Lubrizol Licenses Award-Winning Apisolex™ Excipient to Welton Pharma to Develop a Novel Cancer Therapeutic

On June 20, 2023 The Lubrizol Corporation reported the licensing of its novel excipient polymer technology, Apisolex excipient, to Welton Pharma (Welton) (Press release, The Lubrizol, JUN 20, 2023, View Source [SID1234632811]). The license allows Welton to use the Apisolex excipient worldwide to develop and commercialize a novel formulation of SN-38 to treat colorectal and associated gastro-intestinal cancers.

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Introduced to the market last year, the patented Apisolex excipient is a polyamino-acid polymer designed for parenteral applications. The use of the Apisolex excipient has been proven to increase the solubility of active pharmaceutical ingredients (APIs) by as much as 50,000-fold with the goal of increasing the API’s efficacy in the body. Lubrizol continues to invest in expanding the reach of the Apisolex excipient in the market and nurturing relationships with drug product manufacturers that are facing insoluble API challenges.

Kevin Song, Ph.D. Global Marketing Director, Lubrizol Life Science Health said, "We are continuously innovating to solve challenges for our customers and partners. By delivering differentiated solubility-enhancing solutions to the market, we enable the acceleration of life changing drug products to patients who need them."

Welton is looking to bring life-saving solutions for the treatment of colorectal cancer that impacts 1.9 million people worldwide (2020)1. Combining Welton’s formulation expertise and Lubrizol’s Apisolex excipient, Welton plans to develop a novel formulation of SN-38 to overcome its solubility challenges in water, which has hindered its clinical development. Welton seeks to develop a stable, ready-to-use formulation having higher bioavailability and shorter infusion time to enhance the clinical outcome for cancer patients. In the next 12 months, Welton will focus on advancing their lead formulation with the Apisolex excipient into nonclinical testing and developing plans for the first in-human studies.

Kevin Sill, Ph.D., Welton CEO and cofounder said, "We are thrilled to have access to both this critical excipient and the expertise of Lubrizol. We will be relying on the strong patent protection of the Apisolex excipient, coupled with supply and supporting data as we advance our product."

Request a sample of the Apisolex excipient today by visiting www.apisolex.com.

Blue Earth Therapeutics Highlights Presentations at Upcoming Society of Nuclear Medicine and Molecular Imaging (SNMMI) Annual Meeting

On June 20, 2023 Blue Earth Therapeutics, a Bracco company and emerging leader in the development of innovative next generation therapeutic radiopharmaceuticals, reported upcoming presentations by the Company and a collaborator at the Society of Nuclear Medicine and Molecular Imaging (SNMMI) Annual Meeting, to be held June 24 – 27, 2023 in Chicago, Ill (Press release, Blue Earth Therapeutics, JUN 20, 2023, View Source [SID1234632810]). Presentations on investigational clinical and preclinical studies of therapeutic applications of radiohybrid Prostate-Specific Membrane Antigen (rhPSMA) technology are being made at the conference. They include early clinical experience and a preclinical evaluation of 177Lu-rhPSMA-10.1, currently being investigated by Blue Earth Therapeutics as a potential PSMA-targeted therapeutic radiopharmaceutical candidate for the treatment of prostate cancer.

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NOTE: Currently, therapeutic radiohybrid (rh) PSMA compounds are investigational and have not received regulatory approval. Presentations noted by "*" discuss results that are investigational and are not approved by the FDA.

Investigational 177Lu-rhPSMA-10.1

Poster presentations

NOTE: Poster presentations are available Saturday, June 24, 2023, from 6:00 – 8:00 PM CT and throughout the meeting in the Science Pavilion. Times for Meet the Author sessions are below.

