{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,8,13]],"date-time":"2026-08-13T06:31:38Z","timestamp":1786602698976,"version":"build-2736575974"},"reference-count":21,"publisher":"Springer Science and Business Media LLC","issue":"1","license":[{"start":{"date-parts":[[2026,8,13]],"date-time":"2026-08-13T00:00:00Z","timestamp":1786579200000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.springernature.com\/gp\/researchers\/text-and-data-mining"},{"start":{"date-parts":[[2026,8,13]],"date-time":"2026-08-13T00:00:00Z","timestamp":1786579200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/www.springernature.com\/gp\/researchers\/text-and-data-mining"}],"funder":[{"DOI":"10.13039\/100004319","name":"Pfizer Inc.","doi-asserted-by":"crossref","id":[{"id":"10.13039\/100004319","id-type":"DOI","asserted-by":"crossref"}]},{"name":"Arvinas Estrogen Receptor, Inc"}],"content-domain":{"domain":["link.springer.com"],"crossmark-restriction":false},"short-container-title":["Cancer Chemother Pharmacol"],"DOI":"10.1007\/s00280-026-04921-w","type":"journal-article","created":{"date-parts":[[2026,8,13]],"date-time":"2026-08-13T06:20:05Z","timestamp":1786602005000},"update-policy":"https:\/\/doi.org\/10.1007\/springer_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["A phase 1, open-label study evaluating the pharmacokinetics, safety, and tolerability of vepdegestrant in Chinese patients with ER+\/HER2- advanced breast cancer"],"prefix":"10.1007","volume":"96","author":[{"given":"Binghe","family":"Xu","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jin","family":"Yang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Pin","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wenna","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Liang","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Xiao\u2019ai","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Fei","family":"Guan","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Naihan","family":"Chen","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Huadong","family":"Zhao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Cong","family":"Fei","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"297","published-online":{"date-parts":[[2026,8,13]]},"reference":[{"key":"4921_CR1","doi-asserted-by":"publisher","first-page":"496","DOI":"10.1016\/j.ccell.2020.03.009","volume":"37","author":"AB Hanker","year":"2020","unstructured":"Hanker AB, Sudhan DR, Arteaga CL (2020) Overcoming endocrine resistance in breast cancer. Cancer Cell 37:496\u2013513. https:\/\/doi.org\/10.1016\/j.ccell.2020.03.009","journal-title":"Cancer Cell"},{"key":"4921_CR2","doi-asserted-by":"publisher","first-page":"175883592211136","DOI":"10.1177\/17588359221113694","volume":"14","author":"MR Lloyd","year":"2022","unstructured":"Lloyd MR, Wander SA, Hamilton E, Razavi P, Bardia A (2022) Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer: current and emerging role. Ther Adv Med Oncol 14:17588359221113694. https:\/\/doi.org\/10.1177\/17588359221113694","journal-title":"Ther Adv Med Oncol"},{"key":"4921_CR3","doi-asserted-by":"publisher","first-page":"949","DOI":"10.1016\/j.cell.2019.06.026","volume":"178","author":"J Guan","year":"2019","unstructured":"Guan J, Zhou W, Hafner M, Blake RA, Chalouni C, Chen IP, De Bruyn T, Giltnane JM, Hartman SJ, Heidersbach A, Houtman R, Ingalla E, Kategaya L, Kleinheinz T, Li J, Martin SE, Modrusan Z, Nannini M, Oeh J, Ubhayakar S, Wang X, Wertz IE, Young A, Yu M, Sampath D, Hager JH, Friedman LS, Daemen A, Metcalfe C (2019) Therapeutic ligands antagonize estrogen receptor function by impairing its mobility. Cell 178:949\u2013963. https:\/\/doi.org\/10.1016\/j.cell.2019.06.026","journal-title":"Cell"},{"key":"4921_CR4","doi-asserted-by":"publisher","first-page":"122","DOI":"10.1016\/j.bcp.2011.03.031","volume":"82","author":"SE Wardell","year":"2011","unstructured":"Wardell SE, Marks JR, McDonnell DP (2011) The turnover of estrogen receptor alpha