{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,24]],"date-time":"2026-10-24T03:48:44Z","timestamp":1792813724447,"version":"4.5.0"},"reference-count":72,"publisher":"Innovative Healthcare Institute","issue":"1","license":[{"start":{"date-parts":[[2025,2,1]],"date-time":"2025-02-01T00:00:00Z","timestamp":1738368000000},"content-version":"unspecified","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"},{"start":{"date-parts":[[2025,2,1]],"date-time":"2025-02-01T00:00:00Z","timestamp":1738368000000},"content-version":"unspecified","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2025,2]]},"abstract":"ABSTRACT<\/jats:title>\n Cyclin dependent kinase 2 (CDK2) is responsible for enforcing progression through the G1-S phase transition. Mutations and alterations in the CDK2 signaling pathway are associated with various cancers, most commonly breast, ovarian, prostate, leukemia, and lymphoma. CDK2 inhibitors have shown promising preclinical and early clinical results, and this class of agents may be most effective against cancers with cyclin E overactivity. Common side effects observed include nausea, vomiting, diarrhea, anemia, and fatigue. This clinical review summarizes past and current CDK2 inhibitors in clinical trials.<\/jats:p>","DOI":"10.36401\/jipo-24-22","type":"journal-article","created":{"date-parts":[[2024,12,11]],"date-time":"2024-12-11T19:01:16Z","timestamp":1733943676000},"page":"47-54","source":"Crossref","is-referenced-by-count":33,"title":["Cyclin Dependent Kinase 2 (CDK2) Inhibitors in Oncology Clinical Trials: A Review"],"prefix":"10.36401","volume":"8","author":[{"given":"Isabelle","family":"House","sequence":"first","affiliation":[{"name":"Sarah Cannon Research Institute at HealthONE, Denver, CO, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mari","family":"Valore-Caplan","sequence":"additional","affiliation":[{"name":"Sarah Cannon Research Institute at HealthONE, Denver, CO, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Elijah","family":"Maris","sequence":"additional","affiliation":[{"name":"Sarah Cannon Research Institute at HealthONE, Denver, CO, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Gerald S.","family":"Falchook","sequence":"additional","affiliation":[{"name":"Sarah Cannon Research Institute at HealthONE, Denver, CO, USA"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"22027","reference":[{"key":"i2590-017X-8-1-47-b01","series-title":"Front Cell Dev Biol","first-page":"16","article-title":"Targeting cell cycle regulators in hematologic malignancies","volume":"3","author":"Aleem","year":"2015","unstructured":"Aleem\n E,\n \n \n Arceci\n RJ.\n \n \n Targeting cell cycle regulators in hematologic malignancies. Front Cell Dev Biol. 2015;3:16."},{"key":"i2590-017X-8-1-47-b02","series-title":"Int J Mol Sci","first-page":"1960","article-title":"The roles of cyclin-dependent kinases in cell-cycle progression and therapeutic strategies in human breast cancer","volume":"21","author":"Ding","year":"2020","unstructured":"Ding\n L,\n \n \n Cao\n J,\n \n \n Lin\n W,\n \n et al.\n \n The roles of cyclin-dependent kinases in cell-cycle progression and therapeutic strategies in human breast cancer. Int J Mol Sci. 2020;21:1960."},{"key":"i2590-017X-8-1-47-b03","series-title":"Cancer Re","first-page":"5481","article-title":"Low-molecular-weight cyclin E in human cancer: cellular consequences and opportunities for targeted therapies","volume":"78","author":"Caruso","year":"2018","unstructured":"Caruso\n JA,\n \n \n Duong\n MT,\n \n \n Carey\n JPW,\n \n et al.\n \n Low-molecular-weight cyclin E in human cancer: cellular consequences and opportunities for targeted therapies. Cancer Re. 2018;78:5481\u20135491."},{"key":"i2590-017X-8-1-47-b04","article-title":"CDK2 Gene - GeneCards | CDK2 Protein | CDK2 Antibody","unstructured":"CDK2 Gene - GeneCards | CDK2 Protein | CDK2 Antibody. Accessed Jul 28, 2023. https:\/\/www.genecards.org\/cgi-bin\/carddisp.pl?gene=CDK2"},{"key":"i2590-017X-8-1-47-b05","article-title":"Novel MITF targets identified using a two\u2010step","author":"Hoek","unstructured":"Hoek\n KS.\n \n \n Novel MITF targets identified using a two\u2010step. Accessed Nov 7, 2023. onlinelibrary.wiley.com\/doi\/10.1111\/j.1755\u2013148X.2008.00505.x"},{"key":"i2590-017X-8-1-47-b06","series-title":"Drug Discov Today","first-page":"406","article-title":"Targeting CDK2 in cancer: challenges and opportunities for therapy","volume":"25","author":"Tadesse","year":"2020","unstructured":"Tadesse\n S,\n \n \n Anshabo\n AT,\n \n \n Portman\n N,\n \n et al.