Study of Zanzalintinib in Combination With Immuno-Oncology Agents in Participants With Solid Tumors

NCT ID: NCT05176483

Last Updated: 2026-01-20

Study Results

Results pending

The study team has not published outcome measurements, participant flow, or safety data for this trial yet. Check back later for updates.

Basic Information

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Recruitment Status

ACTIVE_NOT_RECRUITING

Clinical Phase

PHASE1

Total Enrollment

1314 participants

Study Classification

INTERVENTIONAL

Study Start Date

2021-12-14

Study Completion Date

2030-06-28

Brief Summary

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This is a multicenter Phase 1b, open label, dose-escalation and cohort-expansion study, evaluating the safety, tolerability, pharmacokinetics (PK), preliminary antitumor activity, and effect of biomarkers of zanzalintinib administered alone, and in combination with nivolumab (doublet), nivolumab + ipilimumab (triplet) and nivolumab + relatlimab (triplet) in participants with advanced solid tumors.

In the Expansion Stage, the safety and efficacy of zanzalintinib as monotherapy and in combination therapy will be further evaluated in tumor-specific Expansion Cohorts.

Detailed Description

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Conditions

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Renal Cell Carcinoma (RCC) Metastatic Castration-Resistant Prostate Cancer (mCRPC) Urothelial Carcinoma (UC) Solid Tumor Hepatocellular Carcinoma (HCC) Non-small Cell Lung Cancer (NSCLC) Colorectal Cancer (CRC) Head and Neck Squamous Cell Carcinoma (HNSCC) Clear Cell Renal Cell Carcinoma (ccRCC) Non-Clear Cell Renal Cell Carcinoma (nccRCC)

Study Design

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Allocation Method

NON_RANDOMIZED

Intervention Model

SEQUENTIAL

Dose-escalation followed by expansion phase with parallel assignment.
Primary Study Purpose

TREATMENT

Blinding Strategy

NONE

Study Groups

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Zanzalintinib + Nivolumab Dose-Escalation Cohorts

Approximately 12 participants will accrue across 1-2 dose levels of Zanzalintinib following the "rolling 6" design.

Group Type EXPERIMENTAL

Zanzalintinib

Intervention Type DRUG

Zanzalintinib orally once daily (qd)

Nivolumab

Intervention Type DRUG

360 mg IV infusion once every 3 weeks (q3w)

Zanzalintinib + Nivolumab + Ipilimumab Dose-Escalation Cohorts

Approximately 12 participants will accrue across 1-2 dose levels of Zanzalintinib following the "rolling 6" design.

Group Type EXPERIMENTAL

Zanzalintinib

Intervention Type DRUG

Zanzalintinib orally once daily (qd)

Ipilimumab

Intervention Type DRUG

1 mg/kg IV infusion once every 3 weeks (q3w) for maximum of four doses

Nivolumab

Intervention Type DRUG

3 mg/kg IV infusion once every 3 weeks (q3w) for first four doses, and then 480 mg IV infusion once every 4 weeks (q4w)

Zanzalintinib + Nivolumab Expansion Cohorts

The recommended dose from the dose-escalation stage may be further explored in tumor-specific cohorts.

Group Type EXPERIMENTAL

Zanzalintinib

Intervention Type DRUG

Zanzalintinib orally once daily (qd)

Nivolumab

Intervention Type DRUG

480 mg IV infusion once every 4 weeks (q4w)

Zanzalintinib + Nivolumab + Ipilimumab Expansion Cohorts

The recommended dose from the dose-escalation stage may be further explored in tumor-specific cohorts.

Group Type EXPERIMENTAL

Zanzalintinib

Intervention Type DRUG

Zanzalintinib orally once daily (qd)

Ipilimumab

Intervention Type DRUG

1 mg/kg IV infusion once every 3 weeks (q3w) for maximum of four doses

Nivolumab

Intervention Type DRUG

3 mg/kg IV infusion once every 3 weeks (q3w) for first four doses, and then 480 mg IV infusion once every 4 weeks (q4w)

Zanzalintinib Single-Agent Expansion Cohorts

Group Type EXPERIMENTAL

Zanzalintinib

Intervention Type DRUG

Zanzalintinib orally once daily (qd)

Zanzalintinib + Nivolumab + Relatlimab Dose-Escalation Cohorts

Approximately 12 participants will accrue across 1-2 dose levels of Zanzalintinib following the "rolling 6" design.

