Cullgen Announces First-In-Human Dose in Phase I/II Trial of CG001419, a First-in-Class TRK Protein Degrader for Treatment of Cancer Patients

On July 27, 2023 Cullgen Inc., a leading biotechnology company developing small molecule therapeutics based on its proprietary uSMITE platform of targeted protein degradation technology, reported that it has initiated dosing with its orally bioavailable pan-TRK degrader, CG001419, in a Phase I/II clinical trial for patients with solid tumors (Press release, Cullgen, JUL 27, 2023, View Source [SID1234633471]). CG001419 is a potential first-in-class, highly active small molecule developed to selectively degrade both mutant and wild-type TRK proteins. In preclinical research, CG001419 demonstrated strong potency against solid tumors harboring various oncogenic TRK abnormalities, such as NTRK gene fusions and wild-type TRK protein over-expression.

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"We are excited to initiate human dosing for CG001419," said Dr. Ying Luo, Chairman and CEO of Cullgen, "This is a significant milestone for Cullgen as it marks our first entry into the clinic for one of our targeted protein degraders. I am very proud of the progress that our entire company has made to advance our first program into the clinic in only a few years since inception of the program."

The first-in-human trial of CG001419 is a Phase I/II trial with adaptive design. The Phase Ia portion of the trial is an open label, non-randomized, dose escalation study to evaluate the safety, tolerability, PK profile, and preliminary efficacy of CG001419 in patients with advanced or metastatic solid tumors, particularly those harboring NTRK gene fusions, point mutations, amplifications or over-expression. Patients that complete the Phase Ia trial may transition into the Phase Ib or Phase II portions of the trial depending on safety and tolerability results, the patient’s NTRK aberration type, and the judgment of physicians. Compared with traditional kinase inhibitor drugs approved in treating cancer with NTRK gene fusions, CG001419 may offer potential advantages in overcoming secondary drug-resistant mutations in NTRK fusions, as well as an expanded clinical profile to include cancers with other NTRK gene/TRK protein abnormalities.

DELFI Diagnostics Licenses GEMINI Technology from Johns Hopkins University: Study Demonstrates High Performance for Early Stage Lung Cancer Detection When Integrated with DELFI Diagnostics’s Platform

On July 27, 2023 DELFI Diagnostics, a pioneering developer of a new class of high-performance, accessible liquid biopsy tests for early cancer detection and monitoring, reported to have licensed a new, highly accurate method for identifying somatic genomic alterations in cell-free DNA (cfDNA) known as GEMINI, or GEnome-wide Mutational Incidence for Non Invasive detection of cancer (Press release, Delfi Diagnostics, JUL 27, 2023, View Source [SID1234633470]).

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Until now, first-generation liquid biopsy technologies relied on expensive, deep, targeted sequencing to detect mutations associated with cancer. Now, for the first time, researchers have achieved genome-wide detection of tumor-specific mutations from the same low-coverage whole genome sequencing methods that form the basis of the DELFI Diagnostics platform.

In a study published today in Nature Genetics, researchers showed that GEMINI, combined with the approach used by DELFI Diagnostics, could successfully identify early stage lung cancers – those cancers that are most critical to detect to change patient outcome. In a cohort of lung cancer cases and non-cancer controls (n=163), combining the GEMINI analysis with DELFI’s fragmentomics approach yielded an area under the receiver operator curve (AUC), a common measure of diagnostic accuracy, of 0.931. The combined technology also showed high performance in other applications including monitoring response to therapy, and distinguishing small-cell lung cancer from non-small cell lung cancer.

"We founded DELFI Diagnostics to address population-health needs in cancer detection with low-cost, flexibly deployable technology," said Nicholas Dracopoli, PhD, DELFI Diagnostics’s Chief Scientific Officer and Co-Founder. "Whenever we evaluate new technology, it must meet multiple criteria: It must help boost early stage cancer detection, and it must be able to be applied to the sequencing data generated from our low-cost platform. GEMINI fulfills both those requirements and shows how we can further refine the performance of our platform without changing our lab processes."

DELFI Diagnostics’s fragmentomics-based approach applies machine learning-based algorithms to low-coverage, whole genome sequencing data from cfDNA. Beyond the genome-wide analysis of fragment length profiles that reflect the aberrant packaging of DNA in cancer cells, the whole-genome sequencing approach also reveals many other changes in DNA features including somatic genomic alterations, amplifications, deletions, and more.

