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Etrumadenant

Phase 1

Non Small Cell Lung Cancer Metastatic | Small molecule | Oncology |Arcus Biosciences, Inc.|Last Updated: Jul 22, 2025

Target and mechanism

Molecular targetADORA2B, ADORA2A
Target classAntagonist
ModalitySmall molecule
ChEMBLCHEMBL4740383

Success Probability

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Market & Valuation

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Trial Design

CONTROLLED
Total Trials1
Total Enrollment77

FDA Designations

No designations recorded

Clinical trial landscape

Etrumadenant · 8 trials · 22 indications

Phase 1 8
NCT05411146A Study Investigating the Safety, Absorption, and Elimination of Radioactively Labeled Etrumadenant, a New Compound in the Treatment of CancerHealthy Participants
COMPLETED8 Analytics
NCT05277012A Study to Evaluate Pharmacokinetics (PK) of Etrumadenant Tablet and Capsule Formulations in Healthy Adult ParticipantsHealthy Participants
COMPLETED24 Analytics
NCT05154136A Drug-Drug Interaction Study to Evaluate the Effect of Itraconazole on the Pharmacokinetic Profile of Etrumadenant in Healthy Adult ParticipantsHealthy Participants
COMPLETED20 Analytics
NCT04381832Adenosine Receptor Antagonist Combination Therapy for Metastatic Castrate Resistant Prostate CancerProstatic Neoplasms, Castration-Resistant
COMPLETED173 Analytics
NCT03846310A Study to Evaluate Immunotherapy Combinations in Participants With Lung CancerNon Small Cell Lung Cancer Metastatic
COMPLETED77 Analytics
NCT03720678A Study to Evaluate Immunotherapy Combinations in Participants With Gastrointestinal MalignanciesGastroEsophageal Cancer
COMPLETED44 Analytics
NCT03719326A Study to Evaluate Safety/Tolerability of Immunotherapy Combinations in Participants With Triple-Negative Breast Cancer or Gynecologic MalignanciesTNBC - Triple-Negative Breast Cancer
COMPLETED35 Analytics
NCT03629756A Study to Evaluate the Safety and Tolerability of Immunotherapy Combinations in Participants With Advanced MalignanciesNon-small Cell Lung Cancer
COMPLETED48 Analytics
PHASE1COMPLETED
A Study Investigating the Safety, Absorption, and Elimination of Radioactively Labeled Etrumadenant, a New Compound in the Treatment of Cancer
Healthy Participants
NCT054111468
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PHASE1COMPLETED
A Study to Evaluate Pharmacokinetics (PK) of Etrumadenant Tablet and Capsule Formulations in Healthy Adult Participants
Healthy Participants
NCT0527701224
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PHASE1COMPLETED
A Drug-Drug Interaction Study to Evaluate the Effect of Itraconazole on the Pharmacokinetic Profile of Etrumadenant in Healthy Adult Participants
Healthy Participants
NCT0515413620
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PHASE1COMPLETED
Adenosine Receptor Antagonist Combination Therapy for Metastatic Castrate Resistant Prostate Cancer
Prostatic Neoplasms, Castration-Resistant
NCT04381832173
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PHASE1COMPLETED
A Study to Evaluate Immunotherapy Combinations in Participants With Lung Cancer
Non Small Cell Lung Cancer Metastatic
NCT0384631077
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PHASE1COMPLETED
A Study to Evaluate Immunotherapy Combinations in Participants With Gastrointestinal Malignancies
GastroEsophageal Cancer
NCT0372067844
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PHASE1COMPLETED
A Study to Evaluate Safety/Tolerability of Immunotherapy Combinations in Participants With Triple-Negative Breast Cancer or Gynecologic Malignancies
TNBC - Triple-Negative Breast Cancer
NCT0371932635
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PHASE1COMPLETED
A Study to Evaluate the Safety and Tolerability of Immunotherapy Combinations in Participants With Advanced Malignancies
Non-small Cell Lung Cancer
NCT0362975648
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Study Endpoints

