reptides / ITPP

ITPP

ITPP changes hemoglobin oxygen affinity and has published human pharmacokinetic and safety data from a 28-person cancer study. A separate phase II respiratory-failure trial is registered as ended, but its cited registry record does not report analyzable results. Human athletic benefit remains unestablished; the oncology infusion caused frequent calcium abnormalities.

experimental red-blood-cell-permeant hemoglobin allosteric effector

  • The studied intravenous formulation was called OXY111A
  • 28 people received it in a published oncology trial
  • BREATH2 has no analyzable results in the cited registry
  • Mouse treadmill gains have not been tested in people
  • Hypercalcemia was common with the calcium-containing oncology infusion
Identity Mechanism Human evidence Performance claims PK and safety Status China and Russia Tier verdict Respiratory trial Does oxygen unloading produce lasting tissue benefit?

What is ITPP, and is every product called ITPP equivalent to the clinical formulation?

ITPP is myo-inositol trispyrophosphate, a six-phosphate small molecule registered as PubChem CID 10439981. The published human study used OXY111A, an intravenous formulation prepared with sodium, calcium, and added calcium chloride. A material sold under the bare acronym cannot be assumed to match that formulation, purity, counterion composition, or pharmacokinetics.

The formulation contained added calcium

The phase Ib investigators linked much of the hypercalcemia to calcium chloride added because ITPP chelates calcium. Other formulations have no human safety dataset.

PubChem · ITPP identity

Official chemical identity record

National Center for Biotechnology Information. PubChem CID 10439981.

The record identifies myo-inositol trispyrophosphate with formula C6H12O21P6, molecular weight 605.99 g/mol, CAS 802590-64-3, and UNII 116EYZ0PPX.

Study design
Chemical database record

Identity registration is not approval or product authentication.

Read the original source
Phase Ib OXY111A in hepatopancreatobiliary tumors

Primary human study

Schneider MA, Linecker M, Fritsch R, Muehlematter UJ, Stocker D, Pestalozzi B, Samaras P, Jetter A, Kron P, Petrowsky H, Nicolau C, Lehn JM, Humar B, Graf R, Clavien PA, Limani P. Phase Ib dose-escalation study of the hypoxia-modifier Myo-inositol trispyrophosphate in patients with hepatopancreatobiliary tumors. Nature communications. 2021. DOI 10.1038/s41467-021-24069-w.

Twenty-eight patients received nine eight-hour infusions over three weeks; 27 reached the safety endpoint. Hypercalcemia occurred in 19/28, with two significant events at the highest cohort, including one grade-4 dose-limiting event. This uncontrolled dose-escalation study measured human PK and formulation-specific safety. It has no athletic endpoint and does not establish controlled antitumor efficacy.

Participants / model
28 adults with advanced hepatopancreatobiliary tumors or liver metastases; median age 65; 18 men and 10 women
Treatment
Nine eight-hour intravenous OXY111A/ITPP infusions across eight 3+3 escalation cohorts, followed by standard chemotherapy
Follow-up
3-week monotherapy phase plus follow-up with chemotherapy
Study design
Single-center, open-label, nonrandomized 3+3 phase Ib dose-escalation study
Funding
University and compound-development interests disclosed in the full paper
Read the original source

What does ITPP do to hemoglobin?

The original discovery experiments found that ITPP entered red blood cells and lowered hemoglobin's oxygen affinity, shifting oxygen release toward tissues. No healthy-human exercise or clinical outcome was measured.

More oxygen unloading is not automatically better. Oxygen delivery depends on ventilation, cardiac output, blood flow, hemoglobin concentration, tissue demand, and the shape of the dissociation curve. A mechanism can be measurable while its net clinical effect remains uncertain.

Fylaktakidou et al. · ITPP discovery

Chemical synthesis, red-cell, and hemoglobin study

Fylaktakidou KC, Lehn JM, Greferath R, Nicolau C. Bioorganic & Medicinal Chemistry Letters. 2005;15(6):1605-1608. DOI 10.1016/j.bmcl.2005.01.064.

The study described ITPP synthesis and found membrane permeation into red blood cells with a rightward shift in hemoglobin oxygen affinity, supporting enhanced oxygen unloading in the experimental systems.

Participants / model
Purified hemoglobin and red-blood-cell experimental systems
Treatment
Myo-inositol trispyrophosphate
Follow-up
Acute laboratory experiments
Study design
Medicinal chemistry and in-vitro/ex-vivo mechanism study

No human clinical or exercise outcome was tested.