"We have already shown that this platform can detect lung cancer with very high sensitivity," said Peter Bach, MD, DELFI Diagnostics’s Chief Medical Officer. "This new study shows that what was a first-generation approach to cancer detection — looking for genomic mutations — can now be extended genome-wide and enhanced with the DELFI platform, improving early stage cancer detection with no additional sequencing or lab prep cost."

HanAll Biopharma Reports Second Quarter 2023 Financial Results and Provides a Business Update

On July 27, 2023 HanAll Biopharma Co., Ltd. (KRX: 009420. KS), a global biopharmaceutical company committed to discovering and developing innovative medicines for patients, reported financial results for the second quarter and provided business updates (Press release, HanAll Biopharma, JUL 27, 2023, View Source [SID1234633469]).

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HanAll ended the quarter with total revenue of 41.4 billion won, an increase of 58 percent compared to the same period last year, and an operating profit of 8.1 billion won. Net profit recorded 7.3 billion won due to the continued growth of its pharmaceutical products and milestone revenues from the licensed partner.

"We are pleased to announce another successful quarter with strong sales growth and significant advancements in clinical developments. We achieved a meaningful result from the tanfanercept Phase 3 study for dry eye disease, while batoclimab progressed another step further towards commercialization in China. Our commitment to innovation is evident by portfolio expansion and fruitful collaborations in the neurodegenerative domain," said Sean Jeong, M.D., MBA, CEO of HanAll Biopharma.

"In the second half 2023, we anticipate the initiation of a Phase 1 clinical study on Parkinson’s disease (PD), along with the initial results from the anti-FcRn assets batoclimab in Grave’s disease and Phase 1 study of HL161ANS. In addition, we anticipate finalizing the next Phase 3 clinical study design for tanfanercept this year. These upcoming milestones exemplify our dedication to advancing innovative medicines, and we will continue to push the boundaries of science and steadfastly pursue our mission to improve patient outcomes," he added.

SECOND QUARTER 2023 BUSINESS UPDATE
Pipeline Development Highlights
A comprehensive update of HanAll’s pipeline development below includes an overview of research along with lists of compounds, targeted indications, and developmental phase.

AUTOIMMUNE DISEASES PROGRAMS
Batoclimab (HL161BKN)
A novel, fully human, subcutaneously administered antibody targeting FcRn with the potential to address multiple IgG-mediated autoimmune diseases. Batoclimab is designed to selectively bind to and inhibit FcRn, which plays a role in recycling IgG, thus may reduce harmful IgG antibodies.

Harbour BioMed, a licensed partner of HanAll in China, announced the official acceptance of the Biologics License Application (BLA) for batoclimab for the treatment of generalized myasthenia gravis (gMG) in June 2023, based on the positive topline result from the Phase 3 clinical trial in early March this year. The data from the Phase 3 clinical trial met the primary efficacy endpoint as well as key secondary endpoints with a favorable profile. Batoclimab received the ‘Breakthrough Therapy Certificate’ from NMPA in 2021.
Another licensed partner, Immunovant, located in the U.S. and Europe, is currently carrying out global Phase 3 trials on batoclimab in both gMG and TED. The initial results from the Phase 2 trial evaluating batoclimab in Grave’s disease (GD), is expected in the fourth quarter of 2023. The company expects initial results from the pivotal Phase 2b trial of CIDP in the first half of 2024.
HanAll is progressing towards the initiation of a Phase 3 clinical study of batoclimab in gMG in Japan this year. Additionally, HanAll is exploring options for developing batoclimab for TED and chronic inflammatory demyelinating polyneuropathy (CIDP) in Japan.
HL161ANS
Another novel, fully human, subcutaneous antibody molecule that inhibits FcRn-mediated recycling of IgG is designed to deliver maximum lgG reductions while minimizing interference with albumin recycling.

Immunovant is progressing a Phase 1 clinical trial of HL161ANS, a new FcRn inhibitor (Immunovatnt project designation: IMVT-1402), in New Zealand to evaluate the safety, pharmacokinetics, and pharmacodynamics profile in healthy patients. The Initial data readout for single-ascending dose (SAD) cohorts is expected in third quarter of 2023, and multi-ascending dose (MAD) cohorts are expected in the fourth quarter of 2023. Immunovant also received IND clearance for HL161ANS from the U.S. Food and Drug Administration (FDA) in the second quarter of 2023.
OPHTHALMIC DISEASE PROGRAMS
Tanfanercept (HL036)
A novel topical protein therapy for ophthalmic diseases, including dry eye disease (DED), which inhibits TNF alpha, a key mediator of ocular inflammation

