FAP-2286
A cyclic peptide that carries radiation to the scar-like support cells around many solid tumours
FAP-2286 is a ring-shaped peptide that grabs fibroblast activation protein (FAP), found on the support cells that surround many cancers. With gallium-68 attached it lights tumours up on a PET scan; with lutetium-177 attached it delivers radiation to them. Early trials in pancreatic, breast, lung and other advanced cancers have reported, and the LuMIERE trial set a phase 2 dose in 2026, but it is not approved anywhere. It is used only in hospital nuclear medicine units.
Used in human trials: 3.70, 5.55, 7.40 or 9.25 GBq; 9.25 GBq chosen for phase 2, Every 6 weeks, Intravenous (Lutetium-177 FAP-2286, LuMIERE phase 1 (27 patients)) Details ↓
Recommended Dosing
Used in human trials
No manufacturer dose exists for this use: these are amounts given in published trials, not recommendations.
What is it?
A radioligand pairs a homing molecule with a radioactive atom. The homing part finds a target that is common in a tumour and rare in healthy tissue; the atom then either shows up on a scan or delivers radiation where the drug has gathered. Gallium-68, a positron emitter, is used for PET imaging; lutetium-177, a beta emitter whose particles travel a few millimetres, is used for treatment. Doctors usually scan with the gallium version first and treat only if the tumours light up, the approach called theranostics.
FAP-2286 aims at fibroblast activation protein (FAP), an enzyme on the surface of cancer-associated fibroblasts. These are the support cells that build the dense, scar-like tissue around many solid tumours, including pancreatic, breast, colon and bile-duct cancers and sarcomas. Normal adult tissues carry little FAP, which is what makes it attractive. Earlier FAP tracers (the FAPI series) are small molecules that image well but wash out of tumours relatively quickly, a drawback when the aim is treatment. FAP-2286 instead uses a cyclic peptide joined to a DOTA chelator, and in mice it stayed in tumours longer than FAPI-46 and slowed the growth of FAP-positive tumours and sarcoma grafts.
As an imaging agent it has done well. In 64 patients with 15 cancer types, gallium-68 FAP-2286 PET showed every primary tumour and found more involved lymph nodes (98% against 85%) and bone and organ metastases (95% against 67%) than standard FDG PET, with results similar to FAPI-46. It had particular value where FDG is weak: cancers of the stomach, pancreas and liver, peritoneal spread, small lymph nodes in bladder cancer, and bone metastases in breast cancer. The radiation dose of a scan was about 0.0116 mSv per MBq, similar to other FAP tracers.
As a treatment the evidence is early. The first 11 patients, treated in Germany in 2022 with a mean 5.8 GBq, tolerated it with three grade 3 events and showed long tumour retention. In the multicentre phase 1 part of LuMIERE, 27 heavily pretreated patients received 3.70 to 9.25 GBq every 6 weeks; there were two dose-limiting toxicities, one partial response and ten with stable disease, and 9.25 GBq was chosen for phase 2. Chinese single-centre series report disease control in some patients with lung cancer, pleural metastases and pancreatic cancer, with few severe side effects, but most tumours eventually progressed, and in 14 patients with gut cancers only 4 had stable disease.
Clovis Oncology developed FAP-2286 in the clinic; when it filed for bankruptcy in December 2022 it agreed to sell the programme to Novartis. It is not approved by FDA or any other regulator checked, and the European Medicines Agency has no record of it. ClinicalTrials.gov lists LuMIERE and a US imaging study, and a phase 2 trial in cancer of unknown primary. Like every radioligand it is made in a radiopharmacy shortly before use and given only by nuclear medicine staff; there is nothing to buy.
Mechanism of Action
FAP-2286 binds fibroblast activation protein on cancer-associated fibroblasts and carries a radioactive metal in its DOTA chelator for imaging or therapy.
FAP binding
Its cyclic peptide binds recombinant and cell-surface FAP with high affinity; FAP binding matched FAP expression in human tumour samples (preclinical study).
Longer tumour retention
Built to stay in tumours longer than small-molecule FAP inhibitors, which is what a therapy isotope needs (preclinical study and 2026 review).
Radiation to the tumour bed
Lutetium-177 FAP-2286 irradiates the fibroblast-rich tissue and nearby cancer cells; bone metastases received about 3 Gy per GBq in the first patients.
Clearance
Cleared through the kidneys; the bladder wall receives the highest organ dose from the gallium-68 form (dosimetry study).
Published Research
Studies of FAP-2286 labelled with gallium-68 or lutetium-177, read from their PubMed abstracts. Fluorine-18 versions built on a different chelator and other modified FAP-2286 derivatives are different molecules and are not carded.
