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

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

ROLAPITANT FOR THE PREVENTION OF NAUSEA IN PATIENTS RECEIVING CISPLATIN- OR CARBOPLATIN-BASED CHEMOTHERAPY: ALTERNATIVE METHODS FOR EVALUATING NAUSEA (MASCC-ISOO 2017) - P3; "...To evaluate the effects of rolapitant and RM on efficacy assessments for nausea in the phase 3 trials of rolapitant + 5-hydroxytryptamine type 3 (5-HT3) receptor antagonist (RA) + dexamethasone versus control (placebo + 5-HT3 RA + dexamethasone) for CINV prevention...Rolapitant reduced nausea incidence and RM use in patients receiving cisplatin or carboplatin. RM use did not confound these results."

Clinical • Retrospective data • Biosimilar • Oncology

Rolapitant as an Antiemetic in Malignant Glioma Patients Receiving Radiotherapy and Temozolomide (clinicaltrials.gov) - P2 | N=47 | Completed | Sponsor: Duke University | Suspended ➔ Completed | N=160 ➔ 47 | Trial completion date: Apr 2023 ➔ Jun 2022 | Trial primary completion date: Mar 2023 ➔ May 2022

Enrollment change • Monotherapy • Trial completion • Trial completion date • Trial primary completion date • CNS Tumor • Glioma • Oligodendroglioma • Oncology • Solid Tumor

Morphological and Skeletal Abnormalities Induced by Rolapitant: An Antiemetic Agent. (PubMed, Cureus) - "Conclusion Rolapitant is toxic when taken in large doses and for an extended period. As a result, rolapitant should be taken only when a valid diagnosis has been established and only at the recommended dose, not at a larger dose or for an extended period of time."

Journal • Chemotherapy-Induced Nausea and Vomiting • Oncology

Virtual Screening for FDA-Approved Drugs That Selectively Inhibit Arginase Type 1 and 2. (PubMed, Molecules) - "Most notable are the antihypertensive drugs candesartan, irbesartan, indapamide, and amiloride, the antiemetic rolapitant, the anti-angina ivabradine, and the antidiabetic metformin which have minimal side effects. The partial validation also favors the idea that the other half of the top 30 potential drugs could be used in therapeutic settings. The three categories greatly expand the selectivity of arginase inhibition."

FDA event • Journal • Cardiovascular • CNS Disorders • Hypotension • Infectious Disease • Movement Disorders • Nephrology • Oncology • Parkinson's Disease • Renal Disease • ARG2

Switching indication of PEGylated lipid nanocapsules-loaded with rolapitant and deferasirox against breast cancer: Enhanced in-vitro and in-vivo cytotoxicity. (PubMed, Life Sci) - "The in-vivo pharmacodynamics effect of the developed nano-formulations showed superior antitumor effect for the individual drugs rather than their combinations as compared to the control group. The current study confirmed the potential of RP and DFO nanoforms as promising therapeutic agents for BC treatment."

Journal • Preclinical • Breast Cancer • Oncology • Solid Tumor

Neurokinin-1 receptor antagonist rolapitant suppresses anxiety and alcohol intake produced by repeated withdrawal episodes. (PubMed, FEBS J) - "Rolapitant did not affect basal voluntary alcohol intake, but significantly suppressed anxiety-like behavior and alcohol consumption following withdrawal episodes. Our findings suggest that rolapitant should be further investigated as a novel treatment option for relapse prevention in alcohol-dependent patients."

Journal • Addiction (Opioid and Alcohol) • Mood Disorders • Psychiatry

"Varubi" (@shycollie)

New repurposed rolapitant in nanovesicular systems for lung cancer treatment: Development, in-vitro assessment and in-vivo biodistribution study. (PubMed, Eur J Pharm Sci) - "The in-vivo biodistribution results proved the high lung deposition potential of RP-LNVs with a considerable safety. Besides, the developed RP-LNVs were able to reach the metastatic organs of lung cancer, hence they were proven promising as a possible treatment modality for lung cancer."

Journal • Preclinical • Lung Cancer • Oncology • Solid Tumor

Antiemetics for adults for prevention of nausea and vomiting caused by moderately or highly emetogenic chemotherapy: a network meta-analysis. (PubMed, Cochrane Database Syst Rev) - "This field of supportive cancer care is very well researched. However, new drugs or drug combinations are continuously emerging and need to be systematically researched and assessed. For people receiving HEC, synthesised evidence does not suggest one superior treatment for prevention and control of chemotherapy-induced nausea and vomiting.  For people receiving MEC, synthesised evidence does not suggest superiority for treatments including both NK₁ and 5-HT₃ inhibitors when compared to treatments including 5-HT₃ inhibitors only. Rather, the results of our NMA suggest that the choice of 5-HT₃ inhibitor may have an impact on treatment efficacy in preventing CINV.  When interpreting the results of this systematic review, it is important for the reader to understand that NMAs are no substitute for direct head-to-head comparisons, and that results of our NMA do not necessarily rule out differences that could be..."

Journal • Retrospective data • Review • Chemotherapy-Induced Nausea and Vomiting • Hematological Disorders • Hematological Malignancies • Oncology • Solid Tumor

Combinations Offer Multiple Treatment Options in Relapsed/Refractory Multiple Myeloma (Targeted Oncology) - "During a Targeted Oncology Case-Based Roundtable event, Joshua Richter, MD...discussed the case of a 78-year-old woman with multiple myeloma."

Regulatory

"I had to do a ton of support meds. Aloxi, dex, Varubi plus dex for 4 days and I’d still feel horrible. Nausea and exhausted. But alive." (@CANsurvive)

Rolapitant as an Antiemetic in Malignant Glioma Patients Receiving Radiotherapy and Temozolomide (clinicaltrials.gov) - P2; N=160; Recruiting; Sponsor: Duke University; Trial completion date: Apr 2021 ➔ Apr 2023; Trial primary completion date: Mar 2021 ➔ Mar 2023

Clinical • Monotherapy • Trial completion date • Trial primary completion date • Glioma • Oligodendroglioma • Oncology • Solid Tumor