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Bupropion XL

Phase 3

Depressive Disorder, Major | Small molecule | Psychiatry |GSK plc|Last Updated: Sep 13, 2018

Target and mechanism

ModalitySmall molecule

Also known as Bupropion HCl XL tablet 150mg

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindUNCONTROLLED
Total Trials2
Total Enrollment380

FDA Designations

No designations recorded

Clinical trial landscape

Bupropion XL · 2 trials · 1 indication

Phase 3 1Phase 1 1
NCT00093288Major Depressive Disorder In The ElderlyDepressive Disorder, Major
COMPLETED364 Analytics
PHASE3COMPLETED
Major Depressive Disorder In The Elderly
Depressive Disorder, MajorUnlock trial analytics

Study Endpoints

Primary Endpoints

Montgomery-Asberg Depression Rating Scale
Time taken to reach peak plasma concentration (Tmax) of Bupropion HCl and its metabolites after single dose.
Day 1 and Day 2.

Blood sample will be collected at pre-dosing, and 2, 3, 4, 5, 6, 8, 12, 16, and 24 hour (h) post dose.

Maximum observed concentration (Cmax) in plasma of Bupropion HCl and its metabolites after single dose.
Day 1 and Day 2.

Blood sample will be collected at pre-dosing, and 2, 3, 4, 5, 6, 8, 12, 16, and 24 h post dose.

Area under the plasma concentration-time curve from time 0 to 24 hours (AUC [0-24]) of Bupropion HCl and its metabolites after single dose.
Day 1 and Day 2.

Blood sample will be collected at pre-dosing, and 2, 3, 4, 5, 6, 8, 12, 16, and 24 h post dose.

Tmax in plasma of Bupropion HCl and its metabolites after repeated doses
Day 5 to Day 19 .

Blood sample will be collected at pre-dosing, and 2, 5, 8 and 12h post dose after 150 mg dose (Day 5) and first 300 mg (Day 6) dose respectively. Blood sample will be also collected at pre-dosing, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96 and 120 h post dose after 300 mg dose (Day 14 to 19).

Steady state concentration (Css)-Css Minimum (Css_min), Css Maximum (Css_max), Average Css (Css_av) in plasma of Bupropion HCl and its metabolites after repeated dose.
Day 5 to Day 19.

Blood sample will be collected at pre-dosing, and 2, 5, 8 and 12h post dose after 150 mg dose (Day 5) and first 300 mg (Day 6) dose respectively, and pre-dosing, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96 and 120 h post dose after last 300 mg dose (Day 14 to 19).

Elimination half-life (t ½) in plasma of Bupropion HCl and its metabolites after repeated dose.
Day 5 to Day 19.

Blood sample will be collected at pre-dosing, and 2, 5, 8 and 12 h post dose after 150 mg dose (Day 5) and first 300 mg (Day 6) dose respectively, and pre-dosing, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96 and 120 h post dose after last 300 mg dose (Day 14 to 19).

Apparent clearance (CL/F) in plasma of Bupropion HCl and its metabolites after repeated dose.
Day 5 to Day 19.

Blood sample will be collected at pre-dosing, and 2, 5, 8 and 12 h post dose after last 150 mg dose (Day 5) and first 300 mg (Day 6) dose respectively, and pre-dosing, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96 and 120 h post dose after last 300 mg dose (Day 14 to 19).

Area under the concentration-time curve over the dosing interval (AUC [0-tau]) in plasma of Bupropion HCl and its metabolites after repeated dose.
Day 5 to Day 19.

Blood sample will be collected at pre-dosing, and 2, 5, 8 and 12 h post dose after 150 mg dose (Day 5) and first 300 mg (Day 6) dose respectively, and pre-dosing, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, 48, 72, 96 and 120 h post dose after last 300 mg dose (Day 14 to 19).

Secondary Endpoints

Montgomery-Asberg Depression Rating Scale Clinical Global Impression Improvement Scale Clinical Global Impression Severity Scale Hamilton Anxiety Rating Scale
Number of subjects with adverse event (AE) and serious adverse event (SAE).
Up to Day 33.
Number of subjects with abnormal Haematology parameters as a measure of safety.
Up to Day 19.
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Bupropion XL once dailyEXPERIMENTALHealthy subjects will receive Bupropion XL 150milligram (mg) once daily for 5 days (Day 1 to Day 5) and then Bupropion XL 300 mg once daily from Day 6 to Day 14.

Interventions

NameTypeDescription
bupropion XLDRUG -
Bupropion HCl XL tablet 150mgDRUGThe 150 mg of tablet will be given to subject once daily orally. Subject will be instructed to swallow whole tablet with 240 ml of water, without crushed, divided or chewed.
Bupropion HCl XL tablet 300mgDRUGThe 300 mg of tablet will be given to subject once daily orally. Subject will be instructed to swallow whole tablet with 240 ml of water, without crushed, divided or chewed.
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Eligibility Criteria

Age Range65 Years to N/A
SexALL
Healthy VolunteersNo
Study Sites16

Inclusion Criteria: * Primary diagnosis of Major Depressive Disorder with DSM-IV criteria for their current episode for at least 8 weeks. Exclusion Criteria: * Patient has current or past history of seizure disorder or brain injury. * Patient has a diagnosis of anorexia or bulimia within the past...

Countries:AustraliaBelgiumFinlandNetherlandsNorwayRussiaChina
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