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. 2020 Apr 15;11:508. doi: 10.3389/fimmu.2020.00508

Table 3.

Summary of clinical trials for CD73, A2AR, and A2BR in cancer.

Adenosine pathway target Drug(s) Target(s) Therapy modality (adenosine pathway) Phase Details Disease Status ClinicalTrials.gov Identifier
CD73 LY3475070
Pembrolizumab
CD73PD-1 LY3475070:CD73 SmallMolecule Inhibitor Phase 1 Cohort A: LY3475070 administered orallyCohort B: LY3475070 + Pembrolizumab administered IVCohort C1: LY3475070 + Pembrolizumab administered IVCohort C2 LY3475070 administered orallyCohort D1 LY3475070 + Pembrolizumab administered IVCohort D2: LY3475070 administered orallyCohort E: LY3475070 + Pembrolizumab administered IV Advanced SolidMalignancies Recruiting NCT04148937
Oleclumab
(MEDI9447)
Durvalumab
(MEDI4736)
CD73PD-L1 Oleclumab:
CD73 Humanized
Monoclonal
Antibody
Phase 1
Phase 2
Phase I and Phase II Arm A: Paclitaxel, Carboplatin, Durvalumab, + OleclumabPhase II Arm B: Paclitaxel, Carboplatin, + Durvalumab Triple NegativeBreast Cancer Recruiting NCT03616886
Oleclumab
(MEDI9447)
Durvalumab
CD73PD-L1 Oleclumab:CD73 HumanizedMonoclonalAntibody Phase 2 Experimental: Chemotherapy and radiation
Experimental: Chemotherapy and pre-operative radiotherapy + Durvalumab
Experimental: Chemotherapy and pre-operative radiotherapy + Durvalumab and Oleclumab
Luminal B(Breast Cancer) Recruiting NCT03875573
Oleclumab(MEDI9447)Durvalumab CD73PD-L1 Oleclumab:CD73 HumanizedMonoclonalAntibody Phase 1 Experimental: Monotherapy, Oleclumab
Experimental: Combination, Oleclumab and Durvalumab
Solid Tumors Active, not
Recruiting
NCT02503774
TJ004309Atezolizumab CD73PD-L1 TJ004309:CD73 HumanizedMonoclonalAntibody Phase 1 Dose escalated TJ004309 + Atezolizumab Solid TumorsMetastatic Cancer Recruiting NCT03835949
Oleclumab
(MEDI9447)
Durvalumab
AZD9150
AZD6738
Vistusertib
Olaparib
Trasutzumab
Cediranib
CD73
PD-L1
STAT3
ATR
mTOR
PARP
HER2
VEGFR
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
Phase 2 Experimental: Durvalumab + Olaparib
Experimental: Durvalumab + AZD9150
Experimental: Durvalumab + AZD6738
Experimental: Durvalumab + Vistusertib
Experimental: Durvalumab + Oleclumab
Experimental: Durvalumab + Trastuzumab
Experimental: Durvalumab + Cediranib
Non-Small Cell Lung
Cancer
Recruiting NCT03334617
Oleclumab
(MEDI9447)
Durvalumab
Capivasertib
Danvatirsen
Paclitaxel
CD73
PD-L1
AKT
STAT3
Chemotherapy
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
Phase 1
Phase 2
Experimental: Durvalumab + Paclitaxel
Experimental: Durvalumab + Paclitaxel + Capivasertib
Experimental: Durvalumab + Paclitaxel + Danvatirsen
Experimental: Durvalumab + Paclitaxel + Oleclumab
Triple Negative
Breast Cancer
Recruiting NCT03742102
Oleclumab
(MEDI9447)
Durvalumab
Gemcitabine
Nab-paclitaxel
Oxaliplatin
Leucovorin
5-FU
CD73
PD-L1
Chemotherapy
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
Phase 1
Phase 2
Arm A1: Gemcitabine + Nab-paclitaxelArm A2: Oleclumab + Gemcitabine + Nab-paclitaxelArm A3: Oleclumab + Durvalumab + Gemcitabine/Nab-paclitaxelArm B1: Oxaliplatin + Leucovorin + 5-FU (mFOLFOX)Arm B2: Oleclumab + mFOLFOX CarcinomaMetastatic PancreaticAdenocarcinoma Active, notRecruiting NCT03611556
Oleclumab
(MEDI9447)
Durvalumab
CD73PD-L1 Oleclumab:CD73 HumanizedMonoclonal Antibody Phase 1 Experimental: Monotherapy, Durvalumab
Experimental: Combination, Durvalumab + Oleclumab
Muscle InvasiveBladder Cancer Recruiting NCT03773666
BMS-986179
Nivolumab
rHUPH20
CD73PD-1
Hyaluronidase
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
