First-In-Human Clinical Study of the C3 Complement Inhibitor AMY- 101 in Healthy Male Volunteers

NCT ID: NCT03316521

Last Updated: 2018-01-16

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

Get a concise snapshot of the trial, including recruitment status, study phase, enrollment targets, and key timeline milestones.

Recruitment Status

COMPLETED

Clinical Phase

PHASE1

Total Enrollment

50 participants

Study Classification

INTERVENTIONAL

Study Start Date

2017-04-24

Study Completion Date

2017-11-30

Brief Summary

Review the sponsor-provided synopsis that highlights what the study is about and why it is being conducted.

Safety, tolerability, pharmacokinetics (PK) and pharmacodynamics (PD) of a Single Ascending Dose (SAD) and a Multiple Dose (MD) of the complement inhibitor AMY-101. A prospective, single-center, open-label, First-In-Human (FIH) clinical study in healthy male volunteers.

Detailed Description

Dive into the extended narrative that explains the scientific background, objectives, and procedures in greater depth.

AMYNDAS is developing a novel peptidic complement inhibitor AMY-101, based on the third-generation compstatin analogue Cp40. AMY-101 is a selective inhibitor of complement activation in humans and in NHP. It binds to the complement component C3, the central "functional hub" that controls the upstream activation/amplification and downstream effector functions of complement. By binding to C3, AMY-101 inhibits the cleavage of native C3 to its active fragments C3a and C3b. As a consequence, the deposition of C3b, amplification via the alternative pathway and all downstream complement responses are prevented. AMY-101 is being developed to treat complement-mediated diseases, which are largely driven by aberrant C3 activation.

This first-in-human study of the C3-targeting complement inhibitor AMY-101 investigates the safety and PK/PD profile of AMY-101 in healthy male volunteers after Single Ascending Dose (SAD) and Multiple Doses (MD) using subcutaneous (SQ) or intravenous (IV) administration. The study is a prospective, single-center, open-label evaluation in healthy male volunteers.

Conditions

See the medical conditions and disease areas that this research is targeting or investigating.

Complement Mediated Diseases

Study Design

Understand how the trial is structured, including allocation methods, masking strategies, primary purpose, and other design elements.

Allocation Method

RANDOMIZED

Intervention Model

SEQUENTIAL

This is a prospective, single-center, open-label FIH study investigating the safety, tolerability, PK and PD after single and multiple doses of AMY-101 in healthy male volunteers. In the SAD part of the study, a single dose at ascending dose levels of AMY-101 will be administered to different cohorts, following a careful dose-escalation strategy. In the MD part of the study, multiple doses will be administered using different dosing intervals; the cohorts will include a minimum of four (4) subjects each. Additional subjects may be added in the cohorts if necessary.
Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

Review each arm or cohort in the study, along with the interventions and objectives associated with them.

Single Ascending Dose (SAD)

In the SAD arm subjects will be sequentially included in one of up to six cohorts (dose levels). All cohorts will include at least four subjects each. Additional subjects may be added in any cohort if necessary.

AMY-101 will be administered as a SQ or IV injection. Subjects in each cohort will be dosed sequentially, to allow for close safety monitoring. Between each cohort, safety data will be analyzed, evaluated and reviewed by the internal Safety Review Committee. Subsequent dose levels will be administered until either the maximum tolerated dose (MTD) or the study maximum dose (SMD) is reached based on specified dose escalation criteria.

Group Type EXPERIMENTAL

AMY-101

Intervention Type DRUG

AMY-101 is a selective inhibitor of complement activation, which binds to the complement component C3.

Multiple Dose (MD)

Depending on the results of the SAD, multiple doses of AMY-101 will be administered at the dose which has been identified as the dose which saturates target C3, for a duration that results to an exposure level equivalent to the maximum exposure achieved in the SAD. The dose and dosing interval will be determined based on the PK data obtained in the SAD part of the study. Each MD cohort will include at least four subjects and may be expanded with additional subjects if necessary. Between each cohort, safety data will be analyzed, evaluated and reviewed by the internal Safety Review Committee.

Group Type EXPERIMENTAL

AMY-101

Intervention Type DRUG

AMY-101 is a selective inhibitor of complement activation, which binds to the complement component C3.

