Certepetide_Dosage, benefits & legal status
Also known as CEND-1, LSTA1, iRGD, LM-161, certepetide acetate
It does not attack the tumor. It binds integrins to trigger a transport pathway that carries other drugs inside.
Common vial size is what vendors typically sell, not a recommendation. Enter your own vial in the calculator.
What is Certepetide?
Plain language first. The technical label stays, but it never stands alone.Overview
It is a door opener rather than a drug that kills cancer cells. Pushed into a vein between the two chemotherapy drugs, it is meant to make the tumor's own tissue carry the chemotherapy inward. In a 158-patient pancreatic cancer trial run in Australia and New Zealand, the larger cohort missed the primary endpoint outright, with a progression-free survival hazard ratio of 0.96 and a p-value of 0.85. A smaller second cohort that added a dose four hours later reached a hazard ratio of 0.60 (95% CI 0.34 to 1.07, p=0.08) in 42 patients against 21, and its own investigators call that cohort exploratory and not powered to test a hypothesis.
Certepetide is a nine-residue cyclic peptide, CRGDKGPDC, closed by a disulfide bond between its two cysteines. Also known as CEND-1, LSTA1 and iRGD, it binds alpha-v integrins on tumor blood vessels, is then cleaved by a protease, and the cleaved fragment binds neuropilin-1 to switch on a transport pathway through tumor tissue.
What it's used for
An experimental add-on to chemotherapy for pancreatic cancer and other solid tumors, given in trials only. It is not a treatment by itself and is not approved anywhere.
How does Certepetide work?
What it does in the body, and where.Certepetide is the mirror image of how integrin drugs usually work. Cilengitide, already on this site, blocks alpha-v integrins to starve a tumor's blood vessels. Certepetide binds the same receptors on purpose, to be cut apart and start a delivery route.
- 01RGD binds the tumor's blood vesselsThe RGD motif at the center of the ring is the grip point cells use to hold onto the proteins around them. It binds alpha-v beta-3 and alpha-v beta-5 integrins. Those sit on the lining of tumor blood vessels far more than on healthy ones.
- 02A protease cuts the peptideOnce bound, the peptide is cleaved. The published pharmacology does not name the protease responsible.
- 03The fragment binds neuropilin-1 and opens a routeThe cut fragment binds neuropilin-1. That receptor drives movement across the vessel wall and switches on a transport pathway through the tumor tissue itself. Drugs given at the same time can travel that route. In mice, labeled peptide cleared out of most healthy tissues within three hours, the kidney and bladder excepted, while staying in tumors, and none reached the brain.
What else is it used for?
Each group carries its own evidence level.Approved means regulators have cleared it for that purpose. Investigational means it is in trials. Early research means it is being studied and is not established.
Cohort A, the one with full numbers
Investigational- Human trial66 patients received certepetide and 29 placebo, on top of gemcitabine and nab-paclitaxel.
- Human trialMedian progression-free survival was 5.5 months in each arm, hazard ratio 0.96 (95% CI 0.60 to 1.53), log-rank p=0.85. Progression-free survival is this trial's registered primary endpoint, so this cohort missed it.
- Human trialThe 6-month progression-free rate was 49.0% against 40.8%, with overlapping confidence intervals, and the response rate 38.3% against 26.9%, including four complete responses on certepetide.
- Human trialMedian overall survival was 12.42 months against 9.72, a gap of nearly three months, with a hazard ratio of 0.95 (95% CI 0.56 to 1.60) at p=0.82. That survival figure is the one the company leads with, and it did not reach significance either.
- No dataThe presenting author's own summary was that certepetide is safe despite showing no improvement in 6-month progression-free survival, with the survival and response signals warranting further investigation.
Cohort B, the one being quoted
Investigational- Human trialCohort B randomized 63 patients two to one, 42 on certepetide and 21 on placebo, and added a second dose four hours after the first.
- Human trialThe 6-month progression-free rate was 60.8% (95% CI 44.1 to 73.9) against 25.0% (95% CI 9.1 to 44.9), and median progression-free survival 7.5 against 4.7 months. The hazard ratio was 0.60 (95% CI 0.34 to 1.07) at p=0.08, short of significance.
- Human trialThe response rate was 45.2% against 19.0%, disease control 85.9% against 61.9%, and median overall survival 10.3 against 9.2 months.
- No dataThe abstract states that cohort B is exploratory and not powered to test a specific hypothesis. Twenty-one placebo patients is a small comparison group, and that is why its 6-month confidence interval runs from 9.1% all the way to 44.9%.
- Human trialSevere side effects were more common on certepetide: grade 3 to 5 events in 88% against 77%, grade 3 to 4 neutropenia 34.3% against 28.6%, and low platelets 19% against 14.3%.