Read the original source

What happened in the published human administration study?

Twenty-eight adults with advanced hepatopancreatobiliary tumors entered a single-center, open-label phase Ib dose-escalation study. They received nine eight-hour OXY111A infusions over three weeks before standard chemotherapy. Twenty-seven reached the prespecified safety endpoint; the maximum tolerated exposure was defined in this formulation, and two participants at the highest cohort had significant treatment-emergent hypercalcemia, including one grade 4 dose-limiting event.

What the phase Ib trial measured
Study featureMeasuredMissing or limited
Population28 adults with advanced liver, pancreatic, or biliary-region malignancyNot healthy athletes, anemia patients, or a general population
DesignOpen-label 3+3 escalation at one center; nine infusions over three weeksNo randomized placebo group and too small for uncommon harms
Primary purposeSafety, dose escalation, and plasma pharmacokineticsNot exercise performance or validated anticancer efficacy
Tumor observationsAbout half had morphologic stable disease during monotherapyUncontrolled, short, and followed by chemotherapy; no causal efficacy conclusion
Phase Ib OXY111A in hepatopancreatobiliary tumors

Primary human study

Schneider MA, Linecker M, Fritsch R, Muehlematter UJ, Stocker D, Pestalozzi B, Samaras P, Jetter A, Kron P, Petrowsky H, Nicolau C, Lehn JM, Humar B, Graf R, Clavien PA, Limani P. Phase Ib dose-escalation study of the hypoxia-modifier Myo-inositol trispyrophosphate in patients with hepatopancreatobiliary tumors. Nature communications. 2021. DOI 10.1038/s41467-021-24069-w.

Twenty-eight patients received nine eight-hour infusions over three weeks; 27 reached the safety endpoint. Hypercalcemia occurred in 19/28, with two significant events at the highest cohort, including one grade-4 dose-limiting event. This uncontrolled dose-escalation study measured human PK and formulation-specific safety. It has no athletic endpoint and does not establish controlled antitumor efficacy.

Participants / model
28 adults with advanced hepatopancreatobiliary tumors or liver metastases; median age 65; 18 men and 10 women
Treatment
Nine eight-hour intravenous OXY111A/ITPP infusions across eight 3+3 escalation cohorts, followed by standard chemotherapy
Follow-up
3-week monotherapy phase plus follow-up with chemotherapy
Study design
Single-center, open-label, nonrandomized 3+3 phase Ib dose-escalation study
Funding
University and compound-development interests disclosed in the full paper
Read the original source
ClinicalTrials.gov · NCT02528526

Official trial registry record

University Hospital Zurich. ClinicalTrials.gov NCT02528526, first posted 20 August 2015.

The phase I record identifies intravenous OXY111A/ITPP in advanced solid tumors. ClinicalTrials.gov currently labels status UNKNOWN and still lists an estimated enrollment of 69, while the peer-reviewed publication reports 28 treated participants.

Participants / model
Adults with advanced solid tumors
Treatment
Intravenous OXY111A
Follow-up
Phase I program
Study design
Interventional dose-escalation registry entry
Funding
University Hospital Zurich

The registry was last updated in 2015 and labels the trial's status UNKNOWN. Its planning fields are not substituted for the publication's actual cohort.

Read the original source

Does ITPP improve endurance in humans?

The cited evidence includes no controlled human exercise study. A 2009 mouse study reported increased treadmill capacity in normal mice and in a transgenic severe-heart-failure model after ITPP. The experiments used very high animal exposures, several administration routes, small endpoint groups, and a forced treadmill protocol; no human effect size, route, or safety threshold can be calculated from them.

The paper measured forced-treadmill capacity in mice. It collected no race-performance, recovery, altitude, or body-composition data in people.

A later five-week pulmonary-hypertension study randomized 100 male rats. ITPP preserved right-ventricular function and reduced mortality from 52% to 22% in the monocrotaline arms, while pulmonary vasculopathy and vascular resistance did not improve. This disease-model result is separate from healthy endurance.

Biolo et al. · mouse treadmill study

Controlled animal physiology and exercise study

Biolo A, Greferath R, Siwik DA, Qin F, Valsky E, Fylaktakidou KC, Pothukanuri S, Duarte CD, Schwarz RP, Lehn JM, Nicolau C, Colucci WS. Proceedings of the National Academy of Sciences of the United States of America. 2009;106(6):1926-1929. DOI 10.1073/pnas.0812381106.