Primary Endpoints

Excretion of total radioactivity in urine
Up to 25 days
Excretion of total radioactivity in feces
Up to 25 days
Percentage of total radioactivity in urine at selected time points
Up to 25 days
Percentage of total radioactivity in feces at selected time points
Up to 25 days
Mass balance recovery of total radioactivity in urine
Up to 25 days
Mass balance recovery of total radioactivy in feces
Up to 25 days
Number of Participants with Treatment Emergent Adverse Events (TEAEs)
Up to 38 days
Number of participants with abnormal electrocardiogram (ECG) readings, abnormal vital signs, abnormal physical examinations and abnormal clinical laboratory tests results
Up to 38 days
Maximum Observed Plasma Concentration (Cmax) of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Area Under the Plasma Concentration-time Curve From 0 to Last Observed Non-zero Concentration [AUC(0-t)] of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Area Under the Plasma Concentration Time Curve From Time '0' Extrapolated to Infinity [AUC(0-inf)] of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Time to Cmax (Tmax) of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent First-order Terminal Elimination Rate Constant (Kel) of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Percentage of AUC(0-inf) Extrapolation (AUC%extrap) of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent First Order Terminal Elimination Half-life (t1/2) of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent Total Plasma Clearance (CL/F) of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Apparent Volume of Distribution During the Terminal Elimination Phase (Vz/F) of Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Ratio of Etrumadenant metabolites to Etrumadenant
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Ratio of Etrumadenant metabolites to Total Metabolite Concentration
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Treatment Period 1, 2 and 3
Maximum Observed Plasma Concentration (Cmax) of Etrumadenant Administered With or Without Itraconazole
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Period 1; and Days 5, 6, 7, 9, and 11 during Period 2
Area Under the Plasma Concentration-time Curve From 0 to Last Observed Non-zero Concentration [AUC(0-t)] of Etrumadenant Administered With or Without Itraconazole
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Period 1; and Days 5, 6, 7, 9, and 11 during Period 2
Area Under the Plasma Concentration Time Curve From Time '0' Extrapolated to Infinity [AUC(0-inf)] of Etrumadenant Administered With or Without Itraconazole
Multiple timepoint evaluations from pre-dose to 24 hours post-dose at Days 1, 2, 3, 4, 5, and 6 during Period 1; and Days 5, 6, 7, 9, and 11 during Period 2
Objective Response Rate (ORR) in Stage 1 and 2
From study enrolment until participant discontinuation, or first occurrence of progressive disease, or death from any cause, whichever occurs first (approximately 3-5 years)

ORR defined as the composite proportion of participants with a Prostate Specific Antigen (PSA) and/or radiographic complete response (CR) and partial response (PR) determined by the investigator according to the Prostate Cancer Working Group 3 (PCWG3) criteria

Incidence and Severity of AEs and Serious Adverse Events (SAEs) in Stage 1
From first dose date to 90 days after the last dose (approximately 1.5 years)
Percentage of participants with Adverse Events
From first study treatment administration until up to 90 days after the last dose (Approximately 1 year)
Percentage of participants who experience a Dose Limiting Toxicity
From first study treatment administration through Day 21
Incidence of Adverse Events (AEs)
From first dose date to 90 days after the last dose (Approximately 1 year)
Incidence of dose-limiting toxicities (DLTs) during dose escalation phase
From first dose date to 28 days after the first dose
Incidence of dose-limiting toxicities (DLTs) during the dose escalation phase
From first dose date to 28 days after the first dose

Secondary Endpoints

Percentage of total radioactivity in blood
Up to 24 days
Percentage of total radioactivity in plasma
Up to 24 days
Maximum Observed Plasma Concentration (Cmax)
Up to 25 days
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Study Design & Arms

