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Exelixis-Discovered Compounds to Be Featured in 10 Presentations at ESMO 2017 Congress

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- CABOSUN overall survival results and independent radiology review
committee analysis of progression-free survival data to be presented
during poster discussion session on September 10 -

Exelixis,
Inc.
(NASDAQ:EXEL) today announced that data from clinical trials of
cabozantinib and cobimetinib will be the subject of 10 presentations at
the European Society for Medical Oncology (ESMO) 2017 Congress in
Madrid, September 8 – 12, 2017.

Progression-free survival by independent radiology review and updated
overall survival results from CABOSUN, a randomized phase 2 clinical
trial of cabozantinib compared with sunitinib in patients with
previously untreated advanced renal cell carcinoma (RCC), will be
presented as a late-breaking abstract in the Genitourinary Tumours,
Non-Prostate poster discussion session on Sunday, September 10. Final
data from the phase 1 study of cabozantinib in combination with
nivolumab with or without ipilimumab for the treatment of metastatic
urothelial carcinoma and other genitourinary malignancies will be
presented in the Genitourinary Tumours, Non-Prostate oral presentation
session on Saturday, September 9. Additionally, poster presentations
will detail the evaluation of cabozantinib in RCC and advanced penile
squamous cell carcinoma, and of cobimetinib in combination studies in
metastatic melanoma.

"We look forward to this year's ESMO Congress where new data from the
CABOSUN trial of cabozantinib in patients with previously untreated
advanced renal cell carcinoma will be presented, as well as the final
analysis from the study exploring cabozantinib in combination with
nivolumab and ipilimumab in genitourinary tumors, including metastatic
urothelial carcinoma," said Michael M. Morrissey, Ph.D., President and
Chief Executive Officer of Exelixis. "The slate of data featuring
Exelixis-discovered compounds demonstrates our commitment to advancing
our ongoing clinical research program to help improve care and outcomes
for patients with cancer."

Cabozantinib to be featured in eight presentations

The full schedule of cabozantinib presentations expected at the meeting
is as follows:

Oral Presentation

[846O] "Final results of a phase I study of cabozantinib (Cabo) plus
nivolumab (Nivo) and CaboNivo plus Ipilimumab (Ipi) in patients (pts)
with metastatic urothelial carcinoma (mUC) and other genitourinary (GU)
malignancies"

Dr. Rosa Nadal, Sidney Kimmel Comprehensive
Cancer Center, Johns Hopkins University, Baltimore, Maryland, USA
Session:
Genitourinary Tumours, Non-Prostate
Oral presentation Saturday,
September 9, 9:15 – 10:45 a.m. CEST, Madrid Auditorium
Note:
This is a National Cancer Institute Cancer Therapy Evaluation Program
(NCI-CTEP) study.

Poster Discussion

[LBA38] "Progression-free survival (PFS) by independent review and
updated overall survival (OS) results from Alliance A031203 trial
(CABOSUN): cabozantinib versus sunitinib as initial targeted therapy for
patients (pts) with metastatic renal cell carcinoma (mRCC)"

Dr.
Toni Choueiri, Lank Center for Genitourinary Oncology, Dana-Farber
Cancer Institute, Boston, Massachusetts, USA
Session: Genitourinary
Tumours, Non-Prostate
Poster presented Sunday, September 10, 2:45 –
4:15 p.m. CEST, Cordoba Auditorium
Note: This is an NCI-CTEP
study.

Poster Presentations

[872P] "Outcomes based on plasma biomarkers in METEOR, a randomized
phase 3 trial of cabozantinib (C) vs everolimus (E) in advanced renal
cell carcinoma (RCC)"

Dr. Thomas Powles, Barts Cancer
Institute, Cancer Research UK Experimental Cancer Medicine Centre, Queen
Mary University of London, Royal Free NHS Trust, London, England
Session:
Genitourinary Tumours, Non-Prostate
Poster presented Sunday,
September 10, 1:15 – 2:15 p.m. CEST, Hall 8

[876P] "Efficacy of cabozantinib (C) after PD-1/PD-L1 checkpoint
inhibitors in metastatic renal cell carcinoma (mRCC): the Gustave Roussy
experience"

Dr. Lisa Derosa, Gustave Roussy Institute of
Oncology, Villejuif, France
Session: Genitourinary Tumours,
Non-Prostate
Poster presented Sunday, September 10, 1:15 – 2:15
p.m. CEST, Hall 8

[891P] "Outcomes of patients with metastatic renal cell carcinoma
(mRCC) who were treated with second-line (2L) vascular endothelial
growth factor receptor tyrosine kinase inhibitors (VEGFR-TKI) after
first-line (1L) immune checkpoint inhibitor (ICI) therapy"

