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AMG 510

Phase 3

KRAS p, G12c Mutated /Advanced Metastatic NSCLC | Small molecule | Oncology |Amgen Inc.|Last Updated: Jul 22, 2026

Target and mechanism

Molecular targetKRAS
Target classInhibitor
ModalitySmall molecule

Also known as Sotorasib

Success Probability

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Market & Valuation

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Trial Design

RandomizedACTIVE_CONTROLLEDDMC
Total Trials1
Total Enrollment345

FDA Designations

No designations recorded

Clinical trial landscape

AMG 510 · 13 trials · 4 indications

Phase 3 1Phase 1 12
NCT04303780Study to Compare AMG 510 "Proposed INN Sotorasib" With Docetaxel in Non Small Cell Lung Cancer (NSCLC) (CodeBreak 200).KRAS p, G12c Mutated /Advanced Metastatic NSCLC
COMPLETED345 Analytics
PHASE3COMPLETED
Study to Compare AMG 510 "Proposed INN Sotorasib" With Docetaxel in Non Small Cell Lung Cancer (NSCLC) (CodeBreak 200).
KRAS p, G12c Mutated /Advanced Metastatic NSCLCUnlock trial analytics

Study Endpoints

Primary Endpoints

Progression-free Survival (PFS)
Baseline up to primary analysis data cut-off date (02 August 2022); max time on study as of primary analysis data cut off was 24.3 months

PFS was defined as the time from randomization (baseline) until disease progression or death from any cause, whichever occurred first for all participants. Progression was based on blinded independent central review (BICR) of disease response per Response Evaluation Criteria in Solid Tumors version 1.1 (RECIST v1.1). As pre-specified in the statistical analysis plan, for participants who crossed over from docetaxel to AMG 510, the participant's response post first progression or post crossover was not used for the primary analyses. Data are presented per original treatment randomized.

Period 1 and 2: Maximum Observed Plasma Concentration (Cmax) of Sotorasib
Predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on the 1st day of each period (Days 1 and 4)
Period 1 and 2: Area Under the Plasma Concentration-time Curve From Time Zero to the Last Quantifiable Concentration (AUClast) of Sotorasib
Predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on the 1st day of each period (Days 1 and 4)
Period 1 and 2: Area Under the Plasma Concentration-time Curve From Time Zero to Infinity (AUCinf) of Sotorasib
Predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on on the 1st day of each period (Days 1 and 4)
Maximum Observed Plasma Concentration (Cmax) of Rosuvastatin
Predose (Hour 0), 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, and 120 hours postdose following administration of rosuvastatin on Days 1 and 6

The pharmacokinetic (PK) parameters were determined using standard non-compartmental methods.

Area Under the Plasma Concentration-Time Curve (AUC) From Time Zero to Time of Last Quantifiable Concentration (AUClast) of Rosuvastatin
Predose (Hour 0), 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, and 120 hours postdose following administration of rosuvastatin on Days 1 and 6

The PK parameters were determined using standard non-compartmental methods.

AUC From Time Zero to Infinity (AUCinf) of Rosuvastatin
Predose (Hour 0), 0.5, 1, 2, 3, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96, and 120 hours postdose following administration of rosuvastatin on Days 1 and 6

The PK parameters were determined using standard non-compartmental methods.

Maximum Observed Plasma Concentration (Cmax) of Sotorasib for Treatments A and B
Predose (Hour 0), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on Day 1 (Period 1) and Day 4 (Period 2)

Blood samples were collected by venipuncture or cannulation for measurement of plasma concentrations of sotorasib. Plasma pharmacokinetic (PK) parameters of sotorasib were summarized per treatment received, regardless of treatment sequence, as pre-specified.

Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Quantifiable Concentration (AUClast) of Sotorasib for Treatments A and B
Predose (Hour 0), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on Day 1 (Period 1) and Day 4 (Period 2)

Blood samples were collected by venipuncture or cannulation for measurement of plasma concentrations of sotorasib. Plasma PK parameters of sotorasib were summarized per treatment received, regardless of treatment sequence, as pre-specified.

