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This study designed to evaluate the pharmacokinetics and safety of AG-013736 at single doses and multiple doses
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Axitinib | Experimental |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| Axitinib (AG-013736) | Drug | Three single dose level of AG-013736 (5 mg, 7 mg and 10 mg) will be given for all patient. After single dosing at each dose level, multiple doses of 5 mg twice a day (BID) will be started. |
| Measure | Description | Time Frame |
|---|---|---|
| Single Dose: Maximum Observed Plasma Concentration (Cmax) | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose | |
| Area Under the Plasma Concentration-Time Curve From Time Zero to Time Infinity (AUCinf) | AUCinf is obtained from AUC (0 - t) plus AUC (t - infinity). | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose |
| Single Dose: Time to Reach Maximum Observed Plasma Concentration (Tmax) | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose | |
| Single Dose: Plasma Decay Half-Life (t1/2) | Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose |
| Measure | Description | Time Frame |
|---|---|---|
| Multiple Dose: Maximum Observed Plasma Concentration (Cmax) | Cmax at multiple dosing | Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
| Multiple Dose: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) |
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Inclusion Criteria:
Exclusion Criteria:
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| Name | Affiliation | Role |
|---|---|---|
| Pfizer CT.gov Call Center | Pfizer | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Pfizer Investigational Site | Kobe | Hyōgo | Japan |
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| Label | URL |
|---|---|
| To obtain contact information for a study center near you, click here. | View source |
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| ID | Title | Description |
|---|---|---|
| FG000 | AG-013736 | Single Dosing: Participants received single AG-013736 5 mg, followed by 7 mg, and subsequently 10 mg. After the single dose at each dose level, participants were monitored for at least 48 hours prior to the next dosing. Multiple Dosing (28-day cycle ): After the monitoring period following the 10 mg single dose, participants received multiple doses of AG-013736 at 5 mg twice daily (BID) at approximately 12 hours apart. The treatment was continued until participants experienced intolerable toxicity or progressive disease. |
| Title | Milestones | Reasons Not Completed | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Overall Study |
|
|
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| ID | Title | Description |
|---|---|---|
| BG000 | AG-013736 | Single Dosing: Participants received single AG-013736 5 mg, followed by 7 mg, and subsequently 10 mg. After the single dose at each dose level, participants were monitored for at least 48 hours prior to the next dosing. Multiple Dosing (28-day cycle ): After the monitoring period following the 10 mg single dose, participants received multiple doses of AG-013736 at 5 mg twice daily (BID) at approximately 12 hours apart. The treatment was continued until participants experienced intolerable toxicity or progressive disease. |
| Units | Counts |
|---|---|
| Participants |
|
| Title | Description | Population Description | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Denominator Units Selected | Denominators | Classes |
|---|---|---|---|---|---|---|---|---|---|
| Age Continuous | Mean |
| Type | Title | Description | Population Description | Reporting Status | Anticipated Posting Date | Parameter Type | Dispersion Type | Unit of Measure | Calculate Percentage | Time Frame | Units Analyzed | Denominator Units Selected | Arm/Group Information | Denominators | Classes | Analyses | |||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Primary | Single Dose: Maximum Observed Plasma Concentration (Cmax) | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Mean | Standard Deviation | ng/mL | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose |
|
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The same event may appear as both an AE and a SAE. However, what is presented are distinct events. An event may be categorized as serious in one subject and as nonserious in another subject, or one subject may have experienced both a serious and nonserious event during the study.