Dr.
A.Y. Shah, Department of Genitourinary Medical Oncology, The University
of Texas MD Anderson Cancer Center, Houston, Texas, USA
Session:
Genitourinary Tumours, Non-Prostate
Poster presented Sunday,
September 10, 1:15 – 2:15 p.m. CEST, Hall 8

[901P] "Safety and efficacy of cabozantinib for metastatic renal cell
carcinoma (mRCC): real world data from an Italian Expanded Access
Program (EAP)"

Dr. G. Procopio, Department of Medical Oncology,
Fondazione IRCCS - Istituto Nazionale dei Tumori, Milan, Italy
Session:
Genitourinary Tumours, Non-Prostate
Poster presented Sunday,
September 10, 1:15 – 2:15 p.m. CEST, Hall 8

[912P] "Cabozantinib for the treatment of patients with metastatic
variant histology renal cell carcinoma (vhRCC): a retrospective study"

Dr.
M.T. Campbell, Department of Genitourinary Medical Oncology, Division of
Cancer Medicine, The University of Texas MD Anderson Cancer Center,
Houston, Texas, USA
Session: Genitourinary Tumours, Non-Prostate
Poster
presented Sunday, September 10, 1:15 – 2:15 p.m. CEST, Hall 8

[927TiP] "Cabozantinib in patients with advanced penile squamous cell
carcinoma (PSCC): the open-label, single-arm, single-center, phase 2,
CaboPen trial"

Dr. A. Necchi, Experimental Oncology and
Molecular Medicine, Fondazione IRCCS Istituto Nazionale dei Tumori,
Milan, Italy
Session: Genitourinary Tumours, Non-Prostate
Poster
presented Sunday, September 10, 1:15 – 2:15 p.m. CEST, Hall 8

Cobimetinib to be featured in two presentations

Also at the congress, Exelixis' collaborator Genentech, a member of the
Roche Group, will present data on cobimetinib, an Exelixis-discovered
compound, in metastatic melanoma. The full schedule of cobimetinib
presentations expected at the meeting is as follows:

Poster Discussion

[1225PD] "Prognostic impact of early complete metabolic response on
FDG-PET, in BRAF V600 mutant metastatic melanoma patients treated with
combination vemurafenib & cobimetinib"

Dr. Wen Xu, Peter
MacCallum Cancer Centre, Melbourne, Australia
Session: Melanoma and
Other Skin Tumours
Poster presented Monday, September 11, 11:00
a.m. – 12:15 p.m. CEST, Pamplona Auditorium

Poster Presentation

[1241P] "Impact of duration of response (DOR) on overall survival
(OS) in patients with metastatic melanoma treated with dacarbazine
(DTIC), vemurafenib (V), or cobimetinib plus vemurafenib (C+V): a pooled
analysis"

Dr. Karl Lewis, University of Colorado Cancer Center,
Aurora, Colorado, USA
Session: Melanoma and Other Skin Tumours
Poster
presented Sunday, September 10, 1:15 – 2:15 p.m. CEST, Hall 8

About the CABOSUN Study

On May 23, 2016, Exelixis announced that CABOSUN met its primary
endpoint, demonstrating a statistically significant and clinically
meaningful improvement in PFS compared with sunitinib in patients with
advanced intermediate- or poor-risk RCC as determined by investigator
assessment. CABOSUN was conducted by The Alliance for Clinical Trials in
Oncology as part of Exelixis' collaboration with the NCI-CTEP. These
results were first presented by Dr. Toni Choueiri at the ESMO 2016
Congress, and published in the Journal of Clinical Oncology
(Choueiri, JCO, 2016).1 In June 2017, a blinded
independent radiology review committee confirmed that cabozantinib
provided a clinically meaningful and statistically significant
improvement in the primary efficacy endpoint of investigator-assessed
PFS.

CABOSUN was a randomized, open-label, active-controlled phase 2 trial
that enrolled 157 patients with advanced RCC determined to be
intermediate- or poor-risk by the IMDC criteria. Patients were
randomized 1:1 to receive cabozantinib (60 mg once daily) or sunitinib
(50 mg once daily, 4 weeks on followed by 2 weeks off). The primary
endpoint was PFS. Secondary endpoints included overall survival and
objective response rate. Eligible patients were required to have locally
advanced or metastatic clear-cell RCC, ECOG performance status 0-2 and
had to be intermediate or poor risk per the IMDC criteria (Heng, JCO,
2009).2 Prior systemic treatment for RCC was not permitted.

