Recent Updates
Recently added Catalysts

AG-881

Phase 1

Healthy Male Participants | Small molecule | Other |Agios Pharmaceuticals, Inc.|Last Updated: Oct 23, 2019

Success Probability

Subscribe to view

Market & Valuation

Subscribe to view

Trial Design

UNCONTROLLED
Total Trials1
Total Enrollment5

FDA Designations

No designations recorded

Clinical trial landscape

AG-881 · 2 trials · 2 indications

Phase 1 2
NCT04015687A Study to Evaluate the Effect of AG-881 on the Pharmacokinetics of a Single Dose of Lamotrigine in Healthy AdultsHealthy Participants
COMPLETED22 Analytics
NCT03960502A Safety and Pharmacokinetic Study of AG-881 in Healthy Male Participants Following Administration of a Single Oral Dose of [14C] AG-881 and Concomitant Intravenous Microdose of [13C315N3] AG-881Healthy Male Participants
COMPLETED5 Analytics
PHASE1COMPLETED
A Study to Evaluate the Effect of AG-881 on the Pharmacokinetics of a Single Dose of Lamotrigine in Healthy Adults
Healthy Participants
NCT0401568722
Unlock trial analytics
PHASE1COMPLETED
A Safety and Pharmacokinetic Study of AG-881 in Healthy Male Participants Following Administration of a Single Oral Dose of [14C] AG-881 and Concomitant Intravenous Microdose of [13C315N3] AG-881
Healthy Male Participants
NCT039605025
Unlock trial analytics

Study Endpoints

Primary Endpoints

Area under the Concentration-time Curve from Time 0 to Infinity (AUC0-inf) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Area under the Concentration-time Curve from Time 0 to Infinity (AUC0-inf) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Maximum Observed Plasma Concentration (Cmax) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Maximum Observed Plasma Concentration (Cmax) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Area under the Concentration-time Curve, from Time 0 to the Last Observed Non-zero Concentration (t) (AUC0-t) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Area under the Concentration-time Curve, from Time 0 to the Last Observed Non-zero Concentration (t) (AUC0-t) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Percent of AUC0-inf Extrapolated (AUC%extrap) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Percent of AUC0-inf Extrapolated (AUC%extrap) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Time to Maximum Observed Plasma Concentration (Tmax) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Time to Maximum Observed Plasma Concentration (Tmax) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Apparent Terminal Elimination Rate Constant (Kel) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Apparent Terminal Elimination Rate Constant (Kel) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Apparent Terminal Elimination Half-life (t½) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Apparent Terminal Elimination Half-life (t½) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Apparent Total Plasma Clearance after Oral (Extravascular) Administration (CL/F) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Apparent Total Plasma Clearance after Oral (Extravascular) Administration (CL/F) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Apparent Volume of Distribution during the Terminal Elimination Phase after Oral (Extravascular) Administration (Vz/F) for Lamotrigine Administered with Interacting Drug AG-881
At multiple time points daily from Day 14 to Day 21 (or early discontinuation) in Period 2 (21-day period)
Apparent Volume of Distribution during the Terminal Elimination Phase after Oral (Extravascular) Administration (Vz/F) for Lamotrigine Administered without Interacting Drug AG-881
At multiple time points daily from Day 1 to Day 8 in Period 1 (8-day period)
Amount of AG-881 Excreted in Urine (Aeu)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Cumulative Aeu (Cum Aeu) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Percentage of AG-881 excreted in Urine and Feces (feu and fef, Respectively)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Cumulative Percentage of AG-881 Excreted in Urine (Cum feu)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Cumulative Percentage of AG-881 Excreted in Feces (Cum fef)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Renal Clearance (CLR) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Renal Clearance Expressed as a Percentage of Total Clearance (CLR/CL) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Percentage of Total Radioactivity in Total Excreta Calculated as Cumulative Percentage of AG-881 Excreted in Urine and Feces (Cum fe)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Area Under the Concentration-time Curve from Time Zero to the Last Measurable Concentration (AUC0-last) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Area Under the Concentration-time Curve from Time Zero to 72 hours (AUC0-72) of AG-881
Up to 72 hours
Partial Area Under the Concentration-time Curve from Time Zero to Common Time Point (AUC0-t) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Area Under the Concentration-time Curve from Time Zero to Infinity (AUC0-∞) of AG-881 Calculated Using the Observed Value of the Last Quantifiable Concentration
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Maximum Observed Plasma Concentration (Cmax) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Time to Maximum Observed Plasma Concentration (Tmax) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Apparent Terminal Elimination Half-life (t½) of AG-881
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
AUC0-∞ or AUC0-t of AG-881 in Plasma/AUC0-∞ or AUC0-t of Total Radioactivity in Plasma (AUC Plasma AG-881/Total Radioactivity Ratio)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
AUC0-∞ of Total Radioactivity in Whole Blood to AUC0-∞ of Total Radioactivity in Plasma (AUC Blood/Plasma Ratio), Calculated Using the Observed Value of the Last Quantifiable Concentration
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Total Clearance of AG-881 Following Intravenous (IV) Administration (CL)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Apparent Clearance Following Oral Administration of AG-881 (CL/F)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Volume of Distribution of AG-881 at Steady-state Following IV Administration (Vss)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Apparent Volume of Distribution During the Terminal Phase Following Oral Administration of AG-881 (Vz/F)
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Absolute bioavailability (F) for AG-881 Calculated as the Ratio of Dose-normalized AUC0-∞ of Oral/Intravenous Dosing
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Metabolic Profiles of AG-881 in Plasma, Urine, and Feces, When Possible
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks
Structures of AG-881 Metabolites in Plasma, Urine, and, Where Possible, Feces
At multiple time points daily from Day -1 to Day 14; then at 24-hour intervals until discharge (up to 29 days); then weekly up to approximately 8 weeks

