Approval Probability
TA Base Rate
Adjusted LOA
ML Risk
Also known as GW679769 (Casopitant) oral tablets, GW679769 oral tablets, GW679769 (casopitant), Dexamethasone, Aprepitant, Ondansetron, Ondansetron Hydrochloride, Casopitant
GW679769 · 26 trials · 16 indications
Complete response was defined as no vomiting, no retching and no use of anti-emetic rescue medication. Participants who vomited or retched or received rescue medication in the acute phase (0- 24 hours) following administration of oxaliplatin were also considered as complete response failures in the subsequent delayed (24-120 hour) time period, irrespective of actual response in the delayed phase. However, participants who vomited or retched or received rescue medication in the delayed (24-120 hours) phase were not considered as failures in the acute (0-24 hours) phase. The overall phase began at the start of the administration of the oxaliplatin infusion. Percentage of participants who achieved a complete response in the overall phase (0-120 hours) are presented.
Complete response was defined as no vomiting/retching and no rescue therapy) over the first 120 hours following the initiation of their first cycle of a cisplatin-based HEC regimen. Vomiting was defined as the forceful expulsion of gastrointestinal contents through the mouth or nose. Retching was defined as the labored, spasmodic, rhythmic contraction of the respiratory and abdominal muscles in an attempt to vomit, that was not productive of gastrointestinal contents (also known as "dry heaves").
Complete response defined as no vomiting or retching and no rescue therapy during the first 24 hours following placement of the last suture/staple. Vomiting defined as the forceful expulsion of gastrointestinal contents through the mouth or nose. Retching defined as the labored, spasmodic, rhythmic contraction of the respiratory and abdominal muscles in an attempt to vomit that is not productive of gastrointestinal contents (also known as "dry heaves"). Study participants who receive antiemetic rescue medication(s) during the initial 24 hours was considered treatment failures.
WASO was measured from persistent sleep onset to lights on. It was calculated as number of wake epochs from persistent sleep onset to lights on divided by 2. WASO measures was analyzed using a mixed effect model with session and treatment as fixed effect and participants as random effect.
Plasma samples of study drugs
Blood samples will be collected at the indicated time points for pharmacokinetic analysis.
Blood samples will be collected at the indicated time points for pharmacokinetic analysis.
Blood samples for pharmacokinetics (PK) analysis will be collected at the indicated time points. AUC will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. AUC will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. AUC will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. AUC will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GW679769 concentration.
Blood samples for PK analysis will be collected at the indicated time points. AUC will be calculated from plasma GSK525060 concentration.
Blood samples for PK analysis will be collected at the indicated time points. AUC will be calculated from plasma GSK525060 concentration.
Blood samples for PK analysis will be collected at the indicated time points. AUC will be calculated from plasma GSK525060 concentration.
Blood samples for PK analysis will be collected at the indicated time points. AUC will be calculated from plasma GSK525060 concentration.
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GSK525060 concentration.
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GSK525060 concentration
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GSK525060 concentration.
Blood samples for PK analysis will be collected at the indicated time points. Cmax will be calculated from plasma GSK525060 concentration.
| Arm | Type | Description |
|---|---|---|
| Control | PLACEBO_COMPARATOR | Placebo + standard antiemetics |
| Single Dose IV | EXPERIMENTAL | Casopitant + standard antiemetics |
| Single dose oral | EXPERIMENTAL | ondansetron 8 mg oral twice daily on Day 1-3 and dexamethasone 8 mg IV + casopitant 150 mg on Day 1 |
| 3-day oral | EXPERIMENTAL | ondansetron 8 mg oral twice daily on Day 1-3 and dexamethasone 8 mg IV + casopitant 150 mg on Day 1 + 50 mg on days 2 \& 3 |
| 3-day IV/oral | EXPERIMENTAL | ondansetron 8 mg oral twice daily on Day 1-3 and dexamethasone 8 mg IV on Day 1 + 90 mg IV casopitant on day 1 and 50 mg oral casopitant on days 2 \& 3 |
| Arm 1 | EXPERIMENTAL | - |
| GW679769 | EXPERIMENTAL | 120mg once a day |
| Placebo | PLACEBO_COMPARATOR | Placebo once a day |