\n \n Targeting CDK2 in cancer: challenges and opportunities for therapy. Drug Discov Today. 2020;25:406\u2013413."},{"key":"i2590-017X-8-1-47-b07","article-title":"CDK2 | Cancer Genetics Web","unstructured":"CDK2 | Cancer Genetics Web. Accessed Jul 28, 2023. http:\/\/www.cancerindex.org\/geneweb\/CDK2.htm"},{"key":"i2590-017X-8-1-47-b08","article-title":"Expression of CDK2 in cancer - Summary - The Human Protein Atlas","unstructured":"Expression of CDK2 in cancer - Summary - The Human Protein Atlas. Accessed Jul 28, 2023. www.proteinatlas.org\/ENSG00000123374-CDK2\/pathology"},{"key":"i2590-017X-8-1-47-b09","series-title":"The Cell: A Molecular Approach","article-title":"DNA Repair","author":"Cooper","year":"2000","unstructured":"Cooper\n GM.\n \n \n DNA Repair. In: The Cell: A Molecular Approach. 2nd Ed. Sinauer Associates; 2000."},{"key":"i2590-017X-8-1-47-b10","series-title":"Nat Commun","first-page":"2835","article-title":"Inhibition of the CDK2 and Cyclin A complex leads to autophagic degradation of CDK2 in cancer cells","volume":"13","author":"Zhang","year":"2022","unstructured":"Zhang\n J,\n \n \n Gan\n Y,\n \n \n Li\n H,\n \n et al.\n \n Inhibition of the CDK2 and Cyclin A complex leads to autophagic degradation of CDK2 in cancer cells. Nat Commun. 2022;13:2835."},{"key":"i2590-017X-8-1-47-b11","series-title":"Br J Cancer","first-page":"342","article-title":"Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells","volume":"102","author":"Johnson","year":"2010","unstructured":"Johnson\n N,\n \n \n Bentley\n J,\n \n \n Wang\n LZ,\n \n et al.\n \n Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells. Br J Cancer. 2010;102:342\u2013350."},{"issue":"7_Supplement","key":"i2590-017X-8-1-47-b12","series-title":"Cancer Res","first-page":"5994","article-title":"Abstract 5994: INX-315, a potent and selective CDK2 inhibitor, demonstrates robust antitumor activity in CCNE1-amplified cancers","volume":"83","author":"Trub","year":"2023","unstructured":"Trub\n AG,\n \n \n Bisi\n JE,\n \n \n Dietrich\n C,\n \n et al.\n \n Abstract 5994: INX-315, a potent and selective CDK2 inhibitor, demonstrates robust antitumor activity in CCNE1-amplified cancers. Cancer Res. 2023;83(7_Supplement):5994."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b13","series-title":"J Clin Oncol","first-page":"e17546","article-title":"Phase 1\/2 study of ARTS-021, a potent, oral administrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors","volume":"41","author":"Wang","year":"2023","unstructured":"Wang\n Y.\n \n \n Phase 1\/2 study of ARTS-021, a potent, oral administrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors. J Clin Oncol. 2023;41(16_suppl):e17546\u2013e17546."},{"key":"i2590-017X-8-1-47-b14","series-title":"Cancer Chemother Pharmacol","first-page":"723","article-title":"SNS-032 is a potent and selective CDK2, 7, and 9 inhibitor that drives target modulation in patient samples","volume":"64","author":"Conroy","year":"2009","unstructured":"Conroy\n A,\n \n \n Stockett\n DE,\n \n \n Walker\n D,\n \n et al.\n \n SNS-032 is a potent and selective CDK2, 7, and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009;64:723\u2013732."},{"key":"i2590-017X-8-1-47-b15","series-title":"Leukemia","first-page":"1596","article-title":"Cyclin-dependent kinase inhibitor fadraciclib (CYC065) depletes anti-apoptotic protein and synergizes with venetoclax in primary chronic lymphocytic leukemia cells","volume":"36","author":"Chen","year":"2022","unstructured":"Chen\n R,\n \n \n Chen\n Y,\n \n \n Xiong\n P,\n \n et al.\n \n Cyclin-dependent kinase inhibitor fadraciclib (CYC065) depletes anti-apoptotic protein and synergizes with venetoclax in primary chronic lymphocytic leukemia cells. Leukemia. 2022;36:1596\u20131608."},{"issue":"16_Supplement","key":"i2590-017X-8-1-47-b16","series-title":"J Clin Oncol","first-page":"3095","article-title":"BLU-222, an oral, potent, and selective CDK2 inhibitor, in patients with advanced solid tumors: phase 1 monotherapy dose escalation","volume":"41","author":"Patel","year":"2023","unstructured":"Patel\n MR,\n \n \n Juric\n D,\n \n \n Henick\n BS,\n \n et al.\n \n BLU-222, an oral, potent, and selective CDK2 inhibitor, in patients with advanced solid tumors: phase 1 monotherapy dose escalation. J Clin Oncol. 2023;41(16_Supplement):3095."