Leap Therapeutics to Present New Data from DisTinGuish Study of DKN-01 Plus Tislelizumab and WAKING Study of DKN-01 Plus Tecentriq® at the ESMO Congress

On September 4, 2022 Leap Therapeutics, Inc. (NASDAQ: LPTX), a biotechnology company focused on developing targeted and immuno-oncology therapeutics, reported the Company will be presenting data in first-line patients with advanced gastroesophageal adenocarcinoma (GEA) from the DisTinGuish study, a Phase 2a clinical trial evaluating Leap’s anti-Dickkopf-1 (DKK1) antibody, DKN-01, in combination with tislelizumab, BeiGene’s anti-PD-1 antibody, and chemotherapy, at the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress 2022 being held on September 9-12 (Press release, Leap Therapeutics, SEP 4, 2022, View Source [SID1234618975]). Safety and early efficacy data will be presented from the WAKING study, a multicenter Phase 2 non-randomized trial evaluating DKN-01 plus Tecentriq (atezolizumab), Roche’s anti-PD-L1 antibody, in patients with advanced oesophagogastric adenocarcinoma (OGA).

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"Data from the DisTinGuish study continue to demonstrate promising results with the combination of DKN-01 plus tislelizumab and standard chemotherapy as a first-line treatment in patients with advanced gastroesophageal adenocarcinomas," said Samuel Klempner, MD, Associate Professor at Harvard Medical School. "The mature median progression-free survival of 11.3 months compares favorably with recent benchmarks in this patient group. The outcomes in the aggressive DKK1-high and the less checkpoint-inhibitor sensitive PD-L1-low (CPS < 5) subgroups are notable and encouraging. As the last patient enrolled in early April 2021, the overall survival results are also on track to show an increase over current standards. Gastroesophageal cancer patients and physicians want new biomarker-directed therapies to improve the standard of care in first-line treatment, and we are enthusiastic about the upcoming randomized clinical trial involving this encouraging DKN-01 combination."

"Early results from the WAKING study show the promise of boosting anti-tumor activity by targeting the Wnt signaling pathway and DKK1-driven tumor microenvironment modulation with a DKN-01 plus atezolizumab combination therapy strategy in patients with advanced OGA," said Fiona Turkes, MD, Clinical Research Fellow at The Royal Marsden Hospital. "We look forward to continuing to enroll patients and studying the biological mechanisms of this unique chemotherapy-free combination therapy, especially in those patients whose tumors express high levels of DKK1."

Key Findings DisTinGuish
DKN-01 and tislelizumab plus CAPOX was well tolerated in first-line treatment for advanced GEA patients, with a safety profile consistent with previous reports
Overall median progression-free-survival (PFS) of 11.3 months exceeds benchmark results in unselected patients and in all four important biomarker-directed subgroups
11.3 months PFS in DKK1-high and 12.0 months in DKK1-low
10.7 months PFS in PD-L1-low (CPS < 5) and 11.6 months in PD-L1-high (CPS > 5)
Median overall survival (OS) is not mature with only 44% of patients deceased as of the data cut (June 30, 2022), with a median duration on study of 15.7 months and last patient enrolled in early April 2021
High and durable overall response rate (ORR) in unselected and aggressive subgroups (DKK1-high and PD-L1-low) (mITT): 68% (1 CR, 14 PR) overall
DKK1-high: 90% ORR (9 PR)
DKK1-low: 56% ORR (1 CR; 4 PR)
PD-L1-low expression: 79% (11 PR)
100% (6/6) ORR in DKK1-high, PD-L1-low patients
PD-L1-high expression: 67% (1 CR; 3 PR)
75% (3/4) ORR in DKK1-high, PD-L1-high patients
Key Findings WAKING
DKN-01 up to 600mg every 2 weeks in combination with atezolizumab was considered safe
3 patients with the longest time on treatment received the 600mg dose level
At time of data cut off (August 16, 2022), 18 patients were enrolled in the study
12 patients were treated in initial phase
10 patients were response evaluable at the time of data cut-off
1 patient had a PR and DKK1 expression of 81% tumor percentage score (TPS)
Disease control rate: 50% (1 PR, 4 SD, 5 PD)
Elevated baseline DKK1 expression (TPS > 20%) may be associated with clinical response
4 DKK1-high patients: Best ORR 25% (1 PR, 1 SD, 1 PD, 1 NE)
Translational analyses and assessment of PD-L1 status are ongoing
Safety
No dose-limiting toxicity (DLT) was observed, and no formal maximum tolerated dose (MTD) was reached
No treatment-related deaths occurred, and no dose reductions were required
Leap Poster Details:
Title: DKN-01 and Tislelizumab + Chemotherapy as First-line (1L) Investigational Therapy in Advanced Gastroesophageal Adenocarcinoma (GEA): DisTinGuish Trial
First Author: Samuel J. Klempner, Harvard Medical School
Session Category: Poster Session
Session title: Oesophagogastric cancer
Date and time: Monday, September 12, 2022, at 12:00 CET
Poster Number: 1213