Group Type EXPERIMENTAL

Zanzalintinib

Intervention Type DRUG

Zanzalintinib orally once daily (qd)

Nivolumab + Relatlimab

Intervention Type DRUG

IV administration of nivolumab + relatlimab

Zanzalintinib + Nivolumab + Relatlimab Expansion Cohorts

The recommended dose from the dose-escalation stage may be further explored in tumor-specific cohorts.

Group Type EXPERIMENTAL

Zanzalintinib

Intervention Type DRUG

Zanzalintinib orally once daily (qd)

Nivolumab + Relatlimab

Intervention Type DRUG

IV administration of nivolumab + relatlimab

Interventions

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Zanzalintinib

Zanzalintinib orally once daily (qd)

Intervention Type DRUG

Nivolumab

360 mg IV infusion once every 3 weeks (q3w)

Intervention Type DRUG

Ipilimumab

1 mg/kg IV infusion once every 3 weeks (q3w) for maximum of four doses

Intervention Type DRUG

Nivolumab

3 mg/kg IV infusion once every 3 weeks (q3w) for first four doses, and then 480 mg IV infusion once every 4 weeks (q4w)

Intervention Type DRUG

Nivolumab

480 mg IV infusion once every 4 weeks (q4w)

Intervention Type DRUG

Nivolumab + Relatlimab

IV administration of nivolumab + relatlimab

Intervention Type DRUG

Other Intervention Names

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XL092 Opdivo Yervoy Opdivo Opdivo

Eligibility Criteria

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Inclusion Criteria

* Cytologically or histologically confirmed solid tumor that is unresectable, locally advanced or metastatic.
* Dose-Escalation Cohorts: Participants with a solid tumor that is unresectable or metastatic and for which life-prolonging therapies do not exist or available therapies are intolerable or no longer effective.
* Expansion Cohort 1 (ccRCC): Participants with unresectable advanced or metastatic RCC with a clear cell component who have not received prior systemic therapy.

* Note: Prior non-vascular endothelial growth factor (VEGF) targeted adjuvant or neoadjuvant is allowed if disease recurrence occurred 6 months after the last dose.
* Expansion Cohort 2 (ccRCC): Participants with unresectable advanced or metastatic RCC with a clear cell component.

* Must have radiographically progressed after a combination therapy consisting of a Programmed Cell Death Protein 1 (PD-1)/Programmed death-ligand 1 (PD-L1) targeting monoclonal antibody (mAb) with a Vascular endothelial growth factor (receptor) tyrosine kinase inhibitor (VEGFR-TKI) or a PD-1 targeting mAb with a CTLA-4 mAb as the preceding line of therapy.
* Must have received no more than one prior systemic anticancer therapy for unresectable advanced or metastatic renal cell carcinoma.
* Expansion Cohort 3 (mCRPC): Men with metastatic adenocarcinoma of the prostate.

* Must have progressed during or after one novel hormone therapy (NHT) given for castration-sensitive locally advanced (T3 or T4) or metastatic castration-sensitive prostate cancer (CSPC), M0 CRPC, or mCRPC.
* Expansion Cohort 4 (UC, ICI-naive): Participants with histologically confirmed unresectable, locally advanced or metastatic transitional cell carcinoma of the urothelium (including the renal pelvis, ureter, urinary bladder, or urethra).

* Must have progressed during or after prior first-line platinum-based combination therapy, including participants who received prior neoadjuvant or adjuvant platinum-containing therapy with disease recurrence \< 12 months from the end of last therapy.
* Must have received no more than 1 prior line of systemic anticancer therapy for unresectable, locally advanced or metastatic disease.
* Expansion Cohort 5 (post enfortumab vedotin \[EV\] and ICI): Participants with histologically confirmed unresectable, locally advanced or metastatic predominant urothelial carcinoma.

