– Promising findings featuring XL092,
Exelixis’ next-generation oral tyrosine kinase inhibitor, recently
presented at the 32nd EORTC-NCI-AACR (ENA) Symposium –
Exelixis, Inc. (NASDAQ: EXEL) today announced enrollment of the
first patient into the dose-escalation cohort of the combination
arm of the phase 1 trial (NCT03845166) evaluating the safety,
tolerability, pharmacokinetics and preliminary anti-tumor activity
of XL092 alone and in combination with atezolizumab (TECENTRIQ®) in
patients with advanced solid tumors. XL092 is an investigational,
next-generation oral tyrosine kinase inhibitor that targets VEGF
receptors, MET, AXL, MER and other kinases implicated in the growth
and spread of cancer.
“This exciting update follows promising preclinical findings
presented at the ENA Symposium suggesting that XL092, like
cabozantinib, promotes an immune-permissive environment that may
result in synergies with immune checkpoint inhibitors; however, as
seen in the ongoing phase 1 study, XL092 has a much shorter
pharmacokinetic half-life that may help physicians in managing
tolerability,” said Gisela Schwab, M.D., President, Product
Development and Medical Affairs and Chief Medical Officer,
Exelixis. “Enrolling the first patient into the combination therapy
part of this trial is an important step forward in the development
of XL092 as we explore how it may improve outcomes for patients
with difficult-to-treat cancers and build on the success of our
cabozantinib oncology franchise.”
Initiated in February 2019, the dose-escalation evaluation of
the XL092 monotherapy arm of the phase 1 trial is ongoing. Once the
recommended doses of both single-agent XL092 and XL092 in
combination with atezolizumab are established, the trial will begin
to enroll expansion cohorts for patients with clear cell and
non-clear cell renal cell carcinoma, hormone-receptor positive
breast cancer and metastatic castration-resistant prostate
cancer.
More information about this trial is available at
ClinicalTrials.gov.
About XL092
XL092 is a next-generation oral tyrosine kinase inhibitor that
targets VEGF receptors, MET, AXL, MER and other kinases implicated
in cancer’s growth and spread. In designing XL092, Exelixis sought
to build upon the experience and target profile of cabozantinib,
the company’s flagship medicine, while improving key
characteristics, including clinical half-life. XL092 is the first
internally discovered Exelixis compound to enter the clinic
following the company’s reinitiation of drug discovery
activities.
About CABOMETYX® (cabozantinib)
In the U.S., CABOMETYX tablets are approved for the treatment of
patients with advanced RCC and for the treatment of patients with
HCC who have been previously treated with sorafenib. CABOMETYX
tablets have also received regulatory approvals in the European
Union, Japan and additional countries and regions worldwide. In
2016, Exelixis granted Ipsen exclusive rights for the
commercialization and further clinical development of cabozantinib
outside of the United States and Japan. In 2017, Exelixis granted
exclusive rights to Takeda Pharmaceutical Company Limited for the
commercialization and further clinical development of cabozantinib
for all future indications in Japan. Exelixis holds the exclusive
rights to develop and commercialize cabozantinib in the United
States.
Important Safety Information
Warnings and Precautions
Hemorrhage: Severe and fatal hemorrhages occurred with
CABOMETYX. The incidence of Grade 3 to 5 hemorrhagic events was 5%
in CABOMETYX patients in RCC and HCC studies. Discontinue CABOMETYX
for Grade 3 or 4 hemorrhage. Do not administer CABOMETYX to
patients who have a recent history of hemorrhage, including
hemoptysis, hematemesis, or melena.
Perforations and Fistulas: Gastrointestinal (GI)
perforations, including fatal cases, occurred in 1% of CABOMETYX
patients. Fistulas, including fatal cases, occurred in 1% of
CABOMETYX patients. Monitor patients for signs and symptoms of
perforations and fistulas, including abscess and sepsis.
Discontinue CABOMETYX in patients who experience a Grade 4 fistula
or a GI perforation.
Thrombotic Events: CABOMETYX increased the risk of
thrombotic events. Venous thromboembolism occurred in 7% (including
4% pulmonary embolism) and arterial thromboembolism in 2% of
CABOMETYX patients. Fatal thrombotic events occurred in CABOMETYX
patients. Discontinue CABOMETYX in patients who develop an acute
myocardial infarction or serious arterial or venous thromboembolic
event requiring medical intervention.