Title: Safety and efficacy of Wnt inhibition with a DKK1 inhibitor, DKN-01, in combination with atezolizumab in patients with advanced oesophagogastric adenocarcinoma (OGA): Phase IIa results of the WAKING trial
First Author: Fiona Turkes, The Royal Marsden NHS Foundation Trust
Session Category: Poster Session
Session title: Oesophagogastric cancer
Date and time: Monday, September 12, 2022, at 12:00 CET
Poster Number: 1253

About the DisTinGuish Study
The DisTinGuish study (NCT04363801) is a Phase 2a study of DKN-01 in combination with tislelizumab, an anti-PD-1 antibody, with or without chemotherapy as first-line or second-line therapy in patients with inoperable, locally advanced, G/GEJ adenocarcinoma. The study is being conducted in two parts in the United States and the Republic of Korea. Enrollment of Part A has been completed with 25 first-line HER2- G/GEJ cancer patients whose tumors express either high levels of DKK1 (DKK1-high) or low levels of DKK1 (DKK1-low). Part B of the study has completed enrollment patients with second-line DKK1-high G/GEJ cancer. Part C of the study will be a randomized controlled trial of DKN-01 in combination with tislelizumab and chemotherapy compared to tislelizumab and chemotherapy. Leap is conducting this combination study as part of an exclusive option and license agreement with BeiGene.

About the WAKING Study
The WAKING study (NCT04166721) is a Phase IIa/b nonrandomized, open-label, multicenter study to be conducted concurrently in 2 Parts. Approximately 52 patients aged 18 years or older with inoperable, histologically confirmed locally advanced or metastatic G/GEJ adenocarcinoma with measurable disease (RECIST v1.1) requiring therapy will be enrolled in the study. Both parts are designed to evaluate safety, tolerability, and efficacy of the combination therapy of DKN-01 and atezolizumab in immunotherapy naïve, PD-L1 unselected G/GEJ adenocarcinoma patients. Treatment continues in repeating 14-day cycles until patient meets criteria for discontinuation or is no longer deriving clinical benefit. The WAKING study is being led by the Royal Marsden Hospital in the United Kingdom with financial support from Roche.

CatalYm to Present Complete Phase 1 Safety and Efficacy Data on GDF-15 Neutralizing Antibody Visugromab (CTL-002) at the 2022 ESMO Congress

On September 4, 2022 CatalYm reported that the mature results from its Phase 1, first-in-human trial "GDFATHER-1" (GDF-15 antibody-mediated human effector cell relocation) will be presented in an oral presentation at the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress 2022 (Press release, Catalym, SEP 4, 2022, View Source [SID1234618974]). The trial evaluated CatalYm’s lead GDF-15 neutralizing antibody visugromab (previously known as CTL-002), in combination with immune checkpoint inhibitor nivolumab in last-line, anti-PD-1/PD-L1 relapsed/refractory patients. Growth and differentiation factor 15 (GDF-15) is recognized as a negative regulator of antitumoral T cell activity preventing T cell recruitment to the tumor microenvironment as well as potently suppressing an adaptive immune response by additional mechanisms recently identified. The ESMO (Free ESMO Whitepaper) congress will be held in Paris, France, from September 9 to 13, 2022.

