NCT00500903 is a Phase 1 clinical trial of Alisertib in Advanced Malignancies, sponsored by Millennium Pharmaceuticals, Inc..

Who is sponsoring NCT00500903?

NCT00500903 is sponsored by Millennium Pharmaceuticals, Inc..

What drugs are being tested in NCT00500903?

Interventions in NCT00500903: Alisertib.

What condition does NCT00500903 study?

NCT00500903 studies Advanced Malignancies.

Is NCT00500903 still recruiting?

NCT00500903 is currently completed. Last updated 14 March 2019.

Are results published for NCT00500903?

Yes — primary outcome results have been posted to ClinicalTrials.gov. See the outcomes section above for details.

Last reviewed 2019-03-14 · How we verify

NCT00500903

Name: Drug Landscape Pharmaceutical Database
Creator: Drug Landscape
Published: 2026-01-01
License: https://creativecommons.org/licenses/by/4.0/

A Study of MLN8237, a Novel Aurora A Kinase Inhibitor, in Participants With Advanced Solid Tumors

Completed Phase 1 Results posted Last updated 14 March 2019

What this trial tests

Phase 1 trial testing Alisertib in Advanced Malignancies in 87 participants. Completed in 23 February 2011.

Timeline

15 May 2007

Primary endpoint
1 August 2010

23 February 2011

Quick facts

Lead sponsor	Millennium Pharmaceuticals, Inc.
Phase	Phase 1
Status	Completed
Study type	INTERVENTIONAL
Allocation	non randomized
Design	parallel
Masking	none
Primary purpose	treatment
Enrollment	87
Start date	15 May 2007
Primary completion	1 August 2010
Estimated completion	23 February 2011
Sites	1 location across United States

Drugs / interventions tested

Alisertib — full drug profile →

Conditions studied

Advanced Malignancies — all drugs for Advanced Malignancies →

Sponsor

Millennium Pharmaceuticals, Inc. — full company profile →

Who can join

18 and older, any sex, with Advanced Malignancies. Patients with the condition only — healthy volunteers not accepted.

Results — posted to ClinicalTrials.gov

Per-arm endpoint measurements with 95% confidence intervals where reported. Source: trial results section.

Number of Participants With Dose-Limiting Toxicity (DLT) Primary · Cycle 1 Day 1 up to Day 35 (alisertib daily for 7 to 21 days followed by a 14-day recovery period)

DLT was evaluated according to the National Cancer Institute's Common Terminology Criteria for Adverse Events (NCI CTCAE) version 3.0 and was defined as any of the following events related to therapy with alisertib: 1. Grade 4 neutropenia lasting ≥7 consecutive days 2. Grade 4 neutropenia with fever and/or infection 3. Platelet count \<25,000/mm\^3 4. Grade 3 or greater nausea and/or emesis despite use of optimal antiemetic prophylaxis 5. Grade 3 or greater diarrhea despite maximal supportive therapy with loperamide 6. Any other Grade 3 or greater nonhematologic toxicity, with the following e

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	0
Alisertib 10 mg PIC QD 7D	0
Alisertib 20 mg PIC QD 7D	0
Alisertib 40 mg PIC QD 7D	0
Alisertib 80 mg PIC QD 7D	0
Alisertib 110 mg PIC QD 7D	1
Alisertib 150 mg PIC QD 7D	3
Alisertib 25 mg PIC QD 14D	0
Alisertib 25 mg PIC QD 21D	0
Alisertib 50 mg PIC QD 21D	0
Alisertib 70 mg PIC QD 21D	1
Alisertib 50 mg PIC BID 7D	2

Maximum Tolerated Dose (MTD) of Alisertib Primary · From first dose of study drug to 30 days after the last dose (up to 1011 days)

MTD was defined as the highest dose at which DLT occurred in 0/3 or 1/6 patients.

Group	Value	95% CI
Alisertib	50

Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs) Primary · From first dose of study drug to 30 days after the last dose (up to 1011 days)

An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. A Serious Adverse Event (SAE) A serious is any experience that suggests a significant hazard, contraindication, side effect or precaution that: results in death, is life-threatening, required in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or is medically significant.