Hypertension and Hypertensive Crisis: CABOMETYX can cause
hypertension, including hypertensive crisis. Hypertension occurred
in 36% (17% Grade 3 and <1% Grade 4) of CABOMETYX patients. Do
not initiate CABOMETYX in patients with uncontrolled hypertension.
Monitor blood pressure regularly during CABOMETYX treatment.
Withhold CABOMETYX for hypertension that is not adequately
controlled with medical management; when controlled, resume at a
reduced dose. Discontinue CABOMETYX for severe hypertension that
cannot be controlled with anti-hypertensive therapy or for
hypertensive crisis.
Diarrhea: Diarrhea occurred in 63% of CABOMETYX patients.
Grade 3 diarrhea occurred in 11% of CABOMETYX patients. Withhold
CABOMETYX until improvement to Grade 1 and resume at a reduced dose
for intolerable Grade 2 diarrhea, Grade 3 diarrhea that cannot be
managed with standard antidiarrheal treatments, or Grade 4
diarrhea.
Palmar-Plantar Erythrodysesthesia (PPE): PPE occurred in
44% of CABOMETYX patients. Grade 3 PPE occurred in 13% of CABOMETYX
patients. Withhold CABOMETYX until improvement to Grade 1 and
resume at a reduced dose for intolerable Grade 2 PPE or Grade 3
PPE.
Proteinuria: Proteinuria occurred in 7% of CABOMETYX
patients. Monitor urine protein regularly during CABOMETYX
treatment. Discontinue CABOMETYX in patients who develop nephrotic
syndrome.
Osteonecrosis of the Jaw (ONJ): ONJ occurred in <1% of
CABOMETYX patients. ONJ can manifest as jaw pain, osteomyelitis,
osteitis, bone erosion, tooth or periodontal infection, toothache,
gingival ulceration or erosion, persistent jaw pain, or slow
healing of the mouth or jaw after dental surgery. Perform an oral
examination prior to CABOMETYX initiation and periodically during
treatment. Advise patients regarding good oral hygiene practices.
Withhold CABOMETYX for at least 3 weeks prior to scheduled dental
surgery or invasive dental procedures, if possible. Withhold
CABOMETYX for development of ONJ until complete resolution.
Impaired Wound Healing: Wound complications occurred with
CABOMETYX. Withhold CABOMETYX for at least 3 weeks prior to
elective surgery. Do not administer CABOMETYX for at least 2 weeks
after major surgery and until adequate wound healing is observed.
The safety of resumption of CABOMETYX after resolution of wound
healing complications has not been established.
Reversible Posterior Leukoencephalopathy Syndrome (RPLS):
RPLS, a syndrome of subcortical vasogenic edema diagnosed by
characteristic findings on MRI, can occur with CABOMETYX. Evaluate
for RPLS in patients presenting with seizures, headache, visual
disturbances, confusion, or altered mental function. Discontinue
CABOMETYX in patients who develop RPLS.
Embryo-Fetal Toxicity: CABOMETYX can cause fetal harm.
Advise pregnant women and females of reproductive potential of the
potential risk to a fetus. Verify the pregnancy status of females
of reproductive potential prior to initiating CABOMETYX and advise
them to use effective contraception during treatment and for 4
months after the last dose.
Adverse Reactions
The most commonly reported (≥25%) adverse reactions are:
diarrhea, fatigue, decreased appetite, PPE, nausea, hypertension,
and vomiting.
Drug Interactions
Strong CYP3A4 Inhibitors: If coadministration with strong
CYP3A4 inhibitors cannot be avoided, reduce the CABOMETYX dosage.
Avoid grapefruit or grapefruit juice.
Strong CYP3A4 Inducers: If coadministration with strong
CYP3A4 inducers cannot be avoided, increase the CABOMETYX dosage.
Avoid St. John’s wort.
USE IN SPECIFIC POPULATIONS
Lactation: Advise women not to breastfeed during
CABOMETYX treatment and for 4 months after the final dose.
Hepatic Impairment: In patients with moderate hepatic
impairment, reduce the CABOMETYX dosage. CABOMETYX is not
recommended for use in patients with severe hepatic impairment.