ITPP shifted blood oxygen affinity and increased forced-treadmill exercise capacity in normal mice and G-alpha-q transgenic mice with severe heart failure. Active endpoint groups were small, and exposures included intraperitoneal administration and drinking-water experiments.

Participants / model
Normal mice and G-alpha-q transgenic mice with severe heart failure
Treatment
ITPP through intraperitoneal and drinking-water experiments
Follow-up
Acute and short preclinical experiments with testing 16 to 24 hours after treatment in key arms
Study design
Controlled mouse oxygen-affinity and forced-treadmill study
Funding
Academic and compound-development interests disclosed in the paper

Small mouse groups, extreme mass-scaled exposures, mixed routes, transgenic disease, and aversive treadmill conditions block human extrapolation.

Read the original source
Human evidence · no performance trial

PubMed and ClinicalTrials.gov records

PubMed and ClinicalTrials.gov records for ITPP and OXY111A.

The oncology phase Ib report is the only cited publication from a prospective human administration study. The cited records include no controlled human exercise, endurance, altitude, anemia, body-composition, or healthy-volunteer pharmacokinetic study.

Participants / model
Published and registered ITPP records
Read the original source
ITPP in monocrotaline-induced pulmonary hypertension, 2024

Primary preclinical study

Oknińska M, Paterek A, Grzanka M, Zajda K, Surzykiewicz M, Rolski F, Zambrowska Z, Torbicki A, Kurzyna M, Kieda C, Piekiełko-Witkowska A, Mączewski M. British Journal of Pharmacology. 2024;181(20):4050-4066. DOI 10.1111/bph.16482.

One hundred male Wistar rats entered the controlled experiment. Day-35 mortality was 52% with monocrotaline versus 22% with monocrotaline plus ITPP, with preserved right-ventricular oxygenation/function. Pulmonary vascular disease and resistance were not reversed. Survival changes and endpoint-specific surviving samples matter when interpreting imaging/histology. This is not a healthy endurance trial.

Participants / model
100 male Wistar rats; 64 received monocrotaline and 36 saline before randomized ITPP or placebo
Treatment
ITPP or placebo in monocrotaline pulmonary hypertension and saline controls
Follow-up
5 weeks
Study design
Randomized controlled animal disease-model study with survival, imaging, hemodynamic, oxygenation, and histology endpoints
Funding
Polish and European research funding reported in the paper
Read the original source

What human pharmacokinetics and hazards are genuinely known?

In the cancer phase Ib study, plasma concentrations generally peaked around six hours during an eight-hour infusion, then fell rapidly; terminal half-life estimates ranged roughly 1.3 to 3.3 hours across cohorts. Oral bioavailability, healthy-person PK, and tissue residence were not measured.

Observed phase Ib safety findings
FindingInterpretation
Hypercalcemia in 19 of 28 participantsFrequent in this calcium-containing infusion; one grade 4 dose-limiting event at the highest cohort
Hypomagnesemia and hypophosphatemiaConsistent with a formulation and chelation-related electrolyte problem; clinical importance varied
Blood-pressure worsening in three participantsSmall uncontrolled denominator; no incidence estimate beyond this study
No validated interaction studyCancer, comorbidity, infusion components, and later chemotherapy prevent a clean general interaction profile

Safety data cover one formulation

OXY111A produced real electrolyte abnormalities. Other routes and formulations have no human adverse-event data.

Phase Ib OXY111A in hepatopancreatobiliary tumors

Primary human study

Schneider MA, Linecker M, Fritsch R, Muehlematter UJ, Stocker D, Pestalozzi B, Samaras P, Jetter A, Kron P, Petrowsky H, Nicolau C, Lehn JM, Humar B, Graf R, Clavien PA, Limani P. Phase Ib dose-escalation study of the hypoxia-modifier Myo-inositol trispyrophosphate in patients with hepatopancreatobiliary tumors. Nature communications. 2021. DOI 10.1038/s41467-021-24069-w.

Twenty-eight patients received nine eight-hour infusions over three weeks; 27 reached the safety endpoint. Hypercalcemia occurred in 19/28, with two significant events at the highest cohort, including one grade-4 dose-limiting event. This uncontrolled dose-escalation study measured human PK and formulation-specific safety. It has no athletic endpoint and does not establish controlled antitumor efficacy.

