Delving into the Latest Updates on Nintedanib esylate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

CYNEDIV, Intedanib, Nintedanib DPI

+ [24]

Target

CSF-1R x FGFRs x FLT3 x PDGFRs x VEGFR

Action

antagonists, inhibitors

Mechanism

CSF-1R antagonists(Colony stimulating factor 1 receptor antagonists), FGFRs antagonists(Fibroblast growth factor receptors antagonists), FLT3 inhibitors(Tyrosine-protein kinase receptor FLT3 inhibitors)

Therapeutic Areas

NeoplasmsRespiratory DiseasesOther Diseases+ [7]

Active Indication

Locally Advanced Lung Non-Small Cell Carcinomametastatic non-small cell lung cancerRecurrent Non-Small Cell Lung Cancer+ [24]

Inactive Indication

Adenocarcinoma of large intestineAdvanced Colorectal AdenocarcinomaAdvanced Hepatocellular Carcinoma+ [46]

Originator Organization

Boehringer Ingelheim International GmbH

Active Organization

Boehringer Ingelheim GmbH

Meilaipu (Beijing) Pharmaceutical Research Co., Ltd.Boehringer Ingelheim Pharma GmbH & Co., KG

+ [14]

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

United States (15 Oct 2014),

Idiopathic Pulmonary Fibrosis

RegulationFast Track (United States), Orphan Drug (United States), Priority Review (China), Special Review Project (China), Orphan Drug (South Korea), Orphan Drug (Australia), Breakthrough Therapy (United States), Orphan Drug (Japan)

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Structure/Sequence

Molecular FormulaC33H39N5O7S

InChIKeyMMMVNAGRWOJNMW-FJBFXRHMSA-N

CAS Registry656247-18-6

Fibrotic hypersensitivity pneumonitis (f-HP) is an interstitial lung disease in which various antigens in susceptible individuals may play a pathogenetic role. This study evaluates the role of transbronchial lung cryobiopsy (TBLC) and bronchoalveolar lavage (BAL) in identifying a UIP-like pattern and its association with fibrosis progression. We conducted a multicentre retrospective cohort study of patients diagnosed with f-HP who underwent BAL and TBLC between 2011 and 2023. A UIP-like pattern was defined by the presence of (A) patchy fibrosis and fibroblastic foci or (B) honeycombing ± (A). We investigated BAL's role in predicting UIP-like patterns within a clinical-radiological-serological framework, examining disease progression in these patients using spirometry and mortality data. A total of 195 patients were enrolled, 59 (30%) of whom exhibited a UIP-like pattern. These patients showed greater lung function decline, lower BAL lymphocytosis (14.4% vs. 37.4%, p < 0.001), higher nintedanib prescription (35% vs. 14%, p < 0.001), and higher 10-year mortality (HR 2.8, 95% CI 1.3-5.8, p = 0.004). f-HP patients with a UIP-like pattern exhibit worse clinical outcomes and higher mortality. In cases of low BAL lymphocytosis with a high pre-test clinical suspicion of f-HP, lung biopsy may not be necessary as it increases the likelihood of identifying a UIP-like pattern.

01 Dec 2025·LUNG

Continued Treatment with Nintedanib in Patients with Progressive Pulmonary Fibrosis: Data from INBUILD-ON

Article

Author: Chaudhuri, Nazia ; Dumistracel, Mihaela ; Varone, Francesco ; Antin-Ozerkis, Danielle ; Cottin, Vincent ; Wuyts, Wim A ; Song, Jin Woo ; Coeck, Carl ; Miede, Corinna ; Bonella, Francesco

PURPOSE:

In the INBUILD trial in patients with progressive pulmonary fibrosis (PPF), nintedanib slowed the decline in forced vital capacity (FVC) versus placebo, with a safety profile characterised mainly by gastrointestinal events. INBUILD-ON, the open-label extension of INBUILD, assessed the safety of nintedanib during longer-term treatment. Data on FVC were collected.

