-- Daiichi Sankyo-sponsored development program includes phase 3
pivotal trial in Japanese hypertensive patients and six supportive
studies –
-- Enrollment of first patient in phase 3 pivotal trial triggers $15
million milestone payment to Exelixis --
SOUTH SAN FRANCISCO, Calif.--(BUSINESS WIRE)--Sep. 26, 2016--
Exelixis, Inc. (NASDAQ:EXEL) today announced that its partner Daiichi
Sankyo Company, Limited (hereafter, Daiichi Sankyo) has initiated a
phase 3 pivotal trial to evaluate CS-3150 (esaxerenone (r-INN)), an
oral, non-steroidal, selective mineralocorticoid receptor antagonist, as
a treatment for essential hypertension in Japanese patients. As a result
of Daiichi Sankyo enrolling the first patient in the program’s phase 3
pivotal trial, Exelixis is eligible for a $15 million milestone payment,
which it expects to receive in the fourth quarter of 2016.
In March 2006, Daiichi Sankyo and Exelixis entered into a research
collaboration agreement to discover, develop and commercialize novel
therapies targeting the mineralocorticoid receptor. Under the terms of
the agreement, Daiichi Sankyo has exclusive global development,
manufacturing, and commercialization rights for the compounds. CS-3150
is one of the compounds identified during the research collaboration,
and has subsequently been developed by Daiichi Sankyo.
The ESAX-HTN phase 3 pivotal trial is a randomized study of CS-3150
versus eplerenone in Japanese hypertensive patients. The trial will
enroll an estimated 930 patients into three treatment arms: 2.5 mg and 5
mg doses of CS-3150, and 50 mg of eplerenone. The eighteen-week trial
includes a four week washout period, twelve week study period and two
week follow-up period. Among other inclusion criteria, to participate in
the trial patients must be classified as hypertensive with systolic
blood pressure between 140-180 mmHg, diastolic blood pressure between
90-110 mmHg and a mean 24-hour blood pressure reading greater than
130/80 mmHg. The primary objective is to evaluate the antihypertensive
effect and safety of CS-3150 2.5 mg once daily compared to eplerenone; a
secondary objective is to evaluate the effectiveness of the 2.5 and 5 mg
doses of CS-3150.
In addition to ESAX-HTN, Daiichi Sankyo is sponsoring six smaller phase
3 clinical trials of CS-3150 in specific populations of patients with
hypertension, either as monotherapy or in combination with other
therapies used to treat the condition. The largest of these trials,
Study J302, has been active since March 2016 and is a long-term,
open-label study to evaluate the efficacy and safety of CS-3150 in 360
patients with essential hypertension, including forms that
cannot be controlled by angiotensin II receptor blockers (ARB) or
angiotensin converting enzyme (ACE) inhibitors. Another study in the
program, J306, will evaluate the efficacy and safety of CS-3150 as an
add-on to ARB or ACE inhibitor therapy in patients with hypertension and
type 2 diabetes with albuminuria, a population for whom eplerenone is
contraindicated. For more information on the clinical trial program,
please visit http://www.clinicaltrials.gov.
“We are pleased to see our partner Daiichi Sankyo continue to advance
CS-3150 through clinical development and into a well designed phase 3
pivotal trial in Japanese patients with essential hypertension,” said
Michael M. Morrissey, Ph.D., president and chief executive officer of
Exelixis. “While our strategic partners devote their time and resources
to progressing out-licensed Exelixis-discovered compounds, our internal
team is focused on continuing to build a global franchise for
cabozantinib and participating meaningfully in the commercialization of
cobimetinib in the United States.”
Daiichi Sankyo’s decision to take CS-3150 into phase 3 clinical
development was guided by results from multiple phase 2 trials,
including data from a randomized, placebo-controlled double-blind trial
evaluating doses of CS-3150, and open-label eplerenone in 400 patients
with hypertension. Daiichi Sankyo is currently reviewing those data in
advance of potential submission for publication or presentation at a
scientific forum later this year.
About Hypertension in Japan1
According to the 2012 Japan National Health and Nutrition Survey, there
are an estimated 43 million patients with hypertension in the country,
which accounts for 60% of men and 45% of women over the age of 30 in the
general Japanese population.1 Just 30% of men and 40% of
women with hypertension and treatment with antihypertensive medication
typically achieve the goal of systolic and diastolic blood pressure
lower than 140/90mm Hg.
Hypertension is one of the major risk factors for cardiovascular disease
such as stroke and coronary heart disease, and the condition also raises
the risk of chronic kidney disease and end-stage renal disease.
Essential hypertension is the most common form of hypertension and has
heterogeneous factors such as genetics and lifestyle habits, while
secondary hypertension is associated with underlying disease factors.
Essential hypertension is the most common form of hypertension,
affecting 90% of hypertensive patients.
About CS-3150 (esaxerenone (r-INN))
CS-3150 (esaxerenone (r-INN)) is an oral, non-steroidal, selective
antagonist of the mineralocorticoid receptor (MR), a nuclear hormone
receptor implicated in a variety of cardiovascular and metabolic
diseases. MR antagonists can be used to treat hypertension and
congestive heart failure due to their vascular protective effects.
Recent studies have also shown beneficial effects of adding MR
antagonists to the treatment regimen for Type 2 diabetic patients with
nephropathy. As a non-steroidal, selective MR antagonist, CS-3150 may
have potential for the treatment of hypertension, diabetic nephropathy
and congestive heart failure, and may provide protection from end organ
damage due to vascular complications.