* Progressive disease following prior EV or ineligible for EV, and progression following prior PD-1/PD-L1 inhibitor or ineligible for PD-1/PD-L1 inhibitor.
* Prior receipt of platinum-based therapy allowed but not required.
* Prior therapy with other agents allowed but not required.
* Expansion Cohort 6 (nccRCC): Participants with unresectable advanced or metastatic nccRCC of the following subtypes: Papillary, unclassified RCC, and translocation-associated, Fumarate Hydratase (FH) deficient and Succinate Dehydrogenase (SDH) deficient. Among the eligible histologic subtypes, sarcomatoid features are allowed.

* No prior systemic anticancer therapy is allowed except adjuvant or neoadjuvant therapy if disease recurrence occurred at least 6 months after the last dose.
* Expansion Cohort 7 (HCC): Participants with locally advanced, or metastatic and/or unresectable HCC that is not amenable to curative treatment or locoregional therapy.
* Expansion Cohort 8 (NSCLC): Participants with Stage IV non-squamous NSCLC with positive PD-L1 expression (tumor proportion score \[TPS\] 1-49%) and without prior systemic anticancer therapy for metastatic disease.
* Expansion Cohort 9 (NSCLC): Participants with Stage IV non-squamous NSCLC who have radiologically progressed following treatment with one prior immune checkpoint inhibitor (anti-PD-1 or anti-PD-L1) for metastatic disease.
* Expansion Cohort 10 (CRC): Participants with histologically confirmed unresectable, locally advanced, or metastatic adenocarcinoma of the colon or rectum.
* Expansion Cohort 11 (HNSCC): Participant with inoperable, refractory, recurrent or metastatic HNSCC of the oral cavity, oropharynx, hypopharynx, and larynx. PD-L1 combined positive score (CPS) ≥1.
* Expansion Cohort 12 (ccRCC): Participants with unresectable advance or metastatic RCC with a clear cell component, including participants who also have a sacromatoid feature.

* Must have received no more than two prior lines of systemic anticancer therapy for unresectable advanced or metastatic renal cell carcinoma
* Expansion Cohort 13 and Cohort 14 (ccRCC 1L): Participants with unresectable advanced or metastatic RCC with a clear component, including participants who also have a sacromatoid feature.
* For all Expansion Cohorts except Cohort 3: Measurable disease per RECIST 1.1 as determined by the Investigator.
* For Expansion Cohorts 1 - 11 Only: Archival tumor tissue material, if available, or fresh tumor tissue if it can be safely obtained.
* Recovery to baseline or ≤ Grade 1 common terminology criteria for adverse events (CTCAE) v5 from AE(s) related to any prior treatments unless AE(s) are deemed clinically nonsignificant by the Investigator and/or stable on supportive therapy.
* Karnofsky Performance Status (KPS) ≥ 70%.
* Adequate organ and marrow function.
* Sexually active fertile participants and their partners must agree to use highly effective methods of contraception.
* Females of childbearing potential must not be pregnant at screening.