STUDY DESIGN AND METHODS:

Adverse events and changes in FVC in INBUILD-ON were assessed descriptively in all patients and in two subgroups: patients who received nintedanib in INBUILD and continued nintedanib in INBUILD-ON ("continued nintedanib" group) (n = 212) and patients who received placebo in INBUILD and initiated nintedanib in INBUILD-ON ("initiated nintedanib" group) (n = 222). Changes in FVC were based on observed values.

RESULTS:

Median exposure to nintedanib in INBUILD-ON was 22.0 months. Diarrhoea was the most frequent adverse event. Amongst patients who had diarrhoea, 90.0% experienced only events of mild or moderate severity. Adverse events led to discontinuation of nintedanib at a rate of 16.7 per 100 patient-years. Serious and fatal adverse events were reported at rates of 37.2 and 9.5 per 100 patient-years. Mean (SE) changes in FVC from baseline to week 48 were - 71.6 (16.1) mL [- 128.5 (25.5) mL in continued nintedanib group (n = 106), - 14.8 (18.2) mL in initiated nintedanib group (n = 106)].

CONCLUSION:

The safety profile of nintedanib in INBUILD-ON was consistent with that in INBUILD. Change in FVC in INBUILD-ON was consistent with decline in FVC in the nintedanib group of INBUILD. These results support the use of nintedanib in the long-term treatment of PPF.

CLINICAL TRIAL REGISTRATION:

ClinicalTrials.gov; NCT03820726; registered January 29, 2019.

01 Aug 2025·COLLOIDS AND SURFACES B-BIOINTERFACES

Nintedanib loaded iron (III) chelated melanin nanoparticles as an MRI-visible antifibrotic drug delivery system

Article

Author: Ayan, Bugra ; Baysoy, Engin ; Bayrak, Emirhan ; Saygili, Ecem ; Kaleli-Can, Gizem ; Özcan, Alpay ; Bayir, Ece

Idiopathic pulmonary fibrosis (IPF) is a fatal, progressive lung disease characterized by extensive scarring and thickening of lung tissue that leads to respiratory failure. Early and accurate diagnosis is crucial for monitoring disease progression and assessing therapeutic efficacy. While imaging modalities such as radiological X-rays and high-resolution computed tomography (HRCT) are commonly employed, magnetic resonance imaging (MRI) offers significant advantages, including superior soft tissue contrast and the absence of ionizing radiation. However, in lung MRIs are hindered by short transverse relaxation times, low proton density, and motion artifacts which is addressed herein by developing theranostic platform combining MRI imaging with targeted drug delivery using melanin nanoparticles conjugated with nintedanib (MNP-NIN). Chelation with ferric ions (MNP-NIN-Fe³⁺) enhanced MRI visibility enabling non-invasive imaging and drug tracking. MNP-NIN and MNP-NIN-Fe³ ⁺ nanoparticles were built with mean diameters of 189 ± 44 nm and 182 ± 35 nm, respectively and demonstrating successful NIN conjugation. Controlled NIN release followed zero-order kinetics over 36 days. MNP conjugation reduced cytotoxicity in BEAS-2B and A549 cells improving the drug's safety. MRI experiments conducted with a 7.0 T animal scanner demonstrated enhanced imaging contrast with MNP-NIN-Fe solutions compared to saline underscoring their potential for localized visualization and tracking within lung tissues. By integrating MRI diagnostics and targeted drug delivery, the MNP-NIN-Fe³ ⁺ system offers a promising solution to overcome current challenges in IPF management. This theranostic platform addresses the limitations of conventional imaging techniques while providing an innovative strategy for reducing drug-related systemic side effects and improving therapeutic efficacy.