Monday, June 26, 2023

Title:

*Improved therapeutic index with the novel PSMA-ligand 177Lu-rhPSMA-10.1 compared to 177Lu-PSMA I&T – an intrapatient comparison

Presenter:

Ralph Bundschuh, MD, PhD, Nuclear Medicine, Faculty of Medicine, University Hospital Augsburg, Augsburg, Germany

Session Title:

MTA04-A12 Meet the Author: Oncology: Clinical Therapy & Diagnosis – Group A

Session Time:

11:15 – 11:45 AM CT

Area:

Science Pavilion Pod 12: Oncology Clinical Therapy & Diagnosis

Program ID:

346

Tuesday, June 27, 2023

Title:

*Enhanced therapeutic response to 177Lu-rhPSMA-10.1 in pre-clinical models of prostate cancer

Presenter:

Caroline Foxton, Ph.D., Blue Earth Therapeutics, Oxford, UK

Session Title:

MTA 06-B10 Meet the Author: Neurosciences/Oncology Basic & Translational – Group B

Area:

Science Pavilion Pod 10: Oncology Basic and Translational

Session Time:

1:00 – 1:30 PM CT

Program ID:

621

Blue Earth Therapeutics invites participants at the 2023 SNMMI Annual Meeting to learn more about its clinical program in the Medical Affairs information booth of its sister company, Blue Earth Diagnostics, at Booth 6025. For full session details and scientific presentation lists, please see the SNMMI online program here. Information about Blue Earth Diagnostics presence at SNMMI is available here.

About Radiohybrid Prostate-Specific Membrane Antigen (rhPSMA)

Radiohybrid Prostate-Specific Membrane Antigen (rhPSMA) compounds consist of a radiohybrid ("rh") Prostate-Specific Membrane Antigen-targeted receptor ligand which attaches to and is internalized by prostate cancer cells, and they may be radiolabeled with imaging isotopes for PET imaging, or with therapeutic isotopes for therapeutic use – providing the potential for creating a true theranostic technology. Radiohybrid technology and rhPSMA originated from the Technical University of Munich, Germany. Blue Earth Diagnostics acquired exclusive, worldwide rights to rhPSMA diagnostic imaging technology from Scintomics GmbH in 2018, and therapeutic rights in 2020, and sublicensed the therapeutic application to its sister company Blue Earth Therapeutics. Blue Earth Diagnostics received U.S. Food and Drug Administration approval for its radiohybrid PET diagnostic imaging product for use in prostate cancer in 2023. rhPSMA compounds for potential therapeutic use are investigational and have not received regulatory approval.

OSE Immunotherapeutics Receives €1.5 M in Funding from Bpifrance for the Development of a Companion Diagnostic for the Cancer Vaccine Tedopi® in Non-Small Cell Lung Cancer

On June 20, 2023 OSE Immunotherapeutics SA (ISIN: FR0012127173; Mnemo: OSE) reported that the Company has received €1.5 million in non-dilutive funding from Bpifrance – Direction Régionale de Nantes (Press release, OSE Immunotherapeutics, JUN 20, 2023, View Source [SID1234632809]). The "R&D Innovation Loan" program aims at supporting the development of a companion diagnostic for the pivotal Phase 3 clinical trial of Tedopi in NSCLC second line treatment.

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The funding from Bpifrance aims at accelerating the development of an innovative companion diagnostic test based on a simple blood sample. The companion diagnostic is a unique test for a predictive immunological biomarker to identify patients with HLA-A2 genotype who are biological responders to Tedopi. The companion diagnostic will be used for the enrolment of the patient subpopulation in the upcoming registration pivotal Phase 3 of Tedopi. The objective of this final clinical development stage is to confirm the efficacy and safety of Tedopi in second line treatment post-immune checkpoint inhibitor (ICI) failure in HLA-A2 positive NSCLC patients.

NSCLC accounts for 85% of all lung cancers and the HLA-A2 phenotype represents about 45% of the population. Based on selection of patients after ICI failure data, the targeted population for Tedopi in second line is hence considered as rare with high unmet medical needs. Up to 100,000 patients per year are estimated to potentially benefit from Tedopi in 7 major markets across the US, Europe, China and Japan. Tedopi has obtained an orphan drug status designation in the United States and is considered as a precision medicine in Europe for HLA-A2 positive patients.

Nicolas Poirier, Chief Executive Officer of OSE Immunotherapeutics, comments: "We warmly thank Bpifrance – Direction Régionale de Nantes for funding the development of this unique companion diagnostic test to accelerate the final clinical development phase of our cancer vaccine Tedopi in preparation to support the regulatory registration in advanced NSCLC for the HLA-A2 patient subpopulation".

