ITPP (myo-inositol trispyrophosphate) — Safety, Research, Risks & Legal Status

Not medical advice. ITPP (myo-inositol trispyrophosphate) is discussed here for informational and harm-reduction purposes only. We do not endorse use, and any dosing context is informational, not a protocol.

Also known as	myo-inositol trispyrophosphate, OXY111A, inositol trispyrophosphate, ITPP hexasodium, ITPP hexa-triethylamine, CAS 623552-11-4
Category	Research Chemical
Drug class	Membrane-permeant allosteric hemoglobin oxygen-affinity modulator (inositol pyrophosphate)
Development code	OXY111A
CAS number	623552-11-4
Highest human trial stage	Phase Ib/IIa (oncology, ~28 patients); not approved
Route in trials	Intravenous infusion (8-hour infusions)
Sport status	WADA-prohibited oxygen-transport method (M1), banned at all times
US legal status	Not FDA-approved for any indication and not a lawful dietary supplement. ITPP is an investigational compound studied in humans only in one small early-phase oncology trial (as OXY111A); it holds no marketing authorization anywhere. Material sold to consumers online is gray-market, typically labeled "research chemical, not for human consumption," and is not quality-controlled. In sport it is prohibited: the World Anti-Doping Agency treats ITPP as a prohibited hemoglobin/oxygen-transport modulator under Prohibited Methods M1 (manipulation of blood and blood components), banned at all times, and it is also a doping concern in horse racing. It is not a US-scheduled controlled substance, so possessing the bulk chemical is not itself a drug-scheduling offense, but using it as a supplement or drug is unapproved and using it in competition is a doping violation.

What is ITPP (myo-inositol trispyrophosphate)?

ITPP is a synthetic small molecule that acts as an allosteric effector of hemoglobin. It crosses the red blood cell membrane (reportedly via the band 3 anion transporter) and binds hemoglobin, mildly lowering its oxygen-binding affinity. This right-shifts the oxygen-hemoglobin dissociation curve, so red cells unload more oxygen to tissues, especially under low-oxygen (hypoxic) conditions. The research rationale is improved tissue oxygenation: in oncology, to make hypoxic, treatment-resistant tumors more oxygenated and thus potentially more radio- and chemo-sensitive; in cardiovascular research, to improve oxygen delivery to ischemic tissue. The same physiology (more oxygen released to muscle) is why it is discussed as a potential endurance-enhancing doping agent. It is not a stimulant, a hormone, or an EPO-type agent, and it does not raise red-cell mass; it changes how existing hemoglobin releases the oxygen it already carries. Be aware the acronym ITPP is sometimes mislabeled online as "inosine triphosphate," a different molecule; the compound studied for oxygenation is myo-inositol trispyrophosphate.

How it works

ITPP is a membrane-permeant allosteric effector of hemoglobin. Unlike 2,3-bisphosphoglycerate (2,3-BPG), the body's natural intracellular allosteric regulator, ITPP is unusual in that it can cross the erythrocyte membrane, reported to enter via the band 3 anion exchanger. Once inside, it binds hemoglobin and stabilizes the low-affinity (T, deoxygenated) state, reducing oxygen affinity and raising the P50. The practical result is a rightward shift of the oxygen dissociation curve: hemoglobin holds oxygen less tightly and releases more of it to tissues, an effect that is largest where oxygen tension is already low (hypoxic tumor cores, ischemic tissue, exercising muscle). It does not stimulate erythropoiesis and does not change total oxygen-carrying capacity; it redistributes oxygen unloading. This is the same functional endpoint many blood-doping strategies target, which is why anti-doping authorities classify it as an oxygen-transport-enhancing method.

Background & history

ITPP emerged from work by Claude Nicolau and colleagues in the late 2000s on membrane-permeant allosteric hemoglobin effectors, with the goal of improving tissue oxygenation. Early preclinical papers characterized its red-cell permeation and oxygen-affinity effects around 2008-2011. It was developed for oncology under the code OXY111A by a Swiss group, leading to a first-in-human Ib/IIa protocol (published 2016) and Phase Ib dose-escalation results (published 2021) in hepatopancreatobiliary cancers. In parallel it drew attention as a doping agent: anti-doping laboratories developed detection methods for ITPP in urine and in equine plasma in the mid-2010s, and it was placed on the WADA prohibited list as a hemoglobin/oxygen-transport modulator. It has not advanced to approval for any indication.

What the research says

Human evidence is thin and confined to oncology, not performance. The most substantive human data is a single-center, open-label Phase Ib dose-escalation trial in 28 patients with advanced hepatopancreatobiliary and colorectal-metastatic tumors, in which ITPP (OXY111A) was given as nine 8-hour intravenous infusions over three weeks across eight escalating dose cohorts. That study was designed to assess safety, established a maximum tolerated dose, and reported mostly disease stabilization rather than tumor shrinkage; it was not a controlled efficacy trial and cannot establish clinical benefit. The bulk of supporting data is preclinical: rodent tumor-oxygenation and irradiation-response models, cardiovascular/ischemia models, and in-vitro red-cell studies characterizing the hemoglobin-affinity shift. There are no published human trials evaluating ITPP for athletic performance, endurance, or exercise capacity, and no robust human efficacy or long-term safety data for any use. Claims about endurance benefit in people are extrapolated from mechanism and animal work, not demonstrated.