Interventions

Learn about the drugs, procedures, or behavioral strategies being tested and how they are applied within this trial.

AMY-101

AMY-101 is a selective inhibitor of complement activation, which binds to the complement component C3.

Intervention Type DRUG

Eligibility Criteria

Check the participation requirements, including inclusion and exclusion rules, age limits, and whether healthy volunteers are accepted.

Inclusion Criteria

1. Willing and able to give written informed consent for participation in the study.
2. Healthy male subject aged 18-60 years, inclusive at the time of signing the informed consent.
3. Body Mass Index (BMI) ≥ 18 and ≤ 30 kg/m2 and weight at least 50 kg.
4. Clinically normal medical history, physical findings, vital signs, ECG and laboratory values at the time of screening, as judged by the Investigator.
5. Willing to use condom and contraceptive methods with a failure rate of \< 1% to prevent pregnancy and drug exposure of a partner and to refrain from donating sperm from the date of dosing until three (3) months after dosing of the IMP.
6. Willing and able to complete all procedures according to the Protocol.

Exclusion Criteria

1. History of any clinically significant disease or disorder which, in the opinion of the Investigator, may either put the subject at risk because of participation in the study, or influence the results or the subject's ability to participate in the study.
2. History of any Neisseria meningitidis infection
3. History of unexplained, recurrent infection, or infection requiring treatment with systemic antibiotics within the last 60 days prior to dosing.
4. History of latent or active tuberculosis, as assessed by the investigator based on chest X-ray and positive Quantiferon-TB Gold test.
5. History of complement deficiency.
6. History of any type of malignancy. However, completely resolved minor malignancies, at the discretion of the Investigator, may not be an exclusion criterion (for example: Non-Melanoma Skin Cancer).
7. Diagnosis of autoimmune, immunologic or rheumatologic disease (eg, systemic lupus erythematosus, rheumatoid arthritis).
8. Any clinically significant illness, medical/surgical procedure or trauma within four (4) weeks of the administration of IMP.
9. High CRP at screening (\> 0.5 mg/dL).
10. Current evidence or history of bacterial, viral or fungal infection within 14 days prior to (first) dosing or longer according to the judgment of the investigator for e.g. viral infections including herpes simplex or herpes zoster.
11. Any current condition or risk, which, in the opinion of the Investigator, may interfere with the subject's participation in the study, poses an added risk for the subject, or confounds the assessment of the subject or outcome of the study
12. Any clinically significant abnormality in clinical chemistry, hematology, or urinalysis results at the time of screening, as judged by the Investigator.
13. Any positive result on screening for serum hepatitis B surface antigen, hepatitis C antibody and/or Human Immunodeficiency Virus (HIV).
14. After 10 minutes supine rest abnormal vital signs defined as any of the following:

* Systolic BP \> 140 mm Hg
* Diastolic BP \> 95 mm Hg
* HR \< 40 or \> 90 beats per minute
15. Prolonged QTcF (\>450 ms), cardiac arrhythmias or any clinically significant abnormality in the resting ECG, as judged by the Investigator.
16. Any history of any allergy/hypersensitivity or anaphylactic reaction or on-going allergy/hypersensitivity. History of hypersensitivity to antibiotics or drugs with a similar chemical structure or class to AMY-101.
17. Use of any prescribed or non-prescribed medication including antacids, analgesics, herbal remedies, vitamins and minerals within two (2) weeks prior to the administration of IMP, except the occasional intake of paracetamol/acetominophen (maximum 2000 mg/day; and not exceeding 3000 mg/week) or nasal decongestant without cortisone or antihistamine, at the discretion of the Investigator.
18. Administration of another new chemical entity (defined as a compound that has not been approved for marketing) or having participated in any other clinical study that included drug treatment within 30 day or 5 half lives of the last administration of the other IMP. Subjects consented and screened but not dosed in previous phase I studies are not excluded.
19. Immunization with a live-attenuated vaccine one (1) month prior to the first administration of IMP.
20. Current smokers or users of nicotine products. Irregular use of nicotine (e.g. smoking, snuffing, chewing tobacco) less than three (3) times per week is allowed before screening visit.
21. History of alcohol abuse or excessive intake of alcohol, as judged by the Investigator.
22. Positive screen for drugs of abuse at screening or on admission to the unit or positive screen for alcohol at screening or on admission to the unit prior to administration of the IMP.
23. Use of anabolic steroids.
24. Plasma donation within one (1) month of screening or any blood donation/blood loss \> 450 mL during the three (3) months prior to screening.
25. Investigator considers the subject unlikely to comply with study procedures, restrictions and requirements.
Minimum Eligible Age

18 Years

Maximum Eligible Age

60 Years

Eligible Sex

MALE

Accepts Healthy Volunteers

Yes

Sponsors

Meet the organizations funding or collaborating on the study and learn about their roles.