First-in-human therapy
Eleven patients with advanced pancreatic, breast, rectal or ovarian adenocarcinoma received a mean 5.8 GBq (2.4-9.9 GBq). Kidneys received about 1.0 and red marrow 0.05 Gy per GBq, bone metastases about 3.0; there were no grade 4 events and three grade 3 events (pancytopenia, leukopenia, pain flare), and three patients reported less pain.
LuMIERE phase 1
Of 35 patients scanned, 27 received 3.70, 5.55, 7.40 or 9.25 GBq every 6 weeks for up to six cycles. Two dose-limiting toxicities occurred (grade 4 lymphopenia, grade 3 haemoptysis); one patient had a partial response and ten stable disease. The recommended phase 2 activity is 9.25 GBq.
Against FDG and FAPI-46
In 64 patients with 15 cancer types, gallium-68 FAP-2286 showed all 46 primary tumours (FDG missed 9), 98% of involved nodes against 85%, and 95% of bone and organ metastases against 67%. In 19 patients it matched gallium-68 FAPI-46.
Imaging dosimetry
Forty-six patients given about 219 MBq had the highest uptake in sarcoma, cholangiocarcinoma and colon cancer and the lowest in lung and testicular cancer. The effective dose was 0.0116 mSv per MBq, with the bladder wall most exposed, and uptake beat FDG in six cancer types.
Bladder cancer imaging
In 21 patients with muscle-invasive or metastatic urothelial cancer, it found 54 lesions, many of them lymph nodes under 1 cm; lesions averaged SUVmax 9.9 against 4.2 on FDG, and the scan changed management for three patients.
Pleural and peritoneal spread
In 92 patients with suspected pleural or peritoneal metastases, it was more sensitive than FDG PET (95% against 85%), especially for peritoneal disease and for gut, liver, pancreatic and other adenocarcinomas.
Breast cancer imaging and therapy
In 20 women with recurrent or metastatic breast cancer it found more lesions than FDG (85% against 71%), notably liver and bone metastases. Four received one cycle of the lutetium-177 version; none had grade 3/4 events and three had stable disease at 4 months.
Advanced lung cancer therapy
In a prospective study of 9 patients, 44% had a partial metabolic response, median overall survival was 10 months and progression-free survival 6 months; breathlessness and pain improved and no grade 3/4 toxicity was seen.
Pleural metastases
Seventeen pretreated patients received a median of two cycles. Disease was controlled in 59%, median survival was 17.3 months (20.3 with disease control against 6.4 without) and progression-free survival 4.1 months, with no grade 3/4 events.
Gastrointestinal cancers
In a prospective single-arm trial, 14 patients with FAP-positive gut cancers completed 30 cycles. Four had stable disease and ten progressed (disease control 29%); there were no grade 3/4 events, only transient nausea, vomiting and diarrhoea.
Refractory pancreatic cancer
In 22 patients given 34 cycles as salvage therapy, disease control was 41% overall, median survival 127 days and progression-free survival 109 days. Grade 3 blood toxicity occurred in 2, no grade 4 events occurred, and pain scores and performance status improved.
PET response after two cycles
In 30 patients after two cycles, 20% had a partial response, 37% stable disease and 43% progression. A fall of less than 30% in gallium-68 FAP-2286 SUVmax was linked to longer progression-free (10.3 against 4.4 months) and overall survival.
Preclinical evaluation
FAP-2286 and its metal complexes bound human FAP strongly. In mice, gallium-68, indium-111 and lutetium-177 forms went quickly to FAP-positive tumours and stayed, cleared through the kidneys, and the lutetium-177 form slowed tumour growth, outlasting FAPI-46 in tumour retention.
From laboratory to clinic
A review describes FAP-2286 as a FAP-binding peptide joined to DOTA that keeps the imaging qualities of small-molecule FAP inhibitors while staying in tumours much longer, and summarises the preclinical and early clinical results for imaging and therapy.
Dosing Data
FAP-2286 has no approved label. The rows below are administered activities, the radioactivity injected, from the published human studies carded above: a single gallium-68 dose for PET, or lutetium-177 treatment cycles.
Educational information, not medical advice. Each dose above is tagged with its source: an approved label, a published human study, animal data, or amounts reported by users. None is a recommendation for you. An unapproved compound has no established safe or effective human dose, and products sold for “research use only” are not made or tested for people. Talk to a doctor before acting on anything on this site, including before you start, stop or change any medicine or dose. Full medical disclaimer.
What a Buyer Needs to Know
What is sold, how it is mixed, stored and taken, and what is known about its safety, quality and legal status. Each part names its source. Where we have none, it says unknown.
What is sold
Unknown: we hold no regulator's label that says in what form FAP-2286 is supplied. It is a radioactive drug: the next part says where it is prepared and given.
