By leveraging its technology platform, ACEA has discovered and developed a robust pipeline of clinical and preclinical small molecule programs for the treatment of cancer and autoimmune diseases.

|Pre-Clinical |Phase I |Phase II |Phase III

AC0010 (EGFR Inhibitor)

EGFR T790M+ (2nd Line)

EGFRmut + (1st Line)


AC0058 (BTK Inhibitor)

Autoimmune Diseases

AC0246 (Anti-microtubule)


AC0010 – EGFR Inhibitor

AC0010 is a potent, small molecule irreversible third generation tyrosine kinase inhibitor (TKI) that selectively targets mutant forms of epidermal growth factor receptor (EGFR). ACEA is developing AC0010 as a therapeutic agent to be administered orally to patients with mutant EGFR non-small cell lung cancer (NSCLC). AC0010 inhibits the gatekeeper mutation of EGFR (T790M), as well as the common activating mutations (L858R, del19), and has minimal inhibitory activity towards the wild-type (WT) receptor. The T790M mutation of the EGFR is the major cause (approximately 50-60%) of the acquired resistance after treatment with first generation EGFR TKIs such as Tarceva (erlotinib) and Iressa (gefitinib)1.

The proposed initial indication for AC0010 is for the treatment of patients with mutant EGFR NSCLC who have failed prior EGFR-directed therapy due to the emergence of the T790M mutation. ACEA is also evaluating the use of AC0010 as first-line therapy for NSCLC patients with confirmed EGFR mutational status.

For more information on our clinical trials, please visit clinicaltrials.gov.

1 – Yu HA, Arcila ME, Rekhtman N, Sima CS, Zakowski MF, Pao W, Kris MG, Miller VA, Ladanyi M, Riely GJ. Analysis of tumor specimens at the time of acquired resistance to EGFR-TKI therapy in 155 patients with EGFR-mutant lung cancers. Clin Cancer Res. 2013 Apr 15;19(8):2240-7.

AC0058 – BTK Inhibitor

AC0058 is a small molecule compound that potently, selectively and irreversibly inhibits Bruton’s tyrosine kinase (BTK) phosphorylation and downstream signals, resulting in inhibition of inflammatory cytokine production in monocytes and inhibition of lymphocyte activation (predominantly B-cell activation).

The nonclinical program has demonstrated that AC0058 has the potential to interfere with signaling functions mediated by tyrosine kinases and may be useful for controlling excessive or aberrant T- and B-cell activation in autoimmune diseases.

AC0058 was successfully evaluated in a recently completed Phase I clinical trial in the US in healthy volunteers. A total of 56 subjects participated in the 2-part study designed to evaluate the effects of AC0058 in single ascending dose and multiple ascending dose regimens. AC0058 was safe and well-tolerated at all tested doses up to 600 mg total daily dose.

Based on these encouraging results, ACEA is exploring multiple strategic paths forward for the continued global development of AC0058 for the treatment of autoimmune diseases.

For more information on our clinical trials, please visit clinicaltrials.gov.

Management and Advisors

Xiao Xu, MD, President and CEO
Co-founder, UCSF, Scripps, CDC

Li Xu, MD, Chief Medical Officer
Hengri Medicine, Pfizer, Merck

Roger (Feng) Luo, Vice President, Global Clin. Dev.
Janseen, Daiichi Sankyo, BMS, Roche

Andre Basbaum, MBA, Vice President, Business Development
VentiRx, Valeant, Anadys, Pfizer

Professor Peter K. Vogt
The Scripps Research Institute, La Jolla

Chen Kaixian
President, Shanghai University of Traditional Chinese medicine, Chinese Academy of Sciences

Clinical Advisors

Tony Mok, MD
Professor, Department of Clinical Oncology at the Chinese University of Hong Kong.