142

News (Medical) associated with Nintedanib esylate

15 Apr 2025

·www.biospace.com

Boehringer Ingelheim Boosts I&I Portfolio With $357M in Biobucks for Cue

iStock, Mininyx Doodle At the heart of the licensing deal is CUE-501, a bispecific molecule that can selectively deplete B cells to address autoimmune and inflammatory conditions. Boehringer Ingelheim is fronting $12 million to license Cue Biopharma’s investigational B cell depletion therapy for autoimmune diseases, the German biopharma announced on Monday. The star of this back-heavy, multi-year deal is Cue’s CUE-501, a preclinical bispecific molecule that works by binding to a specific protein found on the surface of B cells. At the same time, CUE-501 also engages and activates a specific subset of killer T cells, selectively depleting B cells to suppress autoimmunity and inflammation. According to the biotech’s website , CUE-501 sidesteps the systemic activation of all T cells, which “may offer significant advantages over current cell therapy-based strategies.” For the right to develop and commercialize CUE-501, Boehringer Ingelheim is pledging up to $345 million in research, development and commercial milestones, on top of the $12 million upfront payment. Cue will also be entitled to royalties on net sales of CUE-501. In exchange for this investment, Cue will leverage its platform technologies to further develop CUE-501. Both parties may also expand the partnership to include other anti-B cell bispecifics for autoimmune indications, according to Monday’s release. Carine Boustany, Boehringer Ingelheim’s global head of Immunology and Respiratory Disease Research, said in a statement that Monday’s licensing deal is a “strategic expansion” of the company’s portfolio in the autoimmune and inflammatory space, allowing it to “deliver a more effective treatment option to patients earlier in their disease journey.” Boehringer’s immunology and inflammatory portfolio is anchored by the oral kinase inhibitor Ofev, indicated for idiopathic pulmonary fibrosis (IPF). In 2024, sales of Ofev jumped 7% to rake in approximately $4.26 billion. Meanwhile, the pharma’s asthma drug Spiriva remained one of its top sellers, with more than $1.8 billion in sales last year, despite dipping roughly 17% from the previous year. Additionally, in September 2024, Boehringer Ingelheim reported that its drug candidate nerandomilast aced the Phase III FIBRONEER-IPF study, showing significant lung function benefits in patients with IPF. At the time, the pharma revealed plans to approval application for the drug in this indication, though a specific timeline was not provided. Beyond I&I, Boehringer Ingelheim has also signed several deals in the past year. In January, the pharma entered two antibody-focused partnerships —one with Lonza’s Synaffix and another with Oxford BioTherapeutics—in oncology. In July 2024, Boehringer Ingelheim dropped $1.3 billion to acquire Nerio Therapeutics and its small molecule assets that can “reshape” the immune system to target tumors.

License out/inPhase 3AcquisitionImmunotherapyCell Therapy

02 Apr 2025

·www.fiercepharma.com

Amid uncertainty in the US, Boehringer Ingelheim projects 'slight' revenue increase for '25

Boehringer Ingelheim is projecting a "slight" revenue increase in 2025 but admitted its estimates are clouded by uncertainty over the U.S. regulatory environment and potential U.S. tariffs for pharmaceutical products. Boehringer Ingelheim picked a challenging day to reveal its 2024 financial results and guidance for this year.With President Donald Trump announcing his plan on tariffs on Wednesday and uncertainty surrounding if and how they will affect the export of pharmaceutical products to the U.S., the German company is treading lightly with its projection of a “slight year-on-year increase” in revenue.“We don't even know whether there are going to be tariffs,” Chairman Hubertus von Baumbach said on Wednesday morning during the company’s annual press conference.There are other uncertainties in the U.S. for Boehringer, which is the largest privately-owned company in the industry and has overtaken Bayer as Germany’s top seller of pharmaceuticals.For one, the drugmaker has two key products under review by the FDA, both of which Boehringer hopes to launch in the second half of this year. But with the U.S. regulator in a state of flux, von Baumbach said he isn’t sure “to what extent it will impact our ability to register products.”“All we have is the information that people are being laid off,” he added. “Like in the case of tariffs, let’s wait and see.” As for 2024, Boehringer’s revenue reached 26.8 billion euros ($29 billion), which was a 4.7% increase and a 6.1% bump at constant exchange rates.Jardiance continued as Boehringer’s top product, generating revenue of 8.4 billion euros ($9.1 billion), which was up by 15%. Sales of the aging diabetes medicine have been boosted in recent years by its approval to treat heart failure. However, that momentum is slowing after Boehringer reported increases for Jardiance of 39% in 2022 and 30% in 2023.Boehringer’s second-leading product, Ofev saw a 9% bump in sales to 3.8 billion euros ($4.1 billion). With the company losing patent protection for the idiopathic pulmonary fibrosis treatment by the end of this decade, it is banking on follow-on nerandomilast, which is under review in the U.S. and Europe. Boehringer also hopes to launch zongertinib this year. It would be the first orally administered, targeted therapy for previously treated HER2-mutated lung cancer patients.“As our current pipeline continues to mature and more products come closer to a potential market introduction, we have entered a pivotal phase of high investments,” von Baumbach said in a release, referring to Boehringer’s pharma R&D investment figure of 5.7 billion euros ($6.2 billion), which was 28% of the division’s sales.