AEs

Group	Value	95% CI
PIC Dose Escalation	65
ECT Dose Escalation	2
Relative Bioavailability	20

SAEs

Group	Value	95% CI
PIC Dose Escalation	26
ECT Dose Escalation	0
Relative Bioavailability	1

Cmax: Maximum Observed Concentration for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 1 predose and at multiple time-points (up to 24 hours) postdose and Day 7 predose and at multiple time-points (up to 10 hours) postdose

Day 1

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	208.4	± 27.96
Alisertib 10 mg PIC QD 7D	279.1	± 46.20
Alisertib 20 mg PIC QD 7D	759.3	± 11.82
Alisertib 40 mg PIC QD 7D	1245.4	± 20.60
Alisertib 80 mg PIC QD 7D	1661.3	± 45.20
Alisertib 110 mg PIC QD 7D	2717.8	± 44.62
Alisertib 150 mg PIC QD 7D	4260.3	± 42.62

Day 7

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	285.7	± 32.74
Alisertib 10 mg PIC QD 7D	931.5	± 81.68
Alisertib 20 mg PIC QD 7D	1114.1	± 36.96
Alisertib 40 mg PIC QD 7D	1681.6	± 64.62
Alisertib 80 mg PIC QD 7D	2376.3	± 51.06
Alisertib 110 mg PIC QD 7D	3586.4	± 48.28
Alisertib 150 mg PIC QD 7D	4467.8	± 24.58

Tmax: Time of First Occurrence of Cmax for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 1 predose and at multiple time-points (up to 24 hours) postdose and Day 7 predose and at multiple time-points (up to 10 hours) postdose

Day 1

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	2.000	1.50 – 3.00
Alisertib 10 mg PIC QD 7D	2.000	1.50 – 3.00
Alisertib 20 mg PIC QD 7D	1.500	1.50 – 1.50
Alisertib 40 mg PIC QD 7D	2.000	1.50 – 6.00
Alisertib 80 mg PIC QD 7D	2.000	1.50 – 3.00
Alisertib 110 mg PIC QD 7D	2.000	1.48 – 5.57
Alisertib 150 mg PIC QD 7D	2.000	1.45 – 3.00

Day 7

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	1.500	1.00 – 1.50
Alisertib 10 mg PIC QD 7D	3.750	1.50 – 6.00
Alisertib 20 mg PIC QD 7D	1.500	1.50 – 2.00
Alisertib 40 mg PIC QD 7D	2.000	1.97 – 6.00
Alisertib 80 mg PIC QD 7D	2.000	1.98 – 3.05
Alisertib 110 mg PIC QD 7D	3.710	1.42 – 6.02
Alisertib 150 mg PIC QD 7D	2.000	1.48 – 3.93

AUCt: Area Under the Concentration-Time Curve From Time 0 to Time t for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 1 predose and at multiple time-points (up to 24 hours) postdose and Day 7 predose and at multiple time-points (up to 10 hours) postdose

Day 1

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	1682.4	± 31.06
Alisertib 10 mg PIC QD 7D	2525.8	± 21.87
Alisertib 20 mg PIC QD 7D	5772.1	± 10.68
Alisertib 40 mg PIC QD 7D	12045.4	± 57.01
Alisertib 80 mg PIC QD 7D	20958.1	± 38.92
Alisertib 110 mg PIC QD 7D	29460.7	± 39.43
Alisertib 150 mg PIC QD 7D	38582.1	± 45.95

Day 7

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	2919.5	± 32.31
Alisertib 10 mg PIC QD 7D	10602.9	± 107.87
Alisertib 20 mg PIC QD 7D	10927.5	± 45.27
Alisertib 40 mg PIC QD 7D	21976.0	± 96.64
Alisertib 80 mg PIC QD 7D	27825.5	± 53.59
Alisertib 110 mg PIC QD 7D	46271.1	± 33.38
Alisertib 150 mg PIC QD 7D	53031.9	± 26.22

Terminal Half-Life (t1/2) for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 7 predose and at multiple time-points (up to 10 hours) postdose