CS-3150 is one of the compounds identified during Exelixis’ research
collaboration with Daiichi Sankyo, which the companies entered into in
March 2006. Under the terms of the agreement, Exelixis granted Daiichi
Sankyo an exclusive, worldwide license to certain intellectual property
primarily relating to compounds that modulate MR. In exchange, Exelixis
received a $20 million upfront payment, research funding for a joint
research period, and the potential for substantial clinical development,
regulatory and commercialization milestone payments, as well as
double-digit royalties on sales. Since the conclusion of the joint
research period in November 2007, Daiichi Sankyo has been responsible
for all subsequent preclinical and clinical development, and will also
oversee regulatory, manufacturing and commercialization activities for
the compound.
About Exelixis
Exelixis, Inc. (NASDAQ:EXEL) is a biopharmaceutical company committed to
the discovery, development and commercialization of new medicines with
the potential to improve care and outcomes for people with cancer. Since
its founding in 1994, three medicines discovered at Exelixis have
progressed through clinical development to receive regulatory approval.
Currently, Exelixis is focused on advancing cabozantinib, an inhibitor
of multiple tyrosine kinases including MET, AXL and VEGF receptors,
which has shown clinical anti-tumor activity in more than 20 forms of
cancer and is the subject of a broad clinical development program. Two
separate formulations of cabozantinib have received regulatory approval
to treat certain forms of kidney and thyroid cancer and are marketed for
those purposes as CABOMETYX™ tablets (U.S. and EU) and COMETRIQ®
capsules (U.S. and EU), respectively. Another Exelixis-discovered
compound, COTELLIC® (cobimetinib), a selective inhibitor of
MEK, has been approved in major territories including the United States
and European Union, and is being evaluated for further potential
indications by Roche and Genentech (a member of the Roche Group) under a
collaboration with Exelixis. For more information on Exelixis, please
visit www.exelixis.com
or follow @ExelixisInc
on Twitter.
Forward-Looking Statements
This press release contains forward-looking statements, including,
without limitation, statements related to: Exelixis’ eligibility for a
$15 million milestone payment from Daiichi Sankyo and the expectation
that it will be received in the fourth quarter of 2016; Exelixis’ focus
on continuing to build a global franchise for cabozantinib and
participating meaningfully in the commercialization of cobimetinib in
the United States; the therapeutic potential of CS-3150 for the
treatment of hypertension, diabetic nephropathy and congestive heart
failure, and for protection from end organ damage due to vascular
complications; Exelixis' commitment to the discovery, development and
commercialization of new medicines with the potential to improve care
and outcomes for people with cancer; Exelixis’ focus on advancing
cabozantinib; and the continued development of cobimetinib. Words such
as “eligible,” “expects,” “may,” “potential,” “committed,” “focused,” or
other similar expressions identify forward-looking statements, but the
absence of these words does not necessarily mean that a statement is not
forward-looking. In addition, any statements that refer to expectations,
projections or other characterizations of future events or circumstances
are forward-looking statements. These forward-looking statements are
based upon Exelixis’ current plans, assumptions, beliefs, expectations,
estimates and projections. Forward-looking statements involve risks and
uncertainties. Actual results and the timing of events could differ
materially from those anticipated in the forward-looking statements as a
result of these risks and uncertainties, which include, without
limitation: risks related to the potential failure of CS-3150 to
demonstrate safety and efficacy in clinical testing; Exelixis’
dependence on its relationship with Daiichi Sanyo with respect to
CS-3150 and Exelixis’ ability to maintain its rights under the
collaboration; the degree of market acceptance of CABOMETYX and the
availability of coverage and reimbursement for CABOMETYX; the risk that
unanticipated developments could adversely affect the commercialization
of CABOMETYX; Exelixis’ dependence on its relationship with Ipsen,
including, the level of Ipsen’s investment in the resources necessary to
successfully commercialize cabozantinib in the territories where it is
approved; risks and uncertainties related to regulatory review and
approval processes and Exelixis’ compliance with applicable legal and
regulatory requirements; Exelixis’ ability to conduct clinical trials of
cabozantinib sufficient to achieve a positive completion; risks related
to the potential failure of cabozantinib to demonstrate safety and
efficacy in clinical testing; Exelixis’ dependence on its relationship
with Genentech/Roche with respect to cobimetinib and Exelixis’ ability
to maintain its rights under the collaboration; Exelixis’ dependence on
third-party vendors; Exelixis’ ability to protect the company’s
intellectual property rights; market competition; changes in economic
and business conditions, and other factors discussed under the caption
“Risk Factors” in Exelixis’ quarterly report on Form 10-Q filed with the
Securities and Exchange Commission (SEC) on August 3, 2016, and in
Exelixis’ future filings with the SEC. The forward-looking statements
made in this press release speak only as of the date of this press
release. Exelixis expressly disclaims any duty, obligation or
undertaking to release publicly any updates or revisions to any
forward-looking statements contained herein to reflect any change in
Exelixis’ expectations with regard thereto or any change in events,
conditions or circumstances on which any such statements are based.
Exelixis, the Exelixis logo, COMETRIQ and COTELLIC are registered
U.S. trademarks, and CABOMETYX is a U.S. trademark.
1The Japanese Society of Hypertension Guidelines for the
Management of Hypertension (JSH 2014). Hypertens Research 2014;
37: 253-392.
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Source: Exelixis, Inc.
Exelixis, Inc.
Susan Hubbard, 650-837-8194
Investor
Relations & Public Affairs
shubbard@exelixis.com
or
For
Exelixis, Inc.
Hal Mackins, 415-994-0040
hal@torchcomllc.com