by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy. Biochem Pharmacol 82:122\u2013130. https:\/\/doi.org\/10.1016\/j.bcp.2011.03.031","journal-title":"Biochem Pharmacol"},{"key":"4921_CR5","doi-asserted-by":"publisher","first-page":"619","DOI":"10.3390\/cancers16030619","volume":"16","author":"N Neupane","year":"2024","unstructured":"Neupane N, Bawek S, Gurusinghe S, Ghaffary EM, Mirmosayyeb O, Thapa S, Falkson C, O\u2019Regan R, Dhakal A (2024) Oral SERD, a novel endocrine therapy for estrogen receptor-positive breast cancer. Cancers 16:619. https:\/\/doi.org\/10.3390\/cancers16030619","journal-title":"Cancers"},{"key":"4921_CR6","doi-asserted-by":"publisher","first-page":"206","DOI":"10.1016\/j.ejca.2018.02.026","volume":"94","author":"JFR Robertson","year":"2018","unstructured":"Robertson JFR, Cheung KL, Noguchi S, Shao Z, Degboe A, Lichfield J, Thirlwell J, Fazal M, Ellis MJ (2018) Health-related quality of life from the FALCON phase III randomised trial of fulvestrant 500\u00a0mg versus anastrozole for hormone receptor-positive advanced breast cancer. Eur J Cancer 94:206\u2013215. https:\/\/doi.org\/10.1016\/j.ejca.2018.02.026","journal-title":"Eur J Cancer"},{"key":"4921_CR7","unstructured":"U.S. Food & Drug Administration (2021) FASLODEX - fulvestrant. https:\/\/www.accessdata.fda.gov\/scripts\/cder\/daf\/index.cfm?event=overview.process&ApplNo=021344. Accessed 16 June 2024"},{"key":"4921_CR8","unstructured":"U.S. Food & Drug Administration (2023) ORSERDU - elacestrant. https:\/\/www.accessdata.fda.gov\/scripts\/cder\/daf\/index.cfm?event=overview.process&ApplNo=217639. Accessed 4 April 2024"},{"key":"4921_CR9","doi-asserted-by":"publisher","first-page":"17","DOI":"10.1007\/s40487-017-0046-2","volume":"5","author":"MR Nathan","year":"2017","unstructured":"Nathan MR, Schmid P (2017) A review of fulvestrant in breast cancer. Oncol Ther 5:17\u201329. https:\/\/doi.org\/10.1007\/s40487-017-0046-2","journal-title":"Oncol Ther"},{"key":"4921_CR10","doi-asserted-by":"publisher","first-page":"237","DOI":"10.1007\/s10549-011-1947-7","volume":"133","author":"I Kuter","year":"2012","unstructured":"Kuter I, Gee JM, Hegg R, Singer CF, Badwe RA, Lowe ES, Emeribe UA, Anderson E, Sapunar F, Finlay P, Nicholson RI, Bines J, Harbeck N (2012) Dose-dependent change in biomarkers during neoadjuvant endocrine therapy with fulvestrant: results from NEWEST, a randomized Phase II study. Breast Cancer Res Treat 133:237\u2013246. https:\/\/doi.org\/10.1007\/s10549-011-1947-7","journal-title":"Breast Cancer Res Treat"},{"key":"4921_CR11","doi-asserted-by":"publisher","first-page":"R18","DOI":"10.1186\/bcr3393","volume":"15","author":"JF Robertson","year":"2013","unstructured":"Robertson JF, Dixon JM, Sibbering DM, Jahan A, Ellis IO, Channon E, Hyman-Taylor P, Nicholson RI, Gee JM (2013) A randomized trial to assess the biological activity of short-term (pre-surgical) fulvestrant 500\u00a0mg plus anastrozole versus fulvestrant 500\u00a0mg alone or anastrozole alone on primary breast cancer. Breast Cancer Res 15:R18. https:\/\/doi.org\/10.1186\/bcr3393","journal-title":"Breast Cancer Res"},{"key":"4921_CR12","doi-asserted-by":"publisher","first-page":"3246","DOI":"10.1200\/JCO.22.00338","volume":"40","author":"FC Bidard","year":"2022","unstructured":"Bidard FC, Kaklamani VG, Neven P, Streich G, Montero AJ, Forget F, Mouret-Reynier MA, Sohn JH, Taylor D, Harnden KK, Khong H, Kocsis J, Dalenc F, Dillon PM, Babu S, Waters S, Deleu I, Garcia Saenz JA, Bria E, Cazzaniga M, Lu J, Aftimos P, Cortes J, Liu S, Tonini G, Laurent D, Habboubi N, Conlan MG, Bardia A (2022) Elacestrant (oral selective estrogen receptor degrader) versus standard endocrine therapy for estrogen receptor-positive, human epidermal growth factor receptor 2-negative advanced breast cancer: results from the randomized phase III EMERALD trial. J Clin Oncol 40:3246\u20133256. https:\/\/doi.org\/10.1200\/JCO.22.00338","journal-title":"J Clin Oncol"},{"key":"4921_CR13","doi-asserted-by":"publisher","first-page":"103701","DOI":"10.1016\/j.esmoop.2024.103701","volume":"9","author":"C