Participants / model
28 adults with advanced hepatopancreatobiliary tumors or liver metastases; median age 65; 18 men and 10 women
Treatment
Nine eight-hour intravenous OXY111A/ITPP infusions across eight 3+3 escalation cohorts, followed by standard chemotherapy
Follow-up
3-week monotherapy phase plus follow-up with chemotherapy
Study design
Single-center, open-label, nonrandomized 3+3 phase Ib dose-escalation study
Funding
University and compound-development interests disclosed in the full paper
Read the original source

Is ITPP an approved medicine or allowed performance aid?

The cited regulatory records list no approved indication. ClinicalTrials.gov currently labels NCT02528526 UNKNOWN and still shows an estimated 69 participants; the publication reports 28 treated people. WADA does not name ITPP, while M1.2 prohibits artificial enhancement of oxygen uptake, transport, or delivery.

WADA's list does not name ITPP. The analytical urine paper validates detection chemistry and reports no athlete benefit or safety outcome.

ClinicalTrials.gov · NCT02528526

Official trial registry record

University Hospital Zurich. ClinicalTrials.gov NCT02528526, first posted 20 August 2015.

The phase I record identifies intravenous OXY111A/ITPP in advanced solid tumors. ClinicalTrials.gov currently labels status UNKNOWN and still lists an estimated enrollment of 69, while the peer-reviewed publication reports 28 treated participants.

Participants / model
Adults with advanced solid tumors
Treatment
Intravenous OXY111A
Follow-up
Phase I program
Study design
Interventional dose-escalation registry entry
Funding
University Hospital Zurich

The registry was last updated in 2015 and labels the trial's status UNKNOWN. Its planning fields are not substituted for the publication's actual cohort.

Read the original source
Görgens et al. · urine detection method

Analytical anti-doping method study

Görgens C, Guddat S, Schänzer W, Thevis M. Drug Testing and Analysis. 2014;6(11-12):1102-1107. DOI 10.1002/dta.1700.

The authors developed screening and confirmation methods for ITPP in human urine matrices for doping-control use.

Participants / model
Human urine analytical matrices, not an efficacy cohort
Treatment
Analytical detection of ITPP
Study design
Analytical-method validation

A detection method is not evidence of administered-subject benefit, prevalence, or safety.

Read the original source
WADA 2026 · oxygen-delivery method rule

Official anti-doping standard

World Anti-Doping Agency. The 2026 Prohibited List, effective 1 January 2026.

Method M1.2 prohibits artificial enhancement of the uptake, transport, or delivery of oxygen. The list does not individually name ITPP.

Participants / model
Athletes subject to the World Anti-Doping Code
Follow-up
Calendar year 2026
Study design
Anti-doping prohibited list
Funding
World Anti-Doping Agency

ITPP is not named explicitly; applicability depends on the rule's prohibition of artificial enhancement of oxygen uptake, transport, or delivery.

Read the original source

Do Chinese- or Russian-language records show another clinical or preclinical program?

Chinese-language records include patents mentioning ITPP but no compound-specific administration study. Russian-language records were chemical or secondary index pages. These patents, reagent listings, and summaries provide no human or animal outcome data.

Chinese and Russian records · no additional subject study

Literature and registry records

Chinese and Russian literature and registry records for ITPP.

The cited Chinese records comprise patents, chemical records, and secondary summaries without a clinical or preclinical outcome study. The cited Russian records likewise comprise chemical records and secondary summaries without an additional compound-specific administered-subject dataset.

Participants / model
Chinese- and Russian-language literature, patent, and registry records

The linked Chinese patent is not clinical efficacy evidence. The regional records do not report enough treatment detail to assess outcomes.

Read the original source

Why is ITPP C tier?

ITPP has controlled animal physiology and a published human pharmacokinetic and safety study. Human performance efficacy remains unestablished, and the human safety data concern one oncology infusion formulation.

BREATH2 confirms another registered clinical program, but the cited registry record provides no outcome tables.

Phase Ib OXY111A in hepatopancreatobiliary tumors

Primary human study

Schneider MA, Linecker M, Fritsch R, Muehlematter UJ, Stocker D, Pestalozzi B, Samaras P, Jetter A, Kron P, Petrowsky H, Nicolau C, Lehn JM, Humar B, Graf R, Clavien PA, Limani P. Phase Ib dose-escalation study of the hypoxia-modifier Myo-inositol trispyrophosphate in patients with hepatopancreatobiliary tumors. Nature communications. 2021. DOI 10.1038/s41467-021-24069-w.

