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Caffeine

Phase 1

Healthy Participants | Small molecule | Other |Pfizer, Inc.|Last Updated: Sep 27, 2024

Success Probability

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Market & Valuation

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Trial Design

UNCONTROLLED
Total Trials1
Total Enrollment12

FDA Designations

No designations recorded

Clinical trial landscape

Caffeine · 2 trials · 3 indications

Phase 1 2
NCT04655040Estimation of the Effect of Multiple Dose Ritlecitinib (PF-06651600) on the Pharmacokinetics of a Single Dose of Caffeine in Healthy ParticipantsHealthy Participants
COMPLETED12 Analytics
NCT03864042Pharmacokinetic Drug-drug Interaction Study of Encorafenib and Binimetinib on Probe Drugs in Patients With BRAF V600-mutant Melanoma or Other Advanced Solid TumorsAdvanced Solid Tumors
COMPLETED56 Analytics
PHASE1COMPLETED
Estimation of the Effect of Multiple Dose Ritlecitinib (PF-06651600) on the Pharmacokinetics of a Single Dose of Caffeine in Healthy Participants
Healthy ParticipantsUnlock trial analytics
PHASE1COMPLETED
Pharmacokinetic Drug-drug Interaction Study of Encorafenib and Binimetinib on Probe Drugs in Patients With BRAF V600-mutant Melanoma or Other Advanced Solid Tumors
Advanced Solid TumorsUnlock trial analytics

Study Endpoints

Primary Endpoints

Area under the plasma concentration-time profile from time 0 extrapolated to infinity (AUCinf) of caffeine
Day1 and Day8: Hour 0, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 10, 12, 16, and 24. Day 8: Hour 36 and 48
Maximum Concentration (Cmax) of Plasma Midazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.

Cmax of Plasma Total 1-OH Midazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. The metabolites of midazolam included total 1-OH midazolam, free 1-OH midazolam, and glucuronide conjugated 1-hydroxymidazolam.

Cmax of Plasma Free 1-OH Midazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. The metabolites of midazolam included total 1-OH midazolam, free 1-OH midazolam, and glucuronide conjugated 1-hydroxymidazolam.

Cmax of Plasma Glucuronide Conjugated 1-Hydroxymidazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. The metabolites of midazolam included total 1-OH midazolam, free 1-OH midazolam, and glucuronide conjugated 1-hydroxymidazolam.

Cmax of Plasma Absolute Caffeine on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. Due to dietary caffeine intake may resulted in positive pre-dose concentrations, absolute and/or baseline-adjusted caffeine were analyzed. Baseline adjusted concentration = measured concentration - \[predose concentration\*e\^(-Kel\*t)\], where Kel is terminal elimination rate constant based on actual measured concentration values for each profile and t is the actual sampling time.

Cmax of Plasma Baseline-Adjusted Caffeine on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. Due to dietary caffeine intake may resulted in positive pre-dose concentrations, absolute and/or baseline-adjusted caffeine were analyzed. Baseline adjusted concentration = measured concentration - \[predose concentration\*e\^(-Kel\*t)\], where Kel is terminal elimination rate constant based on actual measured concentration values for each profile and t is the actual sampling time.

Cmax of Plasma Paraxanthine on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. Paraxanthine was the metabolite of caffeine.

Cmax of Plasma Omeprazole on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.

Cmax of Plasma 5-OH Omeprazole on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. 5-OH Omeprazole was the metabolite of omeprazole.

Cmax of Plasma Rosuvastatin on Day -7, Day 1 and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.

Cmax of Plasma Bupropion on Day -7, Day 1 and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.

Cmax of Plasma Hydroxybupropion on Day -7, Day 1 and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. Hydroxybupropion was the metabolite of bupropion.

Area Under the Concentration-Time Profile From Time 0 to The Time of The Last Quantifiable Concentration (AUClast) of Plasma Midazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is area under the concentration-time profile (AUC) from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method.

AUClast of Plasma Total 1-OH Midazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. The metabolites of midazolam included total 1-OH midazolam, free 1-OH midazolam, and glucuronide conjugated 1-hydroxymidazolam.

AUClast of Plasma Free 1-OH Midazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. The metabolites of midazolam included total 1-OH midazolam, free 1-OH midazolam, and glucuronide conjugated 1-hydroxymidazolam.

