User:Enrospv/Nanatinostat

Nanatinostat
Clinical data
Trade namesNstat
Other namesCHR-3996, VRx-3996
Drug classHDAC inhibitor
Identifiers
  • 2-[(1S,5R)-6-[(6-fluoroquinolin-2-yl)methylamino]-3-azabicyclo[3.1.0]hexan-3-yl]-N-hydroxypyrimidine-5-carboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC20H19FN6O2
Molar mass394.41 g·mol−1
3D model (JSmol)
  • C1C2C(C2NCC3=NC4=C(C=C3)C=C(C=C4)F)CN1C5=NC=C(C=N5)C(=O)NO
  • InChI=InChI=1S/C20H19FN6O2/c21-13-2-4-17-11(5-13)1-3-14(25-17)8-22-18-15-9-27(10-16(15)18)20-23-6-12(7-24-20)19(28)26-29/h1-7,15-16,18,22,29H,8-10H2,(H,26,28)/t15-,16+,18+
  • Key:QRGHOAATPOLDPF-BYICEURKSA-N

Nanatinostat is an orally bioavailable HDAC inhibitor developed by Viracta Therapeutics for the treatement of Epstein–Barr virus-associated lymphoproliferative diseases in combination with valganciclovir.[1][2]

Side effects include cytopenias such as thrombocytopenia, neutropenia and lymphopenia[2] and long QT syndrome at high doses[3].

Mechanism of action edit

Solid malignancies edit

References edit

  1. ^ "Clinical Trial on Epstein-Barr Virus Associated Lymphoma: VRx-3996, Valganciclovir - Clinical Trials Registry - ICH GCP". ichgcp.net. Retrieved 2021-02-25.
  2. ^ a b Porcu, Pierluigi; Haverkos, Brad M.; Alpdogan, Onder; Capra, Marcelo; Feldman, Tatyana A.; Brem, Elizabeth; Vallurupalli, Anusha; Brammer, Jonathan E.; Schriefer, Ana; Pereira, Juliana; Tulpule, Anil (2019-11-13). "Combination of Oral Nanatinostat (Nstat), a Novel Histone Deacetylase Inhibitor (HDACi), and the Oral Anti-Viral, Valganciclovir (VGCV), Is Active in Relapsed/Refractory (R/R) Epstein-Barr Virus (EBV)-Positive B-Cell, T-Cell, and Hodgkin Lymphoma: Interim Safety and Efficacy Results from a Phase 1b/2a Study". Blood. 134 (Supplement_1): 465–465. doi:10.1182/blood-2019-132004. ISSN 0006-4971.
  3. ^ PubChem. "Hdac inhibitor CHR-3996". pubchem.ncbi.nlm.nih.gov. Retrieved 2021-02-25.