Pfizer’s TALZENNA® in Combination with XTANDI® Receives U.S. FDA Approval

On June 20, 2023 Pfizer (NYSE: PFE) reported that the U.S. Food and Drug Administration (FDA) has approved TALZENNA (talazoparib), an oral poly ADP-ribose polymerase (PARP) inhibitor, in combination with XTANDI (enzalutamide), for the treatment of adult patients with homologous recombination repair (HRR) gene-mutated metastatic castration-resistant prostate cancer (mCRPC) (Press release, Pfizer, JUN 20, 2023, View Source [SID1234632808]). This approval is based on the statistically significant and clinically meaningful radiographic progression-free survival (rPFS) data from the Phase 3 TALAPRO-2 trial, which demonstrated a 55% reduction in the risk of disease progression or death in patients with mCRPC with prospectively identified HRR gene mutations (ATM, ATR, BRCA1, BRCA2, CDK12, CHEK2, FANCA, MLH1, MRE11A, NBN, PALB2, or RAD51C) treated with TALZENNA plus XTANDI vs placebo plus XTANDI (HR 0.45; 95% CI, 0.33–0.61; p<0.0001).

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Metastatic CRPC is a form of prostate cancer that has spread beyond the prostate gland and has progressed despite medical or surgical treatment to lower testosterone. Approximately 10-20% of patients with prostate cancer develop mCRPC within 5-7 years of diagnosis,1 and in the U.S. in 2020, approximately 60-90 thousand of the three million cases of prostate cancer were mCRPC.2 HRR gene mutations are found in approximately 25% of tumors from men with mCRPC and have been associated with aggressive disease and poor prognosis.3,4,5,6

"Despite treatment advancement in metastatic castration-resistant prostate cancer, the disease can progress quickly, and many patients may only receive one line of therapy. Therefore, new first-line treatment options are needed to reduce the risk of disease progression or death. For patients with mCRPC harboring HRR genetic alterations, outcomes are even worse," said Neeraj Agarwal, M.D., FASCO, Professor and Presidential Endowed Chair of Cancer Research at Huntsman Cancer Institute, University of Utah, and global lead investigator for TALAPRO-2. "The FDA’s approval of the talazoparib and enzalutamide combination is based on the findings from the pivotal TALAPRO-2 study, which demonstrated statistically significant and clinically meaningful reductions in the risk of progression or death among HRR gene-mutated tumors in patients with metastatic castration-resistant prostate cancer. It represents a treatment option deserving of excitement and attention."

"Pfizer has a legacy of bringing medicines to patients with genitourinary cancers and helping improve outcomes for patients suffering from advanced prostate cancer," said Angela Hwang, Chief Commercial Officer, President, Global Biopharmaceuticals Business, Pfizer. "As a global standard of care, XTANDI has shown efficacy in three types of prostate cancer, and the addition of TALZENNA demonstrated significant improvements in delaying or preventing radiographic progression-free survival or death in patients with this type of advanced prostate cancer. With today’s FDA approval of TALZENNA plus XTANDI, we are proud to be able to offer this potentially practice-changing treatment to patients and add to their options in managing this aggressive disease."

The Phase 3 TALAPRO-2 trial is a two-part, two-cohort, multicenter, randomized, double-blind, placebo-controlled study that included two patient cohorts: Cohort 1 (all-comers; n=805 and Cohort 2 (those with HRR mutations [HRRm]; n=399). The primary endpoint of the trial was rPFS, and overall survival (OS) was a key secondary endpoint. The results from the TALAPRO-2 Cohort 1 were previously reported and published in The Lancet. A trend in OS favoring TALZENNA plus XTANDI was also observed, though these data are immature. The final TALAPRO-2 OS data will be reported once the predefined number of survival events has been reached and, if appropriate, may be used to support a potential regulatory filing to benefit broader patient populations. The final OS data is expected in 2024.