Please see Important Safety Information below and full U.S. prescribing
information at https://cabometyx.com/downloads/cabometyxuspi.pdf.

About Genitourinary Cancers

Genitourinary cancers are those that affect the urinary tract, bladder,
kidneys, ureter, prostate, testicles, penis or adrenal glands — parts of
the body involved in reproduction and excretion — and include renal cell
carcinoma (RCC) and urothelial carcinoma.3

The American Cancer Society's 2017 statistics cite kidney cancer as
among the top ten most commonly diagnosed forms of cancer among both men
and women in the U.S.4 Clear cell RCC is the most common type
of kidney cancer in adults.5 If detected in its early stages,
the five-year survival rate for RCC is high; for patients with advanced
or late-stage metastatic RCC, however, the five-year survival rate is
only 12 percent, with no identified cure for the disease.6
Approximately 30,000 patients in the U.S. and 68,000 globally require
treatment, and an estimated 14,000 patients in the U.S. each year are in
need of a first-line treatment for advanced kidney cancer.7

Urothelial cancers encompass carcinomas of the bladder, ureter and renal
pelvis at a ratio of 50:3:1, respectively.8 Urothelial
carcinoma occurs mainly in older people, with 90 percent of patients
aged 55 or older.9 Bladder cancer is the fourth most common
cancer in men and accounts for about five percent of all new cases of
cancer in the U.S. each year.9 In 2013, an estimated 587,426
people were living with bladder cancer in the U.S.10

About CABOMETYX® (cabozantinib)

CABOMETYX is the tablet formulation of cabozantinib. Its targets
include MET, AXL and VEGFR-1, -2 and -3. In preclinical models,
cabozantinib has been shown to inhibit the activity of these receptors,
which are involved in normal cellular function and pathologic processes
such as tumor angiogenesis, invasiveness, metastasis and drug resistance.

CABOMETYX is available in 20 mg, 40 mg or 60 mg doses. The recommended
dose is 60 mg orally, once daily.

On April 25, 2016, the FDA approved CABOMETYX tablets for the treatment
of patients with advanced RCC who have received prior anti-angiogenic
therapy. In February of 2016, Exelixis and Ipsen jointly announced an
exclusive licensing agreement for the commercialization and further
development of cabozantinib indications outside of the United States,
Canada and Japan. This agreement was amended in December of 2016 to
include commercialization rights for Ipsen in Canada. On September 9,
2016, the European Commission approved CABOMETYX tablets for the
treatment of advanced RCC in adults who have received prior vascular
endothelial growth factor (VEGF)-targeted therapy in the European Union,
Norway and Iceland. Ipsen has confirmed its intent to submit the
regulatory dossier for cabozantinib as a treatment for first-line
advanced renal cell carcinoma in the European Union in the third quarter
of 2017.

On January 30, 2017, Exelixis and Takeda Pharmaceutical Company Limited
announced an exclusive licensing agreement for the commercialization and
further clinical development of cabozantinib for all future indications
in Japan, including RCC.

CABOMEYX is not indicated for the treatment of previously untreated
advanced RCC.

U.S. Important Safety Information

Hemorrhage: Severe hemorrhage occurred with CABOMETYX. The
incidence of Grade ≥3 hemorrhagic events was 2.1% in CABOMETYX-treated
patients and 1.6% in everolimus-treated patients. Fatal hemorrhages also
occurred in the cabozantinib clinical program. Do not administer
CABOMETYX to patients that have or are at risk for severe hemorrhage.

Gastrointestinal (GI) Perforations and Fistulas: Fistulas were
reported in 1.2% (including 0.6% anal fistula) of CABOMETYX-treated
patients and 0% of everolimus-treated patients. GI perforations were
reported in 0.9% of CABOMETYX-treated patients and 0.6% of
everolimus-treated patients. Fatal perforations occurred in the
cabozantinib clinical program. Monitor patients for symptoms of fistulas
and perforations. Discontinue CABOMETYX in patients who experience a
fistula that cannot be appropriately managed or a GI perforation.

Thrombotic Events: CABOMETYX treatment results in an increased
incidence of thrombotic events. Venous thromboembolism was reported in
7.3% of CABOMETYX-treated patients and 2.5% of everolimus-treated
patients. Pulmonary embolism occurred in 3.9% of CABOMETYX-treated
patients and 0.3% of everolimus-treated patients. Events of arterial
thromboembolism were reported in 0.9% of CABOMETYX-treated patients and
0.3% of everolimus-treated patients. Fatal thrombotic events occurred in
the cabozantinib clinical program. Discontinue CABOMETYX in patients who
develop an acute myocardial infarction or any other arterial
thromboembolic complication.

