synaptic GABA-A receptors.
March 29, 2019
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Fotivda
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Fotivda (tivozanib; AVEO Oncology/EUSA Pharma/Kyowa Hakko Kirin) is an oral tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 1 (VEGFR-1), VEGFR-2, and VEGFR-3. Inhibition of VEGF signaling in order to prevent angiogenesis is a well-established strategy across many tumor types; however, Fotivda’s potency, selectivity, and long half-life are hypothesized to improve the drug’s efficacy and safety in comparison to its predecessors.
March 6, 2019
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CB-839
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Cancer cells are known to rely on glycolysis as an energy source. CB-839 (Calithera Biosciences) inhibits the glutaminase enzyme, reducing the ability of cancer cells to utilize glutamine in this biochemical pathway, thereby reducing cell proliferation and tumor growth.
March 6, 2019
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abexinostat
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Abexinostat (Xynomic Pharmaceuticals) is a broad histone deacetylase (HDAC) inhibitor. HDAC enzymes (also known as lysine deacetylase) cleave acetyl groups from N-acetyl lysine amino acids on a histone.
March 6, 2019
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Calquence
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Calquence (acalabrutinib; AstraZeneca/Acerta) is a novel, orally available, second-generation Bruton’s tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Inhibition of the BTK protein prevents the activation of the B-cell antigen receptor signaling pathway, which blocks both B-cell activation and BTK-mediated activation of downstream survival pathways.
January 31, 2019
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Copiktra
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Copiktra (duvelisib; Verastem/Yakult Honsha) is a highly selective small molecule inhibitor of the p110-delta and p110-gamma isoforms of the phosphoinositide 3-kinase (PI3K) enzyme.
January 31, 2019
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Zanubrutinib
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Zanubrutinib (BeiGene) is an oral small molecule inhibitor of Bruton’s tyrosine kinase (BTK), developed to be more selective with less off-target effects than Imbruvica (ibrutinib; AbbVie/Johnson & Johnson). BTK is part of the B-cell receptor signaling pathway, which promotes cell proliferation, adhesion, and survival in many B-cell malignancies.
January 31, 2019
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INCB050465
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INCB050465 (Incyte) is an oral phosphoinositide 3-kinase (PI3K) delta-specific inhibitor. The PI3K pathway has been shown to be highly active in a subset of follicular lymphoma (FL), promoting cell proliferation and survival. INCB050465 inhibits the PI3K-delta isoform with a 20,000-fold selectivity over other PI3K isoforms.
February 10, 2019
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Betalutin
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Betalutin is a first-in-class antibody-radionucleotide conjugate targeted to CD37, an alternative to CD20, which is widely targeted in non-Hodgkin’s lymphoma. CD37 is highly expressed in B cells and B-cell lymphomas.
January 31, 2019
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