The safety of TALZENNA plus XTANDI in the TALAPRO-2 trial was generally consistent with the known safety profile of each medicine. Serious adverse reactions (ARs) occurred in 30% of patients treated with TALZENNA plus XTANDI. Serious adverse reactions reported in >2% of patients included anemia (9%) and fracture (3%). Discontinuation of TALZENNA occurred in 10% of patients.

A marketing authorization application (MAA) for the TALZENNA and XTANDI combination has been accepted for review by the European Medicines Agency. Pfizer has also shared data with other regulatory agencies to support regulatory filings.

About TALZENNA (talazoparib)

TALZENNA (talazoparib) is an oral inhibitor of poly ADP-ribose polymerase (PARP), which plays a role in DNA damage repair. Preclinical studies have demonstrated that TALZENNA blocks PARP enzyme activity and traps PARP at the site of DNA damage, leading to decreased cancer cell growth and cancer cell death.

TALZENNA is approved in over 70 countries, including the U.S., as a once-daily monotherapy for the treatment of adult patients with deleterious or suspected deleterious germline breast cancer susceptibility gene (BRCA)-mutated (gBRCAm) human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer. In the U.S., TALZENNA is now approved in combination with XTANDI (enzalutamide) for the treatment of adult patients with homologous recombination repair (HRR) gene-mutated metastatic castration-resistant prostate cancer (mCRPC).

TALZENNA (talazoparib) Indication in the U.S.

TALZENNA (talazoparib) is indicated for the treatment of adult patients with deleterious or suspected deleterious germline breast cancer susceptibility gene (BRCA)-mutated (gBRCAm) human epidermal growth factor receptor 2 (HER2)-negative locally advanced or metastatic breast cancer. Select patients for therapy based on an FDA-approved companion diagnostic for TALZENNA. TALZENNA is indicated in combination with enzalutamide for the treatment of adult patients with homologous recombination repair (HRR) gene-mutated metastatic castration-resistant prostate cancer (mCRPC).

TALZENNA (talazoparib) Important Safety Information

WARNINGS and PRECAUTIONS

Myelodysplastic Syndrome/Acute Myeloid Leukemia (MDS/AML), including cases with a fatal outcome, has been reported in patients who received TALZENNA. Overall, MDS/AML has been reported in 0.4% (3 out of 788) of solid tumor patients treated with TALZENNA as a single agent in clinical studies. In TALAPRO-2, MDS/AML occurred in 2 out of 511 (0.4%) patients treated with TALZENNA and enzalutamide and in 0 out of 517 (0%) patients treated with placebo and enzalutamide. The durations of TALZENNA treatment in these five patients prior to developing MDS/AML were 0.3, 1, 2, 3, and 5 years, respectively. Most of these patients had received previous chemotherapy with platinum agents and/or other DNA damaging agents including radiotherapy.

Do not start TALZENNA until patients have adequately recovered from hematological toxicity caused by previous chemotherapy. Monitor blood counts monthly during treatment with TALZENNA. For prolonged hematological toxicities, interrupt TALZENNA and monitor blood counts weekly until recovery. If counts do not recover within 4 weeks, refer the patient to a hematologist for further investigations including bone marrow analysis and blood sample for cytogenetics. If MDS/AML is confirmed, discontinue TALZENNA.

Myelosuppression consisting of anemia, neutropenia, and/or thrombocytopenia have been reported in patients treated with TALZENNA . In TALAPRO-2, Grade ≥3 anemia, neutropenia, and thrombocytopenia were reported, respectively, in 45%, 18%, and 8% of patients receiving TALZENNA and enzalutamide. Overall, 39% of patients (199/511) required a red blood cell transfusion, including 22% (111/511) who required multiple transfusions. Discontinuation due to anemia, neutropenia, and thrombocytopenia occurred, respectively, in 7%, 3%, and 0.4% of patients.

Withhold TALZENNA until patients have adequately recovered from hematological toxicity caused by previous therapy. Monitor blood counts monthly during treatment with TALZENNA. If hematological toxicities do not resolve within 28 days, discontinue TALZENNA and refer the patient to a hematologist for further investigations including bone marrow analysis and blood sample for cytogenetics.