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Oral presentation details:

Presentation Title: Final results of the first-in-human clinical trial of the GDF-15 neutralizing antibody CTL-002 in combination with nivolumab in subjects with solid tumors relapsed/refractory to prior anti-PD-1/PD-L1 treatment.
Presenter: Dr. Ignacio Melero Bermejo, MD | Universidad de Navarra
Session: Investigational immunotherapy
Session Date and Time: Saturday September 10, 2022, from 2:45 PM – 4:15 PM CEST
Location: In-Person & Live Stream | Paris Expo Porte de Versailles, 7.3.O – Orléans Auditorium
Presentation Number: 729MO

About the GDFATHER-1 Trial
The GDFATHER-1 trial (GDF-15 antibody-mediated human effector cell relocation) is the first-in-human study of visugromab (CTL-002). This dose escalation study recruited 25 patients that received escalating doses of visugromab (CTL-002) in a "3+3" manner with the lead candidate given as a monotherapy for two weeks, then followed by combination with an anti-PD-1 checkpoint inhibitor.

About Visugromab (CTL-002)
Visugromab, formerly known as CTL-002, is a humanized, monoclonal antibody designed to neutralize the tumor-produced Growth Differentiation Factor-15 (GDF-15). GDF-15 secretion by the tumor has been shown to prevent T cell migration into the tumor and suppresses T cell function and the adaptive immune response in the tumor microenvironment. This enables the tumor to evade the immune system and become resistant to standard of care and current immunotherapy approaches such as checkpoint inhibitors. Visugromab counteracts these immuno-suppressive mechanisms by neutralizing GDF-15, enhancing the infiltration of immune cells into the tumor, improving both priming of T cells by dendritic cells and tumor killing by T cells and NK cells.

Wugen Announces Presentation of WU-NK-101 Preclinical Data at the European Society for Medical Oncology (ESMO) Congress 2022

On September 4, 2022 Wugen, Inc., a clinical-stage biotechnology company developing a pipeline of allogeneic cell therapies to treat a broad range of hematological and solid tumor malignancies, reported it will present preclinical data on WU-NK-101, the company’s lead memory natural killer (NK) cell therapy product, at the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress 2022, taking place in Paris, France from September 9-13, 2022 (Press release, Wugen, SEP 4, 2022, View Source [SID1234618973]).

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The results highlight key features of WU-NK-101’s unique cytokine-induced memory-like (CIML) phenotype and support its clinical development for solid tumors. The data reinforced key phenotypic characteristics of WU-NK-101, including its potent anti-tumor cytotoxicity and enhanced metabolic fitness that supports resilience within the immunosuppressive solid tumor microenvironment (TME). Additionally, when used in combination with monoclonal antibodies (mAbs), in preclinical models, WU-NK-101 demonstrated further enhanced anti-tumor activity, with robust tumor penetration and persistence.

The details of Wugen’s presentation at ESMO (Free ESMO Whitepaper) are as follows:

Title: WU-NK-101: An Enhanced NK Cell Therapy Optimized for Function in the Tumor Microenvironment (TME)
Abstract Number: 11P
Date and time: Sunday, September 11, 2022, from 12:00 – 13:00 CEST (6:00 – 7:00 a.m. EDT)
Location: Paris Expo Porte De Versailles, Poster Area, Hall 4
Additional meeting information can be found at View Source

About WU-NK-101

WU-NK-101 is a novel immunotherapy harnessing the power of memory natural killer (NK) cells to treat liquid and solid tumors. Memory NK cells are hyper-functional, long-lasting immune cells that exhibit enhanced anti-tumor activity and a cytokine-induced memory-like (CIML) phenotype. This rare cell population has a superior phenotype, proliferation capacity, and metabolic fitness that makes it better suited for cancer therapy than other NK cell therapies. Wugen is applying its proprietary Moneta platform to advance WU-NK-101 as a commercially scalable, off-the-shelf cell therapy for cancer. WU-NK-101 is currently in development for acute myelogenous leukemia (AML) and solid tumors.

Zymeworks Announces Release of ESMO Abstract for Phase 1 Study of Zanidatamab Zovodotin (ZW49) in Solid Cancers

On September 4, 2022 Zymeworks Inc. (NYSE: ZYME), a clinical-stage biopharmaceutical company developing multifunctional biotherapeutics, reported the release of an abstract by ESMO (Free ESMO Whitepaper) with preliminary results from the company’s Phase 1 study of zanidatamab zovodotin (ZW49), an investigational novel bispecific HER2 targeted antibody-drug conjugate (Press release, Zymeworks, SEP 4, 2022, View Source [SID1234618972]).

