Varubi (rolapitant oral) / OPKO Health, TerSera Therap, GSK - LARVOL DELTA

The efficacy and safety of Fosrolapitant and Palonosetron Hydrochloride for Injection with or without Dexamethasone in the prevention of nausea and vomiting induced by immune checkpoint inhibitors combined with chemotherapy in patients with advanced non-small cell lung cancer (ChiCTR) - P4 | N=132 | Not yet recruiting | Sponsor: Shanghai Pulmonary Hospital; Shanghai Pulmonary Hospital

Checkpoint inhibition • New P4 trial • Chemotherapy-Induced Nausea and Vomiting • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor

Fosrolapitant and Palonosetron for the Prevention of Antibody-drug Conjugate-induced Nausea and Vomiting (clinicaltrials.gov) - P2 | N=124 | Not yet recruiting | Sponsor: Peking University Cancer Hospital & Institute

New P2 trial • Oncology

Tradipitant (Nereus) for motion sickness. (PubMed, Med Lett Drugs Ther) - No abstract available

Journal

Pharmacokinetics, safety, and population pharmacokinetic profiles of Ritanine® in Chinese subjects with impaired or normal liver function: a Phase I trial. (PubMed, Front Pharmacol) - "Ritanine (HR20013) is a fixed-dose combination of fosrolapitant (218 mg, a rolapitant prodrug) and palonosetron (0.25 mg), designed to enhance rolapitant's solubility and reduce allergic reactions associated with intravenous administration. Moderate hepatic impairment has a minimal impact on the pharmacokinetics of Ritanine, suggesting that no dosage adjustment is necessary for patients with moderate hepatic impairment in clinical practice. http://www.chinadrugtrials.org.cn, identifier CTR20233771."

Clinical • Journal • P1 data • PK/PD data • Allergy • Hepatology

Deubiquitinases in lung cancer: Oncogenic mechanisms, metabolic reprogramming, immune evasion, and therapeutic targeting. (PubMed, Pathol Res Pract) - "In LSCC, USP28 stabilizes c-MYC, ΔNp63, and SREBP2; in LUAD, USP22 emerges as an integrative node coupling proliferation, EZH2-mediated MHC-I silencing, PD-L1 stabilization, and ferroptosis resistance; and in SCLC, USP1 mediates NK-cell evasion and MAST1-dependent cisplatin resistance, whereas USP13 sustains FASN-dependent cancer stem cell states. Therapeutic strategies are evolving from small-molecule inhibitors (GNE-6776, AZ1, and SJB2-043) to OTUB1-recruiting deubiquitinase-targeting chimeras (DUBTACs), DCAF-based PROTACs, and repurposed agents (rolapitant, ixazomib, and chidamide). Most evidence remains preclinical; substrate redundancy, validated biomarkers, and selectivity challenges must be addressed before DUB-directed strategies can be translated into biomarker-stratified combination therapies."

IO biomarker • Journal • Review • Lung Adenocarcinoma • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Small Cell Lung Cancer • Solid Tumor • Squamous Cell Carcinoma • Targeted Protein Degradation • CTNNB1 • FASN • KRAS • MYC • OTUB1 • PD-L1 • USP1 • USP13 • USP22 • USP25 • USP7 • VTCN1

Randomized, double-blind phase 3 trial of the fixed-dose combination fosrolapitant/palonosetron (HR20013) plus dexamethasone for prevention of nausea and vomiting in patients receiving moderately emetogenic chemotherapy. (ASCO 2026) - P3 | "In pts receiving MEC, a single dose of fixed-dose combination HR20013 plus DEX was well tolerated and demonstrated superior efficacy in preventing CINV compared to the standard regimen of PALO+DEX, with improved patient-reported outcomes. This single-dose, dual-pathway antiemetic offers a more effective and convenient prophylactic option for MEC."

Clinical • P3 data • Chemotherapy-Induced Nausea and Vomiting • Constipation • Dyslipidemia • Gastroenterology • Gastrointestinal Disorder • Hypertriglyceridemia • Solid Tumor

The Efficacy and Safety of Fosrolapitant and Palonosetron Hydrochloride for Injection in Preventing Nausea and Vomiting Caused by Multi-cycle Immunotherapy and Chemotherapy in Patients With Esophageal Cancer and Lung Cancer (clinicaltrials.gov) - P2 | N=120 | Recruiting | Sponsor: Second Affiliated Hospital, School of Medicine, Zhejiang University

New P2 trial • Esophageal Cancer • Lung Cancer • Oncology • Solid Tumor

An Exploratory Study on Efficacy and Safety of Fosaprepitant and Palonosetron Hydrochloride for Injection in Preventing CINV From Multi-Agent HEC (clinicaltrials.gov) - P4 | N=200 | Recruiting | Sponsor: Shanghai 6th People's Hospital | Not yet recruiting ➔ Recruiting

