Synthesis and evaluation of a deltic guanidinium analogue of a cyclic RGD peptide

Background Middle size peptides (MSPs) have emerged as a promising new pharmaceutical modality. We are seeking the best way to assess the non-clinical safety of MSPs. Consideration The requirements for assessing the genotoxicity of pharmaceuticals differ between small molecule drugs and biotherapeutics. Genotoxicity tests are necessary for small molecule drugs but not for biotherapeutics. MSPs, however, share similarities with both small molecule drugs and biotherapeutics. Here, we describe important points to consider in assessing the genotoxicity of MSP drugs. The current standard of genotoxicity assessment for small molecules may not be entirely appropriate for MSP drugs. MSP drugs need genotoxicity assessment mostly according to the current standard of small molecule drugs. Conclusion We propose a few modifications to the standard test battery of genotoxicity tests, specifically, the inclusion of an in vitro gene mutation test using mammalian cells, and exclusion of (Q)SAR assessment on MSP-related impurities.

show abstract

scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.

Contact Info

customersupport@researchsolutions.com

10624 S. Eastern Ave., Ste. A-614

Henderson, NV 89052, USA

This site is protected by reCAPTCHA and the Google Privacy Policy and Terms of Service apply.

Blog Terms and Conditions API Terms Privacy Policy Contact Cookie Preferences Do Not Sell or Share My Personal Information

Made with 💙 for researchers

Part of the Research Solutions Family.

Synthesis and evaluation of a deltic guanidinium analogue of a cyclic RGD peptide

Abstract: A potential of deltic guanidinium as a bioisostere of guanidinium was evaluated using a cyclic argine–glycine–aspartic acid (RGD) peptide as a parent compound. A deltic guanidinium analogue of a cyclic...

Cited by 4 publications

References 20 publications

Development of probes for radiotheranostics with albumin binding moiety to increase the therapeutic effects of astatine-211 (211At)

Development of probes for radiotheranostics with albumin binding moiety to increase the therapeutic effects of astatine-211 (211At)

Radiofrequency induced UCST-type gel-sol transition of metformin-conjugated nanogels for precisely synergizing thermal ablation and blood-vessel embolization

Considerations for the genotoxicity assessment of middle size peptide drugs containing non-canonical amino acid residues

Contact Info

Product

Resources

About