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Purpose <p>The CIGB-552 peptide is a novel therapeutic alternative for the treatment of cancer. In this study, we aimed to determine the optimal formulation and route of administration for CIGB-552. Other objectives were to characterize the peptide’s pharmacokinetic profile in rats and conduct toxicity studies at different dosage regimens.</p> Methods <p>The antitumor activity of CIGB-552 was evaluated by different routes of administration (intraperitoneal, subcutaneous) and also with different peptide formulations (Tartrate/mannitol, Tartrate/trehalose) using a TC-1 tumor model in C57BL/6 mice. The pharmacokinetic profile of the peptide was also characterized after subcutaneous administration in Sprague-Dawley rats using PK Solver software. In addition, the safety of the peptide was evaluated following single-dose and repeated-dose administration schedules in healthy BALB/c mice.</p> Results <p>In the tumor model, subcutaneous administration of CIGB-552 and its tartrate/trehalose formulation resulted in a significant reduction in tumor volume compared to untreated groups. CIGB-552 exhibited a typical extravascular delivery profile, with rapid absorption, rapid tissue distribution, and rapid blood clearance. The peptide’s half-life was 2.5&#xa0;h, and peak plasma concentration (C<sub>max</sub>) was reached in approximately 15&#xa0;min. Furthermore, CIGB-552 was shown to have nonlinear pharmacokinetics across the evaluated dose and exposure range. On the other hand, CIGB-552 administration in the evaluated regimens was safe, with toxicity and fatal outcomes observed only with the 60&#xa0;mg/kg dose administered subcutaneously every two days until seven doses were completed in total.</p> Conclusions <p>The peptide’s safety profile in repeated dosing, combined with evidence of no systemic accumulation, supports the development of new regimens involving higher and more frequent doses to enhance antitumor efficacy in clinical studies.</p>

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In vivo evaluation of the antitumor peptide CIGB-552: antitumor activity, pharmacokinetics and safety of the subcutaneously administered peptide

  • 期刊论文

  • 发表日期：

    2026年3月6日

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  • Nivaldo Angel Gómez Hernández,
  • Luis Miguel Martínez Durán,
  • Héctor Santana Milian,
  • Hilda Elisa Garay Pérez,
  • Ana Yanci Etchegoyen Amoros,
  • Brizaida Oliva Arguellez,
  • Lizet Aldana Velazco,
  • Jorge Castro Velazco,
  • Ania Cabrales Rico,
  • Mariana Machado Lemos,
  • Julio Raúl Fernández Massó

摘要

Purpose

The CIGB-552 peptide is a novel therapeutic alternative for the treatment of cancer. In this study, we aimed to determine the optimal formulation and route of administration for CIGB-552. Other objectives were to characterize the peptide’s pharmacokinetic profile in rats and conduct toxicity studies at different dosage regimens.

Methods

The antitumor activity of CIGB-552 was evaluated by different routes of administration (intraperitoneal, subcutaneous) and also with different peptide formulations (Tartrate/mannitol, Tartrate/trehalose) using a TC-1 tumor model in C57BL/6 mice. The pharmacokinetic profile of the peptide was also characterized after subcutaneous administration in Sprague-Dawley rats using PK Solver software. In addition, the safety of the peptide was evaluated following single-dose and repeated-dose administration schedules in healthy BALB/c mice.

Results

In the tumor model, subcutaneous administration of CIGB-552 and its tartrate/trehalose formulation resulted in a significant reduction in tumor volume compared to untreated groups. CIGB-552 exhibited a typical extravascular delivery profile, with rapid absorption, rapid tissue distribution, and rapid blood clearance. The peptide’s half-life was 2.5 h, and peak plasma concentration (Cmax) was reached in approximately 15 min. Furthermore, CIGB-552 was shown to have nonlinear pharmacokinetics across the evaluated dose and exposure range. On the other hand, CIGB-552 administration in the evaluated regimens was safe, with toxicity and fatal outcomes observed only with the 60 mg/kg dose administered subcutaneously every two days until seven doses were completed in total.

Conclusions

The peptide’s safety profile in repeated dosing, combined with evidence of no systemic accumulation, supports the development of new regimens involving higher and more frequent doses to enhance antitumor efficacy in clinical studies.