Hypertension and Hypertensive Crisis: CABOMETYX treatment results
in an increased incidence of treatment-emergent hypertension.
Hypertension was reported in 37% (15% Grade ≥3) of CABOMETYX-treated
patients and 7.1% (3.1% Grade ≥3) of everolimus-treated patients.
Monitor blood pressure prior to initiation and regularly during
CABOMETYX treatment. Withhold CABOMETYX for hypertension that is not
adequately controlled with medical management; when controlled, resume
CABOMETYX at a reduced dose. Discontinue CABOMETYX for severe
hypertension that cannot be controlled with anti-hypertensive therapy.
Discontinue CABOMETYX if there is evidence of hypertensive crisis or
severe hypertension despite optimal medical management.

Diarrhea: Diarrhea occurred in 74% of patients treated with
CABOMETYX and in 28% of patients treated with everolimus. Grade 3
diarrhea occurred in 11% of CABOMETYX-treated patients and in 2% of
everolimus-treated patients. Withhold CABOMETYX in patients who develop
intolerable Grade 2 diarrhea or Grade 3-4 diarrhea that cannot be
managed with standard antidiarrheal treatments until improvement to
Grade 1; resume CABOMETYX at a reduced dose. Dose modification due to
diarrhea occurred in 26% of patients.

Palmar-Plantar Erythrodysesthesia Syndrome (PPES): Palmar-plantar
erythrodysesthesia syndrome (PPES) occurred in 42% of patients treated
with CABOMETYX and in 6% of patients treated with everolimus. Grade 3
PPES occurred in 8.2% of CABOMETYX-treated patients and in <1% of
everolimus-treated patients. Withhold CABOMETYX in patients who develop
intolerable Grade 2 PPES or Grade 3 PPES until improvement to Grade 1;
resume CABOMETYX at a reduced dose. Dose modification due to PPES
occurred in 16% of patients.

Reversible Posterior Leukoencephalopathy Syndrome (RPLS): RPLS, a
syndrome of subcortical vasogenic edema diagnosed by characteristic
finding on MRI, occurred in the cabozantinib clinical program. Perform
an evaluation for RPLS in any patient 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 when
administered to a pregnant woman. Advise pregnant women of the potential
risk to a fetus. Advise females of reproductive potential to use
effective contraception during treatment with CABOMETYX and for 4 months
after the last dose.

Adverse Reactions: The most commonly reported (≥25%) adverse
reactions are: diarrhea, fatigue, nausea, decreased appetite, PPES,
hypertension, vomiting, weight decreased, and constipation.

Drug Interactions: Strong CYP3A4 inhibitors and inducers: Reduce
the dosage of CABOMETYX if concomitant use with strong CYP3A4 inhibitors
cannot be avoided. Increase the dosage of CABOMETYX if concomitant use
with strong CYP3A4 inducers cannot be avoided.

Lactation: Advise a lactating woman not to breastfeed during
treatment with CABOMETYX and for 4 months after the final dose.

Reproductive Potential: Contraception―Advise females of
reproductive potential to use effective contraception during treatment
with CABOMETYX and for 4 months after the final dose. Infertility ―CABOMETYX
may impair fertility in females and males of reproductive potential.

Hepatic Impairment: Reduce the CABOMETYX dose in patients with
mild (Child-Pugh score [C-P] A) or moderate (C-P B) hepatic impairment.
CABOMETYX is not recommended for use in patients with severe hepatic
impairment.

Please see full Prescribing Information at https://cabometyx.com/downloads/cabometyxuspi.pdf.

About the Cobimetinib and Vemurafenib Combination

Cobimetinib is a reversible inhibitor that blocks the activity of MEK, a
protein kinase that is part of a key pathway (the RAS-RAF-MEK-ERK
pathway) that promotes cell division and survival. This pathway is
frequently activated in human cancers including melanoma, where mutation
of one of its components (BRAF) causes abnormal activation in about 50%
of cases. Tumors with BRAF mutations may develop resistance and
subsequently progress after treatment with a BRAF inhibitor. About 50%
of patients with BRAF mutation positive melanoma experience a tumor
response when treated with a BRAF inhibitor, however development of
resistance and subsequent tumor progression limits treatment benefit.
Clinical and preclinical analyses indicated that reactivation of the
MEK-ERK pathway may underlie development of resistance to BRAF
inhibitors in many progressing tumors, and that co-treatment with a BRAF
and MEK inhibitor delays the emergence of resistance in the preclinical
setting, providing the rationale for testing the combination of
vemurafenib and cobimetinib in clinical trials. The U.S. Food & Drug
Administration approved cobimetinib for the treatment of unresectable or
metastatic melanoma with a BRAF V600E or V600K mutation, in combination
with vemurafenib, in 2015. Cobimetinib is also being investigated in
combination with several investigational and approved medicines,
including an immunotherapy, in several tumor types, including non-small
cell lung cancer, colorectal cancer, triple-negative breast cancer and
melanoma.