HanAll Biopharma and Daewoong Pharmaceutical announced the top-line results from the Phase 3 VELOS-3 trial evaluating tanfanercept ophthalmic solution for the treatment of DED in May 2023. The Phase 3 VELOS-3 did not demonstrate statistical significance in either of the primary outcome measures of improvement in central corneal staining score (CCSS) or improvement in Eye Dryness Score (EDS) assessed at week 8 in subjects with moderate to severe DED. However, the solution demonstrated a highly statistically significant improvement in the secondary efficacy endpoint of the unanesthesized Schirmer test evaluating the change in tear volume from baseline in patients treated with tanfanercept compared to the vehicle arm assessed at week 8. HanAll and Daewoong plan to finalize the next study design within the second half of 2023 and intend to discuss VELOS-3 data and future plans with the FDA, with plans to begin the next study in the first half of 2024.
Previous notices reflected a significant improvement of p < 0.001 in the secondary efficacy endpoint of unanesthesized Schirmer testing to quantify change from baseline in tear volume in tanfanercept treatment arm relative to vehicle arm assessed at week 8 as well as a statistically different rate of the proportion of subjects whose Schirmer test improved from baseline by 10mm or greater at week 8 in tanfanercept arm (15%) relative to vehicle arm (4%), p < 0.001. Further analyses have revealed an update to those percentages and to the p-values, although there are no interpretation changes. The secondary efficacy endpoint of unanesthesized Schirmer testing to quantify the change from baseline in tear volume in tanfanercept treatment arm relative to vehicle arm assessed at week 8 demonstrated a significant improvement (p = 0.002). Additionally, the proportion of subjects whose Schirmer test improved from baseline by 10mm or greater as assessed at week 8 was statistically significant (p = 0.011) in the tanfanercept arm (13%) relative to the vehicle arm (4%).
Harbour BioMed, a licensed partner of HanAll in China, is discussing further development plans for tanfanercept in China.
ONCOLOGY PROGRAMS
HL187/ HL186
Monoclonal antibodies that respectively target T cell immunoreceptors with immunoglobulin (Ig) and ITIM (Immunoreceptor tyrosine-based inhibitory moti)} domains (TIGIT) and T cell Ig and mucin domain-3 (TIM-3) are being developed in collaboration with Daewoong Pharmaceutical as potential oncology treatments

HanAll is continuing with the pre-clinical development of the HL187 (anti-TIGIT) asset and plans to evaluate the further development of HL186 (anti-TIM-3) based on the strategic portfolio review.
NEUROLOGY PROGRAMS
HL192
A pipeline candidate originated from NurrOn Pharmaceuticals that targets Nurr1, a master regulator in dopaminergic neuron development and maintenance, is being developed to treat neurodegenerative diseases, including Parkinson’s disease (PD)

HanAll entered into joint clinical development with NurrOn Pharmaceuticals and Daewoong Pharmaceutical to develop NurrOn’s leading asset HL192 (NurrOn project designation: ATH-399A) which will be evaluated in an array of neurodegenerative diseases with the primary area of focus targeting PD. The Phase 1 clinical study of HL192 in healthy participants is expected to be initiated this year.
FINANCIAL HIGHLIGHTS (CONSOLIDATED)
Key Highlights

(KRW in billion)

Q2 2023

Q2 2022

% change

Sales

41.4

26.2

+58 %

Gross Profit

27.2

14.9

+82 %

Selling, marketing and administrative expenses

11.3

10.6

+7 %

Research and development expenses

7.8

3.7

+111 %

Operating income

8.1

0.7

+1092 %

Net Income

7.3

(0.1)

N/A

Sales recorded 41.4 billion won in the second quarter of 2023, a 58 percent increase compared to the second quarter of 2022. Strong sales growth from pharmaceuticals continued from major products sold under the names of Biotop, Eligard, and Normix, with Biotop recording sales growth of 70% compared to the same period last year.

Research and development expenses for the second quarter ended June 30, 2023, were 7.8 billion won, up 111 percent from 3.7 billion won for the three months ended June 30, 2022.

Net income for the three months ended June 30, 2023, recorded 7.3 billion won, due to an increase in milestone revenue and pharmaceutical sales.