Phase 1
Phase 2
Arm A: Monotherapy, BMS-986179Arm B: Combination Therapy, BMS-986179 + NivolumabArm C: Combination Therapy, BMS-986179 + rHUPH20 Malignant Solid
Tumor
Recruiting NCT02754141
Oleclumab
(MEDI9447)
MEDI0562
Durvalumab
Tremelilumab
CD73
OX40
PD-L1
CTLA-4
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
Phase 2 Cohort A: Oleclumab + DurvalumabCohort B: MEDI0562 + DurvalumabCohort C: MEDI0562 + Tremelimumab Ovarian Cancer Recruiting NCT03267589
CD73 A2AR CPI-006
Ciforadenant
(CPI-444)
Pembrolizumab
CD73
A2AR
PD-1
CPI-006:
CD73 Humanized
Monoclonal
Antibody
Ciforadenant:
A2AR Antagonist
Phase 1 Cohort 1a: (escalating doses) CPI-006Cohort 1b: (escalating doses) CPI-006 + CiforadenantCohort 1c: (escalating doses) CPI-006 + PembrolizumabCohort 2a: (selective dose) CPI-006Cohort 2b: (selective dose) CPI-006 + CiforadenantCohort 2c: (selective doses) CPI-006 + Pembrolizumab Non-Small Cell Lung Cancer
Renal Cell Cancer
Colorectal Cancer
Triple Negative Breast Cancer
Cervical Cancer
Ovarian Cancer
Pancreatic Cancer
Endometrial Cancer
Sarcoma
Squamous Cell Carcinoma of the Head and Neck
Bladder Cancer
Metastatic Castration Resistant Prostate Cancer
Non-hodgkin Lymphoma
Recruiting NCT03454451
Oleclumab
(MEDI9447)
AZD4635
Durvalumab
CD73
A2AR
PD-L1
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
AZD4635:
A2AR Antagonist
Phase 2 Module 1: Drug: AZD4635; Drug: DurvalumabModule 2: Drug: AZD4635; Drug: Oleclumab Prostate Cancer
Metastatic
Castration-Resistant
Prostate Cancer
Recruiting NCT04089553
Oleclumab
(MEDI9447)
AZD4635
Osimertinib
CD73
A2AR
EGFR
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
AZD4635:
A2AR Antagonist
Phase 1
Phase 2
Arm A: MEDI9447 + OsimertinibArm B: MEDI9447 + AZD4635 Non-Small Cell Lung
Cancer
Recruiting NCT03381274
NZV930NIR178PDR001 CD73
A2AR
PD-1
NZV930:
CD73 Humanized
Monoclonal
Antibody
NIR178:
A2AR Antagonist
Phase 1 Experimental: NZV930
Experimental: NZV930 + PDR001
Experimental: NZV930 + NIR178
Experimental: NZV930, NIR178, PDR001
Non-small Cell Lung
Cancer (NSCLC)
Triple Negative
Breast Cancer
Pancreatic Ductal
Adenocarcinoma
Colorectal Cancer
Microsatellite Stable
Ovarian Cancer
Renal Cell
Carcinoma
Recruiting NCT03549000
Oleclumab
(MEDI9447)
AZD4635
Durvalumab
Abiraterone
Acetate
Enzalutamide
Docetaxel
CD73
A2AR
PD-L1
Hormone
Therapy
Chemotherapy
Oleclumab:
CD73 Humanized
Monoclonal
Antibody
AZD4635:
A2AR Antagonist
Phase 1 Experimental: Arm A: AZD4635 monotherapy as nanoparticle suspension 125 mg BID
Experimental: Arm B: AZD4635 monotherapy as nanoparticle suspension 75 mg QD
Experimental: Arm C: AZD4635 monotherapy as nanoparticle suspension 100 mg QD
Experimental: Arm D: AZD4635 as nanoparticle suspension 75 mg QD plus Durvalumab
Experimental: Arm E: AZD4635 as nanoparticle suspension 100 mg QD plus Durvalumab
Experimental: Arm EA: AZD4635 as nanoparticle suspension plus Enzalutamide
Experimental: Arm AA: AZD4635 as nanoparticle suspension plus Abiraterone Acetate
Experimental: Arm F: AZD4635 as nanoparticle suspension plus Durvaluamb in patients post immunotherapy with non-small cell lung cancer
Experimental: Arm G: AZD4635 monotherapy as nanoparticle suspension in patients post immunotherapy with non-small cell lung cancer
Experimental: Arm H: AZD4635 monotherapy as nanoparticle suspension in patients post immunotherapy with other solid tumors
Experimental: Arm I: AZD4635 as nanoparticle suspension plus Durvalumab in immunotherapy naïve patients with metastatic castration resistant prostate cancer