Twenty-eight patients received nine eight-hour infusions over three weeks; 27 reached the safety endpoint. Hypercalcemia occurred in 19/28, with two significant events at the highest cohort, including one grade-4 dose-limiting event. This uncontrolled dose-escalation study measured human PK and formulation-specific safety. It has no athletic endpoint and does not establish controlled antitumor efficacy.

Participants / model
28 adults with advanced hepatopancreatobiliary tumors or liver metastases; median age 65; 18 men and 10 women
Treatment
Nine eight-hour intravenous OXY111A/ITPP infusions across eight 3+3 escalation cohorts, followed by standard chemotherapy
Follow-up
3-week monotherapy phase plus follow-up with chemotherapy
Study design
Single-center, open-label, nonrandomized 3+3 phase Ib dose-escalation study
Funding
University and compound-development interests disclosed in the full paper
Read the original source
BREATH2 official EU clinical trial record

Official trial registry or sponsor protocol

BREATH2 official EU clinical trial record. https://euclinicaltrials.eu/ctis-public/view/2024-517878-21-00

EUCT 2024-517878-21-00, protocol ABM/COVID19/0034, identifies ITPP adjunctive treatment in progressive respiratory failure from COVID-19 or other pulmonary infections. The official record lists phase II, Poland, a November 28, 2023 start and a June 11, 2025 global end. The sponsor describes the study as randomized and double blind. The registry does not report analyzable results, enrollment, benefit, or safety rates; an "ended" status alone cannot supply them.

Read the original source
BREATH2 sponsor protocol description

Official trial registry or sponsor protocol

BREATH2 sponsor protocol description. https://wim.mil.pl/2020/07/01/projekt-itpp-2/

The Polish Military Institute describes a noncommercial randomized double-blind phase II respiratory-failure project funded by the Medical Research Agency. This verifies a clinical program beyond oncology. It is a project description, not a completed-outcome report.

Read the original source
Biolo et al. · mouse treadmill study

Controlled animal physiology and exercise study

Biolo A, Greferath R, Siwik DA, Qin F, Valsky E, Fylaktakidou KC, Pothukanuri S, Duarte CD, Schwarz RP, Lehn JM, Nicolau C, Colucci WS. Proceedings of the National Academy of Sciences of the United States of America. 2009;106(6):1926-1929. DOI 10.1073/pnas.0812381106.

ITPP shifted blood oxygen affinity and increased forced-treadmill exercise capacity in normal mice and G-alpha-q transgenic mice with severe heart failure. Active endpoint groups were small, and exposures included intraperitoneal administration and drinking-water experiments.

Participants / model
Normal mice and G-alpha-q transgenic mice with severe heart failure
Treatment
ITPP through intraperitoneal and drinking-water experiments
Follow-up
Acute and short preclinical experiments with testing 16 to 24 hours after treatment in key arms
Study design
Controlled mouse oxygen-affinity and forced-treadmill study
Funding
Academic and compound-development interests disclosed in the paper

Small mouse groups, extreme mass-scaled exposures, mixed routes, transgenic disease, and aversive treadmill conditions block human extrapolation.

Read the original source

Was ITPP tested outside cancer?

Yes. BREATH2 studied ITPP as an adjunct in progressive respiratory failure from COVID-19 or other lung infections. The official record lists June 11, 2025 as its global end date but provides no analyzable result tables.

The EU record is 2024-517878-21-00, protocol ABM/COVID19/0034, with a November 28, 2023 start in Poland. The sponsor describes a randomized, double-blind phase II project. The registry does not report analyzable result tables, enrollment totals, benefit estimates, or adverse-event rates.

BREATH2 official EU clinical trial record

Official trial registry or sponsor protocol

BREATH2 official EU clinical trial record. https://euclinicaltrials.eu/ctis-public/view/2024-517878-21-00

EUCT 2024-517878-21-00, protocol ABM/COVID19/0034, identifies ITPP adjunctive treatment in progressive respiratory failure from COVID-19 or other pulmonary infections. The official record lists phase II, Poland, a November 28, 2023 start and a June 11, 2025 global end. The sponsor describes the study as randomized and double blind. The registry does not report analyzable results, enrollment, benefit, or safety rates; an "ended" status alone cannot supply them.

Read the original source
BREATH2 sponsor protocol description

Official trial registry or sponsor protocol

BREATH2 sponsor protocol description. https://wim.mil.pl/2020/07/01/projekt-itpp-2/

The Polish Military Institute describes a noncommercial randomized double-blind phase II respiratory-failure project funded by the Medical Research Agency. This verifies a clinical program beyond oncology. It is a project description, not a completed-outcome report.

