SAD/MAD Phase 1 of the Safety, PK & PD of AST-008 in Healthy Subjects

  • Research type

    Research Study

  • Full title

    A Randomized, Combined SAD/MAD Phase 1 Study of the Safety, Pharmacokinetics and Pharmacodynamics of AST-008 in Healthy Subjects

  • IRAS ID

    222549

  • Contact name

    Ulrike Lorch

  • Contact email

    u.lorch@richmondpharmacology.com

  • Sponsor organisation

    Exicure, Inc.

  • Eudract number

    2016-003327-39

  • Duration of Study in the UK

    0 years, 6 months, 17 days

  • Research summary

    We are conducting a first-in-human clinical study of AST-008 in healthy male and female volunteers. AST-008 is being developed by Exicure as a treatment for cancer.

    AST-008 is a spherical oligonucleotide. Oligonucleotides are comprised of artificial DNA and stimulate the immune system by binding to a receptor called TLR9 on immune system cells. Normally, TLR9 receptors bind to the DNA of bacteria and viruses, activating the immune cells which produces the immune response against the infection. These immune cells are also involved in identifying and destroying cancerous cells. Some cancers reduce the amount of TLR9 receptors on immune cells. This reduces immune system activation and stops immune cells destroying cancerous cells, allowing the cancer to spread. Therefore, activating TLR9 with oligonucleotides increases the activity of the immune system against cancer cells. Linear oligonucleotides have already been researched and found to be effective in amplifying the immune system response and reducing tumour size. However, the spherical structure of AST-008 is expected to allow the drug to enter cells more effectively and produce a bigger immune response against the tumour.

    In this study we will assess the safety and tolerability of subcutaneous AST-008 when it is given as a single dose (SAD) in Part I of the study (up to 84 healthy volunteers in 5 – 7 cohorts) and placebo-controlled multiple doses (MAD) in Part II (up to 48 healthy volunteers in 3 – 4 cohorts). We will also measure the level of AST-008 in the blood (pharmacokinetics) and the effect on the immune system (pharmacodynamics). In both Parts, we plan to increase the dose from one cohort to the next, subject to no safety issues being identified.

    We will also assess safety parameters including physical examination, vital sign measurements, laboratory evaluations, electrocardiogram (ECG), telemetry and monitoring of adverse events (AEs).

  • REC name

    London - London Bridge Research Ethics Committee

  • REC reference

    17/LO/0193

  • Date of REC Opinion

    28 Mar 2017

  • REC opinion

    Unfavourable Opinion