Amyndas Pharmaceuticals S.A.

INDUSTRY

Sponsor Role lead

Responsible Party

Identify the individual or organization who holds primary responsibility for the study information submitted to regulators.

Responsibility Role SPONSOR

Locations

Explore where the study is taking place and check the recruitment status at each participating site.

HighPoint Clinical Trials Center

High Point, North Carolina, United States

Site Status

Countries

Review the countries where the study has at least one active or historical site.

United States

References

Explore related publications, articles, or registry entries linked to this study.

Ricklin D, Lambris JD. Complement in immune and inflammatory disorders: therapeutic interventions. J Immunol. 2013 Apr 15;190(8):3839-47. doi: 10.4049/jimmunol.1203200.

Reference Type BACKGROUND
PMID: 23564578 (View on PubMed)

Ricklin D, Lambris JD. Complement in immune and inflammatory disorders: pathophysiological mechanisms. J Immunol. 2013 Apr 15;190(8):3831-8. doi: 10.4049/jimmunol.1203487.

Reference Type BACKGROUND
PMID: 23564577 (View on PubMed)

Mastellos DC, Yancopoulou D, Kokkinos P, Huber-Lang M, Hajishengallis G, Biglarnia AR, Lupu F, Nilsson B, Risitano AM, Ricklin D, Lambris JD. Compstatin: a C3-targeted complement inhibitor reaching its prime for bedside intervention. Eur J Clin Invest. 2015 Apr;45(4):423-40. doi: 10.1111/eci.12419. Epub 2015 Mar 9.

Reference Type BACKGROUND
PMID: 25678219 (View on PubMed)

Ricklin D, Lambris JD. Therapeutic control of complement activation at the level of the central component C3. Immunobiology. 2016 Jun;221(6):740-6. doi: 10.1016/j.imbio.2015.06.012. Epub 2015 Jun 10.

Reference Type BACKGROUND
PMID: 26101137 (View on PubMed)

Reis ES, Mastellos DC, Yancopoulou D, Risitano AM, Ricklin D, Lambris JD. Applying complement therapeutics to rare diseases. Clin Immunol. 2015 Dec;161(2):225-40. doi: 10.1016/j.clim.2015.08.009. Epub 2015 Sep 1.

Reference Type BACKGROUND
PMID: 26341313 (View on PubMed)

Mastellos DC, Ricklin D, Hajishengallis E, Hajishengallis G, Lambris JD. Complement therapeutics in inflammatory diseases: promising drug candidates for C3-targeted intervention. Mol Oral Microbiol. 2016 Feb;31(1):3-17. doi: 10.1111/omi.12129. Epub 2015 Oct 7.

Reference Type BACKGROUND
PMID: 26332138 (View on PubMed)

Reis ES, DeAngelis RA, Chen H, Resuello RR, Ricklin D, Lambris JD. Therapeutic C3 inhibitor Cp40 abrogates complement activation induced by modern hemodialysis filters. Immunobiology. 2015 Apr;220(4):476-82. doi: 10.1016/j.imbio.2014.10.026. Epub 2014 Nov 3.

Reference Type BACKGROUND
PMID: 25468722 (View on PubMed)

Mastellos DC, Ricklin D, Yancopoulou D, Risitano A, Lambris JD. Complement in paroxysmal nocturnal hemoglobinuria: exploiting our current knowledge to improve the treatment landscape. Expert Rev Hematol. 2014 Oct;7(5):583-98. doi: 10.1586/17474086.2014.953926. Epub 2014 Sep 2.