Embryo-Fetal Toxicity TALZENNA can cause fetal harm when administered to pregnant women. Advise male patients with female partners of reproductive potential or who are pregnant to use effective contraception during treatment with TALZENNA and for 4 months after receiving the last dose.

ADVERSE REACTIONS

Serious adverse reactions reported in >2% of patients included anemia (9%) and fracture (3%). Fatal adverse reactions occurred in 1.5% of patients, including pneumonia, COVID infection, and sepsis (1 patient each).

The most common adverse reactions (≥ 10%, all Grades), including laboratory abnormalities, for patients in the TALAPRO-2 study who received TALZENNA in combination with enzalutamide vs patients receiving placebo with enzalutamide were hemoglobin decreased (79% vs 34%), neutrophils decreased (60% vs 18%), lymphocytes decreased (58% vs 36%), fatigue (49% vs 40%), platelets decreased (45% vs 8%), calcium decreased (25% vs 11%), nausea (21% vs 17%), decreased appetite (20% vs 14%), sodium decreased (22% vs 20%), phosphate decreased (17% vs 13%), fractures (14% vs 10%), magnesium decreased (14% vs 12%), dizziness (13% vs 9%), bilirubin increased (11% vs 7%), potassium decreased (11% vs 7%), and dysgeusia (10% vs 4.5%).

Clinically relevant adverse reactions in <10% of patients who received TALZENNA with enzalutamide included abdominal pain (9%), vomiting (9%), alopecia (7%), dyspepsia (4%), venous thromboembolism (3%) and stomatitis (2%).

Based on animal studies, TALZENNA may impair fertility in males of reproductive potential.

DRUG INTERACTIONS

Coadministration with P-gp inhibitors The effect of coadministration of P-gp inhibitors on talazoparib exposure when TALZENNA is taken in combination with enzalutamide has not been studied. Monitor patients for increased adverse reactions and modify the dosage as recommended for adverse reactions when TALZENNA is coadministered with a P-gp inhibitor.

Coadministration with BCRP inhibitors Monitor patients for increased adverse reactions and modify the dosage as recommended for adverse reactions when TALZENNA is coadministered with a BCRP inhibitor. Coadministration of TALZENNA with BCRP inhibitors may increase talazoparib exposure, which may increase the risk of adverse reactions.

USE IN SPECIFIC POPULATIONS

Renal Impairment The recommended dosage of TALZENNA for patients with moderate renal impairment (CLcr 30 – 59 mL/min) is 0.35 mg taken orally once daily in combination with enzalutamide. The recommended dosage of TALZENNA for patients with severe renal impairment (CLcr 15 – 29 mL/min) is 0.25 mg taken orally once daily in combination with enzalutamide. No dose adjustment is required for patients with mild renal impairment. TALZENNA has not been studied in patients requiring hemodialysis.

Please see full U.S. Prescribing Information and Patient Information for TALZENNA (talazoparib) at www.TALZENNA.com. There may be a delay as the document is updated with the latest information. It will be available as soon as possible. Please check back for the updated full information shortly.

About XTANDI (enzalutamide) and Important Safety Information

XTANDI (enzalutamide) is an androgen receptor signaling inhibitor. XTANDI is a standard of care that has received regulatory approvals for use in men with metastatic hormone-sensitive prostate cancer (mHSPC), metastatic castration-resistant prostate cancer (mCRPC), and non-metastatic castration-resistant prostate cancer (nmCRPC) in the United States and for one or more of these indications in more than 100 countries, including the European Union and Japan. More than one million patients have been treated with XTANDI globally.7

Warnings and Precautions

Seizure occurred in 0.5% of patients receiving XTANDI in seven randomized clinical trials. In a study of patients with predisposing factors for seizure, 2.2% of XTANDI-treated patients experienced a seizure. It is unknown whether anti-epileptic medications will prevent seizures with XTANDI. Patients in the study had one or more of the following predisposing factors: use of medications that may lower the seizure threshold, history of traumatic brain or head injury, history of cerebrovascular accident or transient ischemic attack, and Alzheimer’s disease, meningioma, or leptomeningeal disease from prostate cancer, unexplained loss of consciousness within the last 12 months, history of seizure, presence of a space occupying lesion of the brain, history of arteriovenous malformation, or history of brain infection. Advise patients of the risk of developing a seizure while taking XTANDI and of engaging in any activity where sudden loss of consciousness could cause serious harm to themselves or others. Permanently discontinue XTANDI in patients who develop a seizure during treatment.