| Subjects in Part A | EXPERIMENTAL | Subjects will receive 100 milligrams (mg) of oral dolasetron once daily for 3 days during treatment period 1. In treatment period 2, subjects will receive 100 mg oral dolasetron once daily on days 1, 2 and 3 along with 150 mg oral casopitant on day 1 and 50 mg oral casopitant on days 2 and 3. The treatment periods will be separated by will be separated by a 5 - 14 day wash-out period. |
| Subjects in Part B | EXPERIMENTAL | Subjects will receive 2 mg of oral granisetron once daily for 3 days during treatment period 1. In treatment period 2, subjects will receive 2 mg oral granisetron once daily on days 1, 2 and 3 along with 150 mg oral casopitant once daily on day 1 and 50 mg oral casopitant once daily on days 2 and 3. The treatment periods will be separated by will be separated by a 5 - 14 day wash-out period. |
| Subjects in Part C | EXPERIMENTAL | Subjects will receive 4 mg of oral rosiglitazone once daily for 3 days during treatment period 1. In treatment period 2, subjects will receive 4 mg oral rosiglitazone once daily on days 1, 2 and 3 along with 150 mg oral casopitant once daily on day 1 and 50 mg oral casopitant once daily on days 2 and 3. The treatment periods will be separated by will be separated by a 5 - 14 day wash-out period. |
| Docetaxel | ACTIVE_COMPARATOR | Docetaxel |
| Docetaxel/Casopitant | EXPERIMENTAL | Docetaxel/Casopitant |
| Cohort 1 | EXPERIMENTAL | All subjects in Cohort 1 will receive ketoconazole 400 milligrams (mg) once daily on Day 1 to 9 and oral casopitant 150 mg on Day 4 and 50 mg on Day 5 and Day 6 of treatment period 1. After a washout period of 21 days, subjects will be administered oral casopitant 150 mg on Day 1 and 50 mg on Day 2 and Day 3 of treatment period 2. |
| Cohort 2, Group A | PLACEBO_COMPARATOR | Subjects will receive placebo once daily on Day 1 to Day 3 in treatment period 1. Subjects will receive ketoconazole 400 mg once daily on Day 1 to Day 9 and oral placebo once daily on Days 4, 5 and 6 in treatment period 2. There will be a 14-day washout period between treatment periods 1 and 2. |
| Cohort 2, Group B | EXPERIMENTAL | In treatment period 1, subjects will receive oral casopitant 150 mg on Day 1 and 50 mg on Days 2 and 3. In treatment period 2, they will be administered ketoconazole 400 mg once daily on Day 1 to Day 9 and oral casopitant 150 mg on Day 4 and 50 mg on Days 5 and 6. There will be a 14-day washout period between treatment periods 1 and 2. |
| Treatment Period 1 | EXPERIMENTAL | Subject will receive single oral dose of 150 milligram (mg) of Casopitant. There will be wash out period of 7 days. |
| Treatment Period 2 | EXPERIMENTAL | Subjects will receive rifampin 600 mg once daily on Days 1 - 9. On Day 8 subjects will receive a single dose of oral casopitant 150 mg along with rifampin. |
| Treatment regimen A | EXPERIMENTAL | In treatment regimen A subject will co-administer casopitant and warfarin over three-day period (Day 1 150 milligram per day \[mg/day\], Day 2 50 mg/day, Day 3 50 mg/day) and from Days 4 to 10 subject will administer only warfarin. |
| Treatment regimen B | EXPERIMENTAL | In treatment regimen B subject will co-administer casopitant 60 mg/day and warfarin for 14 days. |
| Treatment regimen C | EXPERIMENTAL | In treatment regimen C subject will co-administer warfarin and casopitant 30 mg/day for 14 days. |
| Cohort 1 Treatment Period 1 | EXPERIMENTAL | Subjects will receive single oral dose of 100 milligram (mg) of Casopitant. There will be wash out period of 7 days. |
| Cohort 1 Treatment Period 2 | EXPERIMENTAL | Subjects will receive ketoconazole 400 mg once daily on Days 1 - 7. On Day 4 subjects will receive a single dose of oral casopitant 100 mg along with ketoconazole. |
| Cohort 2 Treatment Period 1 | EXPERIMENTAL | Subjects will receive single oral dose of 50 mg of Casopitant. There will be wash out period of 7 days. |
| Cohort 2 Treatment Period 2 | EXPERIMENTAL | Subjects will receive ketoconazole 400 mg once daily on Days 1 - 7. On Day 4 subjects will receive a single dose of oral casopitant 50 mg along with ketoconazole. |
| Subjects receiving casopitant | EXPERIMENTAL | Eligible subjects will receive a 100 milligrams oral dose of casopitant once daily for five consecutive days. |
| Healthy subjects receiving GW679769 | EXPERIMENTAL | Healthy Subjects will receive single 100 milligram (mg) oral doses of GW679769 for five consecutive days. |
| Subjects with hepatic impairment receiving GW679769 | EXPERIMENTAL | Subjects with hepatic impairment will receive single 100 mg oral doses of GW679769 for five consecutive days. |
| Name | Type | Description |
|---|---|---|
| Casopitant | DRUG | Experimental NK-1 receptor antagonist |
| Dexamethasone | DRUG | Standard antiemetics |
| Placebo | DRUG | Placebo to match IV casopitant |
| Ondansetron | DRUG | Standard antiemetics |
| Oral Casopitant (GW679769) | DRUG | - |
| IV Casopitant (GW679769) | DRUG | - |
| IV ondansetron hydrochloride | DRUG | - |
| Oral dexamethasone | DRUG | - |
| Casopitant (GW679769) oral tablets | DRUG | - |