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b17","series-title":"J Clin Oncol","first-page":"1056","article-title":"BLU-222, an investigational, oral, potent, and highly selective CDK2 inhibitor (CDK2i), as monotherapy in patients (pts) with advanced solid tumors and in combination with ribociclib (RIBO) and fulvestrant (FUL) in HR+\/HER2\u2212 breast cancer (BC)","volume":"42","author":"Juric","year":"2024","unstructured":"Juric\n D,\n \n \n Patel\n MR,\n \n \n Duska\n LR,\n \n et al.\n \n BLU-222, an investigational, oral, potent, and highly selective CDK2 inhibitor (CDK2i), as monotherapy in patients (pts) with advanced solid tumors and in combination with ribociclib (RIBO) and fulvestrant (FUL) in HR+\/HER2\u2212 breast cancer (BC). J Clin Oncol. 2024;42(16_suppl):1056."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b18","series-title":"J Clin Oncol","first-page":"3010","article-title":"First-in-human phase 1\/2a study of a potent and novel CDK2-selective inhibitor PF-07104091 in patients (pts) with advanced solid tumors, enriched for CDK4\/6 inhibitor resistant HR+\/HER2- breast cancer","volume":"41","author":"Yap","year":"2023","unstructured":"Yap\n TA,\n \n \n Elhaddad\n AM,\n \n \n Grisham\n RN,\n \n et al.\n \n First-in-human phase 1\/2a study of a potent and novel CDK2-selective inhibitor PF-07104091 in patients (pts) with advanced solid tumors, enriched for CDK4\/6 inhibitor resistant HR+\/HER2- breast cancer. J Clin Oncol. 2023;41(16_suppl):3010."},{"issue":"16","key":"i2590-017X-8-1-47-b19","series-title":"J Clin Oncol","first-page":"3173","article-title":"Phase 1\/2 dose escalation study of NUV-422, a potent inhibitor of cyclin-dependent kinases 2, 4, and 6, in recurrent or refractory (r\/r) high-grade gliomas (HGG) and solid tumors","volume":"40","author":"Wen","year":"2022","unstructured":"Wen\n PY,\n \n \n Ahnert\n JR,\n \n \n Powderly\n JD,\n \n et al.\n \n Phase 1\/2 dose escalation study of NUV-422, a potent inhibitor of cyclin-dependent kinases 2, 4, and 6, in recurrent or refractory (r\/r) high-grade gliomas (HGG) and solid tumors. J Clin Oncol. 2022;40(16):3173."},{"key":"i2590-017X-8-1-47-b20","series-title":"Nuvation Bio","article-title":"Nuvation Bio Announces FDA Partial Clinical Hold for Phase 1 Study of NUV-422 in Solid Tumors","year":"2022","unstructured":"Nuvation Bio Announces FDA Partial Clinical Hold for Phase 1 Study of NUV-422 in Solid Tumors. Nuvation Bio. Published Jun 27, 2022. Accessed Jul 7, 2023. https:\/\/investors.nuvationbio.com\/news\/news-details\/2022\/Nuvation-Bio-Announces-FDA-Partial-Clinical-Hold-for-Phase-1-Study-of-NUV-422-in-Solid-Tumors\/default.aspx"},{"key":"i2590-017X-8-1-47-b21","series-title":"J Clin Oncol","first-page":"3528","article-title":"A phase I study of R547, a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases (CDKs)","volume":"25","author":"Diab","year":"2007","unstructured":"Diab\n S,\n \n \n Eckhardt\n S,\n \n \n Tan\n A,\n \n et al.\n \n A phase I study of R547, a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases (CDKs). J Clin Oncol. 2007;25:3528."},{"issue":"18","key":"i2590-017X-8-1-47-b22","series-title":"J Clin Oncol","first-page":"3015","article-title":"Phase I and pharmacologic study of SNS-032, a potent and selective Cdk2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma","volume":"28","author":"Tong","year":"2010","unstructured":"Tong\n WG,\n \n \n Chen\n R,\n \n \n Plunkett\n W,\n \n et al.\n \n Phase I and pharmacologic study of SNS-032, a potent and selective Cdk2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma. J Clin Oncol. 2010;28(18):3015\u20133022."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b23","series-title":"J Clin Oncol","first-page":"3125","article-title":"A phase 1 study evaluating the safety, pharmacokinetics, an efficacy of fadraciclib, an oral CDK2\/9 inhibitor, in patients with advanced solid tumors and lymphomas","volume":"42","author":"Villalona-Calero","year":"2024","unstructured":"Villalona-Calero\n MA,\n \n \n Oh\n D,\n \n \n Garralda\n E,\n \n et al.\n \n A phase 1 study evaluating the safety, pharmacokinetics, an efficacy of fadraciclib, an oral CDK2\/9 inhibitor, in patients with advanced solid tumors and lymphomas. J Clin Oncol. 2024;42(16_suppl):3125."},{"issue":"5_Supplement","key":"i2590-017X-8-1-47-b24","series-title":"Cancer Res","first-page":"P6\u201310\u201307","article-title":"BLU-222, an investigational, potent, and selective CDK2 inhibitor, demonstrated robust antitumor activity in CCNE1-amplified ovarian cancer models","volume":"83","author":"Brown","year":"2023","unstructured":"Brown\n V,\n \n \n Ramsden\n P,\n \n \n House\n N,\n \n et al.\n \n BLU-222, an investigational, potent, and selective CDK2 inhibitor, demonstrated robust antitumor activity in CCNE1-amplified ovarian cancer models. Cancer Res. 2023;83(5_Supplement):P6\u201310\u201307."