Secondary Endpoints

Percentage of Participants with Adverse Events (AEs)
Up to approximately 4 weeks
Columbia-suicide Severity Rating Scale (C-SSRS)
Up to approximately 4 weeks
Percentage of Participants with Abnormalities in 12-lead Electrocardiograms (ECGs)
Up to approximately 4 weeks
Unlock Study Endpoints

Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeBASIC_SCIENCE

Treatment Arms

ArmTypeDescription
AG-881 (Group 1)EXPERIMENTALOn Day 1 of Period 1, Group 1 participants will receive a single 50-milligram (mg) oral dose of lamotrigine at Hour 0. In Period 2, they will receive 50-mg oral doses of AG-881 once daily (QD) for 15 consecutive days (Days 1 to 15), with a single 50-mg oral dose of lamotrigine coadministered at Hour 0 on Day 14.
AG-881 (Group 2)EXPERIMENTALFollowing a safety and tolerability review of the data from at least 7 days of AG-881 dosing of Group 1 participants in Period 2, Group 2 participants will receive a single 50-mg oral dose of lamotrigine at Hour 0 in Period 1, and 50-mg oral doses of AG-881 QD for 15 consecutive days (Days 1 to 15), with a single 50-mg oral dose of lamotrigine coadministered at Hour 0 on Day 14 in Period 2.
AG-881 (Group 3)EXPERIMENTALFollowing a safety and tolerability review of the data from Group 1 participants, and from at least 7 days of AG-881 dosing of Group 2 participants in Period 2, Group 3 participants will receive a single 50-mg oral dose of lamotrigine at Hour 0 in Period 1; and 50-mg oral doses of AG-881 QD for 15 consecutive days (Days 1 to 15) with a single 50-mg oral dose of lamotrigine coadministered at Hour 0 on Day 14 in Period 2.
AG881EXPERIMENTALOn Day 1, after fasting for 10 hours participants, will receive an oral capsule of \[14C\]AG-881 followed 2 hours later by a single intravenous (IV) infusion of \[13C315N3\]AG-881.

Interventions

NameTypeDescription
AG-881DRUGSupplied as uncoated tablets.
LamotrigineDRUGSupplied as tablets of LAMICTAL® or generic equivalent.
[13C315N3]AG-881DRUGSingle IV microdose of approximately 100 μg.
Unlock Study Design Details

Eligibility Criteria

Age Range18 Years to 55 Years
SexALL
Healthy VolunteersYes
Study Sites1

Inclusion criteria * Healthy, adult, male or female participants, 18-55 years of age, inclusive, at screening; * Continuous non-smoker who has not used nicotine-containing products for at least 3 months prior to the first dosing and throughout the study, based on participant self-reporting; * Body ...

Countries:United States
Unlock Eligibility Criteria

Frequently asked questions about AG-881

What is AG-881 used for?

AG-881 is an investigational small molecule being studied in acute myeloid leukemia (AML), myelodysplastic syndrome, and other advanced hematologic malignancies with an IDH1 and/or IDH2 mutation. It has also been studied in healthy participants for safety and pharmacokinetic evaluations. AG-881 is in Phase 1 clinical development.

What does AG-881 target?

AG-881 targets cancers that have an IDH1 and/or IDH2 mutation. It is being evaluated in patients with advanced hematologic malignancies, including acute myeloid leukemia (AML) and myelodysplastic syndrome, that carry these mutations. The drug is designed to act on these specific genetic alterations.

Who makes AG-881?

AG-881 is being developed by Agios Pharmaceuticals, Inc., a biopharmaceutical company. Agios is listed on the NASDAQ under the ticker symbol AGIO. The company is conducting clinical trials to evaluate the safety and efficacy of AG-881 in various patient populations.

What phase is AG-881 in?

AG-881 is in Phase 1 clinical development. All completed trials for AG-881 are Phase 1 studies. These trials have been completed, and the drug remains investigational, meaning it has not been approved by regulatory authorities for commercial use.

What clinical trials is AG-881 in?

AG-881 has been studied in four completed Phase 1 clinical trials. NCT02492737 evaluated AG-881 in patients with advanced hematologic malignancies with an IDH1 and/or IDH2 mutation. NCT03960502 studied its safety and pharmacokinetics in healthy male participants. NCT04015687 examined its effect on lamotrigine pharmacokinetics in healthy adults, and NCT04145128 evaluated it in healthy Japanese and non-Asian participants.

Is AG-881 the same as vorasidenib?

AG-881 is also known as vorasidenib. The drug has been studied under the name AG-881 in clinical trials, and vorasidenib is the alternative name used for the same compound. Both names refer to the same investigational small molecule being developed by Agios Pharmaceuticals.