Valenza","year":"2024","unstructured":"Valenza C, Trapani D, Bidard FC, Gligorov J, Cortes J, Turner N, Dalenc F, Penault-Llorca F, Freyer G, Arnedos M, Villanueva C, Loibl S, Pistilli B, Curigliano G (2024) Elacestrant in ESR1-mutant, endocrine-responsive metastatic breast cancer: should health authorities consider post hoc data to inform priority access? ESMO Open 9:103701. https:\/\/doi.org\/10.1016\/j.esmoop.2024.103701","journal-title":"ESMO Open"},{"key":"4921_CR14","doi-asserted-by":"publisher","first-page":"181","DOI":"10.1038\/s41573-021-00371-6","volume":"21","author":"M Bekes","year":"2022","unstructured":"Bekes M, Langley DR, Crews CM (2022) PROTAC targeted protein degraders: the past is prologue. Nat Rev Drug Discov 21:181\u2013200. https:\/\/doi.org\/10.1038\/s41573-021-00371-6","journal-title":"Nat Rev Drug Discov"},{"key":"4921_CR15","doi-asserted-by":"publisher","first-page":"3549","DOI":"10.1158\/1078-0432.ccr-23-3465","volume":"30","author":"SM Gough","year":"2024","unstructured":"Gough SM, Flanagan JJ, Teh J, Andreoli M, Rousseau E, Pannone M, Bookbinder M, Willard R, Davenport K, Bortolon E, Cadelina G, Gordon D, Pizzano J, Macaluso J, Soto L, Corradi J, Digianantonio K, Drulyte I, Morgan A, Quinn C, B\u00e9k\u00e9s M, Ferraro C, Chen X, Wang G, Dong H, Wang J, Langley DR, Houston J, Gedrich R, Taylor IC (2024) Oral estrogen receptor PROTAC vepdegestrant (ARV-471) is highly efficacious as monotherapy and in combination with CDK4\/6 or PI3K\/mTOR pathway inhibitors in preclinical ER+ breast cancer models. Clin Cancer Res 30:3549\u20133563. https:\/\/doi.org\/10.1158\/1078-0432.ccr-23-3465","journal-title":"Clin Cancer Res"},{"key":"4921_CR16","doi-asserted-by":"publisher","first-page":"S344","DOI":"10.1016\/j.annonc.2023.09.567","volume":"34","author":"EP Hamilton","year":"2023","unstructured":"Hamilton EP, Han H, Schott A, Tan A, Nanda R, Juric D, Hunter N, Munster P, Fang B, Zahrah G, Ranciato J, Gedrich R, Zhi E, Zhang Y, Tan W, Mather C, Perkins J, Anderson S, Hurvitz SA (2023) 390P Vepdegestrant, a proteolysis targeting chimera (PROTAC) estrogen receptor (ER) degrader, in ER+\/human epidermal growth factor receptor 2 (HER2)- advanced breast cancer: update of dose escalation results from a phase I\/II trial. Ann Oncol 34:S344. https:\/\/doi.org\/10.1016\/j.annonc.2023.09.567","journal-title":"Ann Oncol"},{"key":"4921_CR17","doi-asserted-by":"publisher","first-page":"72","DOI":"10.1007\/s10147-024-02648-3","volume":"30","author":"H Iwata","year":"2025","unstructured":"Iwata H, Naito Y, Hattori M, Yoshimura A, Yonemori K, Aizawa M, Mori Y, Yoshimitsu J, Umeyama Y, Mukohara T (2025) Safety and pharmacokinetics of vepdegestrant in Japanese patients with ER+ advanced breast cancer: a phase 1 study. Int J Clin Oncol 30:72\u201382. https:\/\/doi.org\/10.1007\/s10147-024-02648-3","journal-title":"Int J Clin Oncol"},{"key":"4921_CR18","doi-asserted-by":"publisher","first-page":"2447","DOI":"10.1080\/14796694.2024.2377530","volume":"20","author":"EP Hamilton","year":"2024","unstructured":"Hamilton EP, Ma C, De Laurentiis M, Iwata H, Hurvitz SA, Wander SA, Danso M, Lu DR, Perkins Smith J, Liu Y, Tran L, Anderson S, Campone M (2024) VERITAC-2: a phase III study of vepdegestrant, a PROTAC ER degrader, versus fulvestrant in ER+\/HER2- advanced breast cancer. Future Oncol 20:2447\u20132455. https:\/\/doi.org\/10.1080\/14796694.2024.2377530","journal-title":"Future Oncol"},{"key":"4921_CR19","doi-asserted-by":"publisher","first-page":"PO3","DOI":"10.1158\/1538-7445.SABCS23-PO3-05-08","volume":"84","author":"S Hurvitz","year":"2024","unstructured":"Hurvitz S, Schott A, Ma C, Nanda R, Zahrah G, Hunter N, Tan A, Telli M, Anampa Mesias J, Jeselsohn R, Munster P, Zhi E, Duperret E, Mather C, Hamilton E, Han H (2024) Updated results from VERITAC evaluating vepdegestrant, a PROteolysis TArgeting Chimera (PROTAC) estrogen receptor (ER) degrader, in ER\u2013positive\/human epidermal growth