Exclusion Criteria

* For all Dose-Escalation cohorts: Prior treatment with zanzalintinib. For all Expansion Cohorts: Prior treatment with zanzalintinib, nivolumab, ipilimumab or relatlimab with the following exceptions: Prior PD-1/PD-L1, Lymphocyte-activation gene 3 (LAG-3) and cCytotoxic T lymphocyte associated protein 4 (CTLA-4) targeting therapy for locally advanced or metastatic disease is allowed for Cohort 2 (ccRCC), Cohort 5 (UC), Cohort 9 (NSCLC), and Cohort 12 (ccRCC), and prior treatment in the neoadjuvant or adjuvant setting is allowed for Cohort 13 and Cohort 14 (ccRCC 1L).
* For all Dose-Escalation Cohorts and Expansion Cohort 2 (ccRCC), 3 (mCRPC), Cohort 5 (UC), Cohort 9 (NSCLC), Cohort 10 (CRC), and Cohort 12: Receipt of any type of small molecule kinase inhibitor (including investigational kinase inhibitor) within 2 weeks before first dose of study treatment.
* For Cohort 3 (mCRPC): Receipt of abiraterone within 1 week; cyproterone within 10 days; or receipt of flutamide, nilutamide, bicalutamide, enzalutamide, or other androgen receptor inhibitors within 2 weeks before first dose of study treatment.
* For all Dose-Escalation Cohorts and Expansion Cohort 2 (ccRCC), Cohort 3 (mCRPC), Cohort 5 (UC), Cohort 9 (NSCLC) and Cohort 10 (CRC), and Cohort 12: Receipt of any type of anticancer antibody or systemic chemotherapy within 4 weeks before first dose of study treatment.
* Any complementary medications (eg, herbal supplements or traditional Chinese medicines) to treat the disease under study within 2 weeks before first dose of study treatment.
* Prior external radiation therapy for bone metastasis within 2 weeks, for other tumor sites within 4 weeks, and prior radium-223 therapy within 6 weeks before first dose of study treatment, unless otherwise specified.
* Known brain metastases or cranial epidural disease unless adequately treated with radiotherapy and/or surgery (including radiosurgery) and stable for at least 4 weeks before first dose of study treatment.
* Concomitant anticoagulation with oral anticoagulants, except for specified direct factor Xa inhibitors.
* Administration of a live, attenuated vaccine within 30 days prior to first dose.
* Uncontrolled, significant intercurrent or recent illness.
* Corrected QT interval calculated by the Fridericia formula (QTcF) \> 460 ms for females and \> 450 ms for males per electrocardiogram (ECG) within 14 days before first dose of study treatment.
* Participants with inadequately treated adrenal insufficiency.
* Pregnant or lactating females.
* Any other active malignancy within two years before first dose of study treatment, except for superficial skin cancers, or localized, low-grade tumors deemed cured and not treated with systemic therapy. Incidentally diagnosed prostate cancer is allowed if assessed as stage ≤ T2N0M0 and Gleason score ≤ 6.
* For Cohort 2 (ccRCC, 2L): Receipt of a prior triplet therapy including a VEGFR-TKI, a PD1 targeting mAb, and a CTLA-4 mAb.
* For Cohort 3 (mCRPC): Receipt of a taxane-based chemotherapy for mCRPC.
* For Cohort 4 (UC, ICI-naïve): Participants who have had recurrence within the 6 months of completing adjuvant anti-PD-(L)1 treatment.
* For Cohort 6 (nccRCC, 1L): Participants with chromophobe, renal medullary carcinoma, or pure collecting duct nccRCC.
* For Cohort 7 (HCC):

* Documented hepatic encephalopathy (HE) within 6 months before the first dose.
* Clinically meaningful ascites (ie, ascites requiring paracentesis or escalation in diuretics) within 6 months before randomization.
* Participants who have received any local anticancer therapy including surgery, percutaneous ethanol injection (PEI), radiofrequency ablation (RFA), microwave ablation (MWA), transarterial chemoembolization (TACE), or transarterial radioembolization (TARE) within 28 days prior to first dose.
* Participants with known fibrolamellar carcinoma, sarcomatoid HCC, or mixed hepatocellular cholangiocarcinoma
* For Cohort 10 (CRC, 2L+): Receipt of prior therapy with regorafenib and/or trifluridine + tipiracil (TAS-102).
* For Cohort 11 (HNSCC): Primary tumor site of the nasopharyngeal area.
* For Cohorts 1 (ccRCC, 1L), 2 (ccRCC, 2L), 4, 5 (UC), 7 (HCC), 8 (NSCLC 1L PD-L1 low), 9 (NSCLC, 2L+), 10 (CRC, microsatellite stable \[MSS\], 2L+), and 11 (HNSCC):

* Troponin T (TnT) or I (TnI) \> 2 × institutional upper limit of normal (ULN).
Minimum Eligible Age

18 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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Exelixis