Mixing a vial: a worked example
Nothing to mix at home, and no syringe units to work out: FAP-2286 is a radioactive drug, prepared and given in nuclear-medicine departments, and its dose is an amount of radioactivity (MBq or GBq), not a weight.
This page's dosing note: “FAP-2286 is dosed by radioactivity and labelled in a radiopharmacy shortly before injection; no reconstitution maths applies.”
Source: this page's own note in Dosing Data below; the amount of each dose row in Dosing Data below.
Storage before and after mixing
Unknown: no label on file says how FAP-2286 is stored. It is a radioactive drug held by the nuclear-medicine department that prepares and gives it (see the part above); the home rules for a mixed vial in the mixing guide do not apply to it.
How it is taken
As it was given in human studies: Intravenous (Every 6 weeks; Lutetium-177 FAP-2286, LuMIERE phase 1 (27 patients)).
Source: Used in human trials: the route and frequency of each row in Dosing Data below.
What to expect, and when
How long it stays in the body: not established by a measurement cited on this entry.
How long the doses were given: Lutetium-177 FAP-2286, LuMIERE phase 1 (27 patients): Up to 6 cycles; Lutetium-177 FAP-2286, first-in-human (11 patients): 1 or more cycles; Gallium-68 FAP-2286 PET (46 patients): Scan at 60 minutes.
When effects appear: unknown; no source on this page gives a time to effect for FAP-2286. Results reported in the studies are under Published Research.
Source: Used in human trials, the duration of each row in Dosing Data below.
Side effects, and when to stop or get help
From the Side Effects section: Falls in blood counts, including grade 3 pancytopenia or leukopenia in early patients and grade 4 lymphopenia in one LuMIERE patient; Pain flare after treatment; haemoptysis (coughing blood) in one patient at 9.25 GBq; Nausea, vomiting and diarrhoea, usually transient; Liver test changes in about a quarter of patients in one pancreatic cancer series. Full list and cautions ↓
When to stop or get help: unknown; no label or trial on file sets rules for stopping FAP-2286. Treat a severe or unexpected reaction as a reason to stop and see a doctor.
Source: the Side Effects section below (“From the studies above”).
Interactions
Unknown: a PubMed search for human interaction studies of FAP-2286 (reviewed 2026-10-28) found none. Unknown is not the same as safe to combine.
Every peptide's record, with its source: the interaction matrix.
Checking what you bought
Unknown: no published independent test of FAP-2286 products is in our lab-results database yet, so how products sold under this name measure up is not known.
To read a certificate of analysis, paste it into the COA decoder; it checks the measured mass against FAP-2286's expected mass, 1,470.8 Da, from this entry's molecular data. Trust & Verification explains what independent testing can and cannot show.
Legal status
US: In Clinical Trials (Not approved: no Drugs@FDA record (openFDA, searched October 29, 2026) and none in the EMA medicines list). Sport: Prohibited (S0 catch-all).
Country by country ↓ · Regulatory tracker
Source: this entry's approval status and the WADA Prohibited List, as in Legal Status below.
Side Effects & Contraindications
Reported Side Effects
From the studies above.
Contraindications & Cautions
No approved label exists, so there are no official contraindications. Points from the studies above:
Legal Status
FAP-2286 is investigational in every jurisdiction checked.
Frequently Asked Questions
?What does FAP-2286 target?
Fibroblast activation protein, an enzyme on the support cells (fibroblasts) that build the dense tissue around many solid tumours. Healthy adult tissue has little of it.
?How is it different from FAPI tracers?
FAPI tracers are small molecules that wash out of tumours relatively quickly. FAP-2286 is a cyclic peptide designed to stay longer, which matters when the attached isotope is meant to treat rather than just image.
?Does it work as a treatment?
It is too early to say. Phase 1 found it tolerable and chose a dose for phase 2, and small series report disease control in some patients, but most advanced tumours progressed and there are no randomised results.
?Is it approved?
No. It is investigational everywhere checked, with trials registered in the US and studies in China and Germany.
?Can I buy it?
No. It is a radioactive drug made in a radiopharmacy and given only by nuclear medicine staff to selected patients.
References
- [other] PubChem CID 163408889 (synonyms FAP-2286, rofapitide tetraxetan): formula C67H99N13O18S3, molecular weight 1470.8. Read October 28, 2026. https://pubchem.ncbi.nlm.nih.gov/compound/163408889
- [registry] ClinicalTrials.gov API v2, read October 28, 2026: NCT04939610 (LuMIERE, phase 1/2); NCT04621435 (phase 1, imaging of solid tumours, recruiting); NCT07434180 (phase 2, carcinoma of unknown primary, not yet recruiting).
- [other] Clovis Oncology, press release (Business Wire), December 11, 2022: Clovis files for Chapter 11 protection and enters into an agreement to sell FAP-2286 to Novartis. Read October 29, 2026.