01 Apr 2025

·www.globenewswire.com

Avalyn Completes Successful Phase 1 Clinical Trials of AP02, its Novel Inhaled Formulation of Nintedanib, Preparing for Phase 2 Development in Idiopathic Pulmonary Fibrosis

Topline data from the single- and multiple-ascending dose studies confirmed safety and favorable tolerability profile of AP02 at all dose levels Full safety, tolerability, and pharmacokinetics data to be presented at the American Thoracic Society 2025 International Conference in May 2025 Company plans to advance AP02 into a Phase 2 clinical trial in patients with idiopathic pulmonary fibrosis (IPF) CAMBRIDGE, Mass., April 01, 2025 (GLOBE NEWSWIRE) -- Avalyn Pharma Inc., a clinical-stage biopharmaceutical company developing inhaled therapies for the treatment of life-threatening pulmonary diseases, today announced that AP02 (inhaled nintedanib) was safe and well tolerated in multiple single-ascending dose (SAD) and multiple-ascending dose (MAD) Phase 1 clinical trials in healthy adult volunteers and patients with idiopathic pulmonary fibrosis (IPF). IPF is largely untreatable and characterized by scarring of lung tissue, decline in lung function, and reduced exercise capacity and quality of life. There is a clear need to bring treatment options to patients that maximize therapeutic impact while minimizing systemic exposure and transform the disease from a fatal diagnosis into a manageable condition. The most recently completed Phase 1 trial enrolled a total of 60 healthy adult volunteers and consisted of a single-ascending dose (SAD) portion, which assessed AP02 at 2.0 mg, 4.0 mg, and 8.0 mg once-daily (QD); a multi-ascending dose (MAD) portion that evaluated twice-daily (BID) dosing of AP02 at the same dose levels over a seven-day treatment period; and a bronchoalveolar lavage (BAL) portion, which assessed lung exposure following a single 4.0 mg AP02 dose across three timepoints. “We are excited to complete this innovative set of clinical trials for AP02, where we assessed lung exposure in both studies of the inhaled compared to oral nintedanib,” said Lyn Baranowski, Chief Executive Officer of Avalyn. “Through its enhanced drug delivery directly to the lungs, our approach allows us to address the underlying pathophysiology of the disease and positions AP02 as a potential future standard-of-care for patients with IPF.” The company expects to present full topline data from two Phase 1 studies, including safety, tolerability, and pharmacokinetics at the American Thoracic Society 2025 International Conference in May 2025. Based on these results, Avalyn plans to advance AP02 into a Phase 2 clinical program for patients with idiopathic pulmonary fibrosis (IPF). About Avalyn Pharma Avalyn is reimagining the future of pulmonary fibrosis treatment with a pipeline of new inhaled formulations of approved medicines designed to reduce systemic exposure and deliver medication directly to the site of disease. Pulmonary fibrosis is characterized by scarring of lung tissue, decline in lung function, and reduced exercise capacity and quality of life, and is associated with increased mortality. Currently approved therapeutic options slow pulmonary fibrosis progression but are associated with significant toxicities that restrict their use and dosing. Avalyn’s inhaled approach tackles the underlying pathophysiology of pulmonary fibrosis at its source and is designed to reduce systemic exposure and deliver medication directly to the site of disease. Avalyn’s lead program, AP01, is an optimized inhaled formulation of pirfenidone, currently being studied in the ongoing MIST Phase 2b study in progressive pulmonary fibrosis (PPF). AP01 has been assessed in over 150 individuals with different forms of pulmonary fibrosis and demonstrated clinical proof-of-concept with improved efficacy and safety compared to historical data with existing therapies. The company completed two Phase 1 studies for its second program, AP02, inhaled nintedanib, for the treatment of idiopathic pulmonary fibrosis (IPF). For more information, please visit avalynpharma.com and follow us on LinkedIn. Investor Contact:Alex Straus, THRUST alex@thrustsc.comir@avalynpharma.com Media Contact:media@avalynpharma.com