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Results from the study entitled "Preliminary Results From a Phase 1 Study Using the Bispecific, Human Epidermal Growth Factor 2 (HER2)-targeting Antibody-drug Conjugate (ADC) zanidatamab zovodotin (ZW49) in Solid Cancers" will be presented by Komal Jhaveri, MD, FACP, Medical Oncologist, Memorial Sloan Kettering Cancer Center in NYC, in a mini-oral presentation on Monday, September 12 at 5:25 pm CEST during the ESMO (Free ESMO Whitepaper) meeting being held September 9-13, 2022, at the Paris Expo Porte de Versailles in Paris, France.

"Treatment of HER2-expressing solid cancers remains an area with significant unmet need, and these preliminary Phase 1 clinical results for zanidatamab zovodotin (ZW49) show that it offers a manageable safety profile and encouraging single-agent anti-tumor activity in patients with advanced disease that has progressed after treatment with standard of care therapies," said Dr. Jhaveri. "We look forward to continuing enrollment in the trial and to reporting on additional data as it becomes available in the months ahead."

In an ongoing Phase 1 study of 76 patients with HER2+ cancers including gastric (28%) and breast (22%) cancers, preliminary results show that the majority of treatment related adverse events (TRAEs) were Grade 1 or 2 and included keratitis (42%), alopecia (25%) and diarrhea (21%). Among seven patients who experienced TRAEs of grade 3 or higher, two were grade 4 events including infusion-related reaction and decreased neutrophil count. There were three patient discontinuations associated with TRAEs and no reported treatment-related patient deaths or cases of interstitial lung disease. Results also showed encouraging single-agent anti-tumor activity in heavily pretreated patients with HER2+ cancers, including a confirmed objective response rate of 28% and a disease control rate of 72% in 29 patients treated at a dose of 2.5 mg/kg on an every three week (Q3W) schedule.

"We are excited to share our preliminary results from the ongoing Phase 1 study at ESMO (Free ESMO Whitepaper)," said Kenneth Galbraith, Chair and CEO of Zymeworks. "We look forward to Dr. Jhaveri’s presentation of updated study results on September 12th in Paris and discussing the future development of zanidatamab zovodin, on our conference call and webcast following the ESMO (Free ESMO Whitepaper) presentation."

Conference Call and Webcast

Zymeworks will host a conference call and webcast on Monday, September 12th at 4:30 pm Eastern Standard Time (EST) to discuss the clinical data presented at ESMO (Free ESMO Whitepaper) and provide an overview on future clinical development plans for zanidatamab zovodotin. The event will feature a presentation by Komal Jhaveri, MD, FACP, Clinical Oncology, Memorial Sloan Kettering in NYC, and Neil Josephson, M.D., Zymeworks’ Chief Medical Officer. An open question & answer session with all presenters will conclude the event.

Interested parties can access the live webcast via Zymeworks’ website at View Source A recorded replay will be accessible after the event on the Zymeworks website.

Disclosure: Dr. Jhaveri has a consulting relationship with Zymeworks.

New TROPiCS-02 Data In HR+/HER2- Metastatic Breast Cancer Patients Demonstrates Progression-Free Survival Benefit Of Trodelvy® Regardless Of Their HER2 Status

On September 4, 2022 Gilead Sciences, Inc. (Nasdaq: GILD) reported new data from a post hoc subgroup analysis from the Phase 3 TROPiCS-02 study evaluating Trodelvy (sacituzumab govitecan-hziy) versus comparator chemotherapies (physicians’ choice of chemotherapy, TPC) in patients with HR+/HER2- metastatic breast cancer who progressed on endocrine-based therapies and at least two chemotherapies (Press release, Gilead Sciences, SEP 4, 2022, View Source;Metastatic-Breast-Cancer-Patients-Demonstrates-Progression-Free-Survival-Benefit-of-Trodelvy-Regardless-of-Their-HER2-Status/default.aspx [SID1234618971]). The analysis examined progression-free survival (PFS) in the intention-to-treat population by HER2-immunohistochemistry (IHC) status, and the results demonstrated that Trodelvy improved median PFS vs. TPC in both HER2-low (IHC1+ and IHC2+/ISH-negative) and IHC0 groups.

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Summary of results:

Detailed findings will be presented at a mini-oral session (Abstract #1362) during the European Society for Medical Oncology (ESMO) (Free ESMO Whitepaper) Congress 2022 in the Évry Auditorium, Paris Expo Porte de Versailles, on September 10.