},{"key":"i2590-017X-8-1-47-b25","series-title":"Mol Cancer Ther","first-page":"2517","article-title":"Preclinical biomarkers for a cyclin-dependent kinase inhibitor translate to candidate pharmacodynamic biomarkers in phase I patients","volume":"8","author":"Berkofsky-Fessler","year":"2009","unstructured":"Berkofsky-Fessler\n W,\n \n \n Nguyen\n TQ,\n \n \n Delmar\n P,\n \n et al.\n \n Preclinical biomarkers for a cyclin-dependent kinase inhibitor translate to candidate pharmacodynamic biomarkers in phase I patients. Mol Cancer Ther. 2009;8:2517\u20132525."},{"key":"i2590-017X-8-1-47-b26","series-title":"Clin Cancer Res","first-page":"5960","article-title":"Resistance to CDK2 inhibitors is associated with selection of polyploid cells in CCNE1-amplified ovarian cancer","volume":"19","author":"Etemadmoghadam","year":"2013","unstructured":"Etemadmoghadam\n D,\n \n \n Au-Yeung\n G,\n \n \n Wall\n M,\n \n et al.\n \n Resistance to CDK2 inhibitors is associated with selection of polyploid cells in CCNE1-amplified ovarian cancer. Clin Cancer Res. 2013;19:5960\u20135971."},{"key":"i2590-017X-8-1-47-b27","article-title":"A phase 1\/2 study to evaluate the safety, pharmacokinetics, and efficacy of BLU-222 as a single agent and in combination therapy for patients with advanced solid tumors","author":"Blueprint Medicines Corporation","unstructured":"Blueprint Medicines Corporation\n . A phase 1\/2 study to evaluate the safety, pharmacokinetics, and efficacy of BLU-222 as a single agent and in combination therapy for patients with advanced solid tumors. ClinicalTrials.gov identifier: NCT05252416."},{"key":"i2590-017X-8-1-47-b28","article-title":"Pfizer. A phase 1B\/2, open-label, multicenter, dose escalation and dose expansion study to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of PF-07220060 in combination with PF-07104091 plus endocrine therapy in participants with advanced solid tumors","unstructured":"Pfizer. A phase 1B\/2, open-label, multicenter, dose escalation and dose expansion study to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of PF-07220060 in combination with PF-07104091 plus endocrine therapy in participants with advanced solid tumors. ClinicalTrials.gov identifier: NCT05262400."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b29","series-title":"J Clin Oncol","first-page":"17546","article-title":"Phase 1\/2 study of ARTS-021, a potent, oral adminstrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors","volume":"41","author":"Wang","year":"2023","unstructured":"Wang\n Y.\n \n \n Phase 1\/2 study of ARTS-021, a potent, oral adminstrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors. J Clin Oncol. 2023;41(16_suppl):17546."},{"key":"i2590-017X-8-1-47-b30","article-title":"A pharmacologic study of CYC065, a cyclin dependent kinase inhibitor, in patients with advanced cancers","unstructured":"A pharmacologic study of CYC065, a cyclin dependent kinase inhibitor, in patients with advanced cancers. ClinicalTrials.gov identifier: NCT02552953."},{"key":"i2590-017X-8-1-47-b31","article-title":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory CLL","unstructured":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory CLL. ClinicalTrials.gov identifier: NCT03739554."},{"key":"i2590-017X-8-1-47-b32","article-title":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory AML or MDS","unstructured":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory AML or MDS. ClinicalTrials.gov identifier: NCT04017546."},{"key":"i2590-017X-8-1-47-b33","article-title":"Open-label study to evaluate the safety, tolerability, PK, and efficacy of INX-315 in patients with advanced cancer (INX-315\u201301)","unstructured":"Open-label study to evaluate the safety, tolerability, PK, and efficacy of INX-315 in patients with advanced cancer (INX-315\u201301). ClinicalTrials.gov identifier: NCT05735080."},{"key":"i2590-017X-8-1-47-b34","article-title":"A study to investigate fadraciclib (CYC065), in subjects with leukemia or myelodysplastic syndrome (MDS)","unstructured":"A study to investigate fadraciclib (CYC065), in subjects with leukemia or myelodysplastic syndrome (MDS). ClinicalTrials.gov identifier: NCT05168904."},{"key":"i2590-017X-8-1-47-b35","article-title":"A study with NKT3447 for adults with advanced\/metastatic solid tumors","unstructured":"A study with NKT3447 for adults with advanced\/metastatic solid tumors. ClinicalTrials.gov identifier: NCT06264921."