Reference Type BACKGROUND
PMID: 25213458 (View on PubMed)

Risitano AM, Ricklin D, Huang Y, Reis ES, Chen H, Ricci P, Lin Z, Pascariello C, Raia M, Sica M, Del Vecchio L, Pane F, Lupu F, Notaro R, Resuello RR, DeAngelis RA, Lambris JD. Peptide inhibitors of C3 activation as a novel strategy of complement inhibition for the treatment of paroxysmal nocturnal hemoglobinuria. Blood. 2014 Mar 27;123(13):2094-101. doi: 10.1182/blood-2013-11-536573. Epub 2014 Feb 4.

Reference Type BACKGROUND
PMID: 24497537 (View on PubMed)

Mastellos DC, Reis ES, Yancopoulou D, Hajishengallis G, Ricklin D, Lambris JD. From orphan drugs to adopted therapies: Advancing C3-targeted intervention to the clinical stage. Immunobiology. 2016 Oct;221(10):1046-57. doi: 10.1016/j.imbio.2016.06.013. Epub 2016 Jun 16.

Reference Type BACKGROUND
PMID: 27353192 (View on PubMed)

Maekawa T, Briones RA, Resuello RR, Tuplano JV, Hajishengallis E, Kajikawa T, Koutsogiannaki S, Garcia CA, Ricklin D, Lambris JD, Hajishengallis G. Inhibition of pre-existing natural periodontitis in non-human primates by a locally administered peptide inhibitor of complement C3. J Clin Periodontol. 2016 Mar;43(3):238-49. doi: 10.1111/jcpe.12507. Epub 2016 Mar 3.

Reference Type BACKGROUND
PMID: 26728318 (View on PubMed)

Hajishengallis G, Maekawa T, Abe T, Hajishengallis E, Lambris JD. Complement Involvement in Periodontitis: Molecular Mechanisms and Rational Therapeutic Approaches. Adv Exp Med Biol. 2015;865:57-74. doi: 10.1007/978-3-319-18603-0_4.

Reference Type BACKGROUND
PMID: 26306443 (View on PubMed)

Hajishengallis G, Hajishengallis E, Kajikawa T, Wang B, Yancopoulou D, Ricklin D, Lambris JD. Complement inhibition in pre-clinical models of periodontitis and prospects for clinical application. Semin Immunol. 2016 Jun;28(3):285-91. doi: 10.1016/j.smim.2016.03.006. Epub 2016 Mar 24.

Reference Type BACKGROUND
PMID: 27021500 (View on PubMed)

Zhang Y, Shao D, Ricklin D, Hilkin BM, Nester CM, Lambris JD, Smith RJ. Compstatin analog Cp40 inhibits complement dysregulation in vitro in C3 glomerulopathy. Immunobiology. 2015 Aug;220(8):993-8. doi: 10.1016/j.imbio.2015.04.001. Epub 2015 May 5.

Reference Type BACKGROUND
PMID: 25982307 (View on PubMed)

Mastellos DC, Reis ES, Ricklin D, Smith RJ, Lambris JD. Complement C3-Targeted Therapy: Replacing Long-Held Assertions with Evidence-Based Discovery. Trends Immunol. 2017 Jun;38(6):383-394. doi: 10.1016/j.it.2017.03.003. Epub 2017 Apr 14.

Reference Type BACKGROUND
PMID: 28416449 (View on PubMed)

Hajishengallis G, Hasturk H, Lambris JD; Contributing authors. C3-targeted therapy in periodontal disease: moving closer to the clinic. Trends Immunol. 2021 Oct;42(10):856-864. doi: 10.1016/j.it.2021.08.001. Epub 2021 Sep 2.

Reference Type DERIVED
PMID: 34483038 (View on PubMed)

Other Identifiers

Review additional registry numbers or institutional identifiers associated with this trial.

AMY-101/01

Identifier Type: -

Identifier Source: org_study_id

More Related Trials

Additional clinical trials that may be relevant based on similarity analysis.

A Study of SYNT001 in Healthy Volunteers
NCT03643627 COMPLETED EARLY_PHASE1
MT1013 Clinical TRIAL In Healthy Subject
NCT04783090 COMPLETED PHASE1
A Phase 1 Study of JADE101 in Healthy Participants
NCT07059312 ACTIVE_NOT_RECRUITING PHASE1