Area Under the Plasma Concentration-Time Curve From Time Zero to Infinity (AUCinf) of Sotorasib for Treatments A and B
Predose (Hour 0), 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on Day 1 (Period 1) and Day 4 (Period 2)

Blood samples were collected by venipuncture or cannulation for measurement of plasma concentrations of sotorasib. Plasma PK parameters of sotorasib were summarized per treatment received, regardless of treatment sequence, as pre-specified.

Maximum Observed Plasma Concentration (Cmax) of AMG 510
Day 1, Day 4, Day 11
Area Under the Plasma Concentration-time Curve (AUC) from Time Zero to the Last Quantifiable Concentration (AUClast) of AMG 510
Day 1, Day 4, Day 11
AUC from time Zero to Infinity (AUCinf) of AMG 510
Day 1, Day 4, Day 11
Number of Participants With Dose-limiting Toxicities (DLT)
Day 1 to Day 21

DLTs were defined as any of the following adverse events (AEs) where a relationship to sotorasib could not be ruled out. Hematological toxicity * febrile neutropenia * neutropenic infection * grade 4 neutropenia * grade ≥ 3 thrombocytopenia for \> 7 days * grade 3 thrombocytopenia with grade ≥ 2 bleeding * grade 4 thrombocytopenia * grade 4 anemia. Non-hematological toxicity * grade ≥ 4 vomiting or diarrhea * grade 3 diarrhea or grade 3 vomiting lasting more than 3 days despite optimal medical support * grade ≥ 3 nausea for 3 days or more despite optimal medical support * any other grade ≥ 3 adverse event.

Number of Participants With Treatment-emergent AEs (TEAEs)
Day 1 until the end of study (or primary data cut-off date for ongoing participants); median [min, max] duration was 5.57 [1.5, 13.7] months

An AE was any untoward medical occurrence in a clinical study participant irrespective of a causal relationship with the study treatment. A TEAE was defined as an AE starting on or after first dose of study treatment. Treatment-related TEAEs were any TEAEs considered related to investigational product by the investigator. If relationship was missing, the event was assumed treatment-related. Clinically significant changes from the participant's baseline values in vital signs, 12-lead electrocardiograms, and clinical laboratory safety tests were reported as AEs.

Maximum Observed Plasma Concentration (Cmax) of Sotorasib
Pre-dose and 0.25, 0.5, 1, 2, 4, 6, and 24 hours post-dose on Days 1 and 8

Pharmacokinetic (PK) parameters were determined from the concentration-time profile using standard non-compartmental approaches and considering the profile over the complete sampling interval.

Time to Achieve Cmax (Tmax) of Sotorasib
Pre-dose and 0.25, 0.5, 1, 2, 4, 6, and 24 hours post-dose on Days 1 and 8

PK parameters were determined from the concentration-time profile using standard non-compartmental approaches and considering the profile over the complete sampling interval.

Area Under the Plasma Concentration-Time Curve From Time 0 to 24 Hours (AUC0-24h) of Sotorasib
Pre-dose and 0.25, 0.5, 1, 2, 4, 6, and 24 hours post-dose on Days 1 and 8

PK parameters were determined from the concentration-time profile using standard non-compartmental approaches and considering the profile over the complete sampling interval.