Posterior Reversible Encephalopathy Syndrome (PRES): There have been reports of PRES in patients receiving XTANDI. PRES is a neurological disorder that can present with rapidly evolving symptoms including seizure, headache, lethargy, confusion, blindness, and other visual and neurological disturbances, with or without associated hypertension. A diagnosis of PRES requires confirmation by brain imaging, preferably MRI. Discontinue XTANDI in patients who develop PRES.

Hypersensitivity reactions, including edema of the face (0.5%), tongue (0.1%), or lip (0.1%) have been observed with XTANDI in seven randomized clinical trials. Pharyngeal edema has been reported in post-marketing cases. Advise patients who experience any symptoms of hypersensitivity to temporarily discontinue XTANDI and promptly seek medical care. Permanently discontinue XTANDI for serious hypersensitivity reactions.

Ischemic Heart Disease: In the combined data of four randomized, placebo-controlled clinical studies, ischemic heart disease occurred more commonly in patients on the XTANDI arm compared to patients on the placebo arm (2.9% vs 1.3%). Grade 3–4 ischemic events occurred in 1.4% of patients on XTANDI versus 0.7% on placebo. Ischemic events led to death in 0.4% of patients on XTANDI compared to 0.1% on placebo. Monitor for signs and symptoms of ischemic heart disease. Optimize management of cardiovascular risk factors, such as hypertension, diabetes, or dyslipidemia. Discontinue XTANDI for Grade 3–4 ischemic heart disease.

Falls and Fractures occurred in patients receiving XTANDI. Evaluate patients for fracture and fall risk. Monitor and manage patients at risk for fractures according to established treatment guidelines and consider use of bone-targeted agents. In the combined data of four randomized, placebo-controlled clinical studies, falls occurred in 11% of patients treated with XTANDI compared to 4% of patients treated with placebo. Fractures occurred in 10% of patients treated with XTANDI and in 4% of patients treated with placebo.

Embryo-Fetal Toxicity: The safety and efficacy of XTANDI have not been established in females. XTANDI can cause fetal harm and loss of pregnancy when administered to a pregnant female. Advise males with female partners of reproductive potential to use effective contraception during treatment with XTANDI and for 3 months after the last dose of XTANDI.

Adverse Reactions (ARs)

In the data from the four randomized placebo-controlled trials, the most common ARs (≥ 10%) that occurred more frequently (≥ 2% over placebo) in XTANDI-treated patients were asthenia/fatigue, back pain, hot flush, constipation, arthralgia, decreased appetite, diarrhea, and hypertension. In the bicalutamide-controlled study, the most common ARs (≥ 10%) reported in XTANDI-treated patients were asthenia/fatigue, back pain, musculoskeletal pain, hot flush, hypertension, nausea, constipation, diarrhea, upper respiratory tract infection, and weight loss.

In AFFIRM, the placebo-controlled study of metastatic CRPC (mCRPC) patients who previously received docetaxel, Grade 3 and higher ARs were reported among 47% of XTANDI-treated patients. Discontinuations due to adverse events (AEs) were reported for 16% of XTANDI-treated patients. In PREVAIL, the placebo-controlled study of chemotherapy-naive mCRPC patients, Grade 3–4 ARs were reported in 44% of XTANDI patients and 37% of placebo patients. Discontinuations due to AEs were reported for 6% of XTANDI-treated patients. In TERRAIN, the bicalutamide-controlled study of chemotherapy-naive mCRPC patients, Grade 3–4 ARs were reported in 39% of XTANDI patients and 38% of bicalutamide patients. Discontinuations with an AE as the primary reason were reported for 8% of XTANDI patients and 6% of bicalutamide patients.