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| ID | Title | Description | Deaths (Affected) | Deaths (At Risk) | Serious Events (Affected) | Serious Events (At Risk) | Other Events (Affected) | Other Events (At Risk) |
|---|---|---|---|---|---|---|---|---|
| EG000 | AG-013736 | Single Dosing: Participants received single AG-013736 5 mg, followed by 7 mg, and subsequently 10 mg. After the single dose at each dose level, participants were monitored for at least 48 hours prior to the next dosing. Multiple Dosing (28-day cycle ): After the monitoring period following the 10 mg single dose, participants received multiple doses of AG-013736 at 5 mg twice daily (BID) at approximately 12 hours apart. The treatment was continued until participants experienced intolerable toxicity or progressive disease. |
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Disease progression | General disorders | MedDRA 13.0 | Systematic Assessment | Caused death. |
| Term | Organ System | Source Vocabulary | Assessment Type | Notes | Statistical Information |
|---|---|---|---|---|---|
| Thyroiditis chronic | Endocrine disorders | MedDRA 13.0 | Systematic Assessment |
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| Title | Organization | Phone | Extension | |
|---|---|---|---|---|
| Pfizer ClinicalTrials.gov Call Center | Pfizer, Inc. | 1-800-718-1021 | ClinicalTrials.gov_Inquiries@pfizer.com |
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| ID | Term |
|---|---|
| D009369 | Neoplasms |
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| ID | Term |
|---|---|
| D000077784 | Axitinib |
| ID | Term |
|---|---|
| D001549 | Benzamides |
| D000577 | Amides |
| D009930 | Organic Chemicals |
| D001565 | Benzoates |
| D000146 |
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The dosing interval was 12 hours in this study. |
| Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
| Multiple Dose: Time to Reach Maximum Observed Plasma Concentration (Tmax) | Tmax at multiple dosing | Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
| Multiple Dose: Accumulation Ratio for Cmax (Rac Cmax) and Accumulation Ratio for AUCtau (Rac AUCtau) | Rac Cmax is obtained from Cmax (Cycle 1, Day 15) divided by Cmax (Cycle 1, Day 1) Rac AUCtau is obtained from AUCtau (Cycle 1, Day 15) divided by AUCtau (Cycle 1, Day 1) | Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
| Percent Change From Baseline in Soluble Vascular Endothelial Growth Factor Receptor 1, 2, and 3 (s-VEGFR1, s-VEGFR2 and s-VEGFR3), Vascular Endothelial Growth Factor (VEGF), Soluble Stem Cell Factor Receptor (s-KIT ) | Percent change from baseline is obtained from (observed value minus baseline value) divided by baseline value multiplied by 100 in each parameter, i.e., s-VEGFR1, VEGFR2, s-VEGFR3, s-KIT, and VEGF | Prior to the initial dose (baseline) and Day 1 of Cycle 2 |
| Number of Participants With Best Overall Response of Complete Response (CR), Partial Response (PR), Stable Disease (SD), and Progression of Disease (PD) According to the Response Evaluation Criteria in Solid Tumors (RECIST Version 1.0) | CR was defined as the disappearance of all target and nontarget lesions and no appearance of new lesions. PR was defined as at least a 30% decrease in the sum of the longest diameters (SLD) of the targeted lesions. CR and PR had to be documented on 2 occasions separated by at least 4 weeks. SD was defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify as PD being demonstrated during the first 8 weeks. PD was defined as at least a 20% increase in the SLD of target lesions compared to the smallest SLD since the study treatment started. | Up to 470 days |
| Number of Participants With Adverse Events | Number of participants with any adverse events, adverse events graded as Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0 Grade 3 or higher , serious adverse events, and adverse events resulted in discontinuation. | Up to 470 days of treatment plus 28-days follow-up |
| years |
|
| Sex: Female, Male | Count of Participants | Participants |
|
|
|
| Primary | Area Under the Plasma Concentration-Time Curve From Time Zero to Time Infinity (AUCinf) | AUCinf is obtained from AUC (0 - t) plus AUC (t - infinity). | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Mean | Standard Deviation | ng*hr/mL | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose |
|
|
|
| Primary | Single Dose: Time to Reach Maximum Observed Plasma Concentration (Tmax) | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Median | Full Range | hours | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose |
|
|
|
| Primary | Single Dose: Plasma Decay Half-Life (t1/2) | Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Mean | Standard Deviation | hours | Predose, 0.5, 1, 2, 4, 6, 8, 10, 24, and 32-hour postdose |
|
|
|