},{"key":"i2590-017X-8-1-47-b36","article-title":"Study of PF-07224826, as a single agent or in combination with endocrine therapy in participants with breast cancer and other advanced solid tumors","unstructured":"Study of PF-07224826, as a single agent or in combination with endocrine therapy in participants with breast cancer and other advanced solid tumors. ClinicalTrials.gov identifier: NCT05905341."},{"key":"i2590-017X-8-1-47-b01","series-title":"Front Cell Dev Biol","first-page":"16","article-title":"Targeting cell cycle regulators in hematologic malignancies","volume":"3","author":"Aleem","year":"2015","unstructured":"Aleem\n E,\n \n \n Arceci\n RJ.\n \n \n Targeting cell cycle regulators in hematologic malignancies. Front Cell Dev Biol. 2015;3:16."},{"key":"i2590-017X-8-1-47-b02","series-title":"Int J Mol Sci","first-page":"1960","article-title":"The roles of cyclin-dependent kinases in cell-cycle progression and therapeutic strategies in human breast cancer","volume":"21","author":"Ding","year":"2020","unstructured":"Ding\n L,\n \n \n Cao\n J,\n \n \n Lin\n W,\n \n et al.\n \n The roles of cyclin-dependent kinases in cell-cycle progression and therapeutic strategies in human breast cancer. Int J Mol Sci. 2020;21:1960."},{"key":"i2590-017X-8-1-47-b03","series-title":"Cancer Re","first-page":"5481","article-title":"Low-molecular-weight cyclin E in human cancer: cellular consequences and opportunities for targeted therapies","volume":"78","author":"Caruso","year":"2018","unstructured":"Caruso\n JA,\n \n \n Duong\n MT,\n \n \n Carey\n JPW,\n \n et al.\n \n Low-molecular-weight cyclin E in human cancer: cellular consequences and opportunities for targeted therapies. Cancer Re. 2018;78:5481\u20135491."},{"key":"i2590-017X-8-1-47-b04","article-title":"CDK2 Gene - GeneCards | CDK2 Protein | CDK2 Antibody","unstructured":"CDK2 Gene - GeneCards | CDK2 Protein | CDK2 Antibody. Accessed Jul 28, 2023. https:\/\/www.genecards.org\/cgi-bin\/carddisp.pl?gene=CDK2"},{"key":"i2590-017X-8-1-47-b05","article-title":"Novel MITF targets identified using a two\u2010step","author":"Hoek","unstructured":"Hoek\n KS.\n \n \n Novel MITF targets identified using a two\u2010step. Accessed Nov 7, 2023. onlinelibrary.wiley.com\/doi\/10.1111\/j.1755\u2013148X.2008.00505.x"},{"key":"i2590-017X-8-1-47-b06","series-title":"Drug Discov Today","first-page":"406","article-title":"Targeting CDK2 in cancer: challenges and opportunities for therapy","volume":"25","author":"Tadesse","year":"2020","unstructured":"Tadesse\n S,\n \n \n Anshabo\n AT,\n \n \n Portman\n N,\n \n et al.\n \n Targeting CDK2 in cancer: challenges and opportunities for therapy. Drug Discov Today. 2020;25:406\u2013413."},{"key":"i2590-017X-8-1-47-b07","article-title":"CDK2 | Cancer Genetics Web","unstructured":"CDK2 | Cancer Genetics Web. Accessed Jul 28, 2023. http:\/\/www.cancerindex.org\/geneweb\/CDK2.htm"},{"key":"i2590-017X-8-1-47-b08","article-title":"Expression of CDK2 in cancer - Summary - The Human Protein Atlas","unstructured":"Expression of CDK2 in cancer - Summary - The Human Protein Atlas. Accessed Jul 28, 2023. www.proteinatlas.org\/ENSG00000123374-CDK2\/pathology"},{"key":"i2590-017X-8-1-47-b09","series-title":"The Cell: A Molecular Approach","article-title":"DNA Repair","author":"Cooper","year":"2000","unstructured":"Cooper\n GM.\n \n \n DNA Repair. In: The Cell: A Molecular Approach. 2nd Ed. Sinauer Associates; 2000."},{"key":"i2590-017X-8-1-47-b10","series-title":"Nat Commun","first-page":"2835","article-title":"Inhibition of the CDK2 and Cyclin A complex leads to autophagic degradation of CDK2 in cancer cells","volume":"13","author":"Zhang","year":"2022","unstructured":"Zhang\n J,\n \n \n Gan\n Y,\n \n \n Li\n H,\n \n et al.\n \n Inhibition of the CDK2 and Cyclin A complex leads to autophagic degradation of CDK2 in cancer cells. Nat Commun. 2022;13:2835."},{"key":"i2590-017X-8-1-47-b11","series-title":"Br J Cancer","first-page":"342","article-title":"Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells","volume":"102","author":"Johnson","year":"2010","unstructured":"Johnson\n N,\n \n \n Bentley\n J,\n \n \n Wang\n LZ,\n \n et al.\n \n Pre-clinical evaluation of cyclin-dependent kinase 2 and 1 inhibition in anti-estrogen-sensitive and resistant breast cancer cells. Br J Cancer. 2010;102:342\u2013350."},{"issue":"7_Supplement","key":"i2590-017X-8-1-47-b12","series-title":"Cancer Res","first-page":"5994","article-title":"Abstract 5994: INX-315, a potent and selective CDK2 inhibitor, demonstrates robust antitumor activity in CCNE1-amplified cancers","volume":"83","author":"Trub","year":"2023","unstructured":"Trub\n AG,\n \n \n Bisi\n JE,\n \n \n Dietrich\n C,\n \n et al.