Please see accompanying full Prescribing Information
https://cabometyx.com/downloads/CABOMETYXUSPI.pdf.
About Exelixis
Founded in 1994, Exelixis, Inc. (Nasdaq: EXEL) is a commercially
successful, oncology-focused biotechnology company that strives to
accelerate the discovery, development and commercialization of new
medicines for difficult-to-treat cancers. Following early work in
model system genetics, we established a broad drug discovery and
development platform that has served as the foundation for our
continued efforts to bring new cancer therapies to patients in
need. Our discovery efforts have resulted in four commercially
available products, CABOMETYX® (cabozantinib), COMETRIQ®
(cabozantinib), COTELLIC® (cobimetinib) and MINNEBRO®
(esaxerenone), and we have entered into partnerships with leading
pharmaceutical companies to bring these important medicines to
patients worldwide. Supported by revenues from our marketed
products and collaborations, we are committed to prudently
reinvesting in our business to maximize the potential of our
pipeline. We are supplementing our existing therapeutic assets with
targeted business development activities and internal drug
discovery — all to deliver the next generation of Exelixis
medicines and help patients recover stronger and live longer.
Exelixis is a member of the Standard & Poor’s (S&P) MidCap
400 index, which measures the performance of profitable mid-sized
companies. For more information about Exelixis, please visit
www.exelixis.com, follow @ExelixisInc on Twitter or like Exelixis,
Inc. on Facebook.
Forward-Looking Statements
This press release contains forward-looking statements,
including, without limitation, statements related to: Exelixis’
belief that the immune-permissive environment promoted by XL092 may
result in synergies with immune checkpoint inhibitors and that
XL092’s shorter pharmacokinetic half-life may help physicians in
managing tolerability; the potential for XL092 to improve outcomes
for patients with difficult-to-treat cancers and build on the
success of Exelixis’ cabozantinib oncology franchise; and Exelixis’
plans to reinvest in its business to maximize the potential of the
company’s pipeline, including through targeted business development
activities and internal drug discovery. Any statements that refer
to expectations, projections or other characterizations of future
events or circumstances are forward-looking statements and 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: complexities and
the unpredictability of the regulatory review and approval
processes in the U.S. and elsewhere; Exelixis’ continuing
compliance with applicable legal and regulatory requirements; the
potential failure of XL092 or the combination of XL092 and
atezolizumab to demonstrate safety and/or efficacy in NCT03845166
and in future trials; uncertainties inherent in the product
development process; the continuing COVID-19 pandemic and its
impact on Exelixis’ research and development operations, including
Exelixis’ ability to initiate new clinical trials and clinical
trial sites, enroll clinical trial patients, conduct trials per
protocol, and conduct drug research and discovery operations and
related activities; the costs of conducting clinical trials,
including the ability or willingness of Exelixis’ collaboration
partners to invest in the resources necessary to complete the
trials; Exelixis’ dependence on third-party vendors for the
development, manufacture and supply of XL092; Exelixis’ ability to
protect its intellectual property rights; market competition;
changes in economic and business conditions; and other factors
affecting Exelixis and its development programs discussed under the
caption “Risk Factors” in Exelixis’ Quarterly Report on Form 10-Q
filed with the Securities and Exchange Commission (SEC) on August
6, 2020, and in Exelixis’ future filings with the SEC. All
forward-looking statements in this press release are based on
information available to Exelixis as of the date of this press
release, and Exelixis undertakes no obligation to update or revise
any forward-looking statements contained herein, except as required
by law.
Exelixis, the Exelixis logo, CABOMETYX,
COMETRIQ and COTELLIC are registered U.S. trademarks. MINNEBRO is a
Japanese trademark.
TECENTRIQ® (atezolizumab) is a registered
trademark of Genentech, a member of the Roche Group.
View source
version on businesswire.com: https://www.businesswire.com/news/home/20201026005160/en/
Investors Contact: Susan Hubbard EVP, Public Affairs and
Investor Relations Exelixis, Inc. (650) 837-8194
shubbard@exelixis.com
Media Contact: Lindsay Treadway Senior Director, Public
Affairs and Advocacy Relations Exelixis, Inc. (650) 837-7522
ltreadway@exelixis.com
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