"These data demonstrate Trodelvy’s efficacy across HER2-low and IHC0 status in pre-treated metastatic breast cancer patients in the TROPiCS-02 trial," said Professor Peter Schmid, Professor of Cancer Medicine; Centre Lead, Centre of Experimental Cancer Medicine; Director, Barts Breast Cancer Centre. "Once patients have developed resistance to endocrine-based therapies, their prognosis is extremely poor. The results highlight the potential for Trodelvy as a treatment option for people living with pre-treated HR+/HER2- metastatic breast cancer, regardless of their HER2-negative status."

"These results show Trodelvy improved progression-free survival regardless of HER2 status in this pre-treated patient population and reinforce the strength of clinical activity in a population where need is highest," said Bill Grossman, MD, PhD, Senior Vice President, Therapeutic Area Head, Gilead Oncology. "Trodelvy is already transforming the standard of care in second-line metastatic triple-negative breast cancer, and we’re excited about its potential in other breast cancers where there is significant need for new treatment options."

In the study, HER2 negativity was defined per American Society of Clinical Oncology (ASCO) (Free ASCO Whitepaper) and the College of American Pathologists (CAP) criteria as immunohistochemistry (IHC) score of 0, IHC 1+ or IHC 2+ with a negative in-situ hybridization (ISH) test.

Trodelvy has not been approved by any regulatory agency for the treatment of HR+/HER2- metastatic breast cancer. Its safety and efficacy have not been established for this indication. Gilead has submitted a supplemental Biologics License Application (sBLA) to the U.S. Food and Drug Administration (FDA) based on data from TROPiCS-02; these data will also be shared with health authorities outside the U.S.

Sacituzumab govitecan is currently included in the National Comprehensive Cancer Network (NCCN) Clinical Practice Guidelines in Oncology (NCCN Guidelines)i. This includes a Category 1 recommendation for use in adult patients with second-line metastatic triple-negative breast cancer (defined as those who received at least two prior therapies, with at least one line for metastatic disease). It also has a Category 2A preferred recommendation for investigational use in HR+/HER2- advanced breast cancer after prior treatment including endocrine therapy, a CDK4/6 inhibitor and at least two lines of chemotherapy.

Trodelvy has a Boxed Warning for severe or life-threatening neutropenia and severe diarrhea; please see below for additional Important Safety Information.

About HR+/HER2- Breast Cancer

Hormone receptor-positive/human epidermal growth factor receptor 2-negative (HR+/HER2-) breast cancer is the most common type of breast cancer and accounts for approximately 70% of all new cases, or nearly 400,000 diagnoses worldwide each year. Almost one in three cases of early-stage breast cancer eventually become metastatic, and among patients with HR+/HER2- metastatic disease, the five-year relative survival rate is 30%. As patients with HR+/HER2- metastatic breast cancer become resistant to endocrine-based therapy, their primary treatment option is limited to single-agent chemotherapy. In this setting, it is common to receive multiple lines of chemotherapy regimens over the course of treatment, and the prognosis remains poor.

About the TROPiCS-02 Study

The TROPiCS-02 study is a global, multicenter, open-label, Phase 3 study, randomized 1:1 to evaluate Trodelvy versus physicians’ choice of chemotherapy (eribulin, capecitabine, gemcitabine, or vinorelbine) in 543 patients with HR+/HER2- metastatic breast cancer who were previously treated with endocrine therapy, CDK4/6 inhibitors and two to four lines of chemotherapy for metastatic disease. The primary endpoint is progression-free survival per Response Evaluation Criteria in Solid Tumors (RECIST 1.1) as assessed by blinded independent central review (BICR) for participants treated with Trodelvy compared to those treated with chemotherapy. Secondary endpoints include overall survival, overall response rate, clinical benefit rate and duration of response, as well as assessment of safety and tolerability and quality of life measures. More information about TROPiCS-02 is available at View Source

About Trodelvy

Trodelvy (sacituzumab govitecan-hziy) is a first-in-class Trop-2 directed antibody-drug conjugate. Trop-2 is a cell surface antigen highly expressed in multiple tumor types, including in more than 90% of breast and bladder cancers. Trodelvy is intentionally designed with a proprietary hydrolyzable linker attached to SN-38, a topoisomerase I inhibitor payload. This unique combination delivers potent activity to both Trop-2 expressing cells and the microenvironment.