European Commission Approves Gilead’s Trodelvy® For Pre-Treated HR+/HER2- Metastatic Breast Cancer

On July 27, 2023 Gilead Sciences, Inc. (Nasdaq: GILD) reported that the European Commission (EC) approved Trodelvy (sacituzumab govitecan) as a monotherapy for the treatment of adult patients with unresectable or metastatic hormone receptor (HR)-positive, HER2-negative breast cancer who have received endocrine-based therapy, and at least two additional systemic therapies in the advanced setting (Press release, Gilead Sciences, JUL 27, 2023, View Source;Metastatic-Breast-Cancer/default.aspx [SID1234633467]).

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The approval by the European Commission follows the positive opinion of the Committee for Medicinal Products and is based on the Phase 3 TROPiCS-02 study, in which Trodelvy demonstrated a statistically significant and clinically meaningful overall survival (OS) benefit of 3.2 months versus comparator single-agent chemotherapy (treatment of physician’s choice; TPC) (median OS: 14.4 months vs. 11.2 months; hazard ratio [HR]=0.79; 95% CI: 0.65-0.96; p=0.02). Trodelvy also demonstrated a 34% reduction in risk of disease progression or death (median PFS: 5.5 versus 4.0 months; HR: 0.66; 95% CI: 0.53-0.83; p=0.0003). Three times as many people treated with Trodelvy were progression-free at one year versus those treated with chemotherapy (21% versus 7%).

"The European approval of sacituzumab govitecan is an important milestone for the European breast cancer community," said Dr. Javier Cortes, Head of the International Breast Cancer Center, in Madrid and Barcelona, Spain. "We now have a new treatment option that has delivered a proven and clinically meaningful survival benefit for women in Europe with pre-treated HR+/HER2- metastatic breast cancer."

"Trodelvy could change the outlook for women with pre-treated HR+/HER2- metastatic breast cancer by replacing the standard-of-care chemotherapy that has been their only option for decades," said Bill Grossman, M.D., Ph.D., Senior Vice President, Therapeutic Area Head, Gilead Oncology. "We look forward to working with European authorities to ensure access for these patients who need new treatment options."

"Women living with pre-treated HR+/HER2- metastatic breast cancer are focused on time with their loved ones and do not want to worry about running out of treatment options," said Eva Schumacher-Wulf, Chief Editor, Mamma Mia! Magazine and Metastatic Breast Cancer Patient. "We welcome the approval of this needed new option that gives pre-treated HR+/HER2- metastatic patients the potential for a longer life."

In the TROPiCS-02 study, Trodelvy also significantly improved additional secondary endpoint measures, including objective response rate and time to deterioration (TTD) assessed by the Global Health Status/Quality of Life and Fatigue scale per EORTC-QLQ-C30. No statistically significant difference in TTD in Pain Scale was observed.

The safety profile for Trodelvy is well-characterized and consistent with prior studies, with no new safety signals identified in this patient population. In TROPiCS-02, the most frequent serious adverse reactions (>1%) were diarrhea (5%), febrile neutropenia (4%), neutropenia (3%), and abdominal pain, colitis, neutropenic colitis, pneumonia, and vomiting (each 2%). No patients treated with Trodelvy in TROPiCS-02 experienced interstitial lung disease (ILD). In the TROPiCS-02 study, the discontinuation rate due to adverse reactions was 6% for Trodelvy and 4% for patients on single-agent chemotherapy.

The ESMO (Free ESMO Whitepaper) Living Guidelines have been updated to include Trodelvy as a category I, A, magnitude of clinical benefit (MCBS) score 3, for women with HR+/HER2- metastatic breast cancer.i

Trodelvy is also recommended as a Category 1, preferred treatment for metastatic HR+/HER2- breast cancer by the National Comprehensive Cancer Network (NCCN) as defined in the Clinical Practice Guidelines in Oncology (NCCN Guidelines).ii

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- Metastatic 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. 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 34%. 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 inhibitor 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. 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. 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 40 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. for the treatment of adult patients with unresectable locally advanced or metastatic HR+/HER2- breast cancer who have received endocrine-based therapy and at least two additional systemic therapies in the metastatic setting and has an accelerated approval for treatment of certain patients with second-line metastatic urothelial cancer; see below for full U.S. indication statements.

Trodelvy is also being developed for potential investigational use in other TNBC and HR+/HER2- metastatic and adjuvant breast cancer populations. It is also being investigated across a range of tumors, including metastatic urothelial cancer, metastatic non-small cell lung cancer (NSCLC), metastatic small cell lung cancer (SCLC), head and neck cancer, and endometrial cancer.

