Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as bupropion immediate release (IR)
bupropion immediate release · 1 trial · 2 indications
Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.
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 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 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 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 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 is the maximum plasma concentration which was observed directly from the concentration-time data. Paraxanthine was the metabolite of caffeine.
Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.
Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. 5-OH Omeprazole was the metabolite of omeprazole.
Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.
Cmax is the maximum plasma concentration which was observed directly from the concentration-time data.
Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. Hydroxybupropion was the metabolite of bupropion.
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 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 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 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 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 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 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 is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method.
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 is AUC from time 0 to the time of the last quantifiable concentration. It was calculated using the linear trapezoidal/linear interpolation method.
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 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.
Ae0-8 is the amount excreted into the urine over the collection interval of 0 to 8 hours.
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 is the amount excreted into the urine over the collection interval of 0 to 8 hours.
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 is the maximum plasma concentration which was observed directly from the concentration-time data.
Cmax is the maximum plasma concentration which was observed directly from the concentration-time data. LHY746 was the metabolite of encorafenib.
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 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.
| Arm | Type | Description |
|---|---|---|
| Arm 1 - CYP Probe Cocktail | EXPERIMENTAL | Patients 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 Bupropion | EXPERIMENTAL | Patients 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 - Modafinil | EXPERIMENTAL | Patients 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) |
| Name | Type | Description |
|---|---|---|
| losartan | DRUG | taken orally |
| dextromethorphan | DRUG | taken orally |
| caffeine | DRUG | taken orally |
| omeprazole | DRUG | taken orally |
| midazolam | DRUG | taken orally |
| rosuvastatin | DRUG | taken orally |
| bupropion immediate release (IR) | DRUG | taken orally |
| encorafenib | DRUG | taken orally |
| binimetinib | DRUG | taken orally |
| modafinil | DRUG | taken orally |
Key Inclusion Criteria - Patients must meet all of the inclusion criteria to be eligible for enrollment into the study: * Histologically confirmed diagnosis of locally advanced, unresectable or metastatic cutaneous melanoma or unknown primary melanoma American Joint Committee on Cancer (AJCC) Stage...
| Company | Ticker | Trials | Lead Phase | Drugs |
|---|---|---|---|---|
| Merck & Co., Inc. | MRK | 3 | PHASE2 | Pembrolizumab, Gardasil 9 |
| Incyte Corporation | INCY | 1 | PHASE2 | Retifanlimab |
| Novartis AG Sponsored ADR | NVS | 1 | PHASE1 | KFA115 |
| Iovance Biotherapeutics Inc | IOVA | 2 | PHASE2 | Aldesleukin |
| AstraZeneca PLC | AZN | 1 | - | Trastuzumab deruxtecan |
Bupropion immediate release (IR) is a small molecule drug candidate being studied by Pfizer, Inc. (ticker PFE) in oncology. It is in Phase 1 development for advanced solid tumors. The immediate release designation refers to the formulation, which releases the active ingredient rapidly after administration.
Bupropion immediate release is being investigated for use in patients with advanced solid tumors, including metastatic melanoma. It was evaluated as part of a pharmacokinetic drug-drug interaction study. The research explores its potential role in this oncology setting.
Bupropion immediate release targets SLC6A3 and SLC6A2, which are transporters also known as the dopamine transporter and norepinephrine transporter. It acts as an inhibitor of these targets. This mechanism is being studied in the context of advanced solid tumors.
Bupropion immediate release is being developed by Pfizer, Inc., which trades under the ticker symbol PFE. Pfizer is the sponsor of the clinical research program for this drug candidate in oncology.
Bupropion immediate release is in Phase 1 clinical development. It is an investigational drug and has not been approved by the FDA for the studied indication. The Phase 1 program includes one completed trial.
Bupropion immediate release has been studied in one completed clinical trial, NCT03864042. This Phase 1 trial was titled a pharmacokinetic drug-drug interaction study of encorafenib and binimetinib on probe drugs in patients with BRAF V600-mutant melanoma or other advanced solid tumors. It enrolled 56 patients across the United States, Belgium, Canada, Netherlands, and Spain.
Yes, bupropion immediate release is also known as bupropion immediate release (IR) or simply bupropion IR. The IR abbreviation stands for immediate release, indicating the formulation's rapid drug release profile. Both names refer to the same drug candidate.