About Exelixis

Exelixis,
Inc.
(NASDAQ:EXEL) is a biopharmaceutical company committed to the
discovery, development and commercialization of new medicines to improve
care and outcomes for people with cancer. Since its founding in 1994,
three products discovered at Exelixis have progressed through clinical
development, received regulatory approval, and entered the marketplace.
Two are derived from cabozantinib, an inhibitor of multiple tyrosine
kinases including VEGF, MET, AXL and RET receptors: CABOMETYX®
tablets approved for previously treated advanced renal cell carcinoma
and COMETRIQ® capsules approved for progressive, metastatic
medullary thyroid cancer. The third product, COTELLIC®, is a
formulation of cobimetinib, a reversible inhibitor of MEK, is marketed
under a collaboration with Genentech (a member of the Roche Group), and
is approved as part of a combination regimen to treat advanced melanoma.
Both cabozantinib and cobimetinib have shown potential in a variety of
forms of cancer and are the subjects of broad clinical development
programs. For more information about Exelixis, please visit www.exelixis.com
or follow @ExelixisInc on Twitter.

Forward-Looking Statement Disclaimer

This press release contains forward-looking statements, including,
without limitation, statements related to: future data presentations
from clinical trials of cabozantinib and cobimetinib at ESMO; Exelixis'
commitment to advancing the company's ongoing clinical research program
to help improve care and outcomes for patients with cancer; Ipsen's
confirmation of its intent to submit the regulatory dossier for
cabozantinib as a treatment for first-line advanced RCC in the European
Union in the third quarter of 2017; and the therapeutic potential and
continued development of both cabozantinib and cobimetinib. Words such
as "will," "look forward," "commitment," "intent," "potential," 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: the availability of data at the referenced times; Exelixis'
ability to conduct clinical trials of cabozantinib sufficient to achieve
a positive completion; risks related to the potential failure of
cabozantinib or cobimetinib to demonstrate safety and efficacy in
clinical testing; risks and uncertainties related to regulatory review
and approval processes; 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; Exelixis' dependence on its relationship with
Genentech with respect to the development of cobimetinib; 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 May 1, 2017, 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.

References:

1. Choueiri, T.K., et al. Cabozantinib Versus Sunitinib As
Initial Targeted Therapy for Patients With Metastatic Renal Cell
Carcinoma of Poor or Intermediate Risk: The Alliance A031203 CABOSUN
Trial. Journal of Clinical Oncology. 2016; 35:6, 591-597.

2. Heng D.Y., Xie W., Regan M.M., et al. Prognostic factors for overall
survival in patients with metastatic renal cell carcinoma treated with
vascular endothelial growth factor-targeted agents: Results from a
large, multicenter study. Journal of Clinical Oncology. 2009;
27:5794-5799.

3. The University of Arizona Cancer Center. What are genitourinary
cancers? http://uacc.arizona.edu/patients/clinic/gucancer/what-are-gu-cancers.
Accessed August 2017.

4. American Cancer Society. Cancer Facts & Figures 2017. Atlanta:
American Cancer Society; 2017.

5. Jonasch, E., Gao, J., Rathmell, W., Renal cell carcinoma. BMJ. 2014;
349:g4797.

6. Ko, J. , Choueiri, T., et al. First-, second- third-line therapy for
mRCC: benchmarks for trial design from the IMDC. British Journal of
Cancer.
2014; 110:1917-1922.

7. Decision Resources Report: Renal Cell Carcinoma. October 2014
(internal data on file).

8. Hurwitz, M. et al. Urothelial and Kidney Cancers. Cancer Management. http://www.cancernetwork.com/cancer-management/urothelial-and-kidney-cancers.
Accessed August 2017.

9. American Cancer Society. Bladder Cancer Key Statistics. http://www.cancer.org/cancer/bladdercancer/detailedguide/bladder-cancer-key-statistics.
Accessed August 2017.

10. National Cancer Institute. SEER Stat Fact Sheets: Bladder Cancer. http://seer.cancer.gov/statfacts/html/urinb.html.
Accessed August 2017.

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