AllocationNA
MaskingNONE
ModelSINGLE_GROUP
PurposeBASIC_SCIENCE

Treatment Arms

ArmTypeDescription
[14C]-etrumadenantEXPERIMENTALParticipants will receive a single dose of \[14C\]-etrumadenant.
Treatment sequence ABCEXPERIMENTALParticipants will be sequentially administered with Treatment A, B then C (Treatment A: etrumadenant capsule in fasted state; Treatment B: etrumadenant tablet in fasted state; Treatment C: etrumadenant tablet in fed state). Each treatment will be separated by a washout period of 7 days.
Treatment sequence BCAEXPERIMENTALParticipants will be sequentially administered with Treatment B, C then A. Each treatment will be separated by a washout period of 7 days.
Treatment sequence CABEXPERIMENTALParticipants will be sequentially administered with Treatment C, A then B. Each treatment will be separated by a washout period of 7 days.
Etrumadenant then Etrumadenant + ItraconazoleEXPERIMENTALParticipants will receive the Treatment A (etrumadenant) followed by Treatment B (etrumadenant + itraconazole). A washout period of 5 days will be maintained between the two treatments.
Stage 1 and 2: Etrumadenant + zimberelimab + enzalutamideEXPERIMENTALParticipants will receive oral etrumadenant in combination with intravenous (IV) zimberelimab and standard oral enzalutamide
Stage 2: enzalutamideACTIVE_COMPARATORParticipants will receive standard oral enzalutamide
Stage 1 and 2: Etrumadenant + zimberelimab + docetaxelEXPERIMENTALParticipants will receive oral etrumadenant in combination with IV zimberelimab and standard IV docetaxel
Stage 2: docetaxelACTIVE_COMPARATORParticipants will receive standard dose of IV docetaxel
Stage 1 and 2: Etrumadenant + zimberelimabEXPERIMENTALOral etrumadenant in combination IV zimberelimab
Stage 2: Etrumadenant + zimberelimab + quemliclustatEXPERIMENTALParticipants will receive oral etrumadenant in combination with IV zimberelimab and IV quemliclustat
Stage 2: Etrumadenant + quemliclustatEXPERIMENTALParticipants will receive oral etrumadenant in combination with IV quemliclustat
Stage 1: Etrumadenant + zimberelimab PK Sub-StudyEXPERIMENTALParticipants will receive oral etrumadenant in combination with IV zimberelimab
Stage 1 and 2: Etrumadenant + SGEXPERIMENTALParticipants will receive oral etrumadenant in combination with IV SG.
Stage 1 and 2: Etrumadenant + Zimberelimab + SGEXPERIMENTALParticipants will receive oral etrumadenant in combination with IV zimberelimab and SG.
Dose Escalation Arm AEXPERIMENTALDose escalation is a 3+3 design, including a Dose Limiting Toxicity (DLT) evaluation period. The RDE of etrumadenant will be determined in this part with escalating doses of etrumadenant in combination with standard doses of carboplatin/pemetrexed chemotherapy regimen in participants with Non-Small Cell Lung Cancer.
Dose Escalation Arm BEXPERIMENTALDose escalation is a 3+3 design, including a Dose Limiting Toxicity (DLT) evaluation period. The RDE of etrumadenant will be determined in this part with escalating doses of etrumadenant in combination with standard doses of carboplatin/pemetrexed chemotherapy regimen and pembrolizumab in participants with Non-Small Cell Lung Cancer.
Dose Expansion Arm 1EXPERIMENTALZimberelimab will be administered in combination with standard carboplatin and pemetrexed chemotherapy regimen in participants with Non-Small Cell Lung Cancer harboring a sensitizing EGFR mutation.
Dose Expansion Arm 2EXPERIMENTALThe etrumadenant at RDE determined from the dose escalation phase will be administered in combination with standard carboplatin and pemetrexed chemotherapy regimen and zimberelimab in participants with Non-Small Cell Lung Cancer harboring a sensitizing EGFR mutation.
Dose EscalationEXPERIMENTALDose escalation is a 3+3 design, including a Dose Limiting Toxicity (DLT) evaluation period. The RDE of etrumadenant will be determined in this part with escalating doses of etrumadenant in combination with the standard mFOLFOX chemotherapy regimen in participants with gastroesophageal or colorectal cancer.
Dose Expansion-GEEXPERIMENTALThe RDE of etrumadenant will be determined from the dose escalation part. Etrumadenant will be given in combination with the standard mFOLFOX chemotherapy regimen in participants with gastroesophageal cancer
Dose Expansion-CRCEXPERIMENTALThe RDE of etrumadenant will be determined from the dose escalation part. Etrumadenant will be given in combination with the standard mFOLFOX chemotherapy regimen in participants with colorectal cancer
Dose Escalation-Arm AEXPERIMENTALDose escalation is a 3+3 design, including a Dose Limiting Toxicity (DLT) evaluation period.
Dose Escalation-Arm BEXPERIMENTALDose escalation is a 3+3 design, including a Dose Limiting Toxicity (DLT) evaluation period.
Dose Escalation-Arm CEXPERIMENTALDose escalation is a 3+3 design, including a Dose Limiting Toxicity (DLT) evaluation period.
Dose Expansion-TNBC-Arm 1EXPERIMENTALThe dose given will be determined from the dose escalation part (Arm A).
Dose Expansion-Ovarian Cancer-Arm 2EXPERIMENTALThe dose given will be determined from the dose escalation part (Arm A).
Dose Expansion-TNBC-Arm 3EXPERIMENTALThe dose given will be determined from the dose escalation part (Arm B). .
Dose Expansion-TNBC-Arm 4EXPERIMENTALThe dose expansion will be determined from the dose escalation part (Arm C).
Dose Expansion-advanced clear-cell RCCEXPERIMENTALEtrumadenant at RP2D + zimberelimab
Dose Expansion-mCRPCEXPERIMENTALEtrumadenant at RP2D + zimberelimab

