Clinical Trials

Multiple clinical trials have evaluated alvelestat (AZD9668) across Phase 1 pharmacokinetic and bioavailability studies to Phase 1b/2 and Phase 2 efficacy trials for metabolic conditions such as type 2 diabetes mellitus and inflammatory pulmonary diseases including chronic obstructive pulmonary disease, cystic fibrosis, alpha-1 antitrypsin deficiency, bronchiolitis obliterans syndrome, and COVID-19. Sponsored by pharmaceutical entities like AstraZeneca and Mereo BioPharma alongside academic and government institutes including the University of Alabama at Birmingham and the National Cancer Institute, these studies range in status from completed or active to withdrawn.

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02669251 ACTIVE_NOT_RECRUITING
Chronic Graft vs Host Disease; Chronic Graft-Versus-Host Disease; Bronchiolitis Obliterans Syndrome
National Cancer Institute (NCI)
 2016-04-28 PHASE1; PHASE2
NCT03679598 COMPLETED
Alpha-1 Antitrypsin Deficiency (AATD); Pi*ZZ, Pi*SZ, Pi*Null, Another Rare Phenotype/Genotype Known to be Associated With Either Low or Functionally Impaired AAT Including F or I Mutations; Emphysema or COPD
University of Alabama at Birmingham
 2019-04-08 PHASE2
NCT03636347 COMPLETED
Alpha 1-Antitrypsin Deficiency; Emphysema; COPD
Mereo BioPharma
 2018-10-29 PHASE2
NCT04539795 COMPLETED
Covid19
University of Alabama at Birmingham
 2021-01-25 PHASE1; PHASE2
NCT02597101 COMPLETED
Type 2 Diabetes Mellitus; Insulin Resistance
Nick Giannoukakis, PhD
 2015-11 PHASE2
NCT01214122 WITHDRAWN
Pharmacokinetics; Pharmacodynamics
AstraZeneca
 2010-11 PHASE1
NCT01054170 COMPLETED
Chronic Obstructive Pulmonary Disease (COPD)
AstraZeneca
 2010-01 PHASE2
NCT01214122 Withdrawn
Pharmacokinetics|Pharmacodynamics
AstraZeneca
 2010-11 Phase 1
NCT00949975 COMPLETED
Chronic Obstructive Pulmonary Disease
AstraZeneca
 2009-07 PHASE2
NCT01023516 COMPLETED
Chronic Obstructive Pulmonary Disease (COPD)
AstraZeneca
 2009-11 PHASE2
NCT01147549 COMPLETED
Healthy
AstraZeneca
 2010-06 PHASE1
NCT01161355 COMPLETED
Healthy
AstraZeneca
 2010-06 PHASE1
NCT01161355 Completed
Healthy
AstraZeneca
 2010-06 Phase 1
NCT01147549 Completed
Healthy
AstraZeneca
 2010-06 Phase 1
NCT01035411 COMPLETED
Chronic Obstructive Pulmonary Disease
AstraZeneca
 2009-11 PHASE1
NCT01034982 COMPLETED
Chronic Obstructive Pulmonary Disease
AstraZeneca
 2009-11 PHASE1
NCT01035411 Completed
Chronic Obstructive Pulmonary Disease
AstraZeneca
 2009-11 Phase 1
NCT01034982 Completed
Chronic Obstructive Pulmonary Disease
AstraZeneca
 2009-11 Phase 1
NCT00757848 COMPLETED
Cystic Fibrosis
AstraZeneca
 2008-10 PHASE2
NCT00769119 COMPLETED
Bronchiectasis
AstraZeneca
 2008-09 PHASE2
NCT00703391 COMPLETED
Chronic Obstructive Pulmonary Disease (COPD)
AstraZeneca
 2008-06 PHASE2

(data from https://clinicaltrials.gov, updated on 2026-09-01)

Check the Alvelestat (AZD9668) product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.

Compliance for Clinical Use

Mechanism and Biochemical Profile

Alvelestat is a highly selective oral inhibitor of neutrophil elastase that binds the enzyme target to block the enzymatic breakdown of extracellular matrix components and suppress neutrophil-mediated tissue inflammation. By mitigating excessive proteolytic degradation and pulmonary tissue injury, this mechanism underpins its therapeutic investigation in neutrophil-driven inflammatory conditions such as chronic obstructive pulmonary disease, alpha-1 antitrypsin deficiency, and COVID-19 respiratory disease.

Appendix RUO and cGMP Quality Standards

Quality Dimension RUO (Research Use Only) cGMP (Current Good Manufacturing Practice)
Clinical Applicability Prohibited in human clinical trials or medical diagnostics. Mandatory for human clinical trials (Phase I–III) and therapies.
Regulatory Status Non-regulated grade; exempt from drug manufacturing laws. Legally enforced by health authorities (e.g., FDA, EMA, NMPA).
Facility Environment Unclassified analytical or research laboratories. Validated Cleanrooms (ISO Class 5–8) with continuous monitoring.
Quality Control Basic purity and activity testing. Rigorous safety release testing (Sterility, Endotoxin, Mycoplasma).
Process Validation Basic equipment calibration; no process validation required. Full qualification (IQ/OQ/PQ) and complete batch records.
Quality Assurance Vendor self-declared without required formal QMS. Mandatory QA/QC unit, Change Control, CAPA, and vendor audits.
Regulatory Impact High risk of IND rejection if used as a critical raw material. Required for IND/NDA filings, supported by Drug Master Files (DMF).

Footnotes

Regulatory Note: Governed by FDA (21 CFR Parts 210/211/312), EMA (EudraLex Vol 4), ICH Guidelines (E6/Q7/Q9/Q10), and compendial standards (USP <71>/<85>/<1043>).

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Note: Technical data last updated: Sep 1, 2026.