Trodelvy is approved in more than 35 countries, with multiple additional regulatory reviews underway worldwide, for the treatment of adult patients with unresectable locally advanced or metastatic triple-negative breast cancer (TNBC) who have received two or more prior systemic therapies, at least one of them for metastatic disease. Trodelvy is also approved in the U.S. under the accelerated approval pathway for the treatment of adult patients with locally advanced or metastatic urothelial cancer (UC) who have previously received a platinum-containing chemotherapy and either programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor.

Trodelvy is also being developed for potential investigational use in other TNBC and metastatic UC populations, as well as a range of tumor types where Trop-2 is highly expressed, including hormone receptor-positive/human epidermal growth factor receptor 2-negative (HR+/HER2-) metastatic breast cancer, metastatic non-small cell lung cancer (NSCLC), metastatic small cell lung cancer (SCLC), head and neck cancer, and endometrial cancer.

U.S. Indications for Trodelvy

In the United States, Trodelvy is indicated for the treatment of:

Adult patients with unresectable locally advanced or metastatic TNBC who have received two or more prior systemic therapies, at least one of them for metastatic disease.
Adult patients with locally advanced or metastatic UC who have previously received a platinum-containing chemotherapy and either programmed death receptor-1 (PD-1) or programmed death-ligand 1 (PD-L1) inhibitor. This indication is approved under accelerated approval based on tumor response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial.
U.S. Important Safety Information for Trodelvy

BOXED WARNING: NEUTROPENIA AND DIARRHEA

Severe or life-threatening neutropenia may occur. Withhold Trodelvy for absolute neutrophil count below 1500/mm3 or neutropenic fever. Monitor blood cell counts periodically during treatment. Consider G-CSF for secondary prophylaxis. Initiate anti-infective treatment in patients with febrile neutropenia without delay.
Severe diarrhea may occur. Monitor patients with diarrhea and give fluid and electrolytes as needed. Administer atropine, if not contraindicated, for early diarrhea of any severity. At the onset of late diarrhea, evaluate for infectious causes and, if negative, promptly initiate loperamide. If severe diarrhea occurs, withhold Trodelvy until resolved to ≤Grade 1 and reduce subsequent doses.
CONTRAINDICATIONS

Severe hypersensitivity reaction to Trodelvy.
WARNINGS AND PRECAUTIONS

Neutropenia: Severe, life-threatening, or fatal neutropenia can occur and may require dose modification. Neutropenia occurred in 61% of patients treated with Trodelvy. Grade 3-4 neutropenia occurred in 47% of patients. Febrile neutropenia occurred in 7%. Withhold Trodelvy for absolute neutrophil count below 1500/mm3 on Day 1 of any cycle or neutrophil count below 1000/mm3 on Day 8 of any cycle. Withhold Trodelvy for neutropenic fever.

Diarrhea: Diarrhea occurred in 65% of all patients treated with Trodelvy. Grade 3-4 diarrhea occurred in 12% of patients. One patient had intestinal perforation following diarrhea. Neutropenic colitis occurred in 0.5% of patients. Withhold Trodelvy for Grade 3-4 diarrhea and resume when resolved to ≤Grade 1. At onset, evaluate for infectious causes and if negative, promptly initiate loperamide, 4 mg initially followed by 2 mg with every episode of diarrhea for a maximum of 16 mg daily. Discontinue loperamide 12 hours after diarrhea resolves. Additional supportive measures (e.g., fluid and electrolyte substitution) may also be employed as clinically indicated. Patients who exhibit an excessive cholinergic response to treatment can receive appropriate premedication (e.g., atropine) for subsequent treatments.

Hypersensitivity and Infusion-Related Reactions: Serious hypersensitivity reactions including life-threatening anaphylactic reactions have occurred with Trodelvy. Severe signs and symptoms included cardiac arrest, hypotension, wheezing, angioedema, swelling, pneumonitis, and skin reactions. Hypersensitivity reactions within 24 hours of dosing occurred in 37% of patients. Grade 3-4 hypersensitivity occurred in 2% of patients. The incidence of hypersensitivity reactions leading to permanent discontinuation of Trodelvy was 0.3%. The incidence of anaphylactic reactions was 0.3%. Pre-infusion medication is recommended. Observe patients closely for hypersensitivity and infusion-related reactions during each infusion and for at least 30 minutes after completion of each infusion. Medication to treat such reactions, as well as emergency equipment, should be available for immediate use. Permanently discontinue Trodelvy for Grade 4 infusion-related reactions.