Experimental: Arm J: AZD4635 as nanoparticle suspension plus Durvalumab in immunotherapy naïve patients with metastatic castration resistant prostate cancer
Advanced Solid
Malignancies
Non-Small Cell Lung
Cancer
Metastatic Castrate-Resistant
Prostate Carcinoma
Colorectal
Carcinoma
Recruiting NCT02740985
Experimental: Arm K: AZD4635 monotherapy as nanoparticle suspension in immunotherapy naïve patients with colorectal carcinoma
Experimental: Arm KD: AZD4635 as nanoparticle suspension plus Durvalumab in immunotherapy-naïve patients with colorectal carcinoma
Experimental: Arm L: AZD4635 monotherapy as nanoparticle suspension in immunotherapy naïve patients with other solid tumours
Experimental: Arm CA: AZD4635 capsule formulation monotherapy 75 mg QD
Experimental: Arm CB: AZD4635 capsule formulation 50 mg QD plus Durvalumab and Oleclumab
Experimental: Arm CC: AZD4635 capsule formulation 50 mg QD plus Docetaxel
A2AR NIR178PDR001 A2ARPD-1 NIR178:
A2AR Antagonist
Phase 2 Experimental (1): NIR178 + PDR001
Experimental (2): NIR178 BID Intermittent + PDR001
Experimental (3): Part 3, initiation of part 3 will depend on results from parts 1 and 2
Experimental (4): Japanese safety run-in part, two different dosing schedules of NIR178 will be explored
Non-small Cell Lung Cancer
Renal Cell Cancer
Pancreatic Cancer
Urothelial Cancer
Head and Neck Cancer
Diffused Large B Cell Lymphoma
Microsatellite Stable Colon Cancer
Triple Negative Breast Cancer
Melanoma
Recruiting NCT03207867
PBF-509PDR001 A2ARPD-1 PBF-509:
A2AR Antagonist
Phase 1
Phase 2
Drug: PBF-509_80 mgDrug: PBF-509_160 mgDrug: PBF-509_320 mgDrug: PBF-509_640 mgDrug: Combo PBF-509 (160 mg) + PDR001Drug: Combo PBF-509 (320 mg) + PDR001Drug: Combo PBF-509 (640 mg) + PDR001Drug: RP2D (PBF-509+PDR001)_immuno naïveDrug:
Experimental: RP2D (PBF-509+PDR001)_immuno treated
Non-small Cell Lung Cancer Recruiting NCT02403193
NIR178
Spartalizumab
LAG525
Capmatinib
MCS110
Canakinumab
A2ARPD-1LAG-3c-MetM-CSFIL-1β NIR178:
A2AR Antagonist
Phase 1 Experimental: Spartalizumab + LAG525 + NIR178
Experimental: Spartalizumab + LAG525 + Capmatinib
Experimental: spartalizumab + LAG525 + MCS110
Experimental: spartalizumab + LAG525 + Canakinumab
Triple Negative
Breast Cancer
Recruiting NCT03742349
Ciforadenant
(CPI-444)
Atezolizumab
A2AR
PD-L1
Ciforadenant:
A2AR Antagonist
Phase 1 Experimental: Ciforadenant, 100 mg orally twice daily for the first 14 days of each 28-day cycle
Experimental: Ciforadenant, 100 mg orally twice daily for 28 days of each 28-day cycle
Experimental: Ciforadenant, 200 mg orally once daily for the first 14 days of each 28-day cycle
Experimental: Ciforadenant + Atezolizumab
Experimental: Ciforadenant, start with 150 mg orally twice daily for 28-day cycles; then, increase increments by 100 mg/day for 6 dose levels
Non-Small Cell Lung Cancer
Malignant Melanoma Renal Cell Cancer
Triple Negative Breast Cancer
Colorectal Cancer
Bladder Cancer
Metastatic Castration Resistant Prostate Cancer
Recruiting NCT02655822
Ciforadenant
(CPI-444)
Atezolizumab
Cobimetinib
RO6958688
Docetaxel
Pemetrexed
Carboplatin
Gemcitabine
Linagliptin
Tocilizumab
Ipatasertib
Idasanutlin
A2AR
PD-L1
MEK
CEA
Chemotherapy
IL-6R
AKT
MDM2
Ciforadenant:
A2AR Antagonist
Phase 1
Phase 2
Active Comparator: Stage 1: Cohort 1: Atezolizumab
Experimental: Stage 1: Cohort 1: Atezolizumab + Cobimetinib
Experimental: Stage 1: Cohort 1: Atezolizumab + RO6958688
Active Comparator: Stage 1: Cohort 2: Docetaxel
Experimental: Stage 1: Cohort 2: Atezolizumab + Cobimetinib
Experimental: Stage 1: Cohort 2: Atezolizumab + Ciforadenant