Read the original source

Does oxygen unloading produce lasting tissue benefit?

In mice, ITPP plus checkpoint blockade improved CT26 tumor control and survival, but did not significantly improve survival over checkpoint blockade alone in the 4T1 model. An initial oxygenation signal was not sustained after later administrations.

ITPP plus checkpoint blockade improved CT26 tumor control and survival in mice. In the 4T1 model, survival versus checkpoint blockade alone was not statistically significant. Tumor experiments used small groups and endpoint-specific samples. Neither result establishes sustained red-cell benefit or anticancer efficacy in people.

The human plasma half-life, roughly 1.3 to 3.3 hours during the oncology program, does not measure how long an intracellular red-cell effect lasts. The sodium/calcium infusion formulation and its calcium-related toxicity also cannot be transferred to a different product.

Phase Ib OXY111A in hepatopancreatobiliary tumors

Primary human study

Schneider MA, Linecker M, Fritsch R, Muehlematter UJ, Stocker D, Pestalozzi B, Samaras P, Jetter A, Kron P, Petrowsky H, Nicolau C, Lehn JM, Humar B, Graf R, Clavien PA, Limani P. Phase Ib dose-escalation study of the hypoxia-modifier Myo-inositol trispyrophosphate in patients with hepatopancreatobiliary tumors. Nature communications. 2021. DOI 10.1038/s41467-021-24069-w.

Twenty-eight patients received nine eight-hour infusions over three weeks; 27 reached the safety endpoint. Hypercalcemia occurred in 19/28, with two significant events at the highest cohort, including one grade-4 dose-limiting event. This uncontrolled dose-escalation study measured human PK and formulation-specific safety. It has no athletic endpoint and does not establish controlled antitumor efficacy.

Participants / model
28 adults with advanced hepatopancreatobiliary tumors or liver metastases; median age 65; 18 men and 10 women
Treatment
Nine eight-hour intravenous OXY111A/ITPP infusions across eight 3+3 escalation cohorts, followed by standard chemotherapy
Follow-up
3-week monotherapy phase plus follow-up with chemotherapy
Study design
Single-center, open-label, nonrandomized 3+3 phase Ib dose-escalation study
Funding
University and compound-development interests disclosed in the full paper
Read the original source
ITPP plus checkpoint blockade in mouse tumors, 2025

Primary preclinical study

Tran RL, Liang X, de la Cerda J, Schuler FW, Pagel MD. Potentiation of immune checkpoint blockade with an ITPP radiosensitizer studied with oxygen saturation measurements from photoacoustic imaging. Scientific reports. 2025. DOI 10.1038/s41598-025-05930-0.

Female BALB/cJ mice bearing CT26 or 4T1 tumors were studied with vehicle, ITPP, checkpoint blockade or combination. Tumor-growth/survival experiments used groups of five repeated three times; imaging/biomarker denominators varied and some samples were lost/excluded. Initial photoacoustic hemoglobin saturation fell, interpreted as oxygen unloading, but that difference was not durable after later administrations. Combination improved CT26 control/survival; in 4T1, survival versus checkpoint blockade alone was not statistically significant. These are tumor-model combination results, not proof of human efficacy or sustained red-cell benefit. Public NIH/CPRIT funding was reported.

Read the original source

Studies and sources

PubChem · ITPP identity

Official chemical identity record

National Center for Biotechnology Information. PubChem CID 10439981.

The record identifies myo-inositol trispyrophosphate with formula C6H12O21P6, molecular weight 605.99 g/mol, CAS 802590-64-3, and UNII 116EYZ0PPX.

Study design
Chemical database record

Identity registration is not approval or product authentication.

Read the original source
Fylaktakidou et al. · ITPP discovery

Chemical synthesis, red-cell, and hemoglobin study

Fylaktakidou KC, Lehn JM, Greferath R, Nicolau C. Bioorganic & Medicinal Chemistry Letters. 2005;15(6):1605-1608. DOI 10.1016/j.bmcl.2005.01.064.

The study described ITPP synthesis and found membrane permeation into red blood cells with a rightward shift in hemoglobin oxygen affinity, supporting enhanced oxygen unloading in the experimental systems.

Participants / model
Purified hemoglobin and red-blood-cell experimental systems
Treatment
Myo-inositol trispyrophosphate
Follow-up
Acute laboratory experiments
Study design
Medicinal chemistry and in-vitro/ex-vivo mechanism study

No human clinical or exercise outcome was tested.