| Secondary | Multiple Dose: Maximum Observed Plasma Concentration (Cmax) | Cmax at multiple dosing | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Mean | Standard Deviation | ng/mL | Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
|
|
|
| Secondary | Multiple Dose: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) | The dosing interval was 12 hours in this study. | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Mean | Standard Deviation | ng*h/mL | Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
|
|
|
| Secondary | Multiple Dose: Time to Reach Maximum Observed Plasma Concentration (Tmax) | Tmax at multiple dosing | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Median | Full Range | hours | Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
|
|
|
| Secondary | Multiple Dose: Accumulation Ratio for Cmax (Rac Cmax) and Accumulation Ratio for AUCtau (Rac AUCtau) | Rac Cmax is obtained from Cmax (Cycle 1, Day 15) divided by Cmax (Cycle 1, Day 1) Rac AUCtau is obtained from AUCtau (Cycle 1, Day 15) divided by AUCtau (Cycle 1, Day 1) | Pharmacokinetic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacokinetic blood sampling for at least 1 day. | Posted | Mean | Standard Deviation | ratio | Cycle 1 Day 15 predose in the morning, and 0.5, 1, 2, 4, 8 and 12 hour postdose |
|
|
|
| Secondary | Percent Change From Baseline in Soluble Vascular Endothelial Growth Factor Receptor 1, 2, and 3 (s-VEGFR1, s-VEGFR2 and s-VEGFR3), Vascular Endothelial Growth Factor (VEGF), Soluble Stem Cell Factor Receptor (s-KIT ) | Percent change from baseline is obtained from (observed value minus baseline value) divided by baseline value multiplied by 100 in each parameter, i.e., s-VEGFR1, VEGFR2, s-VEGFR3, s-KIT, and VEGF | Pharmacodynamic analysis set was defined as all enrolled participants who received at least 1 dose of the study medication and who completed pharmacodynamic blood sampling for at least 1 day. | Posted | Median | Full Range | percent | Prior to the initial dose (baseline) and Day 1 of Cycle 2 |
|
|
|
| Secondary | Number of Participants With Best Overall Response of Complete Response (CR), Partial Response (PR), Stable Disease (SD), and Progression of Disease (PD) According to the Response Evaluation Criteria in Solid Tumors (RECIST Version 1.0) | CR was defined as the disappearance of all target and nontarget lesions and no appearance of new lesions. PR was defined as at least a 30% decrease in the sum of the longest diameters (SLD) of the targeted lesions. CR and PR had to be documented on 2 occasions separated by at least 4 weeks. SD was defined as neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify as PD being demonstrated during the first 8 weeks. PD was defined as at least a 20% increase in the SLD of target lesions compared to the smallest SLD since the study treatment started. | Anti-tumor response analysis set was defined as all participants with at least 1 target lesion according to RECIST and who received at least 1 dose of study drug. | Posted | Number | participants | Up to 470 days |
|
|
|
| Secondary | Number of Participants With Adverse Events | Number of participants with any adverse events, adverse events graded as Common Terminology Criteria for Adverse Events (CTCAE) Version 3.0 Grade 3 or higher , serious adverse events, and adverse events resulted in discontinuation. | Safety analysis set was defined as all enrolled participants who received the study drug at least once in this study (same as the full analysis set:FAS). | Posted | Number | participants | Up to 470 days of treatment plus 28-days follow-up |
|
|
|
| 1 |
| 6 |
| 6 |
| 6 |
|
| Eye irritation | Eye disorders | MedDRA 13.0 | Systematic Assessment |
|
| Abdominal pain upper | Gastrointestinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Ascites | Gastrointestinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Cheilitis | Gastrointestinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Constipation | Gastrointestinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Diarrhoea | Gastrointestinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Nausea | Gastrointestinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Stomatitis | Gastrointestinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Chest pain | General disorders | MedDRA 13.0 | Systematic Assessment |
|
| Fatigue | General disorders | MedDRA 13.0 | Systematic Assessment |
|
| Mucosal inflammation | General disorders | MedDRA 13.0 | Systematic Assessment |
|
| Oedema | General disorders | MedDRA 13.0 | Systematic Assessment |
|
| Jaundice cholestatic | Hepatobiliary disorders | MedDRA 13.0 | Systematic Assessment |
|
| Nasopharyngitis | Infections and infestations | MedDRA 13.0 | Systematic Assessment |
|
| Paronychia | Infections and infestations | MedDRA 13.0 | Systematic Assessment |
|