AUClast of Plasma Glucuronide Conjugated 1-Hydroxymidazolam on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. The metabolites of midazolam included total 1-OH midazolam, free 1-OH midazolam, and glucuronide conjugated 1-hydroxymidazolam.

AUClast of Plasma Absolute Caffeine on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. Due to dietary caffeine intake may resulted in positive pre-dose concentrations, absolute and/or baseline-adjusted caffeine were analyzed. Baseline adjusted concentration = measured concentration - \[predose concentration\*e\^(-Kel\*t)\], where Kel is terminal elimination rate constant based on actual measured concentration values for each profile and t is the actual sampling time.

AUClast of Plasma Baseline-Adjusted Caffeine on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. Due to dietary caffeine intake may resulted in positive pre-dose concentrations, absolute and/or baseline-adjusted caffeine were analyzed. Baseline adjusted concentration = measured concentration - \[predose concentration\*e\^(-Kel\*t)\], where Kel is terminal elimination rate constant based on actual measured concentration values for each profile and t is the actual sampling time.

AUClast of Plasma Paraxanthine on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. Paraxanthine was the metabolite of caffeine.

AUClast of Plasma Omeprazole on Day -7, Day 1, and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method.

AUClast of Plasma 5-OH Omeprazole in Arm 1 on Day -7, Day 1 and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. 5-OH Omeprazole was the metabolite of omeprazole.

AUClast of Plasma Rosuvastatin on Day -7, Day 1 and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method.

AUClast of Plasma Bupropion on Day -7, Day 1 and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method.

AUClast of Plasma Hydroxybupropion on Day -7, Day 1 and Day 14
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day -7, Day 1 and Day 14

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. Hydroxybupropion was the metabolite of bupropion.

The Amount Eliminated Via Urine Over an 8-Hour Period (Ae0-8) of Losartan on Day -7, Day 1 and Day 14
0 to 8 hours after dosing on Days -7, 1 and 14

Ae0-8 is the amount excreted into the urine over the collection interval of 0 to 8 hours.

Ae0-8 of E-3174 on Day -7, Day 1 and Day 14
0 to 8 hours after dosing on Days -7, 1 and 14

Ae0-8 is the amount excreted into the urine over the collection interval of 0 to 8 hours. E-3174 was the metabolite of losartan.

Ae0-8 of Dextromethorphan on Day -7, Day 1 and Day 14
0 to 8 hours after dosing on Days -7, 1 and 14

Ae0-8 is the amount excreted into the urine over the collection interval of 0 to 8 hours.

Ae0-8 of Dextrorphan on Day -7, Day 1 and Day 14
0 to 8 hours after dosing on Days -7, 1 and 14

Ae0-8 is the amount excreted into the urine over the collection interval of 0 to 8 hours. Dextrorphan was the metabolite of dextromethorphan.

Cmax of Plasma Encorafenib on Day 14 and Day 21 in Arm 3
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day 14 and Day 21

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.

Cmax of Plasma LHY746 on Day 14 and Day 21 in Arm 3
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day 14 and Day 21

Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. LHY746 was the metabolite of encorafenib.

AUClast of Plasma Encorafenib on Day 14 and Day 21 in Arm 3
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day 14 and Day 21

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method.

AUClast of Plasma LHY746 on Day 14 and Day 21 in Arm 3
Predose, and 1, 2, 3, 4, 6 and 8 hours postdose on Day 14 and Day 21

AUClast is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method. LHY746 was the metabolite of encorafenib.

Secondary Endpoints

Incidence of treatment-emergent adverse events
Baseline through Day 28
Incidence of clinically significant abnormalities in vital signs
Baseline through Day 11
Incidence of clinically significant abnormalities in clinical laboratory values
Baseline through Day 11
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeBASIC_SCIENCE