In PROSPER, the placebo-controlled study of non-metastatic CRPC (nmCRPC) patients, Grade 3 or higher ARs were reported in 31% of XTANDI patients and 23% of placebo patients. Discontinuations with an AE as the primary reason were reported for 9% of XTANDI patients and 6% of placebo patients.

In ARCHES, the placebo-controlled study of metastatic CSPC (mCSPC) patients, Grade 3 or higher AEs were reported in 24% of XTANDI-treated patients. Permanent discontinuation due to AEs as the primary reason was reported in 5% of XTANDI patients and 4% of placebo patients.

Lab Abnormalities: Lab abnormalities that occurred in ≥ 5% of patients, and more frequently (> 2%) in the XTANDI arm compared to placebo in the pooled, randomized, placebo-controlled studies are neutrophil count decreased, white blood cell decreased, hyperglycemia, hypermagnesemia, hyponatremia, and hypercalcemia.

Hypertension: In the combined data from four randomized placebo-controlled clinical trials, hypertension was reported in 12% of XTANDI patients and 5% of placebo patients. Hypertension led to study discontinuation in < 1% of patients in each arm.

Drug Interactions

Effect of Other Drugs on XTANDI Avoid strong CYP2C8 inhibitors, as they can increase the plasma exposure to XTANDI. If co-administration is necessary, reduce the dose of XTANDI. Avoid strong CYP3A4 inducers as they can decrease the plasma exposure to XTANDI. If co-administration is necessary, increase the dose of XTANDI.

Effect of XTANDI on Other Drugs Avoid CYP3A4, CYP2C9, and CYP2C19 substrates with a narrow therapeutic index, as XTANDI may decrease the plasma exposures of these drugs. If XTANDI is co-administered with warfarin (CYP2C9 substrate), conduct additional INR monitoring.

Please see Full Prescribing Information for additional safety information.

Accutar Biotechnology Announces First Patient Dosed with AC0676 in Phase 1 Study in Patients with Relapsed/Refractory B-cell Malignancies

On June 20, 2023 Accutar Biotechnology, Inc., a biotechnology company focusing on artificial intelligence (AI)-empowered drug discovery, reported the dosing of the first patient in a Phase 1 study of AC0676, an orally bioavailable, chimeric degrader molecule designed to target and degrade Bruton’s Tyrosine Kinase (BTK) with high potency, selectivity, and broad mutant coverage (Press release, Accutar Biotechnology, JUN 20, 2023, View Source [SID1234632807]).

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"The initiation of this study distinguishes Accutar as the first company to successfully bring oral chimeric degraders against three different targets into the clinic," said Jie Fan, Ph.D., Chief Executive Officer of Accutar Biotechnology, Inc. "Leveraging our protein crystallography and AI-empowered PPI-TAC (Protein-Protein Interaction Targeting Chimera) platforms, AC0676 was designed to potently and selectively degrade both wildtype BTK and BTK mutations that confer drug resistance to both covalent and non-covalent BTK inhibitors, including but not limited to C481S and kinase dead mutations such as L528W. We are excited about the differentiated therapeutic profile of AC0676 and its broad potential to treat patients with B-cell malignancies."

The purpose of the Phase 1 multi-center, open-label study is to assess the safety, tolerability, pharmacokinetics, and preliminary anti-tumor activity of AC0676 treatment in patients with relapsed/refractory B-cell malignancies, including Chronic Lymphocytic Leukemia (CLL), Small Lymphocytic Lymphoma (SLL), non-GCB Diffuse Large B-cell Lymphoma (DLBCL), Mantle Cell Lymphoma (MCL), Follicular Lymphoma (FL), , Marginal Zone Lymphoma (MZL), or Waldenström Macroglobulinemia (WM). Additional information on this clinical trial can be found on www.clinicaltrials.gov (NCT05780034).

About AC0676

AC0676 is an investigational orally bioavailable, chimeric degrader of Bruton’s Tyrosine Kinase (BTK) for the potential treatment of relapsed/refractory B-cell malignancies. In preclinical studies, AC0676 has demonstrated potent and selective BTK protein degradation with broad coverage of BTK wildtype and mutants (including C481S, L528W, and others), favorable pharmacological properties, as well as promising anti-tumor activity in animal models.