factor receptor 2 (HER2)\u2013negative advanced breast cancer. Cancer Res 84:PO3\u201305. https:\/\/doi.org\/10.1158\/1538-7445.SABCS23-PO3-05-08","journal-title":"Cancer Res"},{"key":"4921_CR20","doi-asserted-by":"publisher","first-page":"556","DOI":"10.1056\/NEJMoa2505725","volume":"393","author":"M Campone","year":"2025","unstructured":"Campone M, De Laurentiis M, Jhaveri K, Hu X, Ladoire S, Patsouris A, Zamagni C, Cui J, Cazzaniga M, Cil T, Jerzak KJ, Fuentes C, Yoshinami T, Rodriguez-Lescure A, Sezer A, Fontana A, Guarneri V, Molckovsky A, Mouret-Reynier M-A, Demirci U, Zhang Y, Valota O, Lu DR, Martignoni M, Parameswaran J, Zhi X, Hamilton EP (2025) Vepdegestrant, a PROTAC estrogen receptor degrader, in advanced breast cancer. N Engl J Med 393:556\u2013568. https:\/\/doi.org\/10.1056\/NEJMoa2505725","journal-title":"N Engl J Med"},{"key":"4921_CR21","doi-asserted-by":"publisher","unstructured":"Hamilton EP, Han H, Schott A, Tan A, Nanda R, Juric D, Hunter N, Munster P, Fang B, Zahrah G, Ranciato J, Gedrich R, Zhi E, Zhang Y, Tan W, Mather C, Perkins J, Anderson S, Hurvitz SA. Vepdegestrant, a proteolysis targeting chimera (PROTAC) estrogen receptor (ER) degrader, in ER+\/human epidermal growth factor receptor 2 (HER2)- advanced breast cancer: update of dose escalation results from a phase I\/II trial. Ann Oncol. 2023;34(suppl 2):S344. https:\/\/doi.org\/10.1016\/j.annonc.2023.09.567","DOI":"10.1016\/j.annonc.2023.09.567"}],"container-title":["Cancer Chemotherapy and Pharmacology"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/link.springer.com\/content\/pdf\/10.1007\/s00280-026-04921-w.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/link.springer.com\/article\/10.1007\/s00280-026-04921-w","content-type":"text\/html","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/link.springer.com\/content\/pdf\/10.1007\/s00280-026-04921-w.pdf","content-type":"application\/pdf","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2026,8,13]],"date-time":"2026-08-13T06:20:08Z","timestamp":1786602008000},"score":1,"resource":{"primary":{"URL":"https:\/\/link.springer.com\/10.1007\/s00280-026-04921-w"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2026,8,13]]},"references-count":21,"journal-issue":{"issue":"1","published-online":{"date-parts":[[2026,12]]}},"alternative-id":["4921"],"URL":"https:\/\/doi.org\/10.1007\/s00280-026-04921-w","relation":{},"ISSN":["1432-0843"],"issn-type":[{"value":"1432-0843","type":"electronic"}],"subject":[],"published":{"date-parts":[[2026,8,13]]},"assertion":[{"value":"11 September 2025","order":1,"name":"received","label":"Received","group":{"name":"ArticleHistory","label":"Article History"}},{"value":"29 June 2026","order":2,"name":"accepted","label":"Accepted","group":{"name":"ArticleHistory","label":"Article History"}},{"value":"13 August 2026","order":3,"name":"first_online","label":"First Online","group":{"name":"ArticleHistory","label":"Article History"}},{"value":"This trial was conducted in accordance with principles derived from international guidelines, including the Declaration of Helsinki, Council for International Organizations of Medical Sciences, International Ethical Guidelines, International Council for Harmonisation Good Clinical Practice Guidelines, and other applicable laws and regulations, including privacy laws. The trial protocol and other relevant documents were approved by an institutional review board before the initiation of the study, and all patients provided written informed consent.","order":1,"name":"Ethics","label":"Ethics approval and consent to participate","group":{"name":"EthicsHeading","label":"Declarations"}},{"value":"BX reports personal advisory fees from AstraZeneca and Novartis, outside the submitted work. YC, JY, PZ, WW, LZ, and XZ report no competing interests. FG, NC, HZ, and CF are employees of Pfizer (China) R&D Co., Ltd.","order":2,"name":"Ethics","label":"Competing interests","group":{"name":"EthicsHeading","label":"Declarations"}}],"article-number":"90"}}