Fujifilm Begins U.S. Clinical Phase 2a Study of FF-10832 in Combination with KEYTRUDA® (pembrolizumab, Merck & Co., Inc., Rahway, N.J., U.S.A.) for Patients with Advanced Solid Tumors

TOKYO ― FUJIFILM Corporation (President and CEO, Representative Director: Teiichi Goto) today announced that it has begun implementation of a phase 2a study in the U.S. to evaluate safety, tolerability, and preliminary efficacy of FF-10832, a liposomal drug candidate, in combination therapy with Merck & Co., Inc., Rahway, N.J., U.S.A.’s anti-PD-1 therapy KEYTRUDA^® (pembrolizumab) for patients with advanced solid tumors.

FF-10832 is a liposomal formulation which encapsulates gemcitabine^*1, an approved anti-cancer agent indicated for the treatment of a variety of solid tumors. The primary focus of the trial is to establish the safety and tolerability of FF-10832 in combination with KEYTRUDA in patients with advanced solid tumors, and evaluate its preliminary efficacy in non-small cell lung cancer (NSCLC)*² and urothelial cancer (UC)*³ patients who have progressed after standard therapy, including immune checkpoint inhibitor therapy. This trial will enroll up to 100 patients in two indications (UC and NSCLC) into one of two treatment arms (monotherapy or in combination with KEYTRUDA). Fujifilm has completed the phase 1 dose escalation of FF-10832 monotherapy, and is currently conducting an expansion phase.

FF-10832 is administered as an intravenous infusion. It consists of liposomes, artificially constructed lipid vesicles that resemble biological membranes in composition and physical properties, encapsulating gemcitabine. Encapsulating a therapeutic agent in liposomes is believed to enhance pharmacological efficacy of that agent by prolonging its circulation and improving delivery of it specifically at the tumor site. An exploratory endpoint of the clinical phase 2a study is to determine whether encapsulating gemcitabine in liposomes enhances pharmacological efficacy.

“Fujifilm is harnessing its advanced nano-dispersion technology, analysis technology, and process technology cultivated through the photographic film business to promote the research and development of nanoparticle carriers such as liposomes and lipid nanoparticles (LNPs)*⁴. Fujifilm is focused on the development of liposomes/LNPs to meet unmet medical needs, including hard-to-treat cancers such as advanced solid tumors,” said Junji Okada, general manager of pharmaceutical products division, FUJIFILM Corporation.

Preclinical studies have demonstrated that the combination*⁵ of FF-10832 and immune checkpoint inhibitors impact CD8-positive T cells*⁶ and may lead to longer survival compared to monotherapy^*7. KEYTRUDA is an anti-PD-1 immune checkpoint inhibitor therapy.

KEYTRUDA^® is a registered trademark of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc., Rahway, NJ, USA.

Subject to the outcome of clinical studies of specific liposome-drug combinations, including the clinical phase 2a study, liposomes are believed to be capable of delivering active ingredients to tumor sites.

Investigational Use Only: Not For Sale in the United States.

^{*1:  An antimetabolite cytotoxic agent developed by Eli Lilly and Company (generic name: gemcitabine; brand name: Gemzar). It is registered in the US for the treatment of various cancers.}

^{*2: Cancer of the lung which is not of the small cell carcinoma type. The most common types of NSCLC are adenocarcinoma, squamous cell carcinoma, and large cell undifferentiated carcinoma.}

^{*3: Cancer that begins in urothelial cells that line the urethra, bladder, ureters, renal pelvis, and other related organs.}

^{*4: A nanoparticle that is composed by using, as a primary ingredient, phospholipid, etc., an organic component of cell membranes and biomembranes}

^{*5: Combined administration of FF-10832 and anti-CTLA-4 antibody and PD-1 antibody. Tumor cells can evade attack by cells of the immune system by sending an “off” signal that prevents immune cell activation. Anti-CTLA-4 and anti-PD-1 antibodies are immune checkpoint inhibitors that block proteins like CTLA-4 and PD-1 from binding with their partners, preventing the “off” signal to be sent and ultimately allowing for the activation of immune cells that can now recognize and attack cancer cells.}

^{*6: A subtype of T cells of the immune system that attack aberrant cells, such as cancer cells, infected cells (particularly with   viruses), or cells that are damaged in another way.}

^{*7: A poster presentation at the American Association of Cancer Research (AACR) 2019 annual meeting (#3953).}