- No dataBoth cohorts come from the same 158-patient trial, so the contrast between them is a comparison of two dosing schedules rather than two separate studies.
The headline numbers people quote are cohort B's: a 6-month progression-free rate of 60.8% against 25.0%. Both cohorts' full statistics are published, and neither reached significance. Cohort A, the larger one at 66 against 29, had a progression-free hazard ratio of 0.96 at p=0.85, and its presenting author said plainly that there was no improvement in 6-month progression-free survival. Cohort B reached 0.60 at p=0.08 in 42 patients against 21, and its own abstract calls that cohort exploratory and not powered to test a hypothesis. The overall survival figure of 12.42 against 9.72 months in cohort A is the one the company leads with; its hazard ratio is 0.95 at p=0.82. The trial is also widely called phase 2b; the registry calls it phase 2, and it is led by an Australian trials group rather than by Lisata. Certepetide and iRGD are the same molecule, not a peptide and its analog.
The published record
Papers and trials about Certepetide
267 papers tagged human · 243 not reviews or lab · 1 clinical trial publications
8 registered trials · 1 with posted results
Furthest stage reached: Phase 2, results posted
Counted from Europe PMC indexing, not read by a person; a human tag can land on reviews, commentary or lab papers; clinical trial publications is the narrower count. 440 papers and 8 trials indexed in detail.
At a glance
Four things to know about Certepetide
Evidence
Investigational
Category
Longevity and energy
Common vial
Varies
Half-life
About 2 hours in patients
How much, and do you cycle it?
The range, and whether you take breaks.3.2 mg/kg as a 1-minute push into a vein, the dose chosen for phase 2, with each chemotherapy dose; cohort b added a second dose 4 hours later. Given with each chemotherapy dose Trial dose
It is not taken on its own schedule. In the trials it is pushed into a vein between the two chemotherapy drugs, on the chemotherapy calendar, with cohort B adding a second dose four hours later.
About 2 hours in patientsHuman study
Median 1.6 to 1.8 hours in patients with metastatic pancreatic cancer given it into a vein. It clears much faster in animals: 20 to 25 minutes in mice, 30 in rats, 40 in dogs and about 55 minutes in monkeys.
Source: International Journal of Molecular Sciences, 2023
You can compare this against the whole library to see where it sits.
How is it given?
Dosing context and source notes.Given in hospital from a prepared product, so there is nothing to mix.
Trial dose: 3.2 mg/kg per dose. Jarvelainen et al., International Journal of Molecular Sciences, 2023
How do you store it?
Before mixing, and after.Given in a hospital or trial clinic, so the pharmacy stores it.
Certepetide goes into a vein and is prepared by hospital, clinic or trial pharmacy staff, following the product label or the trial protocol. Some products like this are ready-made solutions and others are powders mixed just before use, often with hours rather than weeks of shelf life once prepared. It is not a medicine people store at home.
What are the side effects and cautions?
Known cautions and warnings for this compound.Solubility, computed: 67% charged residues, 33% hydrophobic. Water usually sufficient.
A first-pass rule from peptide manufacturers' guidance. It does not account for disulfide bridges, salt form or how the powder was dried, and it predicts what should be easy rather than what will happen in your vial.
Who should avoid it
- Any use outside a trial: it is not approved anywhere and is not sold as a medicine
- Use on its own: it has no anticancer activity of its own and is only ever given with chemotherapy
Stop and get help
- Not applicable outside a trial, where the protocol governs stopping rules
Common effects
- Grade 3 to 4 neutropenia in 34.3% against 28.6% on placebo, and low platelets in 19% against 14.3%, in the smaller cohort
Where this page says nothing is established, that means nobody has studied it, not that a compound is safe.
Is Certepetide approved?
And where the numbers on this page come from.No. Certepetide is not approved anywhere and is currently in company-run clinical trials. There is no legal route to obtain it outside a trial.
- Approval statusInvestigational
- RouteInto a vein (1-minute push, between the two chemotherapy drugs)
- Checked23 October 2026
- DoseFrom published clinical trials. Not approved by a regulator for this dose.
- Vial sizeFrom what vendors typically list; not a recommendation.