Enrollment open • Chemotherapy-Induced Nausea and Vomiting

Observational Study of Fosrolapitant and Palonosetron Hydrochloride for Injection for the Prevention of Treatment-Related Nausea and Vomiting in Cancer Patients (ChiCTR) - P=N/A | N=300 | Sponsor: Shanghai General Hospital; Shanghai General Hospital

New trial • Chemotherapy-Induced Nausea and Vomiting • Gastrointestinal Cancer • Oncology

An Exploratory Study on Efficacy and Safety of Fosaprepitant and Palonosetron Hydrochloride for Injection in Preventing CINV From Multi-Agent HEC (clinicaltrials.gov) - P4 | N=200 | Not yet recruiting | Sponsor: Shanghai 6th People's Hospital

New P4 trial • Chemotherapy-Induced Nausea and Vomiting

A Cohort Study on the Prevention of Nausea and Vomiting Induced by Concurrent Chemoradiotherapy for Lung Cancer Using Rolapitant and Palonosetron (clinicaltrials.gov) - P=N/A | N=238 | Not yet recruiting | Sponsor: Henan Cancer Hospital

New trial • Lung Cancer • Oncology • Solid Tumor

The dual role of OTUD3 in cancer: mechanisms and therapeutic implications. (PubMed, Cancer Cell Int) - "The development of OTUD3-targeted inhibitors like Rolapitant, Rupatadine, and OTUDin3 shows promise in preclinical models, particularly in combination with immunotherapy. However, its tissue-specific duality poses both challenges and opportunities for therapeutic intervention. Further research is needed to elucidate OTUD3's mechanistic networks and advance its clinical translation as a prognostic biomarker and therapeutic target in precision oncology."

IO biomarker • Journal • Review • Oncology • Ovarian Cancer • Solid Tumor • Targeted Protein Degradation • HSPA5 • PD-L1 • PTEN • YY1

HR20013, a fixed-dose intravenous combination of fosrolapitant and palonosetron, for the prevention of cisplatin-induced nausea and vomiting: putting the PROFIT trial into perspective. (PubMed, Ann Palliat Med) - No abstract available

Journal • Chemotherapy-Induced Nausea and Vomiting

Virtual screening of drugs against multiple targets of Alzheimer's disease. (PubMed, J Alzheimers Dis) - "BackgroundDrug repurposing offers a rapid, cost-effective approach for discovering therapies against multiple targets.ObjectiveHere, we screen virtual ligand libraries consisting of 3468 approved drugs against 11 protein targets associated with Alzheimer's disease (AD).MethodsWe employ blind molecular docking, and target amyloid-β (Aβ), microtubule-associated protein tau (MAPT), Apolipoprotein E4 (APOE4), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), amyloid-β protein precursor (AβPP), β-secretase (BACE1), brain-derived neurotrophic factor (BDNF), presenilin 1 (PSEN1) and 2 (PSEN2), and α-synuclein (SNCA) proteins using AutoDock Vina.ResultsNotably, multitarget binding recurs among the top-10 ligands with Ergotamine and Dihydroergotamine potentially binding 8; Dutasteride 7; Drospirenone and Nilotinib 6; Adapalene and Conivaptan 5; Bromocriptine 4; and Rolapitant, Irinotecan, Plerixafor, Saquinavir, and Telmisartan 3, out of 11 protein targets. Likewise,..."

Journal • Alzheimer's Disease • Cardiovascular • CNS Disorders • Hypertension • Inflammation • Pain • APOE • BDNF • MAPT • SNCA

Fosrolapitant/Palonosetron: First Approval. (PubMed, Drugs) - "On the 29th of May 2025, fosrolapitant/palonosetron received its first approval in China for the prevention of acute and delayed nausea and vomiting caused by highly emetogenic chemotherapy in adults. This article summarizes the milestones in the development of fosrolapitant/palonosetron leading to this first approval in chemotherapy-induced nausea and vomiting."

Journal • Chemotherapy-Induced Nausea and Vomiting

Pharmacokinetics, safety, and efficacy of mixed formulation of fosrolapitant and palonosetron (HR20013) in combination with dexamethasone in patients with solid tumors scheduled for highly emetogenic cisplatin-based chemotherapy: a phase I trial. (PubMed, BMC Med) - P1 | "HR20013 plus dexamethasone had a favorable PK profile, manageable safety, and durable antiemetic efficacy."

Journal • P1 data • PK/PD data • Constipation • Gastroenterology • Gastrointestinal Disorder • Oncology • Solid Tumor

Phase II randomized glioma study to evaluate efficacy and satisfaction of rolapitant plus ondansetron in preventing chemoradiation-induced nausea and vomiting. (PubMed, Neurooncol Pract) - "In patients receiving radiation with concurrent temozolomide, chemoradiation-induced nausea; vomiting (cRINV) rates are 35% and 26%, respectively, which reduce quality of life, treatment adherence, and cancer control. Although not a positive study, less vomiting occurred with rolapitant/ondansetron. While patients prefer ondansetron monotherapy, most perceived better effectiveness with rolapitant/ondansetron."

