Tamatinib HCl (formerly known as R406 HCl) is a novel potent and ATP competitive Syk inhibitor with IC50 of 41 nM in cell-free assays, it strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 impairs platelet activation and monocyte tissue factor expression triggered by heparin-PF4 complex directed antibodies. R406 blocks fc receptor […]

S 38093 is a novel brain-penetrant antagonist (inverse agonist) of the H3 (histamine H3) receptor with Ki of 8.8, 1.44 and 1.2 µM for rat, mouse and human H3 receptors, respectively. It may provide an innovative strategy to improve age-associated cognitive deficits. In cellular models, S 38093 is able to antagonize mice H3 receptors (KB=0.65 […]

Sarecycline (formerly known as WC-3035 and P005672; trade name: Seysara) is the first narrow spectrum tetracycline-class antibiotic being developed for acne treatment. In Oct 2018, FDA approved Sarecycline for the treatment of inflammatory lesions of non-nodular moderate to severe acne vulgaris in patients 9 years of age and older. In addition to exhibiting activity against […]

RG7834 R-isomer is the R-enantiomer of RG7834 (RO-7020322) which is a novel, potent and orally bioavailable inhibitor of HBV viral gene expression which blocks viral antigen and virion production. RG7834 is highly selective for HBV, and has a unique antiviral profile that is clearly differentiated from nucleos(t)ide analogues. RG7834 (also known as RO 7020322) is […]

Taniborbactam (VNRX5133) is a novel, Phase 3-ready, reversible, selective, and injectable ß-lactamase inhibitor (BLI) that features uniquely potent and selective activity against both serine- and metallo-beta-lactamases. VNRX-5133 is under investigation in a fixed combination with the fourth generation cephalosporin, cefepime. Cefepime/VNRX-5133 may have the potential to provide a best-in-class broad-spectrum treatment option for infections due […]

SNAP-398299 (also known as SNAP398299), a more water soluble analog of HT-2157 (SNAP 37889), is a selective, high-affinity, and competitive antagonists of galanin-3 receptor (Gal3) that has the potential for the treatment of major depressive disorder. Acute administration of SNAP 37889 or SNAP 398299 enhanced rat social interaction. Furthermore, acute SNAP 37889 was also shown […]

Migalastat hydrochloride (formerly GR-181413A; AT1001; GR181413A; AT-1001; Galafold), the hydrochloride salt of migalastate, is an inhibitor of α-galactosidase A (α-Gal A) and a medication approved by FDA in August 2018 to treat adults with Fabry disease. It is a pharmacological chaperone that potently and selectively binds, stabilizes, and increases cellular levels of α-Gal A with […]

AZD-5153 (AZD5153) is a potent, selective, and orally bioavailable BET/BRD4 (bromodomain and extraterminal) bromodomain inhibitor with anticancer activity. It inhibits BRD4 with a pKi of 8.3 and possesses a bivalent binding mode. Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously. AZD5153 treatment markedly affects transcriptional programs of MYC, E2F, and mTOR. […]

Vinflunine (F 12158, BMS 710485) is a new and semi-synthetic analog of the vinca alkaloid vinorelbine that is bi-fluorinated strucuturally. As a mitotic or tubulin inhibitor, it has anticancer, anti-angiogenic, vascular-disrupting and anti-metastatic properties. The major effects of Vinflunine on dynamic instability are a slowing of the microtubule growth rate, an increase in growth duration, […]