\n \n Abstract 5994: INX-315, a potent and selective CDK2 inhibitor, demonstrates robust antitumor activity in CCNE1-amplified cancers. Cancer Res. 2023;83(7_Supplement):5994."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b13","series-title":"J Clin Oncol","first-page":"e17546","article-title":"Phase 1\/2 study of ARTS-021, a potent, oral administrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors","volume":"41","author":"Wang","year":"2023","unstructured":"Wang\n Y.\n \n \n Phase 1\/2 study of ARTS-021, a potent, oral administrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors. J Clin Oncol. 2023;41(16_suppl):e17546\u2013e17546."},{"key":"i2590-017X-8-1-47-b14","series-title":"Cancer Chemother Pharmacol","first-page":"723","article-title":"SNS-032 is a potent and selective CDK2, 7, and 9 inhibitor that drives target modulation in patient samples","volume":"64","author":"Conroy","year":"2009","unstructured":"Conroy\n A,\n \n \n Stockett\n DE,\n \n \n Walker\n D,\n \n et al.\n \n SNS-032 is a potent and selective CDK2, 7, and 9 inhibitor that drives target modulation in patient samples. Cancer Chemother Pharmacol. 2009;64:723\u2013732."},{"key":"i2590-017X-8-1-47-b15","series-title":"Leukemia","first-page":"1596","article-title":"Cyclin-dependent kinase inhibitor fadraciclib (CYC065) depletes anti-apoptotic protein and synergizes with venetoclax in primary chronic lymphocytic leukemia cells","volume":"36","author":"Chen","year":"2022","unstructured":"Chen\n R,\n \n \n Chen\n Y,\n \n \n Xiong\n P,\n \n et al.\n \n Cyclin-dependent kinase inhibitor fadraciclib (CYC065) depletes anti-apoptotic protein and synergizes with venetoclax in primary chronic lymphocytic leukemia cells. Leukemia. 2022;36:1596\u20131608."},{"issue":"16_Supplement","key":"i2590-017X-8-1-47-b16","series-title":"J Clin Oncol","first-page":"3095","article-title":"BLU-222, an oral, potent, and selective CDK2 inhibitor, in patients with advanced solid tumors: phase 1 monotherapy dose escalation","volume":"41","author":"Patel","year":"2023","unstructured":"Patel\n MR,\n \n \n Juric\n D,\n \n \n Henick\n BS,\n \n et al.\n \n BLU-222, an oral, potent, and selective CDK2 inhibitor, in patients with advanced solid tumors: phase 1 monotherapy dose escalation. J Clin Oncol. 2023;41(16_Supplement):3095."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b17","series-title":"J Clin Oncol","first-page":"1056","article-title":"BLU-222, an investigational, oral, potent, and highly selective CDK2 inhibitor (CDK2i), as monotherapy in patients (pts) with advanced solid tumors and in combination with ribociclib (RIBO) and fulvestrant (FUL) in HR+\/HER2\u2212 breast cancer (BC)","volume":"42","author":"Juric","year":"2024","unstructured":"Juric\n D,\n \n \n Patel\n MR,\n \n \n Duska\n LR,\n \n et al.\n \n BLU-222, an investigational, oral, potent, and highly selective CDK2 inhibitor (CDK2i), as monotherapy in patients (pts) with advanced solid tumors and in combination with ribociclib (RIBO) and fulvestrant (FUL) in HR+\/HER2\u2212 breast cancer (BC). J Clin Oncol. 2024;42(16_suppl):1056."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b18","series-title":"J Clin Oncol","first-page":"3010","article-title":"First-in-human phase 1\/2a study of a potent and novel CDK2-selective inhibitor PF-07104091 in patients (pts) with advanced solid tumors, enriched for CDK4\/6 inhibitor resistant HR+\/HER2- breast cancer","volume":"41","author":"Yap","year":"2023","unstructured":"Yap\n TA,\n \n \n Elhaddad\n AM,\n \n \n Grisham\n RN,\n \n et al.\n \n First-in-human phase 1\/2a study of a potent and novel CDK2-selective inhibitor PF-07104091 in patients (pts) with advanced solid tumors, enriched for CDK4\/6 inhibitor resistant HR+\/HER2- breast cancer. J Clin Oncol. 2023;41(16_suppl):3010."},{"issue":"16","key":"i2590-017X-8-1-47-b19","series-title":"J Clin Oncol","first-page":"3173","article-title":"Phase 1\/2 dose escalation study of NUV-422, a potent inhibitor of cyclin-dependent kinases 2, 4, and 6, in recurrent or refractory (r\/r) high-grade gliomas (HGG) and solid tumors","volume":"40","author":"Wen","year":"2022","unstructured":"Wen\n PY,\n \n \n Ahnert\n JR,\n \n \n Powderly\n JD,\n \n et al.\n \n Phase 1\/2 dose escalation study of NUV-422, a potent inhibitor of cyclin-dependent kinases 2, 4, and 6, in recurrent or refractory (r\/r) high-grade gliomas (HGG) and solid tumors. J Clin Oncol. 2022;40(16):3173."