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	24.950	± 20.4354
Alisertib 10 mg PIC QD 7D	35.150	± 23.4052
Alisertib 20 mg PIC QD 7D	26.400	± 19.7684
Alisertib 40 mg PIC QD 7D	18.155	± 12.5087
Alisertib 80 mg PIC QD 7D	39.333	± 18.8006
Alisertib 110 mg PIC QD 7D	13.427	± 4.3465
Alisertib 150 mg PIC QD 7D	16.766	± 9.7804

Accumulation Ratio (Rac) for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 7 predose and at multiple time-points (up to 10 hours) postdose

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	1.753	± 0.2754
Alisertib 10 mg PIC QD 7D	6.350	± 7.2408
Alisertib 20 mg PIC QD 7D	2.037	± 0.9708
Alisertib 40 mg PIC QD 7D	1.997	± 0.9393
Alisertib 80 mg PIC QD 7D	1.535	± 0.3323
Alisertib 110 mg PIC QD 7D	1.677	± 0.6788
Alisertib 150 mg PIC QD 7D	1.588	± 0.4129

Peak/Trough Ratio for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 7 predose and at multiple time-points (up to 10 hours) postdose

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	4.107	± 0.8460
Alisertib 10 mg PIC QD 7D	5.195	± 3.9527
Alisertib 20 mg PIC QD 7D	5.430	± 2.4856
Alisertib 40 mg PIC QD 7D	3.907	± 2.3944
Alisertib 80 mg PIC QD 7D	3.850	± 2.0612
Alisertib 110 mg PIC QD 7D	4.922	± 2.5890
Alisertib 150 mg PIC QD 7D	4.610	± 0.5314

CLss/F: Apparent Oral Clearance at Steady State for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 7 predose and at multiple time-points (up to 10 hours) postdose

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	3.302	± 35.8915
Alisertib 10 mg PIC QD 7D	1.817	± 107.8347
Alisertib 20 mg PIC QD 7D	3.525	± 49.1267
Alisertib 40 mg PIC QD 7D	3.511	± 72.1346
Alisertib 80 mg PIC QD 7D	5.545	± 41.0258
Alisertib 110 mg PIC QD 7D	4.348	± 61.5266
Alisertib 150 mg PIC QD 7D	5.450	± 37.3021

Ae: Amount of Alisertib Excreted in Urine Over the Collection Period for Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 1 predose and at multiple time-points (up to 24 hours) postdose

Group	Value	95% CI
Alisertib 5 mg PIC QD 7D	0.0	± 0.00
Alisertib 10 mg PIC QD 7D	0.0	± 0.00
Alisertib 20 mg PIC QD 7D	0.0	± 0.00
Alisertib 40 mg PIC QD 7D	4806.7	± 8325.39
Alisertib 80 mg PIC QD 7D	18815.0	± 1675.84
Alisertib 110 mg PIC QD 7D	13813.3	± 16387.22
Alisertib 150 mg PIC QD 7D	14473.3	± 15603.71

CLr: Renal Clearance of Alisertib as Powder-in-Capsule (PIC) With Once Daily for 7 Days (QD7D) Dosing Secondary · Cycle 1 Day 1 predose and at multiple time-points (up to 24 hours) postdose

Group	Value	95% CI
Alisertib 40 mg PIC QD 7D	0.0012630	± NA
Alisertib 80 mg PIC QD 7D	0.0013860	± NA
Alisertib 110 mg PIC QD 7D	0.0009414	± 0.00063956
Alisertib 150 mg PIC QD 7D	0.0006710	± 0.00060091

Adverse events — posted to ClinicalTrials.gov

Time frame: From first dose of study drug to 30 days after the last dose (up to 1011 days). Reporting threshold: 5%. Adverse-event reports describe events observed during the trial — not all are caused by the drug.