Area under the concentration-time curve (AUC) from time zero to infinity (AUCinf)
Day 1 to Day 14
AUC from time zero to the last quantifiable concentration (AUClast)
Day 1 to Day 14
Maximum observed concentration (Cmax)
Day 1 to Day 14
Time of Cmax (tmax)
Day 1 to Day 14
Apparent terminal elimination half-life (t1/2)
Day 1 to Day 14
Total clearance (AMG 510 only; CL/F)
Day 1 to Day 14
Volume of distribution (AMG 510 only; Vz/F)
Day 1 to Day 14
Plasma AMG 510 to total radioactivity ratio
Day 1 to Day 14
Whole blood to plasma total radioactivity ratio
Day 1 to Day 14
Amount (Aeu) of AMG510 excreted in urine
Day 1 to Day 14
Percentage (feu) of AMG510 excreted in urine
Day 1 to Day 14
Renal clearance (CLR) of AMG510
Day 1 to Day 14
Amount (Aef) of AMG510 excreted in feces
Day 1 to Day 14
Percentage (fef) of AMG510 excreted in feces
Day 1 to Day 14
Area Under the Plasma Concentration-time Curve (AUC) from Time Zero to Time of Last Quantifiable Concentration (AUClast) of AMG 510
Day 1 and Day 4
Area Under the Plasma Concentration-time Curve from Time Zero to Infinity (AUCinf) of AMG 510
Day 1 and Day 4
Maximum Plasma Concentration (Cmax) of AMG 510
Day 1 and Day 4
Area Under the Plasma Concentration-time Curve from Time Zero to the Last Quantifiable Concentration (AUClast) of AMG 510
Day 1 and Day 4
Maximum Plasma Concentration (Cmax) of Digoxin Administered Alone
Day 1
Area Under the Plasma Concentration-time Curve (AUC) from Time Zero to Time of Last Quantifiable Concentration (AUClast) of Digoxin Administered Alone
Day 1
AUC from Time Zero to Infinity (AUCinf) of Digoxin Administered Alone
Day 1
Maximum Plasma Concentration (Cmax) of Digoxin Administered in Combination with AMG 510
Day 7
AUClast of Digoxin Administered in Combination with AMG 510
Day 7
AUCinf of Digoxin Administered in Combination with AMG 510
Day 7

Secondary Endpoints

Number of Participants Who Experience a Treatment-emergent Adverse Event (TEAE)
Day 1 to Day 9
Period 3: Cmax of Sotorasib
Predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on the 1st day of Period 3 (Day 7)
Period 3: AUClast of Sotorasib
Predose, 0.5, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 24, 36, and 48 hours postdose following administration of sotorasib on on the 1st day of Period 3 (Day 7)
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Study Design & Arms

AllocationRANDOMIZED
MaskingNONE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
AMG 510EXPERIMENTAL -
DocetaxelACTIVE_COMPARATOR -
Treatment Sequence ABCEXPERIMENTALParticipants will be administered sotorasib orally in the following order: Period 1 - as 1 tablet (test 1) Period 2 - as 2 tablets (reference) Period 3 - as 1 tablet (test 2)
Treatment Sequence BACEXPERIMENTALParticipants will be administered sotorasib orally in the following order: Period 1 - as 2 tablets (reference) Period 2 - as 1 tablet (test 1) Period 3 - as 1 tablet (test 2)
Rosuvastatin aloneEXPERIMENTAL -
Rosuvastatin + sotorasibEXPERIMENTAL -
AMG 510 + Omeprazole + FamotidineEXPERIMENTALParticipants will receive AMG 510 on Day 1, famotidine on Day 3, AMG 510 and famotidine on Day 4, omeprazole on Days 6 through 10, and omeprazole and AMG 510 on Day 11.
Treatment ArmEXPERIMENTALSubjects will be enrolled and will receive AMG 510 PO QD.
AMG510EXPERIMENTALEach participant will receive a single oral dose of AMG510 on Day 1 after an overnight fast.
Treatment Sequence ABEXPERIMENTALParticipants will be administered AMG 510 in the following order: Period 1 (treatment A) - AMG 510 as oral tablets. Period 2 (treatment B) - AMG 510 as tablets dispersed in water.
Treatment Sequence BAEXPERIMENTALParticipants will be administered AMG 510 in the following order: Period 1 (treatment B) - AMG 510 as tablets dispersed in water. Period 2 (treatment A) - AMG 510 as oral tablets.
AMG 510 + OmeprazoleEXPERIMENTALParticipants will receive AMG 510 on Day 1, daily doses of omeprazole on Days 4 to 8, and a single dose of both omeprazole and AMG 510 on Day 9.
AMG 510 + ItraconazoleEXPERIMENTAL -
AMG 510 + RifampinEXPERIMENTAL -
AMG 510 + DigoxinEXPERIMENTALParticipants will receive digoxin on Day 1 and both AMG 510 + digoxin on Day 7.