INDUSTRY

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Medical Director

Role: STUDY_DIRECTOR

Exelixis

Locations

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Exelixis Clinical Site #67

Phoenix, Arizona, United States

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Exelixis Clinical Site #1

Tucson, Arizona, United States

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Exelixis Clinical Site #123

Palo Alto, California, United States

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Exelixis Clinical Site #59

Santa Barbara, California, United States

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Exelixis Clinical Site #87

Littleton, Colorado, United States

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Exelixis Clinical Site #62

New Haven, Connecticut, United States

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Exelixis Clinical Site #49

Newark, Delaware, United States

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Exelixis Clinical Site #48

Celebration, Florida, United States

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Exelixis Clinical Site #11

Gainesville, Florida, United States

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Exelixis Clinical Site #78

Jacksonville, Florida, United States

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Exelixis Clinical Site #47

Miami, Florida, United States

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Exelixis Clinical Site #61

Plantation, Florida, United States

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Exelixis Clinical Site #8

Tampa, Florida, United States

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Exelixis Clinical Site #26

Chicago, Illinois, United States

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Exelixis Clinical Site #4

Indianapolis, Indiana, United States

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Exelixis Clinical Site #122

Louisville, Kentucky, United States

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Exelixis Clinical Site #14

Baltimore, Maryland, United States

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Exelixis Clinical Site #7

Boston, Massachusetts, United States

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Exelixis Clinical Site #65

Detroit, Michigan, United States

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Exelixis Clinical Site #13

Detroit, Michigan, United States

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Exelixis Clinical Site #68

Rochester, Minnesota, United States

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Exelixis Clinical Site #2

Omaha, Nebraska, United States

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Exelixis Clinical Site #5

Omaha, Nebraska, United States

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Exelixis Clinical Site #55

Las Vegas, Nevada, United States

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Exelixis Clinical Site #88

East Brunswick, New Jersey, United States

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Exelixis Clinical Site #105

Hackensack, New Jersey, United States

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Exelixis Clinical Site #60

New York, New York, United States

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Exelixis Clinical Site #6

New York, New York, United States

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Exelixis Clinical Site #76

Syracuse, New York, United States

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Exelixis Clinical Site #12

Durham, North Carolina, United States

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Exelixis Clinical Site #10

Cleveland, Ohio, United States

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Exelixis Clinical Site #51

Portland, Oregon, United States

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Exelixis Clinical Site #104

Hershey, Pennsylvania, United States

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Exelixis Clinical Site #98

Philadelphia, Pennsylvania, United States

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Exelixis Clinical Site #32

Pittsburgh, Pennsylvania, United States

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Exelixis Clinical Site #24

Pittsburgh, Pennsylvania, United States

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Exelixis Clinical Site #9

Myrtle Beach, South Carolina, United States

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Exelixis Clinical Site #3

Nashville, Tennessee, United States

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Exelixis Clinical Site #46

Austin, Texas, United States

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Exelixis Clinical Site #111

Dallas, Texas, United States

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Exelixis Clinical Site #89

Dallas, Texas, United States

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Exelixis Clinical Site #73

Irving, Texas, United States

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Exelixis Clinical Site #50

Plano, Texas, United States

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Exelixis Clinical Site #70

Tyler, Texas, United States

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Exelixis Clinical Site #66

Charlottesville, Virginia, United States

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Exelixis Clinical Site #33

Milwaukee, Wisconsin, United States

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Exelixis Clinical Site #116

Albury, , Australia

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Exelixis Clinical Site #35

Birtinya, , Australia

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Exelixis Clinical Site #16

Brisbane, , Australia

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Exelixis Clinical Site #42

Saint Leonards, , Australia

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Exelixis Clinical Site #36

Sydney, , Australia

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Exelixis Clinical Site #94

Graz, , Austria

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Exelixis Clinical Site #31

Salzburg, , Austria

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Exelixis Clinical Site #29

Vienna, , Austria

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Exelixis Clinical Site #106

Wein, , Austria

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Exelixis Clinical Site #39

Anderlecht, , Belgium

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Exelixis Clinical Site #37

Kortrijk, , Belgium

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Exelixis Clinical Site #85

Besançon, , France

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Exelixis Clinical Site #96

Bordeaux, , France

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Exelixis Clinical Site #79