},{"key":"i2590-017X-8-1-47-b20","series-title":"Nuvation Bio","article-title":"Nuvation Bio Announces FDA Partial Clinical Hold for Phase 1 Study of NUV-422 in Solid Tumors","year":"2022","unstructured":"Nuvation Bio Announces FDA Partial Clinical Hold for Phase 1 Study of NUV-422 in Solid Tumors. Nuvation Bio. Published Jun 27, 2022. Accessed Jul 7, 2023. https:\/\/investors.nuvationbio.com\/news\/news-details\/2022\/Nuvation-Bio-Announces-FDA-Partial-Clinical-Hold-for-Phase-1-Study-of-NUV-422-in-Solid-Tumors\/default.aspx"},{"key":"i2590-017X-8-1-47-b21","series-title":"J Clin Oncol","first-page":"3528","article-title":"A phase I study of R547, a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases (CDKs)","volume":"25","author":"Diab","year":"2007","unstructured":"Diab\n S,\n \n \n Eckhardt\n S,\n \n \n Tan\n A,\n \n et al.\n \n A phase I study of R547, a novel, selective inhibitor of cell cycle and transcriptional cyclin dependent kinases (CDKs). J Clin Oncol. 2007;25:3528."},{"issue":"18","key":"i2590-017X-8-1-47-b22","series-title":"J Clin Oncol","first-page":"3015","article-title":"Phase I and pharmacologic study of SNS-032, a potent and selective Cdk2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma","volume":"28","author":"Tong","year":"2010","unstructured":"Tong\n WG,\n \n \n Chen\n R,\n \n \n Plunkett\n W,\n \n et al.\n \n Phase I and pharmacologic study of SNS-032, a potent and selective Cdk2, 7, and 9 inhibitor, in patients with advanced chronic lymphocytic leukemia and multiple myeloma. J Clin Oncol. 2010;28(18):3015\u20133022."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b23","series-title":"J Clin Oncol","first-page":"3125","article-title":"A phase 1 study evaluating the safety, pharmacokinetics, an efficacy of fadraciclib, an oral CDK2\/9 inhibitor, in patients with advanced solid tumors and lymphomas","volume":"42","author":"Villalona-Calero","year":"2024","unstructured":"Villalona-Calero\n MA,\n \n \n Oh\n D,\n \n \n Garralda\n E,\n \n et al.\n \n A phase 1 study evaluating the safety, pharmacokinetics, an efficacy of fadraciclib, an oral CDK2\/9 inhibitor, in patients with advanced solid tumors and lymphomas. J Clin Oncol. 2024;42(16_suppl):3125."},{"issue":"5_Supplement","key":"i2590-017X-8-1-47-b24","series-title":"Cancer Res","first-page":"P6\u201310\u201307","article-title":"BLU-222, an investigational, potent, and selective CDK2 inhibitor, demonstrated robust antitumor activity in CCNE1-amplified ovarian cancer models","volume":"83","author":"Brown","year":"2023","unstructured":"Brown\n V,\n \n \n Ramsden\n P,\n \n \n House\n N,\n \n et al.\n \n BLU-222, an investigational, potent, and selective CDK2 inhibitor, demonstrated robust antitumor activity in CCNE1-amplified ovarian cancer models. Cancer Res. 2023;83(5_Supplement):P6\u201310\u201307."},{"key":"i2590-017X-8-1-47-b25","series-title":"Mol Cancer Ther","first-page":"2517","article-title":"Preclinical biomarkers for a cyclin-dependent kinase inhibitor translate to candidate pharmacodynamic biomarkers in phase I patients","volume":"8","author":"Berkofsky-Fessler","year":"2009","unstructured":"Berkofsky-Fessler\n W,\n \n \n Nguyen\n TQ,\n \n \n Delmar\n P,\n \n et al.\n \n Preclinical biomarkers for a cyclin-dependent kinase inhibitor translate to candidate pharmacodynamic biomarkers in phase I patients. Mol Cancer Ther. 2009;8:2517\u20132525."},{"key":"i2590-017X-8-1-47-b26","series-title":"Clin Cancer Res","first-page":"5960","article-title":"Resistance to CDK2 inhibitors is associated with selection of polyploid cells in CCNE1-amplified ovarian cancer","volume":"19","author":"Etemadmoghadam","year":"2013","unstructured":"Etemadmoghadam\n D,\n \n \n Au-Yeung\n G,\n \n \n Wall\n M,\n \n et al.\n \n Resistance to CDK2 inhibitors is associated with selection of polyploid cells in CCNE1-amplified ovarian cancer. Clin Cancer Res. 2013;19:5960\u20135971."},{"key":"i2590-017X-8-1-47-b27","article-title":"A phase 1\/2 study to evaluate the safety, pharmacokinetics, and efficacy of BLU-222 as a single agent and in combination therapy for patients with advanced solid tumors","author":"Blueprint Medicines Corporation","unstructured":"Blueprint Medicines Corporation\n . A phase 1\/2 study to evaluate the safety, pharmacokinetics, and efficacy of BLU-222 as a single agent and in combination therapy for patients with advanced solid tumors. ClinicalTrials.gov identifier: NCT05252416."