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AG-181

Phase 1

Healthy Volunteers | Small molecule | Other |Agios Pharmaceuticals, Inc.|Last Updated: Aug 27, 2026

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindCONTROLLED
Total Trials1
Total Enrollment88

FDA Designations

No designations recorded

Clinical trial landscape

AG-181 · 2 trials · 2 indications

Phase 1 2
NCT07241234A Study to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of AG-181 in Subjects With PhenylketonuriaPhenylketonuria
RECRUITING20 Analytics
NCT06286033Single and Multiple Ascending Dose Study and Food Effect Study for AG181Healthy Volunteers
COMPLETED88 Analytics
PHASE1RECRUITING
A Study to Evaluate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of AG-181 in Subjects With Phenylketonuria
PhenylketonuriaUnlock trial analytics
PHASE1COMPLETED
Single and Multiple Ascending Dose Study and Food Effect Study for AG181
Healthy VolunteersUnlock trial analytics

Study Endpoints

Primary Endpoints

Number of Subjects with Adverse Events (AEs) and Serious Adverse Events (SAEs) by Type, Severity, and Relationship to the Study Drug
Up to Day 42
SAD: Number of Participants with Adverse Events (AEs) and Serious Adverse Events (SAEs) by Type, Severity, and Relationship to Study Drug
Up to Day 7
MAD: Number of Participants with AEs and SAEs by Type, Severity, and Relationship to Study Drug
Up to Day 26
Food Effect: Maximum Observed Plasma Concentration (Cmax) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4
Food Effect: Area Under the Concentration-time Curve up to the Last Quantifiable Concentration (AUC0-last) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4
Food Effect: Area Under the Concentration-time Curve From Time 0 to Infinity (AUC0-inf) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4
Food Effect: Time to Reach Maximum Observed Concentration (tmax) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4
Food Effect: Terminal Elimination Rate Constant (Kel) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4
Food Effect: Terminal Elimination Half-Life (t1/2) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4
Food Effect: Apparent Oral Clearance (CL/F) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4
Food Effect: Apparent Volume of Distribution at Terminal Phase (Vz/F) of AG-181
Predose and multiple time points postdose from Day 1 to Day 4

Secondary Endpoints

Plasma Concentration of AG-181
Up to Day 28
Maximum Concentration (Cmax) of AG-181
Up to Day 28
Time to Maximum (Peak) Concentration (Tmax) of AG-181
Up to Day 28
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Study Design & Arms

AllocationNON_RANDOMIZED
MaskingNONE
ModelSEQUENTIAL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
Cohort 1: AG-181EXPERIMENTALSubjects will receive AG-181 from Day 1 to Day 28.
Cohort 2 (Optional Cohort): AG-181EXPERIMENTALSubjects will receive AG-181.
Part 1: Single Ascending Dose (SAD)EXPERIMENTALParticipants will receive a range of doses of AG-181 or placebo, orally, once on Day 1. AG-181 will be given under fasted conditions.
Part 2: Multiple Ascending Dose (MAD)EXPERIMENTALParticipants will receive a range of doses of AG-181 or placebo twice daily (BID) for 13 days and a single dose on Day 14 under fasted conditions.
Part 3: Food Effect - Sequence 1: ABEXPERIMENTALParticipants will receive single oral dose of AG-181 on Day 1 of Period 1 under fasted condition (A) followed by single oral dose of AG-181 on Day 1 of Period 2 under fed (high fat meal) condition (B). Each period will be separated by a washout period of 1 week.
Part 3: Food Effect - Sequence 2: BAEXPERIMENTALParticipants will receive a single oral dose of AG-181 on Day 1 of Period 1 under fed (high fat meal) condition (B) followed by single oral dose of AG-181 on Day 1 of Period 2 under fasted condition (A). Each period will be separated by a washout period of 1 week.

Interventions

NameTypeDescription
AG-181DRUGAG-181 film-coated tablets
PlaceboDRUGAG-181 matched-placebo tablets
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Eligibility Criteria

Age Range18 Years to 69 Years
SexALL
Healthy VolunteersNo
Study Sites4

Key Inclusion Criteria: * Diagnosis of PKU, defined as documented presence of 2 mutant alleles in the phenylalanine hydroxylase (PAH) gene, of which at least 1 is the R408W mutation, as determined during Screening per the genotyping performed by the study central genotyping laboratory. * At least 1...

Countries:United StatesPoland
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Recent Changes (Last 90 Days)

LOWAug 27, 2026NCT07241234lastUpdatePostDate: changed
LOWAug 27, 2026NCT07241234lastUpdatePostDate: changed
LOWJul 30, 2026NCT07241234lastUpdatePostDate: changed
LOWJul 30, 2026NCT07241234lastUpdatePostDate: changed
LOWJun 23, 2026NCT07241234lastUpdatePostDate: changed
LOWJun 23, 2026NCT07241234lastUpdatePostDate: changed

Frequently asked questions about AG-181

What is AG-181 used for?

AG-181 is an investigational small molecule being studied for the treatment of phenylketonuria (PKU). It is also being evaluated in healthy volunteers to assess its safety and tolerability. The drug is currently in Phase 1 clinical development and is not yet approved by regulatory authorities.

Who makes AG-181?

AG-181 is being developed by Agios Pharmaceuticals, Inc., a biopharmaceutical company traded on the NASDAQ under the ticker symbol AGIO. The company is conducting clinical trials to evaluate the drug's safety, tolerability, pharmacokinetics, and pharmacodynamics in patients with phenylketonuria.

What phase is AG-181 in?

AG-181 is in Phase 1 clinical development. It is an investigational drug and has not been approved by the FDA or any other regulatory agency. The ongoing Phase 1 trials are designed to evaluate safety, tolerability, and how the drug is processed in the body.

What clinical trials is AG-181 in?

AG-181 is being studied in two Phase 1 clinical trials. The first, NCT06286033, is a completed single and multiple ascending dose and food effect study in healthy volunteers. The second, NCT07241234, is an ongoing study in patients with phenylketonuria, currently recruiting participants in the United States and Poland.

Is AG-181 the same as AG-181?

AG-181 is the primary name for this investigational drug. No alternative names have been reported for it in clinical trial registries. It is distinct from other compounds with similar names, and researchers refer to it consistently as AG-181 across studies.