- SourcesFDA GSRS substance record, certepetide (UNII 7PF4546T2P)Jarvelainen et al., pharmacokinetics of CEND-1, International Journal of Molecular Sciences, 2023ASCEND trial record, ClinicalTrials.gov NCT05042128ASCEND cohort A results, presented at the 2025 Gastrointestinal Cancers SymposiumDean et al., ASCEND cohort B progression-free survival, Annals of Oncology 36 Supplement 1, ESMO GI 2025Lisata and Qilu mutual license termination, January 27, 2026
What has happened recently
Not approved anywhere. It has an International Nonproprietary Name, certepetide, and a US adopted name, LM-161, with FDA substance record UNII 7PF4546T2P and CAS 2580154-02-3, so its identity is settled even though no product exists. The ASCEND trial (NCT05042128) is registered as phase 2 and led by the Australasian Gastro-Intestinal Trials Group rather than by Lisata Therapeutics; the registry marks its status unknown, last verified in April 2024. Effective January 23, 2026 and announced four days later, Lisata and Qilu Pharmaceutical mutually ended the Greater China license signed in February 2021, returning those rights to Lisata while Qilu keeps the obligation to complete and wind down its own phase 2. Lisata's own position has since weakened: its mid-2026 filings report substantial doubt about its ability to continue as a going concern, delayed preparation for a planned phase 3 in metastatic pancreatic cancer, and a board weighing options that include liquidation and dissolution. The final ASCEND study report has still not been published.
You can compare this against the whole library, or read how to check a seller.
What else is like Certepetide?
Others in Longevity and energy, side by side.If you're weighing Certepetide, it's worth reading MOTS-c, Epitalon, and NAD+ in the same class.
It does not attack the tumor. It binds integrins to trigger a transport pathway that carries other drugs inside.
- Dose
- 3.2 mg/kg as a 1-minute push into a vein, the dose chosen for phase 2
- How often
- With each chemotherapy dose; cohort B added a second dose 4 hours later
A shot people use for energy, metabolism, and healthy aging.
- Dose
- 1 up to 5 mg per day (start low, increase slowly)
- How often
- Daily
A longevity peptide taken in short courses for sleep and anti-aging.
- Dose
- 5 up to 10 mg per day (start low, increase slowly)
- How often
- 10-20 day courses
A cellular fuel taken for energy, focus, and anti-aging.
- Dose
- 50 up to 100 mg per dose (start low, increase slowly)
- How often
- 2-3x/week
Guides for this compound
- How to Reconstitute a Peptide
Mix peptide powder with bacteriostatic water, step by step.
- How to Read an Insulin Syringe
Read the units, convert to millilitres, and draw the exact dose.
- mcg vs mg: The Peptide Dosing Mistake to Avoid
Your vial says mg and your protocol says mcg. Here is the conversion and how to check it.
- How to Read a Peptide COA
What the purity number does and does not tell you, and how to spot an edited report.
- How to Vet a Peptide Vendor
Independent COAs, HPLC purity, and the red flags that mean walk away.
Sources
- FDA GSRS substance record, certepetide (UNII 7PF4546T2P)(2026)Nine-residue complete sequence CRGDKGPDC with one disulfide bond joining residue 1 to residue 9. Tagged both INN and USAN; USAN LM-161, CAS 2580154-02-3.
- Jarvelainen et al., pharmacokinetics of CEND-1, International Journal of Molecular Sciences, 2023(2023)Half-life by vein was 20 to 25 minutes in mice, 30 in rats, 40 in dogs, about 55 in monkeys and about 2 hours in patients with metastatic pancreatic cancer. Human doses 1.6 and 3.2 mg/kg, with 3.2 recommended for phase 2.
- ASCEND trial record, ClinicalTrials.gov NCT05042128(2024)Registered as phase 2, lead sponsor the Australasian Gastro-Intestinal Trials Group with the University of Sydney. 158 patients actual, started April 13, 2022, primary outcome progression-free survival, 22 sites in Australia and 2 in New Zealand. Status unknown, last verified April 2024.
- ASCEND cohort A results, presented at the 2025 Gastrointestinal Cancers Symposium(2025)66 patients on certepetide against 29 on placebo. Median progression-free survival 5.5 months in both arms, hazard ratio 0.96 (95% CI 0.60 to 1.53), log-rank p=0.85. Median overall survival 12.42 against 9.72 months, hazard ratio 0.95 (95% CI 0.56 to 1.60), p=0.82. Response rate 38.3% against 26.9%, with four complete responses.
- Dean et al., ASCEND cohort B progression-free survival, Annals of Oncology 36 Supplement 1, ESMO GI 2025(2025)Cohort A, 66 against 29 patients: median progression-free survival 5.5 months in both arms, hazard ratio 0.96 (95% CI 0.60 to 1.53), log-rank p=0.85. Cohort B, 42 against 21: 7.5 against 4.7 months, hazard ratio 0.60 (95% CI 0.34 to 1.07), p=0.08.
- Lisata and Qilu mutual license termination, January 27, 2026(2026)Ends the February 2021 Greater China license; rights revert to Lisata and Qilu must complete and wind down its own phase 2 in metastatic pancreatic cancer.
Beyond these, 448 records are indexed. Browse the records