},{"key":"i2590-017X-8-1-47-b28","article-title":"Pfizer. A phase 1B\/2, open-label, multicenter, dose escalation and dose expansion study to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of PF-07220060 in combination with PF-07104091 plus endocrine therapy in participants with advanced solid tumors","unstructured":"Pfizer. A phase 1B\/2, open-label, multicenter, dose escalation and dose expansion study to evaluate the safety, tolerability, pharmacokinetics, pharmacodynamics, and antitumor activity of PF-07220060 in combination with PF-07104091 plus endocrine therapy in participants with advanced solid tumors. ClinicalTrials.gov identifier: NCT05262400."},{"issue":"16_suppl","key":"i2590-017X-8-1-47-b29","series-title":"J Clin Oncol","first-page":"17546","article-title":"Phase 1\/2 study of ARTS-021, a potent, oral adminstrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors","volume":"41","author":"Wang","year":"2023","unstructured":"Wang\n Y.\n \n \n Phase 1\/2 study of ARTS-021, a potent, oral adminstrated, selective CDK2 inhibitor, in advanced or metastatic solid tumors. J Clin Oncol. 2023;41(16_suppl):17546."},{"key":"i2590-017X-8-1-47-b30","article-title":"A pharmacologic study of CYC065, a cyclin dependent kinase inhibitor, in patients with advanced cancers","unstructured":"A pharmacologic study of CYC065, a cyclin dependent kinase inhibitor, in patients with advanced cancers. ClinicalTrials.gov identifier: NCT02552953."},{"key":"i2590-017X-8-1-47-b31","article-title":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory CLL","unstructured":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory CLL. ClinicalTrials.gov identifier: NCT03739554."},{"key":"i2590-017X-8-1-47-b32","article-title":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory AML or MDS","unstructured":"CYC065 CDK inhibitor and venetoclax study in relapsed\/refractory AML or MDS. ClinicalTrials.gov identifier: NCT04017546."},{"key":"i2590-017X-8-1-47-b33","article-title":"Open-label study to evaluate the safety, tolerability, PK, and efficacy of INX-315 in patients with advanced cancer (INX-315\u201301)","unstructured":"Open-label study to evaluate the safety, tolerability, PK, and efficacy of INX-315 in patients with advanced cancer (INX-315\u201301). ClinicalTrials.gov identifier: NCT05735080."},{"key":"i2590-017X-8-1-47-b34","article-title":"A study to investigate fadraciclib (CYC065), in subjects with leukemia or myelodysplastic syndrome (MDS)","unstructured":"A study to investigate fadraciclib (CYC065), in subjects with leukemia or myelodysplastic syndrome (MDS). ClinicalTrials.gov identifier: NCT05168904."},{"key":"i2590-017X-8-1-47-b35","article-title":"A study with NKT3447 for adults with advanced\/metastatic solid tumors","unstructured":"A study with NKT3447 for adults with advanced\/metastatic solid tumors. ClinicalTrials.gov identifier: NCT06264921."},{"key":"i2590-017X-8-1-47-b36","article-title":"Study of PF-07224826, as a single agent or in combination with endocrine therapy in participants with breast cancer and other advanced solid tumors","unstructured":"Study of PF-07224826, as a single agent or in combination with endocrine therapy in participants with breast cancer and other advanced solid tumors. ClinicalTrials.gov identifier: NCT05905341."}],"container-title":["Journal of Immunotherapy and Precision Oncology"],"original-title":[],"link":[{"URL":"https:\/\/innovationsjournals-jipo.kglmeridian.com\/view\/journals\/jipo\/8\/1\/article-p47.xml","content-type":"text\/html","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/meridian.allenpress.com\/innovationsjournals-JIPO\/article-pdf\/8\/1\/47\/3461103\/10.36401_jipo-24-22.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"syndication"},{"URL":"https:\/\/innovationsjournals-jipo.kglmeridian.com\/downloadpdf\/journals\/jipo\/8\/1\/article-p47.xml","content-type":"text\/html","content-version":"vor","intended-application":"syndication"},{"URL":"https:\/\/innovationsjournals-jipo.kglmeridian.com\/downloadpdf\/journals\/jipo\/8\/1\/article-p47.xml","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,2,21]],"date-time":"2026-02-21T00:44:34Z","timestamp":1771634674000},"score":1,"resource":{"primary":{"URL":"https:\/\/innovationsjournals-jipo.kglmeridian.com\/view\/journals\/jipo\/8\/1\/article-p47.xml"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2025,2]]},"references-count":72,"journal-issue":{"issue":"1"},"URL":"https:\/\/doi.org\/10.36401\/jipo-24-22","relation":{},"ISSN":["2590-017X","2666-2345"],"issn-type":[{"value":"2590-017X","type":"electronic"},{"value":"2666-2345","type":"print"}],"subject":[],"published":{"date-parts":[[2025,2]]}}}