Plinabulin Explained

Plinabulin (provisional name BPI-2358, formerly NPI-2358) is a small molecule under development by BeyondSpring Pharmaceuticals, and has completed a world-wide Phase 3 clinical trial for non-small cell lung cancer.[1] Plinabulin is being investigated for the reduction of chemotherapy-induced neutropenia[2] and for anti-cancer effects in combination with immune checkpoint inhibitors[3] [4] and in KRAS mutated tumors.[5]

Plinabulin blocks the polymerization of tubulin in a unique manner, resulting in multi-factorial effects including an enhanced immune-oncology response,[6] [7] [8] activation of the JNK pathway[9] and disruption of the tumor blood supply.

Notes and References

  1. Web site: 2021-05-23 . Completed: Docetaxel + Plinabulin Compared to Docetaxel + Placebo in Patients With Advanced NSCLC (DUBLIN-3), Phase Three . 2024-07-19 . clinicaltrials.gov.
  2. Randomized Phase 2 Trial of Plinabulin (NPI-2358) Plus Docetaxel in Patients with Advanced Non-Small Lung Cancer (NSCLC). Heist . R.S.. Aren . O.R.. Mita . A.C.. Polikoff . J.. Bazhenova . L.. Lloyd . G.K.. Mikrut . W.. Reich . W.. Spear . M.A.. Huang . L.. 2014. J Clin Oncol 32:5s.
  3. Web site: Nivolumab and Plinabulin in Treating Patients With Stage IIIB-IV, Recurrent, or Metastatic Non-small Cell Lung Cancer.
  4. Nivolumab in Combination With Plinabulin in Patients With Metastatic Non-Small Cell Lung Cancer (NSCLC).
  5. Activity of Plinabulin in Tumor Models with Kras Mutations. Lloyd . G.K.. Du . L.. Lee . G.. Dalsing-Hernandez . J.. Kotlarczyk . K.. Gonzalez . K.. Nawrocki . S.. Carew . J.. Huang . L.. October 5–9, 2015. Proceedings of the International Conference on Molecular Targets and Cancer Therapeutics. Boston MA.
  6. Kashyap . Abhishek S. . Fernandez-Rodriguez . Laura . Zhao . Yun . Monaco . Gianni . Trefny . Marcel P. . Yoshida . Naohiro . Martin . Kea . Sharma . Ashwani . Olieric . Natacha . Shah . Pankaj . Stanczak . Michal . Kirchhammer . Nicole . Park . Sung-Moo . Wieckowski . Sebastien . Laubli . Heinz . September 2019 . GEF-H1 Signaling upon Microtubule Destabilization Is Required for Dendritic Cell Activation and Specific Anti-tumor Responses . Cell Reports . 28 . 13 . 3367–3380.e8 . Zagani . Rachid . Kasenda . Benjamin . Steinmetz . Michel O. . Reinecker . Hans-Christian . Zippelius . Alfred.
  7. Natoli . Marina . Herzig . Petra . Pishali Bejestani . Elham . Buchi . Melanie . Ritschard . Reto . Lloyd . G. Kenneth . Mohanlal . Ramon . Tonra . James R. . Huang . Lan . Heinzelmann . Viola . Trüb . Marta . Zippelius . Alfred . Kashyap . Abhishek S. . 3 March 2021 . Plinabulin, a Distinct Microtubule-Targeting Chemotherapy, Promotes M1-Like Macrophage Polarization and Anti-tumor Immunity . Frontiers in Oncology . 11.
  8. La Sala . Giuseppina . Olieric . Natacha . Sharma . Ashwani . Viti . Federica . de Asis Balaguer Perez . Francisco . Huang . Lan . Tonra . James R. . Lloyd . G. Kenneth . Decherchi . Sergio . Díaz . José Fernando . Steinmetz . Michel O. . Cavalli . Andrea . November 2019 . Structure, Thermodynamics, and Kinetics of Plinabulin Binding to Two Tubulin Isotypes . Chem . 5 . 11 . 2969–2986.
  9. Singh . A.V.. Bandi . M.. Raje . N.. Richardson . P.. Palladino . M.A.. Chauhan . D.. Anderson . K.. A Novel Vascular Disrupting Agent Plinabulin Triggers JNK-Mediated Apoptosis and Inhibits Angiogenesis in Multiple Myeloma Cells. Blood. 2011. 117. 21. 5692–5700. 10.1182/blood-2010-12-323857. 21454451. 3110026.

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