Important Safety Information for Trodelvy as Included in the U.S. Prescribing Information for Trodelvy

Recommendations for the use of Trodelvy in the EU (including final safety information for prescribers) have been assessed as part of the Marketing Authorization Application and are detailed in full in the EU SmPC.

Recommendations for the use of Trodelvy in other countries outside of the U.S. are subject to assessment by the relevant local regulatory authority as part of the registration/marketing authorization process. Once approved, recommendations are detailed in the local prescribing information.

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 unresectable locally advanced or metastatic HR+/HER2- (IHC 0, IHC 1+ or IHC 2+/ISH–) breast cancer who have received endocrine-based therapy and at least two additional systemic therapies in the metastatic setting.
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 confirmatory trials.
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. At the onset of 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 64% of patients treated with Trodelvy. Grade 3-4 neutropenia occurred in 49% of patients. Febrile neutropenia occurred in 6%. Neutropenic colitis occurred in 1.4%. 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. Administer G-CSF as clinically indicated or indicated in Table 1 of USPI.

Diarrhea: Diarrhea occurred in 64% of all patients treated with Trodelvy. Grade 3-4 diarrhea occurred in 11% of patients. One patient had intestinal perforation following diarrhea. Diarrhea that led to dehydration and subsequent acute kidney injury occurred in 0.7% of all 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 35% of patients. Grade 3-4 hypersensitivity occurred in 2% of patients. The incidence of hypersensitivity reactions leading to permanent discontinuation of Trodelvy was 0.2%. The incidence of anaphylactic reactions was 0.2%. Pre-infusion medication is recommended. Have medications and emergency equipment to treat such reactions available for immediate use. Observe patients closely for hypersensitivity and infusion-related reactions during each infusion and for at least 30 minutes after completion of each infusion. Permanently discontinue Trodelvy for Grade 4 infusion-related reactions.

Nausea and Vomiting: Nausea occurred in 64% of all patients treated with Trodelvy and Grade 3-4 nausea occurred in 3% of these patients. Vomiting occurred in 35% of patients and Grade 3-4 vomiting occurred in 2% 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 58% in patients homozygous for the UGT1A1*28, 49% in patients heterozygous for the UGT1A1*28 allele, and 43% in patients homozygous for the wild-type allele. The incidence of Grade 3-4 anemia was 21% in patients homozygous for the UGT1A1*28 allele, 10% in patients heterozygous for the UGT1A1*28 allele, and 9% 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 pooled safety population, the most common (≥ 25%) adverse reactions including laboratory abnormalities were decreased leukocyte count (84%), decreased neutrophil count (75%), decreased hemoglobin (69%), diarrhea (64%), nausea (64%), decreased lymphocyte count (63%), fatigue (51%), alopecia (45%), constipation (37%), increased glucose (37%), decreased albumin (35%), vomiting (35%), decreased appetite (30%), decreased creatinine clearance (28%), increased alkaline phosphatase (28%), decreased magnesium (27%), decreased potassium (26%), and decreased sodium (26%).

In the ASCENT study (locally advanced or metastatic triple-negative breast cancer), the most common adverse reactions (incidence ≥25%) were fatigue, diarrhea, nausea, alopecia, 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 TROPiCS-02 study (locally advanced or metastatic HR-positive, HER2-negative breast cancer), the most common adverse reactions (incidence ≥25%) were diarrhea, fatigue, nausea, alopecia, and constipation. The most frequent serious adverse reactions (SAR) (>1%) were diarrhea (5%), febrile neutropenia (4%), neutropenia (3%), abdominal pain, colitis, neutropenic colitis, pneumonia, and vomiting (each 2%). SAR were reported in 28% of patients, and 6% discontinued therapy due to adverse reactions. The most common Grade 3-4 lab abnormalities (incidence ≥25%) in the TROPiCS-02 study were reduced neutrophils and leukocytes.

In the TROPHY study (locally advanced or metastatic urothelial cancer), the most common adverse reactions (incidence ≥25%) were diarrhea, fatigue, nausea, any infection, alopecia, decreased appetite, constipation, vomiting, rash, and abdominal pain. 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 reduced in patients concomitantly receiving UGT1A1 enzyme inducers. Avoid administering UGT1A1 inducers with Trodelvy.

Please see full Prescribing Information , including BOXED WARNING.

Company Overview

On July 27, 2023 Verrica Pharmaceuticals presented its corporate presentation (Presentation, Verrica Pharmaceuticals, JUL 27, 2023, View Source [SID1234633465]).

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