Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Caffeine · 1 trial · 1 indication
Plasma AUC (0-inf) of probe and metabolite (where applicable) when administered alone, in combination with other probes/inhibitors
| Arm | Type | Description |
|---|---|---|
| Probe drugs | EXPERIMENTAL | Caffeine 100 mg CYP1A2 Pioglitazone 15 mg CYP2C8 Flurbiprofen 40 mg CYP2C9 Omeprazole 20 mg CYP2C19 Dextromethorphan 45 mg CYP2D6 Midazolam 3 mg (Part 1, Part 2 Cohorts B and C) 1 mg (Part 2 Cohort A) CYP3A4/5 Rosuvastatin 10 mg OATP1B1 |
| Default Inhibitors | EXPERIMENTAL | A Ketoconazole 400 mg once-daily Day 1 through Day 9 CYP3A4 B Fluconazole 400 mg x1 dose on Day 1 200 mg once-daily Day 2 through Day 9 CYP2C9 C Rifampin 600 mg x1 dose on Day 1 and Day 8 OATP1B1 |
| Name | Type | Description |
|---|---|---|
| Caffeine | DRUG | Caffeine dosed at 100 mg as probe for CYP1A2 pathway |
| Rosiglitazone | DRUG | Dosed at 4 mg as probe for CYP2C8 pathway |
| Flurbiprofen | DRUG | Dosed at 40 mg, probe for CYP2C9 pathway |
| Omeprazole | DRUG | Dosed at 20 mg, probe for CYP2C19 pathway |
| Dextromethorphan | DRUG | Dosed at 30 mg, probe for CYP2D6 pathway |
| Midazolam | DRUG | Dosed at 3 mg for Part 1, Part 2 cohorts B and C and 1 mg for Part 2 Cohort A, probe drug for CYP3A4/5 pathway |
| Rosuvastatin | DRUG | Dosed at 10 mg, probe drug for OATP1B1 pathway |
| Ketoconazole | DRUG | Dosed at 400 mg once-daily Day 1 through Day 9, inhibitor of CYP3A4 |
| Fluconazole | DRUG | Dosed at 400 mg x 1 dose on day 1, 200 mg once daily on days 2 through 9, inhibitor of CYP2C9 pathway |
| Rifampin | DRUG | Dosed at 600 mg x 1 dose on Day 1 and Day 8, inhibitor of OATP1B1 pathway |
Inclusion Criteria: * Healthy as determined by a responsible physician * Subjects are not poor metabolizers based on genotyping for the major CYP2C9, 2C19, 2D6 alleles * Male or female between 20 and 50 years of age at the time of screening, inclusive. * A female subject is eligible to participate ...
Caffeine is being studied as a probe compound in drug interaction research. It is used in a clinical trial to validate multiple probe compounds for evaluating drug interactions. The study involves healthy volunteers and is designed to assess how caffeine interacts with other substances, helping to understand its role in drug metabolism and interaction assessments.
Caffeine is being developed by GSK plc, a global pharmaceutical company traded under the ticker GSK. GSK is conducting clinical research on caffeine as part of a drug interaction validation study. The company is evaluating caffeine's utility as a probe compound in pharmacokinetic studies.
Caffeine is in Phase 1 clinical development. The Phase 1 trial, NCT00964106, has been completed. This early-stage study focused on validating caffeine as a probe compound for drug interaction evaluation. Caffeine remains investigational and is not approved for this specific use.
Caffeine is associated with one completed clinical trial, NCT00964106, titled 'Validation Study of Multiple Probe Compounds for Drug Interaction Evaluation.' This Phase 1 study enrolled 87 participants in South Korea and involved healthy volunteers aged 20 years and older. The trial was controlled but not double-blinded.
Caffeine is a small molecule that acts as a central nervous system stimulant. In the context of drug interaction studies, it is used as a probe compound to assess the activity of drug-metabolizing enzymes, particularly cytochrome P450 enzymes. By measuring caffeine metabolism, researchers can evaluate potential drug interactions.