Read the original source
Phase Ib OXY111A in hepatopancreatobiliary tumors

Primary human study

Schneider MA, Linecker M, Fritsch R, Muehlematter UJ, Stocker D, Pestalozzi B, Samaras P, Jetter A, Kron P, Petrowsky H, Nicolau C, Lehn JM, Humar B, Graf R, Clavien PA, Limani P. Phase Ib dose-escalation study of the hypoxia-modifier Myo-inositol trispyrophosphate in patients with hepatopancreatobiliary tumors. Nature communications. 2021. DOI 10.1038/s41467-021-24069-w.

Twenty-eight patients received nine eight-hour infusions over three weeks; 27 reached the safety endpoint. Hypercalcemia occurred in 19/28, with two significant events at the highest cohort, including one grade-4 dose-limiting event. This uncontrolled dose-escalation study measured human PK and formulation-specific safety. It has no athletic endpoint and does not establish controlled antitumor efficacy.

Participants / model
28 adults with advanced hepatopancreatobiliary tumors or liver metastases; median age 65; 18 men and 10 women
Treatment
Nine eight-hour intravenous OXY111A/ITPP infusions across eight 3+3 escalation cohorts, followed by standard chemotherapy
Follow-up
3-week monotherapy phase plus follow-up with chemotherapy
Study design
Single-center, open-label, nonrandomized 3+3 phase Ib dose-escalation study
Funding
University and compound-development interests disclosed in the full paper
Read the original source
ClinicalTrials.gov · NCT02528526

Official trial registry record

University Hospital Zurich. ClinicalTrials.gov NCT02528526, first posted 20 August 2015.

The phase I record identifies intravenous OXY111A/ITPP in advanced solid tumors. ClinicalTrials.gov currently labels status UNKNOWN and still lists an estimated enrollment of 69, while the peer-reviewed publication reports 28 treated participants.

Participants / model
Adults with advanced solid tumors
Treatment
Intravenous OXY111A
Follow-up
Phase I program
Study design
Interventional dose-escalation registry entry
Funding
University Hospital Zurich

The registry was last updated in 2015 and labels the trial's status UNKNOWN. Its planning fields are not substituted for the publication's actual cohort.

Read the original source
Biolo et al. · mouse treadmill study

Controlled animal physiology and exercise study

Biolo A, Greferath R, Siwik DA, Qin F, Valsky E, Fylaktakidou KC, Pothukanuri S, Duarte CD, Schwarz RP, Lehn JM, Nicolau C, Colucci WS. Proceedings of the National Academy of Sciences of the United States of America. 2009;106(6):1926-1929. DOI 10.1073/pnas.0812381106.

ITPP shifted blood oxygen affinity and increased forced-treadmill exercise capacity in normal mice and G-alpha-q transgenic mice with severe heart failure. Active endpoint groups were small, and exposures included intraperitoneal administration and drinking-water experiments.

Participants / model
Normal mice and G-alpha-q transgenic mice with severe heart failure
Treatment
ITPP through intraperitoneal and drinking-water experiments
Follow-up
Acute and short preclinical experiments with testing 16 to 24 hours after treatment in key arms
Study design
Controlled mouse oxygen-affinity and forced-treadmill study
Funding
Academic and compound-development interests disclosed in the paper

Small mouse groups, extreme mass-scaled exposures, mixed routes, transgenic disease, and aversive treadmill conditions block human extrapolation.

Read the original source
Görgens et al. · urine detection method

Analytical anti-doping method study

Görgens C, Guddat S, Schänzer W, Thevis M. Drug Testing and Analysis. 2014;6(11-12):1102-1107. DOI 10.1002/dta.1700.

The authors developed screening and confirmation methods for ITPP in human urine matrices for doping-control use.

Participants / model
Human urine analytical matrices, not an efficacy cohort
Treatment
Analytical detection of ITPP
Study design
Analytical-method validation

A detection method is not evidence of administered-subject benefit, prevalence, or safety.

Read the original source
Human evidence · no performance trial

PubMed and ClinicalTrials.gov records

PubMed and ClinicalTrials.gov records for ITPP and OXY111A.

The oncology phase Ib report is the only cited publication from a prospective human administration study. The cited records include no controlled human exercise, endurance, altitude, anemia, body-composition, or healthy-volunteer pharmacokinetic study.

Participants / model
Published and registered ITPP records
Read the original source
WADA 2026 · oxygen-delivery method rule

Official anti-doping standard

World Anti-Doping Agency. The 2026 Prohibited List, effective 1 January 2026.