| Casopitant (GW679769) intravenous | DRUG | - |
| Dexamethasone intravenous | DRUG | - |
| Ondansetron oral tablets | DRUG | - |
| GW679769 (casopitant) | DRUG | - |
| GW679769 | DRUG | - |
| GW679769 oral tablets | DRUG | 2x GW679769 60mg tablets |
| Aprepitant | DRUG | - |
| Ondansetron Hydrochloride | DRUG | - |
| dolasetron | DRUG | The dose of oral dolasetron will be comprised of 100 mg (one 100 mg tablet or two 50 mg tablets). Dolasetron will be taken with 240 mL of water on an empty stomach following at least 2 hour fast. |
| granisetron | DRUG | The dose of oral granisetron will be comprised of 2 mg (two 1 mg tablets). Granisetron will be taken with 240 mL of water on an empty stomach following at least 2 hour fast. |
| rosiglitazone | DRUG | The dose of oral rosiglitazone will be comprised of 4 mg (two 2 mg tablets or one 4 mg tablet). Rosiglitazone will be taken with 240 mL of water on an empty stomach following at least 2 hour fast. |
| Docetaxel | DRUG | Docetaxel |
| Casopitant/Docetaxel | DRUG | Casopitant/Docetaxel |
| Casopitant 150 mg | DRUG | Casopitant 150 mg will be available as white, film-coated tablets. Casopitant tablets will be taken with 240 milliliters (mL) of water at room temperature on an empty stomach. |
| Ketoconazole | DRUG | Ketoconazole will be available as 200 mg tablets which will be taken with 240 mL of water on an empty stomach (after a 2 hour fast on Day 4 of Treatment Period 2 and after a 1 hour fast on all other dosing days). |
| Casopitant 150 mg matching placebo | DRUG | Casopitant 150 mg matching placebo will be available as white, film-coated tablets. |
| Casopitant 50 mg | DRUG | Casopitant 50 mg will be available as pale orange, film-coated tablets. Casopitant tablets will be taken with 240 mL of water at room temperature on an empty stomach. |
| Casopitant 50 mg matching placebo | DRUG | Casopitant 50 mg matching placebo will be available as pale orange, film-coated tablets. |
| GW679769 (Casopitant) oral tablets | DRUG | Casopitant tablets will be available with dose strength of 50 mg. Subjects will receive three 50 mg tablets for the dose of 150 mg. On Day 8 of Treatment Period 2, the dose of casopitant and rifampin is to be taken at the same time. |
| Rifampin oral capsules | DRUG | Rifampin capsules will be available with dose strength of 300 mg. Subjects will receive two 300 mg capsules for the dose of 600 mg. On Day 8 of Treatment Period 2, the dose of casopitant and rifampin is to be taken at the same time. |
| Warfarin oral tablets | DRUG | Warfarin will be available in the dose strength of 5 mg |
| casopitant 100 mg | DRUG | Casopitant tablets will be available with dose strength of 50 mg. Subjects will receive two 50 mg tablets for the dose of 100 mg. On Day 4 of Treatment Period 2, the dose of casopitant and ketoconazole is to be taken at the same time |
Inclusion Criteria: * A subject will be considered eligible for initial inclusion in this study, and progression into subsequent cycles of therapy within the study, only if all of the following criteria apply: * Subject understands the nature and purpose of this study and the study procedures and h...
GW679769 has been studied in clinical trials for major depressive disorder, chemotherapy-induced nausea and vomiting, postoperative nausea and vomiting, overactive bladder and urinary incontinence, nonulcer dyspepsia, and primary insomnia. It is an investigational small molecule and is not described as approved for any indication.
GW679769 is developed by GSK plc, which trades under the ticker GSK. The company sponsored the Phase 2 and Phase 1 studies of the compound, including trials in major depressive disorder and in chemotherapy-induced nausea and vomiting.
GW679769 is in Phase 2 development. Four trials are recorded, all completed, with no active trials: two Phase 2 studies and two Phase 1 studies. The Phase 2 program covered major depressive disorder and primary insomnia, and the compound remains investigational.
Four completed trials are registered for GW679769: NCT00413023, a Phase 2 study in major depressive disorder with 348 patients; NCT00650871, a Phase 2 study of sleep and cognitive function in primary insomnia with 48 patients; NCT00405080, a Phase 1 rifampin drug interaction study in 12 healthy subjects; and NCT00359177, a Phase 1 study in hepatic impairment with 24 subjects.
Yes. GW679769 is also known as casopitant, and the oral tablet form is referred to as GW679769 (casopitant) oral tablets. Searches for casopitant, GW679769 oral tablets, or GW679769 (casopitant) refer to the same investigational compound.
The four completed GW679769 trials enrolled a total of 917 participants. The largest was the Phase 2 major depressive disorder study NCT00413023 with 348 patients, followed by the Phase 2 insomnia study NCT00650871 with 48, and two Phase 1 studies with 24 and 12 subjects.