PIC Dose Escalation

Serious: 26/65 (40%)

Deaths: —

ECT Dose Escalation

Serious: 0/2 (0%)

Deaths: —

Relative Bioavailability

Serious: 1/20 (5%)

Deaths: —

Serious adverse events (43 terms)

Reaction	System	PIC Dose Escalation	ECT Dose Escalation	Relative Bioavailability
Febrile neutropenia	Blood and lymphatic system disorders	—	—	—
Anaemia	Blood and lymphatic system disorders	—	—	—
Thrombocytopenia	Blood and lymphatic system disorders	—	—	—
Diarrhoea	Gastrointestinal disorders	—	—	—
Nausea	Gastrointestinal disorders	—	—	—
Neutropenia	Blood and lymphatic system disorders	—	—	—
Vomiting	Gastrointestinal disorders	—	—	—
Intestinal obstruction	Gastrointestinal disorders	—	—	—
Urinary tract infection	Infections and infestations	—	—	—
Dyspnoea	Respiratory, thoracic and mediastinal disorders	—	—	—
Small intestinal obstruction	Gastrointestinal disorders	—	—	—
Abdominal pain	Gastrointestinal disorders	—	—	—
Gastrointestinal haemorrhage	Gastrointestinal disorders	—	—	—
Stomatitis	Gastrointestinal disorders	—	—	—
Klebsiella bacteraemia	Infections and infestations	—	—	—
Enterococcal bacteraemia	Infections and infestations	—	—	—
Pneumonia	Infections and infestations	—	—	—
Staphylococcal infection	Infections and infestations	—	—	—
Bacteraemia	Infections and infestations	—	—	—
Hyperbilirubinaemia	Hepatobiliary disorders	—	—	—
Jaundice cholestatic	Hepatobiliary disorders	—	—	—
Bile duct obstruction	Hepatobiliary disorders	—	—	—
Bile duct stenosis	Hepatobiliary disorders	—	—	—
Asthenia	General disorders	—	—	—
Fatigue	General disorders	—	—	—

Other adverse events (104 terms — click to expand)

Reaction	System	PIC Dose Escalation	ECT Dose Escalation	Relative Bioavailability
Nausea	Gastrointestinal disorders	—	—	—
Diarrhoea	Gastrointestinal disorders	—	—	—
Fatigue	General disorders	—	—	—
Anorexia	Metabolism and nutrition disorders	—	—	—
Neutropenia	Blood and lymphatic system disorders	—	—	—
Somnolence	Nervous system disorders	—	—	—
Alopecia	Skin and subcutaneous tissue disorders	—	—	—
Vomiting	Gastrointestinal disorders	—	—	—
Anaemia	Blood and lymphatic system disorders	—	—	—
White blood cell count decreased	Investigations	—	—	—
Stomatitis	Gastrointestinal disorders	—	—	—
Abdominal pain	Gastrointestinal disorders	—	—	—
Oedema peripheral	General disorders	—	—	—
Dizziness	Nervous system disorders	—	—	—
Constipation	Gastrointestinal disorders	—	—	—
Pyrexia	General disorders	—	—	—
Asthenia	General disorders	—	—	—
Cough	Respiratory, thoracic and mediastinal disorders	—	—	—
Headache	Nervous system disorders	—	—	—
Dehydration	Metabolism and nutrition disorders	—	—	—
Dyspnoea	Respiratory, thoracic and mediastinal disorders	—	—	—
Thrombocytopenia	Blood and lymphatic system disorders	—	—	—
Hypokalaemia	Metabolism and nutrition disorders	—	—	—
Hyperglycaemia	Metabolism and nutrition disorders	—	—	—
Hypocalcaemia	Metabolism and nutrition disorders	—	—	—
Hyponatraemia	Metabolism and nutrition disorders	—	—	—
Insomnia	Psychiatric disorders	—	—	—
Paraesthesia	Nervous system disorders	—	—	—
Hyperkalaemia	Metabolism and nutrition disorders	—	—	—
Blood alkaline phosphatase increased	Investigations	—	—	—
Weight decreased	Investigations	—	—	—
Muscle spasms	Musculoskeletal and connective tissue disorders	—	—	—
Urinary tract infection	Infections and infestations	—	—	—
Flatulence	Gastrointestinal disorders	—	—	—
Abdominal distension	Gastrointestinal disorders	—	—	—
Rash	Skin and subcutaneous tissue disorders	—	—	—
Pruritus	Skin and subcutaneous tissue disorders	—	—	—
Blood creatinine increased	Investigations	—	—	—
Back pain	Musculoskeletal and connective tissue disorders	—	—	—
Shoulder pain	Musculoskeletal and connective tissue disorders	—	—	—

Most-reported serious reactions: Febrile neutropenia, Anaemia, Thrombocytopenia, Diarrhoea, Nausea, Neutropenia, Vomiting, Intestinal obstruction.