Method M1.2 prohibits artificial enhancement of the uptake, transport, or delivery of oxygen. The list does not individually name ITPP.

Participants / model
Athletes subject to the World Anti-Doping Code
Follow-up
Calendar year 2026
Study design
Anti-doping prohibited list
Funding
World Anti-Doping Agency

ITPP is not named explicitly; applicability depends on the rule's prohibition of artificial enhancement of oxygen uptake, transport, or delivery.

Read the original source
Chinese and Russian records · no additional subject study

Literature and registry records

Chinese and Russian literature and registry records for ITPP.

The cited Chinese records comprise patents, chemical records, and secondary summaries without a clinical or preclinical outcome study. The cited Russian records likewise comprise chemical records and secondary summaries without an additional compound-specific administered-subject dataset.

Participants / model
Chinese- and Russian-language literature, patent, and registry records

The linked Chinese patent is not clinical efficacy evidence. The regional records do not report enough treatment detail to assess outcomes.

Read the original source
ITPP in monocrotaline-induced pulmonary hypertension, 2024

Primary preclinical study

Oknińska M, Paterek A, Grzanka M, Zajda K, Surzykiewicz M, Rolski F, Zambrowska Z, Torbicki A, Kurzyna M, Kieda C, Piekiełko-Witkowska A, Mączewski M. British Journal of Pharmacology. 2024;181(20):4050-4066. DOI 10.1111/bph.16482.

One hundred male Wistar rats entered the controlled experiment. Day-35 mortality was 52% with monocrotaline versus 22% with monocrotaline plus ITPP, with preserved right-ventricular oxygenation/function. Pulmonary vascular disease and resistance were not reversed. Survival changes and endpoint-specific surviving samples matter when interpreting imaging/histology. This is not a healthy endurance trial.

Participants / model
100 male Wistar rats; 64 received monocrotaline and 36 saline before randomized ITPP or placebo
Treatment
ITPP or placebo in monocrotaline pulmonary hypertension and saline controls
Follow-up
5 weeks
Study design
Randomized controlled animal disease-model study with survival, imaging, hemodynamic, oxygenation, and histology endpoints
Funding
Polish and European research funding reported in the paper
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BREATH2 official EU clinical trial record

Official trial registry or sponsor protocol

BREATH2 official EU clinical trial record. https://euclinicaltrials.eu/ctis-public/view/2024-517878-21-00

EUCT 2024-517878-21-00, protocol ABM/COVID19/0034, identifies ITPP adjunctive treatment in progressive respiratory failure from COVID-19 or other pulmonary infections. The official record lists phase II, Poland, a November 28, 2023 start and a June 11, 2025 global end. The sponsor describes the study as randomized and double blind. The registry does not report analyzable results, enrollment, benefit, or safety rates; an "ended" status alone cannot supply them.

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BREATH2 sponsor protocol description

Official trial registry or sponsor protocol

BREATH2 sponsor protocol description. https://wim.mil.pl/2020/07/01/projekt-itpp-2/

The Polish Military Institute describes a noncommercial randomized double-blind phase II respiratory-failure project funded by the Medical Research Agency. This verifies a clinical program beyond oncology. It is a project description, not a completed-outcome report.

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ITPP plus checkpoint blockade in mouse tumors, 2025

Primary preclinical study

Tran RL, Liang X, de la Cerda J, Schuler FW, Pagel MD. Potentiation of immune checkpoint blockade with an ITPP radiosensitizer studied with oxygen saturation measurements from photoacoustic imaging. Scientific reports. 2025. DOI 10.1038/s41598-025-05930-0.

Female BALB/cJ mice bearing CT26 or 4T1 tumors were studied with vehicle, ITPP, checkpoint blockade or combination. Tumor-growth/survival experiments used groups of five repeated three times; imaging/biomarker denominators varied and some samples were lost/excluded. Initial photoacoustic hemoglobin saturation fell, interpreted as oxygen unloading, but that difference was not durable after later administrations. Combination improved CT26 control/survival; in 4T1, survival versus checkpoint blockade alone was not statistically significant. These are tumor-model combination results, not proof of human efficacy or sustained red-cell benefit. Public NIH/CPRIT funding was reported.

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Why is ITPP in C tier?

C reflects human pharmacokinetic and safety data from a 28-person cancer trial. The calcium-containing infusion frequently caused calcium abnormalities. Human endurance has not been tested, and BREATH2's cited registry record provides no analyzable results.

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