| Contusion | Injury, poisoning and procedural complications | MedDRA 13.0 | Systematic Assessment |
|
| Fracture | Injury, poisoning and procedural complications | MedDRA 13.0 | Systematic Assessment |
|
| Alanine aminotransferase increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Aspartate aminotransferase increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood alkaline phosphatase increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood amylase increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood cholesterol increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood lactate dehydrogenase increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood potassium increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood thyroid stimulating hormone decreased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood thyroid stimulating hormone increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Blood urine present | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Lipase increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Neutrophil count decreased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Platelet count decreased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Thyroglobulin increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Thyroxine free decreased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Thyroxine free increased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Tri-iodothyronine free decreased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Weight decreased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| White blood cell count decreased | Investigations | MedDRA 13.0 | Systematic Assessment |
|
| Decreased appetite | Metabolism and nutrition disorders | MedDRA 13.0 | Systematic Assessment |
|
| Back pain | Musculoskeletal and connective tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Myalgia | Musculoskeletal and connective tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Neck pain | Musculoskeletal and connective tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Cancer pain | Neoplasms benign, malignant and unspecified (incl cysts and polyps) | MedDRA 13.0 | Systematic Assessment |
|
| Dizziness | Nervous system disorders | MedDRA 13.0 | Systematic Assessment |
|
| Headache | Nervous system disorders | MedDRA 13.0 | Systematic Assessment |
|
| Neuropathy peripheral | Nervous system disorders | MedDRA 13.0 | Systematic Assessment |
|
| Somnolence | Nervous system disorders | MedDRA 13.0 | Systematic Assessment |
|
| Proteinuria | Renal and urinary disorders | MedDRA 13.0 | Systematic Assessment |
|
| Menstruation irregular | Reproductive system and breast disorders | MedDRA 13.0 | Systematic Assessment |
|
| Cough | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Dysphonia | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Epistaxis | Respiratory, thoracic and mediastinal disorders | MedDRA 13.0 | Systematic Assessment |
|
| Dermatitis | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Dermatitis acneiform | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Haemorrhage subcutaneous | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Palmar-plantar erythrodysaesthesia syndrome | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Pruritus | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Rash | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Telangiectasia | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Urticaria | Skin and subcutaneous tissue disorders | MedDRA 13.0 | Systematic Assessment |
|
| Hypertension | Vascular disorders | MedDRA 13.0 | Systematic Assessment |
|
| Hypotension | Vascular disorders | MedDRA 13.0 | Systematic Assessment |
|
Pfizer has the right to review disclosures, requesting a delay of less than 60 days. Investigator will postpone single center publications until after disclosure of pooled data (all sites), less than 12 months from study completion/termination at all participating sites. Investigator may not disclose previously undisclosed confidential information other than study results.
| Acids, Carbocyclic |
| D002264 | Carboxylic Acids |
| D001555 | Benzene Derivatives |
| D006841 | Hydrocarbons, Aromatic |
| D006844 | Hydrocarbons, Cyclic |
| D006838 | Hydrocarbons |
| D007191 | Indazoles |
| D011720 | Pyrazoles |
| D001393 | Azoles |
| D006573 | Heterocyclic Compounds, 1-Ring |
| D006571 | Heterocyclic Compounds |
| D006574 | Heterocyclic Compounds, 2-Ring |
| D000072471 | Heterocyclic Compounds, Fused-Ring |
| Title | Measurements |
|---|---|
|
| Title | Measurements |
|---|---|
|
| Title | Measurements |
|---|---|
|
| Title | Measurements |
|---|---|
|
| s-KIT |
|
| VEGF |
|
| Title | Measurements |
|---|
|
| PD |
|
| Title | Measurements |
|---|---|
|
| Any Grade-5 adverse events (= death) |
|
| Discontinuation due to adverse events |
|