Interventions

NameTypeDescription
[14C]-etrumadenantDRUGAdministered as specified in the treatment arm.
EtrumadenantDRUGEtrumadenant capsule and tablet formulations
ItraconazoleDRUGCapsule
ZimberelimabDRUGZimberelimab is an anti-PD-1 antibody
QuemliclustatDRUGQuemliclustat is a Cluster of Differentiation (CD)73 Inhibitor.
EnzalutamideDRUGEnzalutamide is an androgen receptor inhibitor
DocetaxelDRUGDocetaxel is type of chemotherapy
SGDRUGSacituzumab govitecan is an antibody-drug conjugate
CarboplatinDRUGCarboplatin administered as part of standard chemotherapy regimen
PemetrexedDRUGPemetrexed administered as part of standard chemotherapy regimen
PembrolizumabDRUGPembrolizumab is a humanized anti-PD-1 monoclonal antibody
mFOLFOXDRUGOxaliplatin, Leucovorin and 5-fluorouracil given as part of standard mFOLFOX chemotherapy regimen
IPI-549DRUGIPI-549 is a phosphoinositide-3-kinase-gamma inhibitor for oral use
Pegylated liposomal doxorubicin (PLD)DRUGDoxil is an anthracycline topoisomerase II inhibitor that is encapsulated in liposomes for intravenous (IV) use
nanoparticle albumin-bound paclitaxel (NP)DRUGNP is a microtubule inhibitor for intravenous (IV) use
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Eligibility Criteria

Age Range18 Years to 55 Years
SexMALE
Healthy VolunteersYes
Study Sites1

Inclusion Criteria: * BMI between 18.0 to 32.0 kg/m2 * Body weight ≥50 kg * Good physical and mental health on the basis of medical history, physical examination, clinical laboratory, ECG, and vital signs, as judged by the Investigator. * All clinical laboratory test results within the normal range...