Heather Wakelee, MD
Associate Professor of Medicine (Oncology) at Stanford University Medical Center

Pasi Janny, MD
Director, Lowe Center for Thoracic Oncology;
Scientific Director, Belfer Instit.ute for Applied Cancer Science; Professor of Medicine, Harvard Medical School

Dong-Wan Kim, MD
Professor, Seoul National University Hospital

Yi-Long Wu, MD
Vice President, Guangdong General Hospital & Guangdong Academy of Medical Sciences and Director of Guangdong Lung Cancer Institute;
Professor and President of CSCO

Jean-Charles Soria
Professor of Medicine and Medical Oncology at South-Paris University


Lilly Asia Ventures

Lilly Asia Ventures, founded in 2008, is dedicated to venture capital investments in the life sciences and healthcare sectors in Asia, particularly in China. Its investors include Eli Lilly & Co., a Fortune 500 company and one of the most globalized and innovative pharmaceutical companies in the world. As a leading biomedical venture fund in China, Lilly Asia Ventures provides wise capital, industry expertise, and global resources to its portfolio companies to accelerate their growth.

Lilly Asia


Founded in 2006, Qiming is a leading China venture capital firm with offices in Shanghai, Beijing, Suzhou and Hong Kong. In 2016, Qiming raised a US healthcare fund, and set up Qiming US office in Seattle. Currently Qiming manages five US Dollar funds and four RMB funds with US $2.7 billion assets under management.

Recent News

  • Connector.

    ACEA Biosciences Announces Successful Completion of Phase I Clinical Study of Novel Autoimmune Disease Drug

    ACEA Biosciences today announced the completion of its Phase 1 clinical study of AC0058, a novel irreversible Bruton’s Tyrosine Kinase (BTK) inhibitor, which is in development for the treatment of B cell-related autoimmune diseases, including rheumatoid arthritis and systemic lupus erythematosus. Fifty-six (56) healthy subjects participated in the double-blind, placebo-controlled trial, which served to evaluate AC0058’s … Read More

  • Connector.

    ACEA Biosciences Presents Efficacy and Safety Data From AC0010 Phase I/II Clinical Trial for Treatment of Advanced Non-Small Cell Lung Cancer at the WCLC 2016 Conference

    Novel EGFR tyrosine kinase inhibitor AC0010 displays high efficacy, tolerability, and safety in phase I/II clinical trials. ACEA Biosciences, Inc. presented today updated efficacy and safety data from its phase I/II dose escalation and expansion clinical trial for its lead drug candidate, AC0010, at the World Conference on Lung Cancer (WCLC) 2016 in Vienna, Austria. The purpose of the trial … Read More

  • Connector.

    ACEA Biosciences Announces Data Presentation at WCLC 2016 Conference: New AC0010 Data to Be Presented

    Clinical trial results for novel EGFR inhibitor AC0010 will be presented December 7th at World Conference on Lung Cancer. ACEA Biosciences, Inc. announced today that it will be presenting updated efficacy and safety data from its Phase I/II clinical trials for AC0010 at the World Conference on Lung Cancer 2016, taking place in Vienna, Austria December 3rd-8th. “We look forward … Read More

  • Connector.

    ACEA Biosciences Appoints Li Xu, M.D. as Chief Medical Officer

    Former Vice President and Head of the Oncology Business Unit at Jiangsu Hengrui Medicine assumes position as Chief Medical Officer at ACEA Biosciences. ACEA Biosciences Inc. (ACEA), a privately owned biotechnology company focused on pioneering cell analysis instrumentation as well as the discovery and development of novel pharmaceuticals for the treatment of chronic diseases, today announced that Dr. Li … Read More

  • Connector.

    ACEA Biosciences Announces the Successful Completion of 30 Million USD in Venture Funding

    ACEA Biosciences looks to its future with investments from Lilly Asia Ventures and Qiming Venture Partners. ACEA Biosciences, Inc., a privately held drug discovery and scientific instrumentation company, announced today that it has closed a new round of venture funding in the amount of $30 million. The funding was provided by Lilly Asia Ventures and Qiming Venture Partners. Over the … Read More

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Chief Executive Officer
Email: xxu@aceabio.com


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Vice President, Business Development
Email: abasbaum@aceabio.com



ACEA Biosciences Headquarters

6779 Mesa Ridge Rd #100
San Diego, CA 92121
Phone: 858.724.0928
Email: info@aceabio.com