Treatment Arms

ArmTypeDescription
Caffeine and RitlecitinibEXPERIMENTALIn Period 1 Day 1, participants will be dosed with a single oral administration of caffeine 100 milligram (mg) tablet. In Period 2 Day 1 to Day 7, participants will be dosed with a single oral administration of ritlecitinib 200 milligram (mg) tablet. On Day 8, participants will be dosed with caffeine 100 milligram (mg) tablet within 5 minutes after administration of a 200 milligram (mg) dose of ritlecitinib on the morning of Day 8. Dosing with oral 200 milligram (mg) ritlecitinib QD will continue until Day 9.
Arm 1 - CYP Probe CocktailEXPERIMENTALPatients will receive a single oral dose of the CYP Probe Cocktail on Day -7, Day 1, and Day 14: * 25 mg losartan oral tablet * 30 mg dextromethorphan oral capsule * 50 mg caffeine oral liquid * 20 mg omeprazole oral capsule * 2 mg midazolam oral syrup encorafenib/binimetinib continuous daily dosing starting Day 1: * 450 mg (6 x 75 mg) encorafenib oral capsules once daily (QD) * 45 mg (3 x 15 mg) binimetinib oral tablet twice daily (BID) All drugs will be taken within 10 minutes.
Arm 2 - Rosuvastatin and BupropionEXPERIMENTALPatients will receive a single oral dose of rosuvastatin and bupropion once on Day -7, Day 1 and Day 14: * 10 mg rosuvastatin oral tablet * 75 mg bupropion immediate release (IR) oral tablet encorafenib/binimetinib continuous daily dosing starting Day 1: * 450 mg (6 x 75 mg) encorafenib oral capsules once daily (QD) * 45 mg (3 x 15 mg) binimetinib oral tablet twice daily (BID) All drugs will be taken within 10 minutes.
Arm 3 - ModafinilEXPERIMENTALPatients will begin encorafenib/binimetinib continuous daily dosing starting Day 1: * 450 mg (6 x 75 mg) encorafenib oral capsules once daily (QD) * 45 mg (3 x 15 mg) binimetinib oral tablet twice daily (BID) then receive continuous treatment of modafinil on Day 15 through Day 21: \- 400 mg modafinil tablet once daily (QD)

Interventions

NameTypeDescription
CaffeineDRUG100milligram (mg) tablet taken orally in period 1 and period 2
RitlecitinibOTHER200 milligrams (mg) taken orally once a day(QD) for 8 days
losartanDRUGtaken orally
dextromethorphanDRUGtaken orally
omeprazoleDRUGtaken orally
midazolamDRUGtaken orally
rosuvastatinDRUGtaken orally
bupropion immediate release (IR)DRUGtaken orally
encorafenibDRUGtaken orally
binimetinibDRUGtaken orally
modafinilDRUGtaken orally
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Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: -Male and female participants must be 18 to 55 years of age, inclusive, at the time of signing the ICD. -BMI of 17.5 to 30.5 kg/m2; and a total body weight \>50 kg (110 lb). - * Male and female participants who are healthy as determined by medical evaluation including medical ...

Countries:United StatesBelgiumCanadaNetherlandsSpain
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Frequently asked questions about Caffeine

What is Caffeine used for?

Caffeine is an investigational small molecule being studied in clinical trials for healthy participants and advanced solid tumors. It is being evaluated as a probe drug in pharmacokinetic interaction studies, not as a therapeutic treatment for these conditions. The drug is in Phase 1 clinical development.

What does Caffeine target?

Caffeine does not have a specific molecular target or target class associated with its use in the clinical trials. It is being studied as a probe drug to assess potential drug-drug interactions with other investigational agents, rather than for its own therapeutic mechanism of action.

Who makes Caffeine?

Caffeine is being developed by Pfizer, Inc., a biopharmaceutical company listed on the New York Stock Exchange under the ticker symbol PFE. The company is conducting clinical trials to evaluate caffeine as a probe drug in pharmacokinetic studies.

What phase is Caffeine in?

Caffeine is in Phase 1 clinical development. It is an investigational drug and has not been approved by regulatory authorities for any indication. The clinical trials involving caffeine are early-stage studies focused on pharmacokinetic interactions.

What clinical trials is Caffeine in?

Caffeine has been studied in two completed Phase 1 clinical trials. NCT03864042 evaluated drug-drug interactions in patients with advanced solid tumors or metastatic melanoma, enrolling 56 participants. NCT04655040 assessed the effect of ritlecitinib on caffeine pharmacokinetics in healthy participants, enrolling 12 participants.

Is Caffeine the same as other drugs?

Caffeine is not known to have alternative names in the context of these clinical trials. It is being studied as a probe drug to evaluate potential interactions with other medications, but no other names for caffeine itself have been reported in the trial data.