Caen, , France

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Exelixis Clinical Site #118

Clermont-Ferrand, , France

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Exelixis Clinical Site #109

Lyon, , France

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Exelixis Clinical Site #92

Marseille, , France

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Exelixis Clinical Site #64

Nice, , France

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Exelixis Clinical Site #83

Paris, , France

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Exelixis Clinical Site #91

Paris, , France

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Exelixis Clinical Site #80

Rennes, , France

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Exelixis Clinical Site #63

Saint-Herblain, , France

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Exelixis Clinical Site #75

Strasbourg, , France

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Exelixis Clinical Site #84

Vandœuvre-lès-Nancy, , France

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Exelixis Clinical Site #115

Villejuif, , France

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Exelixis Clinical Site #103

Essen, , Germany

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Exelixis Clinical Site #113

Hamburg, , Germany

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Exelixis Clinical Site #108

Heidelberg, , Germany

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Exelixis Clinical Site #82

Herne, , Germany

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Exelixis Clinical Site #93

Jena, , Germany

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Exelixis Clinical Site #112

München, , Germany

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Exelixis Clinical Site #102

Nürtingen, , Germany

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Exelixis Clinical Site #107

Trier, , Germany

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Exelixis Clinical Site #95

Tübingen, , Germany

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Exelixis Clinical Site #86

Beersheba, , Israel

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Exelixis Clinical Site #72

Haifa, , Israel

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Exelixis Clinical Site #52

Jerusalem, , Israel

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Exelixis Clinical Site #71

Petah Tikva, , Israel

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Exelixis Clinical Site #69

Tel Aviv, , Israel

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Exelixis Clinical Site #38

Ẕerifin, , Israel

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Exelixis Clinical Site #121

Ancona, , Italy

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Exelixis Clinical Site #117

Bologna, , Italy

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Exelixis Clinical Site #90

Florence, , Italy

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Exelixis Clinical Site #101

Milan, , Italy

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Exelixis Clinical Site #81

Milan, , Italy

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Exelixis Clinical Site #40

Napoli, , Italy

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Exelixis Clinical Site #74

Ravenna, , Italy

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Exelixis Clinical Site #30

Grafton, , New Zealand

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Exelixis Clinical Site #45

Hamilton, , New Zealand

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Exelixis Clinical Site #20

Bydgoszcz, , Poland

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Exelixis Clinical Site #28

Gdansk, , Poland

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Exelixis Clinical Site #34

Otwock, , Poland

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Exelixis Clinical Site #54

Poznan, , Poland

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Exelixis Clinical Site #114

Wroclaw, , Poland

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Exelixis Clinical Site #41

Badajoz, , Spain

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Exelixis Clinical Site #53

Barcelona, , Spain

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Exelixis Clinical Site #15

Barcelona, , Spain

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Exelixis Clinical Site #27

Barcelona, , Spain

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Exelixis Clinical Site #120

L'Hospitalet de Llobregat, , Spain

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Exelixis Clinical Site #57

Madrid, , Spain

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Exelixis Clinical Site #43

Madrid, , Spain

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Exelixis Clinical Site #58

Madrid, , Spain

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Exelixis Clinical Site #77

Madrid, , Spain

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Exelixis Clinical Site #19

Madrid, , Spain

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Exelixis Clinical Site #100

Madrid, , Spain

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Exelixis Clinical Site #18

Pamplona, , Spain

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Exelixis Clinical Site #119

Santander, , Spain

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Exelixis Clinical Site #23

Seville, , Spain

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Exelixis Clinical Site #56

Valencia, , Spain

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Exelixis Clinical Site #25

Valencia, , Spain

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Exelixis Clinical Site #21

Chur, , Switzerland

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Exelixis Clinical Site #22

Sankt Gallen, , Switzerland

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Exelixis Clinical Site #44

Winterthur, , Switzerland

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Exelixis Clinical Site #110

Cambridge, , United Kingdom

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Exelixis Clinical Site #99

London, , United Kingdom

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Exelixis Clinical Site #97

Middlesex, , United Kingdom

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Countries

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United States Australia Austria Belgium France Germany Israel Italy New Zealand Poland Spain Switzerland United Kingdom

Other Identifiers

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2023-510061-10-00

Identifier Type: CTIS

Identifier Source: secondary_id

XL092-002

Identifier Type: -

Identifier Source: org_study_id

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