Phase 1Phase 2

100 Deals associated with Nintedanib esylate

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External Link

KEGG	Wiki	ATC	Drug Bank
D10396 D10481	Nintedanib esylate	L01XE31	DB09079

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Locally Advanced Lung Non-Small Cell Carcinoma	Australia	Boehringer Ingelheim Pty Ltd.	01 Sep 2015
metastatic non-small cell lung cancer	Australia	Boehringer Ingelheim Pty Ltd.	01 Sep 2015
Recurrent Non-Small Cell Lung Cancer	Australia	Boehringer Ingelheim Pty Ltd.	01 Sep 2015
Interstitial lung disease due to systemic disease	European Union	Boehringer Ingelheim International GmbH	14 Jan 2015
Interstitial lung disease due to systemic disease	Iceland	Boehringer Ingelheim International GmbH	14 Jan 2015
Interstitial lung disease due to systemic disease	Liechtenstein	Boehringer Ingelheim International GmbH	14 Jan 2015
Interstitial lung disease due to systemic disease	Norway	Boehringer Ingelheim International GmbH	14 Jan 2015
Progressive fibrotic interstitial lung disease	European Union	Boehringer Ingelheim International GmbH	14 Jan 2015
Progressive fibrotic interstitial lung disease	Iceland	Boehringer Ingelheim International GmbH	14 Jan 2015
Progressive fibrotic interstitial lung disease	Liechtenstein	Boehringer Ingelheim International GmbH	14 Jan 2015
Progressive fibrotic interstitial lung disease	Norway	Boehringer Ingelheim International GmbH	14 Jan 2015
Adenocarcinoma of Lung	European Union	Boehringer Ingelheim International GmbH	21 Nov 2014
Adenocarcinoma of Lung	Iceland	Boehringer Ingelheim International GmbH	21 Nov 2014
Adenocarcinoma of Lung	Liechtenstein	Boehringer Ingelheim International GmbH	21 Nov 2014
Adenocarcinoma of Lung	Norway	Boehringer Ingelheim International GmbH	21 Nov 2014
Idiopathic Pulmonary Fibrosis	United States	Boehringer Ingelheim Pharmaceuticals, Inc.	15 Oct 2014

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Chronic interstitial lung disease	NDA/BLA	European Union	Accord Healthcare SLU	22 Feb 2024
Lung Diseases, Interstitial	NDA/BLA	United States	Boehringer Ingelheim GmbH	25 Jul 2023
Pterygium	Phase 3	United States	Cloudbreak Therapeutics LLCStartup	30 Jun 2022
Pterygium	Phase 3	China	Cloudbreak Therapeutics LLCStartup	30 Jun 2022
Pterygium	Phase 3	Australia	Cloudbreak Therapeutics LLCStartup	30 Jun 2022
Pterygium	Phase 3	India	Cloudbreak Therapeutics LLCStartup	30 Jun 2022
Pterygium	Phase 3	New Zealand	Cloudbreak Therapeutics LLCStartup	30 Jun 2022
Scleroderma	Phase 3	United States	Boehringer Ingelheim International GmbH	05 Dec 2017
Scleroderma	Phase 3	Japan	Boehringer Ingelheim International GmbH	05 Dec 2017
Scleroderma	Phase 3	Argentina	Boehringer Ingelheim International GmbH	05 Dec 2017

