The safety and efficacy of this agent(s), or use in this setting, has not been established or is subject to confirmation. For an agent(s) whose safety and efficacy has not been established or confirmed, future regulatory approval or commercial availability is not guaranteed.

SHP2 Tyrosine Phosphatase Inhibitor

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SHP2 Tyrosine Phosphatase Inhibitor

PF-07284892

PF-07284892 is an investigational compound. Its safety and efficacy have not been established.

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Overview + Rationale

• PF-07284892 is an oral small molecule inhibitor of SHP2 (PTPN11) with potential antineoplastic activity

  • Deregulation of signaling through receptor tyrosine kinases (RTKs) and the RAS pathway plays a role in oncogenesis 
  • SHP2 is a node in multiple signaling pathways and has been shown to regulate cell survival, differentiation and proliferation 
  • Pathways associated with SHP2 are often utilized by tumors to impart resistance to targeted therapies. 
  • Inhibition of SHP2 may potentially provide additional treatment strategies

Mechanism of Action

SHP2 inhibitor PF-07284892 targets, binds to, and inhibits the activity of SHP2 • This is thought to prevent SHP2-mediated signaling via upregulated RTKs, inhibits RAS signaling, and has been shown to inhibit the growth of tumor cells

Stage of Development

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Advanced Solid Tumors
Phase 1 Monotherapy and Combination*

*Closed to Enrollment

REFERENCES:  NCI Thesaurus. https://ncithesaurus.nci.nih.gov/ncitbrowser/pages/home.jsf  Accessed  August 13, 2021; Jackson Lab. https://ckb.jax.org/drug/show/10366.  Accessed  August 13, 2021; Chen, H., et al. Oncogene 39, 7166–7180; Clinicaltrials.gov. https://clinicaltrials.gov/study/NCT04800822.  Accessed July 23, 2024.