Motolimod

Motolimod (VTX-2337) is a drug which acts as a potent and selective agonist of toll-like receptor 8 (TLR8), a receptor involved in the regulation of the immune system. It is used to stimulate the immune system, and has potential application as an adjuvant therapy in cancer chemotherapy, although clinical trials have shown only modest benefits.[1][2] It also worsens neuropathic pain in animal models and has been used to research the potential of targeting TLR8 in some kinds of chronic pain syndromes.[3][4]

Motolimod
Identifiers
  • 2-amino-N,N-dipropyl-8-[4-(pyrrolidine-1-carbonyl)phenyl]-3H-1-benzazepine-4-carboxamide
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC28H34N4O2
Molar mass458.606 g·mol−1
3D model (JSmol)
  • CCCN(CCC)C(=O)C1=CC2=C(C=C(C=C2)C3=CC=C(C=C3)C(=O)N4CCCC4)N=C(C1)N
  • InChI=1S/C28H34N4O2/c1-3-13-31(14-4-2)28(34)24-17-23-12-11-22(18-25(23)30-26(29)19-24)20-7-9-21(10-8-20)27(33)32-15-5-6-16-32/h7-12,17-18H,3-6,13-16,19H2,1-2H3,(H2,29,30)
  • Key:QSPOQCXMGPDIHI-UHFFFAOYSA-N

See also

References
  1. Monk BJ, Brady MF, Aghajanian C, Lankes HA, Rizack T, Leach J, et al. (May 2017). "A phase 2, randomized, double-blind, placebo-controlled study of chemo-immunotherapy combination using motolimod with pegylated liposomal doxorubicin in recurrent or persistent ovarian cancer: a Gynecologic Oncology Group partners study". Annals of Oncology. 28 (5): 996–1004. doi:10.1093/annonc/mdx049. PMC 5406764. PMID 28453702.
  2. Ferris RL, Saba NF, Gitlitz BJ, Haddad R, Sukari A, Neupane P, et al. (November 2018). "Effect of Adding Motolimod to Standard Combination Chemotherapy and Cetuximab Treatment of Patients With Squamous Cell Carcinoma of the Head and Neck: The Active8 Randomized Clinical Trial". JAMA Oncology. 4 (11): 1583–1588. doi:10.1001/jamaoncol.2018.1888. PMC 6248084. PMID 29931076.
  3. Zhang ZJ, Guo JS, Li SS, Wu XB, Cao DL, Jiang BC, et al. (December 2018). "TLR8 and its endogenous ligand miR-21 contribute to neuropathic pain in murine DRG". The Journal of Experimental Medicine. 215 (12): 3019–3037. doi:10.1084/jem.20180800. PMC 6279408. PMID 30455267.
  4. Zhao LX, Jiang M, Bai XQ, Cao DL, Wu XB, Zhang J, et al. (December 2020). "TLR8 in the Trigeminal Ganglion Contributes to the Maintenance of Trigeminal Neuropathic Pain in Mice". Neuroscience Bulletin. doi:10.1007/s12264-020-00621-4. PMC 8055805. PMID 33355900.


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