- [other] US FDA, Drugs@FDA (openFDA): no application for FAP-2286 or rofapitide. European Medicines Agency medicines list: no record. Searched October 29, 2026.
- [pubmed] Baum RP, et al. "Feasibility, Biodistribution, and Preliminary Dosimetry in Peptide-Targeted Radionuclide Therapy of Diverse Adenocarcinomas Using (177)Lu-FAP-2286: First-in-Humans Results." J Nucl Med, 2022;63(3):415-423. PMID: 34168013.
- [clinical-trial] McConathy J, et al. "Targeting Fibroblast Activation Protein with [177Lu]Lu-FAP-2286 in Patients with Advanced Solid Tumors in the Phase I LuMIERE Trial." Clin Cancer Res, 2026;32(17):3757-3767. PMID: 42223513.
- [pubmed] Pang Y, et al. "PET Imaging of Fibroblast Activation Protein in Various Types of Cancer Using (68)Ga-FAP-2286: Comparison with (18)F-FDG and (68)Ga-FAPI-46 in a Single-Center, Prospective Study." J Nucl Med, 2023;64(3):386-394. PMID: 36215571.
- [pubmed] Kline B, et al. "(68)Ga-FAP-2286 PET of Solid Tumors: Biodistribution, Dosimetry, and Comparison with (18)F-FDG." J Nucl Med, 2024;65(6):938-943. PMID: 38697672.
- [pubmed] Koshkin VS, et al. "Initial Experience with (68)Ga-FAP-2286 PET Imaging in Patients with Urothelial Cancer." J Nucl Med, 2024;65(2):199-205. PMID: 38212070.
- [pubmed] Liu H, et al. "Comparison of the diagnostic value of [(68)Ga]Ga-FAP-2286 PET/CT and [(18)F]-FDG PET/CT imaging in different types of pleural and peritoneal metastatic tumors." Eur J Nucl Med Mol Imaging, 2025;52(11):3990-4000. PMID: 40272499.
- [pubmed] Liu W, et al. "Comparative evaluation of [(68)Ga]Ga-FAP-2286 and [(18)F]FDG PET/CT in breast cancer and initial experience with [(177)Lu]Lu-FAP-2286 therapy." Eur J Nucl Med Mol Imaging, 2026;53(6):3749-3759. PMID: 41553532.
- [clinical-trial] Xie Y, et al. "Efficacy and Safety Evaluation of 177Lu-FAP-2286 in the Treatment of Advanced Lung Cancer." Clin Nucl Med, 2024;49(9):830-837. PMID: 39102810.
- [pubmed] Li L, et al. "Initial Results and Clinical Experiences of [(177)Lu]Lu-FAP-2286 for Pleural Metastases: A Single-Center Retrospective Study." J Nucl Med, 2026;67(4):548-554. PMID: 41571431.
- [clinical-trial] Bai X, et al. "A preliminary study on the safety and efficacy of (177)Lu-FAP-2286 in gastrointestinal tumours with positive FAP expression." Radiother Oncol, 2025;213:111195. PMID: 41052603.
- [pubmed] Xu T, et al. "177 Lu-FAP-2286 Targeted Radionuclide Therapy in Advanced Pancreatic Cancer : A Real-World Retrospective Salvage Study." Clin Nucl Med, 2026;51(11):980-990. PMID: 42545179.
- [pubmed] Fan M, et al. "Posttreatment ⁶⁸Ga-FAP-2286 PET/CT Parameters for Response and Survival Assessment After ¹⁷⁷Lu-FAP-2286 Radioligand Therapy in Advanced Solid Tumors." Clin Nucl Med, 2026;51(10):877-884. PMID: 42397089.
- [pubmed] Zboralski D, et al. "Preclinical evaluation of FAP-2286 for fibroblast activation protein targeted radionuclide imaging and therapy." Eur J Nucl Med Mol Imaging, 2022;49(11):3651-3667. PMID: 35608703.
- [review] Liu H, et al. "The Current Status of Radionuclide Tumor Targeting Diagnosis and Therapy Based on FAP-2286: From Preclinical Studies to Clinical Application." Mol Diagn Ther, 2026;30(2):281-293. PMID: 41582290.
Sources & Citations
Studies were read from their PubMed abstracts on October 29, 2026; regulatory status from Drugs@FDA (openFDA), the EMA medicines list and ClinicalTrials.gov, and the December 2022 sale from Clovis Oncology's announcement, read October 28-29, 2026. The formula is PubChem's.
Medical Disclaimer: This content is for educational and informational purposes only. It is not medical advice, and nothing here is an instruction to obtain or use any compound. Talk to a licensed clinician about your own situation.