Journal • P2 data • Brain Cancer • Glioblastoma • Glioma • High Grade Glioma • Oncology • Solid Tumor

Randomized, Phase III Trial of Mixed Formulation of Fosrolapitant and Palonosetron (HR20013) in Preventing Cisplatin-Based Highly Emetogenic Chemotherapy-Induced Nausea and Vomiting: PROFIT. (PubMed, J Clin Oncol) - "HR20013 + DEX was noninferior to FAPR + PALO + DEX for preventing HEC-CINV and well tolerated, with the potential to reduce the impact of CINV on daily life."

CINV • Journal • P3 data • Chemotherapy-Induced Nausea and Vomiting

Overcoming amphotericin B resistance in Candida auris using the antiemetic drug rolapitant. (PubMed, Antimicrob Agents Chemother) - "Moreover, rolapitant enhanced the in vivo activity of AmB in a mouse model of disseminated C. auris infection, as the combination reduced the fungal burden in murine kidneys by ~1 log (~90%) colony forming units. Our findings warrant further investigation of using rolapitant to overcome AmB resistance in C. auris and other fungal species."

Journal • Infectious Disease

Rolapitant treats lung cancer by targeting deubiquitinase OTUD3. (PubMed, Cell Commun Signal) - "In summary, the present study identifies Rolapitant as a novel inhibitor of deubiquitinase OTUD3 and establishes that the OTUD3-GRP78 axis is a potential therapeutic target for lung cancer."

Journal • Lung Cancer • Oncology • Solid Tumor • Targeted Protein Degradation • HSPA5 • TNFRSF10B

Prophylactic Neurokinin-1 Receptor Antagonist Use Pre- and Post- Choosing Wisely Initiative among Women with Breast Cancer (SABCS 2023) - "All approved antiemetics - aprepitant, fosaprepitant, rolapitant, and netupitant/palonosetron) were included. This study highlights a significant but modest decline in the inappropriate use of prophylactic NK1-RAs after the implementation of CW antiemetic recommendation. Continued statewide or local educational efforts for dissemination of CW recommendations are needed to facilitate appropriate prophylactic use of NK1-RAs. Adjusted* Interrupted Time Series Segmented Regression Analysis of Prophylactic NK1-RA use among women with breast cancer before and after the Choosing Wisely initiative *Adjusted for insurance, health plan type, age, comorbidity, and emetic risk"

Clinical • Breast Cancer • Oncology • Solid Tumor

Homology modeling, virtual screening, molecular docking, and ADME approaches to identify a potent agent targeting NK2R protein. (PubMed, Biotechnol Appl Biochem) - "Molecular docking was performed using a library of 910 structurally similar molecules to four NK1R antagonists: aprepitant, casopitant, fosaprepitant, and rolapitant. The evaluation of the in silico ADME profile, solubility, and permeability of the ligand molecules has revealed that the small molecules are potentially nontoxic and have the chance of exhibiting biological activity after oral administration. Further experimental studies (in vitro and in vivo assays) are required to evaluate the effectiveness of these inhibitors as therapeutic targets."

Journal • Asthma • Immunology • Inflammation • Pulmonary Disease • Respiratory Diseases

Simulation of drug-drug interactions between breast cancer chemotherapeutic agents and antiemetic drugs. (PubMed, Daru) - "It is critical to recognize that these interactions can get amplified in cancer patients because of the severity of the disease and chemotherapy toxicities. Clinicians need to be aware of the DDI likelihood of the drug combinations used in BCa treatment."

Journal • Breast Cancer • Chemotherapy-Induced Nausea and Vomiting • Oncology • Solid Tumor • CYP3A4

Predictors of Neurokinin-Receptor Antagonist (NK1-RA) Overuse Among Women with Breast Cancer (ISPOR 2023) - "We included all approved NK1-RAs: aprepitant, fosaprepitant, rolapitant, and netupitant/palonosetron. A little less than 10% of patients with breast cancer initiating low/minimal/moderate emetic risk chemotherapy were prescribed NK1-RAs. Variability in NK1-RAs overuse was driven by certain patient and healthcare related factors. Continued education about these recommendations is important to achieve value-based cancer care."

Clinical • Breast Cancer • Oncology • Solid Tumor

Phase II randomized study to evaluate efficacy and satisfaction of rolapitant plus ondansetron vs. ondansetron monotherapy in preventing nausea/vomiting for gliomas receiving radiation/temozolomide. (SNO 2022) - "While patients prefer ondansetron monotherapy, there was no difference in cRINV-CR between the first 2-week treatments and some had less vomiting with rolapitant plus ondansetron. We will present overall N/V results."

Clinical • Monotherapy • P2 data • Brain Cancer • Constipation • Fatigue • Gastroenterology • Gastrointestinal Disorder • Glioblastoma • Glioma • Oncology • Solid Tumor