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03820726 (INBUILD-ON, Pubmed \| Lung)	Phase 3	Progressive fibrotic interstitial lung disease	-	Continued Nintedanib	bgejihbmgs(vobffewoex) = Diarrhoea was the most frequent adverse event. Amongst patients who had diarrhoea, 90.0% experienced only events of mild or moderate severity fjldtukmim (yzenekrsnt ) View more	Positive	01 Dec 2025
NCT02496585 (CTgov)	Phase 2	Radiation Pneumonitis \| Secondary malignant neoplasm of lung	34	prednisone+nintedanib (Nintedanib + Prednisone)	ywcxjrojdc = wmnqjcrjww wvtvfbfcys (edsiywpbuo, xaqwifiuci - oqgshrwlod) View more	-	16 Apr 2025
				Placebo+prednisone (Placebo + Prednisone)	ywcxjrojdc = nlxpsdayjb wvtvfbfcys (edsiywpbuo, wvdztvfolp - ciwwvaoghq) View more
NCT03377023 (CTgov)	Phase 1/2	metastatic non-small cell lung cancer	66	Ipilimumab+Nivolumab+Nintedanib (Phase 1-Dose Escalation)	xzuepsucmn = trilgmqnih ykjadmdusp (rvsyekdzgj, anchkefjxs - kjkxkczebo)	-	25 Mar 2025
				ipilimumab+Nivolumab+Nintedanib (Phase 2 - Arm A)	emmupzkpqp = vxjovoygxb fryhwvrrnt (bguxlxbnsw, ajxzlpxppy - rdjorjkyow) View more
Literature Manual	Phase 2	HER2-negative breast cancer	111	nintedanib	ayibahmliu(vcqcymrgsq): P-Value = 0.37	Positive	11 Oct 2024
				paclitaxel
NCT02863055 (EORTC-08112-LCG, ESMO2024) Manual	Phase 2	Malignant Pleural Mesothelioma Maintenance	37	Nintedanib 200mg BID	ulzfpsdkoz(usbhsllyqg) = jchkzgfjqm zforbfeiib (mebgxatkul ) View more	Negative	14 Sep 2024
				Placebo	ulzfpsdkoz(usbhsllyqg) = hoowzbyfmx zforbfeiib (mebgxatkul ) View more
ESMO2024 Manual	Not Applicable	Non-Small Cell Lung Cancer Third line \| Second line	173	Docetaxel with Nintedanib (D+N)	kwzuwxhggt(abzouzgmxk) = plovtczyes tpzbffovtf (asjubzcxrp ) View more	Negative	14 Sep 2024
				Docetaxel with Ramucirumab (D+R)	kwzuwxhggt(abzouzgmxk) = yifsaiwnwx tpzbffovtf (asjubzcxrp ) View more
NCT02902484 (ESMO_GI2024) Manual	Phase 1	Pancreatic Cancer	13	Nintedanib combination with chemotherapy gemcitabine (Gem) and nab-paclitaxel (Nab-P)	yxpzanadkz(pcesbniltw) = nintedanib was 200 mg twice daily dtgkzkbrtb (tfphiwndsh ) View more	Positive	27 Jun 2024
EULAR2024	Not Applicable	Lung Diseases, Interstitial	67	Nintedanib 150mg twice daily	bapllrnbtw(wuednzojmk) = Adverse events led to NINTE withdrawal in 13 patients dzoupctsis (duvrmfpnod ) View more	Positive	05 Jun 2024
NCT02902484 (CTgov)	Phase 1/2	Pancreatic Cancer	14	Nab-paclitaxel+gemcitabine+nintedanib (All Participants)	aynpxrtfzo = dyervmyqxb sgydioeutt (ulmwttlcqr, cqrwjkwaid - isjikhsdmt)	-	03 Jun 2024
				Nintedanib (Nintedanib 150 mg)	gdhekimrur(cuopmlkbgo) = cctjzrpdng wwkvgqszdr (szyhthvqbp, gyninrbtfa - swkbnotxzd) View more
NCT02299141 (pilot study of nintedanib, Pubmed)	Phase 2	Advanced Lung Non-Small Cell Carcinoma TP53 \| VEGFR1-3 \| PDGFR-A ... View more	20	Nintedanib 200 mg	hnxlkxhpvi(wuidwaxozy) = wcseqedhtp krkvpocxwe (rspbmsqdsc ) View more	Positive	01 Jun 2024