Experimental: Stage 1: Cohort 2: Atezolizumab + RO6958688
Experimental: Stage 1: Cohort 2: Atezolizumab + Ipatasertib
Experimental: Stage 1: Cohort 2: Idasanutlin + Docetaxel
Experimental: Stage 2: Cohort 1: Atezolizumab + Pemetrexed + Carboplatin
Carcinoma, Non-Small-Cell Lung Recruiting NCT03337698
A2AR A2BR AB928
IPI-549
Doxorubicin
Paclitaxel
A2AR/A2BR
PI3Kγ
Chemotherapy
AB928:
Dual A2AR and
A2BR Antagonist
Phase 1 Experimental: Dose Escalation-Arm A, AB928 + Pegylated Liposomal Doxorubicin
Experimental: Dose Escalation-Arm B, AB928 + Nanoparticle Albumin-bound Paclitaxel
Experimental: Dose Escalation-Arm C, AB928 + Pegylated Liposomal Doxorubicin + Nanoparticle Albumin-bound Paclitaxel
Experimental: Dose Expansion-TNBC-Arm 1, dose from Arm A for AB928 + Pegylated Liposomal Doxorubicin
Experimental: Dose Expansion-Ovarian-Arm 2, dose from Arm A for AB928 + Pegylated Liposomal Doxorubicin
Experimental: Dose Expansion-TNBC-Arm 3, dose from Arm B for AB928 + Nanoparticle Albumin-bound Paclitaxel
Experimental: Dose Expansion-TNBC-Arm 4, dose from Arm C for AB928 + IPI-549 + Pegylated Liposomal Doxorubicin
Triple Negative
Breast Cancer
(TNBC)
Ovarian Cancer
Recruiting NCT03719326
AB928
mFOLFOX
A2AR/A2BR
Chemotherapy
AB928:
Dual A2AR and
A2BR Antagonist
Phase 1 Experimental: Dose Escalation, AB928 + mFOLFOX
Experimental: Dose Expansion-GE, dose from escalation for AB928 + mFOLFOX
Experimental: Dose Expansion-CRC, dose from escalation for AB928 + mFOLFOX
GastroEsophageal
Cancer (GE)
Colorectal Cancer
(CRC)
Recruiting NCT03720678
AB928
Zimberelimab
(AB122)
A2AR/A2BR
PD-1
AB928:
Dual A2AR and
A2BR Antagonist
Phase 1 Experimental: Dose Escalation, AB928 + fixed dose of Zimberelimab (AB122)
Experimental: Dose Expansion-Renal Cell Carcinoma, recommended dose for expansion AB928 + Zimberelimab (AB122)
Experimental: Dose Expansion, recommended dose for expansion AB928 + Zimberelimab (AB122)
Non-small Cell Lung Cancer
Squamous Cell Carcinoma of the Head and Neck
Breast Cancer
Colorectal Cancer
Melanoma Bladder Cancer
Ovarian Cancer
Endometrial Cancer
Merkel Cell Carcinoma GastroEsophageal Cancer
Renal Cell Carcinoma Castration-resistant Prostate Cancer
Recruiting NCT03629756
AB928
AB154
Zimberelimab
(AB122)
A2AR/A2BR
TIGIT
PD-1
AB928:
Dual A2AR and
A2BR Antagonist
Phase 2 Experimental: Arm 1, Zimberelimab
Experimental: Arm 2, AB154 + Zimberelimab
Experimental: Arm 3, AB928 + AB154 + Zimberelimab
Non-Small Cell Lung Cancer
Non-squamous Non-Small Cell Lung Cancer
Squamous Non-Small Cell Lung Cancer
Lung Cancer
Recruiting NCT04262856
AB928
Zimberelimab
(AB122)
Carboplatin
Pemetrexed
Pembrolizumab
A2AR/A2BR
PD-1
Chemotherapy
AB928:
Dual A2AR and
A2BR Antagonist
Phase 1 Experimental: Dose Escalation Arm A, AB928 + Carboplatin + Pemetrexed
Experimental: Dose Escalation Arm B, AB928 + Carboplatin + Pemetrexed + Pembrolizumab
Experimental: Dose Expansion Arm 1, recommended dose for expansion AB928 + Carboplatin + Pemetrexed in patients harboring sensitizing EGFR mutation
Experimental: Dose Expansion Arm 2, recommended dose for expansion AB928 + Carboplatin + Pemetrexed + AB122 in patients harboring sensitizing EGFR mutation
Non-Small Cell Lung Cancer
Metastatic Non-Small Cell Lung Cancer
Non-squamous Non-small Cell Neoplasm of Lung Sensitizing EGFR Gene Mutation
Recruiting NCT03846310
A2BR PBF-1129 A2BR PBF-1129: A2BR Antagonist Phase 1 Experimental: PBF-1129_40 mg
Experimental: PBF-1129_80 mg
Experimental: PBF-1129_160 mg
Experimental: PBF-1129_320 mg
Non-Small Cell Lung Cancer Recruiting NCT03274479