Discovery Process of Enlicitide: A Macrocyclic Peptide Therapeutic

Hubert Josien published a dataset on figshare on 2026-05-27 describing the discovery process of enlicitide (MK-0616), an orally active macrocyclic peptide therapeutic targeting PCSK9 for LDL-C reduction. The dataset likely contains information on the design-make-test-analyze (DMTA) cycle and preclinical profiling of candidate compounds. The modular fragment assembly strategy used to overcome development bottlenecks in a prior lead compound is a central feature.

Use Cases

• Analyze structure-activity relationships based on the modular fragment assembly (North/East/South/West/tail) approach described.
• Study pharmacokinetic (PK) property optimization based on the mention of improved solubility, stability, and PK in selected compounds.
• Benchmark design-make-test-analyze (DMTA) cycle acceleration strategies based on the novel scalable solution-phase assembly method reported.

Strengths

• The description details specific chemical modifications (northern lactam staple, southern spacer, RCM-derived cross-link) used to improve compound properties.
• The dataset is associated with a specific, clinically progressed compound (enlicitide/MK-0616).

Limitations

• Column-level documentation is absent; field semantics must be inferred after download.
• Row count is unknown, which may limit suitability assessment.
• The dataset is very small (6.2 KB), indicating limited scope.

Provenance

Source

figshare

Collection Method

Likely contains data generated during the drug discovery process for enlicitide.

Freshness

Last updated 2026-05-27 14:40:41; freshness should be verified.