Nausea and Vomiting: Nausea occurred in 66% of all patients treated with Trodelvy and Grade 3 nausea occurred in 4% of these patients. Vomiting occurred in 39% of patients and Grade 3-4 vomiting occurred in 3% of these patients. Premedicate with a two or three drug combination regimen (e.g., dexamethasone with either a 5-HT3 receptor antagonist or an NK1 receptor antagonist as well as other drugs as indicated) for prevention of chemotherapy-induced nausea and vomiting (CINV). Withhold Trodelvy doses for Grade 3 nausea or Grade 3-4 vomiting and resume with additional supportive measures when resolved to Grade ≤1. Additional antiemetics and other supportive measures may also be employed as clinically indicated. All patients should be given take-home medications with clear instructions for prevention and treatment of nausea and vomiting.

Increased Risk of Adverse Reactions in Patients with Reduced UGT1A1 Activity: Patients homozygous for the uridine diphosphate-glucuronosyl transferase 1A1 (UGT1A1)*28 allele are at increased risk for neutropenia, febrile neutropenia, and anemia and may be at increased risk for other adverse reactions with Trodelvy. The incidence of Grade 3-4 neutropenia was 67% in patients homozygous for the UGT1A1*28, 46% in patients heterozygous for the UGT1A1*28 allele and 46% in patients homozygous for the wild-type allele. The incidence of Grade 3-4 anemia was 25% in patients homozygous for the UGT1A1*28 allele, 10% in patients heterozygous for the UGT1A1*28 allele, and 11% in patients homozygous for the wild-type allele. Closely monitor patients with known reduced UGT1A1 activity for adverse reactions. Withhold or permanently discontinue Trodelvy based on clinical assessment of the onset, duration and severity of the observed adverse reactions in patients with evidence of acute early-onset or unusually severe adverse reactions, which may indicate reduced UGT1A1 function.

Embryo-Fetal Toxicity: Based on its mechanism of action, Trodelvy can cause teratogenicity and/or embryo-fetal lethality when administered to a pregnant woman. Trodelvy contains a genotoxic component, SN-38, and targets rapidly dividing cells. Advise pregnant women and females of reproductive potential of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with Trodelvy and for 6 months after the last dose. Advise male patients with female partners of reproductive potential to use effective contraception during treatment with Trodelvy and for 3 months after the last dose.

ADVERSE REACTIONS

In the ASCENT study (IMMU-132-05), the most common adverse reactions (incidence ≥25%) were fatigue, neutropenia, diarrhea, nausea, alopecia, anemia, constipation, vomiting, abdominal pain, and decreased appetite. The most frequent serious adverse reactions (SAR) (>1%) were neutropenia (7%), diarrhea (4%), and pneumonia (3%). SAR were reported in 27% of patients, and 5% discontinued therapy due to adverse reactions. The most common Grade 3-4 lab abnormalities (incidence ≥25%) in the ASCENT study were reduced neutrophils, leukocytes, and lymphocytes.

In the TROPHY study (IMMU-132-06), the most common adverse reactions (incidence ≥25%) were diarrhea, fatigue, neutropenia, nausea, any infection, alopecia, anemia, decreased appetite, constipation, vomiting, abdominal pain, and rash. The most frequent serious adverse reactions (SAR) (≥5%) were infection (18%), neutropenia (12%, including febrile neutropenia in 10%), acute kidney injury (6%), urinary tract infection (6%), and sepsis or bacteremia (5%). SAR were reported in 44% of patients, and 10% discontinued due to adverse reactions. The most common Grade 3-4 lab abnormalities (incidence ≥25%) in the TROPHY study were reduced neutrophils, leukocytes, and lymphocytes.

DRUG INTERACTIONS

UGT1A1 Inhibitors: Concomitant administration of Trodelvy with inhibitors of UGT1A1 may increase the incidence of adverse reactions due to potential increase in systemic exposure to SN-38. Avoid administering UGT1A1 inhibitors with Trodelvy.

UGT1A1 Inducers: Exposure to SN-38 may be substantially reduced in patients concomitantly receiving UGT1A1 enzyme inducers. Avoid administering UGT1A1 inducers with Trodelvy.