Data from ClinicalTrials.gov NCT00500903 adverse events section.

Sponsor's own description

To determine the dose-limiting toxicity (DLT) and maximum tolerated dose (MTD) of MLN8237 when given by mouth (PO) for a minimum of 7 and a maximum of 21 consecutive days, followed by a 14-day recovery period.

Publications & conference data

8 peer-reviewed publications reference this trial (live from Europe PMC):

Aurora A kinase (AURKA) in normal and pathological cell division.
Nikonova AS, Astsaturov I, Serebriiskii IG, Dunbrack RL, et al · · 2013 · cited 368× · PMID 22864622 · DOI 10.1007/s00018-012-1073-7
The two sides of chromosomal instability: drivers and brakes in cancer.
Hosea R, Hillary S, Naqvi S, Wu S, et al · · 2024 · cited 102× · PMID 38553459 · DOI 10.1038/s41392-024-01767-7
Aurora kinase A in gastrointestinal cancers: time to target.
Katsha A, Belkhiri A, Goff L, El-Rifai W. · · 2015 · cited 74× · PMID 25987188 · DOI 10.1186/s12943-015-0375-4
Second-Generation Antimitotics in Cancer Clinical Trials.
Novais P, Silva PMA, Amorim I, Bousbaa H. · · 2021 · cited 37× · PMID 34371703 · DOI 10.3390/pharmaceutics13071011
Seize the engine: Emerging cell cycle targets in breast cancer.
Fuentes-Antrás J, Bedard PL, Cescon DW. · · 2024 · cited 21× · PMID 38264947 · DOI 10.1002/ctm2.1544
Global population pharmacokinetics of the investigational Aurora A kinase inhibitor alisertib in cancer patients: rationale for lower dosage in Asia.
Zhou X, Mould DR, Takubo T, Sheldon-Waniga E, et al · · 2018 · cited 17× · PMID 28891222 · DOI 10.1111/bcp.13430
Aurora Kinases as Therapeutic Targets in Head and Neck Cancer.
Nguyen TT, Silva FN, Golemis EA. · · 2022 · cited 8× · PMID 36165728 · DOI 10.1097/ppo.0000000000000614
Aurora Kinase A: Integrating Insights into Cancer, Inflammation, and Infectious Diseases.
Varshney N, Pandey RK, Mishra A, Kumar S, et al · · 2024 · PMID 41907711 · DOI 10.1080/29933935.2024.2419069

Verify or expand the search:

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Verify against primary sources

ClinicalTrials.gov — authoritative US registry record
WHO ICTRP — international registry index
EU Clinical Trials Register
Sponsor press releases (Google)

Data sources for this page

Trial protocol + status: ClinicalTrials.gov NCT00500903 (US National Library of Medicine, public domain)
Publications: Europe PMC API search by NCT ID, retrieved 10 June 2026
Drug + disease cross-links: matched in real time against Drug Landscape's normalised drug + company + condition tables
Sponsor: as reported to ClinicalTrials.gov by Millennium Pharmaceuticals, Inc.
Last refreshed: 14 March 2019

Drug Landscape aggregates and links these public records for informational use only. Always verify against the primary source before clinical or regulatory decisions. Canonical URL: https://druglandscape.com/trial/NCT00500903.

Primary sources · FDA · ClinicalTrials.gov · EMA · SEC EDGAR · ChEMBL · Wikidata · full sourcing

NCT00500903

Quick facts

Drugs / interventions tested

Conditions studied

Sponsor

Who can join

Results — posted to ClinicalTrials.gov

Adverse events — posted to ClinicalTrials.gov

Serious adverse events (43 terms)

Sponsor's own description

Publications & conference data

Related trials

Other trials of Alisertib

Other recruiting trials for Advanced Malignancies

Other Millennium Pharmaceuticals, Inc. trials

Verify against primary sources