Countries:NetherlandsUnited StatesCanadaSingaporeSouth KoreaTaiwanAustralia
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Competitive Landscape -Non-Small Cell Lung Cancer 389 trials (matched to "Non Small Cell Lung Cancer Metastatic")

Top 20 of 84 competitors

CompanyTickerTrialsLead PhaseDrugs
Merck & Co., Inc.MRK24PHASE3Pembrolizumab, Olaparib, Etoposide, Carboplatin, Cisplatin
AstraZeneca PLCAZN62PHASE3Datopotamab deruxtecan, Durvalumab, Carboplatin, Pembrolizumab, Cisplatin
Revolution Medicines, Inc.RVMD8PHASE3daraxonrasib, docetaxel
Eli Lilly and CompanyLLY18PHASE3Selpercatinib, Carboplatin, Cisplatin, Pemetrexed, Pembrolizumab
AbbVie, Inc.ABBV10PHASE3Telisotuzumab Vedotin, Docetaxel
Bristol-Myers Squibb CompanyBMY18PHASE3Repotrectinib, Crizotinib
BioNTech SE Sponsored ADRBNTX7PHASE3Gotistobart, Docetaxel
Gilead Sciences, Inc.GILD4PHASE3Sacituzumab Govitecan-hziy, Docetaxel
Pfizer Inc.PFE16PHASE3Lorlatinib, Crizotinib
Johnson & JohnsonJNJ17PHASE3Lazertinib, Amivantamab, Pemetrexed, Carboplatin
ArriVent BioPharma, Inc.AVBP9PHASE3Firmonertinib
GSK plc Sponsored ADRGSK4PHASE3Dostarlimab, Belrestotug, Pembrolizumab
Amgen Inc.AMGN4PHASE3ABP 234, Pembrolizumab
Novartis AG Sponsored ADRNVS9PHASE3JDQ443, docetaxel
Summit Therapeutics IncSMMT2PHASE3Ivonescimab, Pembrolizumab
Nuvation Bio, Inc. Class ANUVB4PHASE3Taletrectinib, Crizotinib
Genmab A/S Sponsored ADRGMAB4PHASE3Acasunlimab, Pembrolizumab, Docetaxel
Regeneron Pharmaceuticals, Inc.REGN6PHASE2Cemiplimab, Platinum-based chemotherapy, REGN7075
BeOne Medicines Ltd. Sponsored ADRONC6PHASE3Tislelizumab, Cisplatin, Paclitaxel, Pemetrexed Disodium, Carboplatin
BeyondSpring Inc.BYSI1PHASE3Plinabulin, Docetaxel
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Frequently asked questions about Etrumadenant

What is Etrumadenant used for?

Etrumadenant is an investigational small molecule being studied for use in several oncology indications, including non-small cell lung cancer, gastroesophageal cancer, triple-negative breast cancer, and castration-resistant prostate cancer. It has also been evaluated in healthy participants in an early-stage study. Etrumadenant is in Phase 1 clinical development.

What does Etrumadenant target?

Etrumadenant targets the adenosine receptors ADORA2A and ADORA2B, acting as an antagonist. By blocking these receptors, it is designed to modulate the tumor microenvironment. Etrumadenant is being developed by Arcus Biosciences for the treatment of various solid tumors.

Who makes Etrumadenant?

Etrumadenant is being developed by Arcus Biosciences, Inc., a biopharmaceutical company traded on the NYSE under the ticker symbol RCUS. The company is conducting clinical trials of Etrumadenant in oncology indications, including non-small cell lung cancer and triple-negative breast cancer.

What phase is Etrumadenant in?

Etrumadenant is in Phase 1 clinical development. It is an investigational drug and has not been approved by the FDA. All completed trials of Etrumadenant are Phase 1 studies, which have evaluated the drug in patients with advanced malignancies and in healthy participants.

What clinical trials is Etrumadenant in?

Etrumadenant has been studied in three completed Phase 1 clinical trials. These include NCT03629756 in advanced malignancies, NCT03719326 in triple-negative breast cancer and gynecologic malignancies, and NCT03720678 in gastrointestinal malignancies. A fourth study, NCT05411146, investigated the absorption and elimination of radioactively labeled Etrumadenant in healthy male participants.

Is Etrumadenant the same as AB928?

Etrumadenant is also known by the code name AB928, though this alternative name is not provided in the available information. Etrumadenant is the international nonproprietary name for the compound. It is a small molecule antagonist of the adenosine receptors ADORA2A and ADORA2B.

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