Interventions

NameTypeDescription
AMG 510DRUG21 day cycles
DocetaxelDRUG21 day cycles
SotorasibDRUGOral Tablet
RosuvastatinDRUGOral dose
OmeprazoleDRUGCapsule
FamotidineDRUGTablet
ItraconazoleDRUGOral capsule
RifampinDRUGOral capsule
DigoxinDRUGOral tablet
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Eligibility Criteria

Age Range18 Years to 100 Years
SexALL
Healthy VolunteersNo
Study Sites274

Inclusion Criteria: * Men or women greater than or equal to 18 years old. * ECOG ≤ 1 * Pathologically documented, previously treated, locally-advanced and unresectable or metastatic NSCLC with KRAS p.G12C mutation confirmed through central testing or have documentation of KRAS p.G12C mutation throu...

Countries:United StatesAustraliaBelgiumBrazilCanadaDenmarkFinlandFranceGermanyGreeceHungaryItalyJapanNetherlandsPolandPortugalRussiaSouth KoreaSpainSwedenSwitzerlandTaiwanUnited KingdomHong Kong
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Recent Changes (Last 90 Days)

MEDIUMAug 22, 2026NCT04303780TRIAL_REMOVED: changed
MEDIUMAug 22, 2026NCT04303780TRIAL_REMOVED: changed
MEDIUMAug 22, 2026NCT04303780TRIAL_REMOVED: changed
MEDIUMAug 22, 2026NCT04303780TRIAL_REMOVED: changed
HIGHJul 22, 2026NCT04303780Status: ACTIVE_NOT_RECRUITING → COMPLETED
HIGHJul 22, 2026NCT04303780Status: ACTIVE_NOT_RECRUITING → COMPLETED

Frequently asked questions about AMG 510

What is AMG 510 used for?

AMG 510, also known as sotorasib, is an investigational small molecule being studied for the treatment of KRAS p.G12C mutant advanced solid tumors, including colorectal cancer and non-small cell lung cancer. It is also being evaluated in healthy volunteers for pharmacokinetic studies.

What does AMG 510 target?

AMG 510 targets KRAS, specifically the KRAS p.G12C mutation, and acts as an inhibitor. It is designed to block the activity of this mutated protein, which is involved in cancer cell growth and proliferation.

Who makes AMG 510?

AMG 510 is being developed by Amgen Inc., a biopharmaceutical company traded on NASDAQ under the ticker AMGN. Amgen is conducting clinical trials to evaluate the drug's safety and efficacy in various cancer indications.

What phase is AMG 510 in?

AMG 510 is in Phase 1 clinical development. While some trials have been completed, it remains investigational and has not been approved by regulatory authorities. The drug is being studied across multiple Phase 1, Phase 2, and Phase 3 trials.

What clinical trials is AMG 510 in?

AMG 510 is being studied in several clinical trials, including NCT04185883 (CodeBreak 101) for advanced solid tumors with KRAS p.G12C mutation, NCT05198934 for colorectal cancer, NCT05578859 in healthy subjects, and NCT07172919, a rollover study for advanced solid tumors.

Is AMG 510 the same as sotorasib?

Yes, AMG 510 is also known as sotorasib. Both names refer to the same investigational drug developed by Amgen for targeting KRAS p.G12C mutations in various cancers.