Reported effects

Right-shifts the oxygen-hemoglobin dissociation curve, increasing oxygen release from red cells to tissue (demonstrated in vitro and in animals)
Increases oxygenation of hypoxic tissue, including tumor tissue, in rodent models
Proposed (unproven in humans) enhancement of exercise/endurance capacity via greater oxygen delivery to muscle
In the human oncology trial, produced mostly disease stabilization rather than measurable tumor regression
No confirmed performance or ergogenic effect has been shown in any human study
Does not increase red blood cell count or hemoglobin mass (distinct from EPO or blood transfusion)

Dosing & administration (informational)

Informational only, not a protocol and not an endorsement of use. The only well-documented human dosing comes from the Phase Ib oncology trial, where ITPP was given intravenously as nine 8-hour infusions over three weeks in escalating cohorts (reported in the literature spanning roughly 1,866 up to 14,500 mg/m2, with a maximum tolerated dose around 12,390 mg/m2) under continuous medical supervision in a hospital trial setting. Those figures are body-surface-area, hospital-administered oncology doses and have no bearing on the oral or self-injected amounts sold to consumers, for which no validated, safe, or effective dose exists. There is no established human dose for performance or general use, and no legitimate dosing guidance can be given here.

This is general research/context information, not medical advice or a recommended protocol.

Safety & side effects

No robust human safety data outside one small IV oncology trial; oral or injectable consumer use is entirely unstudied and unmonitored
In the Phase Ib trial the most common related finding was hypercalcemia (about two-thirds of patients), along with electrolyte disturbances (low magnesium, low phosphate) and mild hypertension
Altering hemoglobin oxygen affinity affects oxygen delivery system-wide; consequences of chronic or high-dose exposure in healthy people are unknown
As a phosphate/pyrophosphate-class compound, there is plausible concern for calcium/phosphate and mineral-metabolism disturbance and effects on bone, none well characterized long-term
Gray-market products have no verified identity, purity, dose, or sterility; injectable use of unverified material adds infection and contamination risk
Not evaluated in pregnancy, and no data on drug interactions or cumulative dosing in humans
Because it is a banned method in sport, use carries anti-doping sanction risk in addition to health uncertainty

Drug & supplement interactions

F
o
r
m
a
l
h
u
m
a
n
d
r
u
g
-
i
n
t
e
r
a
c
t
i
o
n
s
t
u
d
i
e
s
h
a
v
e
n
o
t
b
e
e
n
p
u
b
l
i
s
h
e
d
.
M
e
c
h
a
n
i
s
t
i
c
a
l
l
y
,
c
o
m
b
i
n
i
n
g
I
T
P
P
w
i
t
h
a
n
y
t
h
i
n
g
e
l
s
e
t
h
a
t
a
l
t
e
r
s
o
x
y
g
e
n
d
e
l
i
v
e
r
y
o
r
b
l
o
o
d
p
h
y
s
i
o
l
o
g
y
(
E
P
O
,
b
l
o
o
d
t
r
a
n
s
f
u
s
i
o
n
o
r
b
l
o
o
d
d
o
p
i
n
g
,
o
t
h
e
r
h
e
m
o
g
l
o
b
i
n
m
o
d
u
l
a
t
o
r
s
,
a
l
t
i
t
u
d
e
o
r
h
y
p
o
x
i
c
t
r
a
i
n
i
n
g
)
c
o
u
l
d
c
o
m
p
o
u
n
d
c
a
r
d
i
o
v
a
s
c
u
l
a
r
s
t
r
a
i
n
a
n
d
i
s
p
r
e
c
i
s
e
l
y
t
h
e
k
i
n
d
o
f
s
t
a
c
k
i
n
g
a
n
t
i
-
d
o
p
i
n
g
r
u
l
e
s
t
a
r
g
e
t
.
B
e
c
a
u
s
e
t
h
e
h
u
m
a
n
t
r
i
a
l
s
h
o
w
e
d
h
y
p
e
r
c
a
l
c
e
m
i
a
a
n
d
e
l
e
c
t
r
o
l
y
t
e
s
h
i
f
t
s
,
c
o
n
c
u
r
r
e
n
t
d
r
u
g
s
a
f
f
e
c
t
i
n
g
c
a
l
c
i
u
m
,
p
h
o
s
p
h
a
t
e
,
o
r
m
a
g
n
e
s
i
u
m
(
v
i
t
a
m
i
n
D
,
c
a
l
c
i
u
m
s
u
p
p
l
e
m
e
n
t
s
,
d
i
u
r
e
t
i
c
s
,
b
i
s
p
h
o
s
p
h
o
n
a
t
e
s
)
a
r
e
a
t
h
e
o
r
e
t
i
c
a
l
c
o
n
c
e
r
n
.
T
h
e
m
i
l
d
b
l
o
o
d
-
p
r
e
s
s
u
r
e
e
f
f
e
c
t
s
e
e
n
i
n
t
r
i
a
l
s
m
e
a
n
s
i
n
t
e
r
a
c
t
i
o
n
s
w
i
t
h
a
n
t
i
h
y
p
e
r
t
e
n
s
i
v
e
s
o
r
o
t
h
e
r
c
a
r
d
i
o
v
a
s
c
u
l
a
r
d
r
u
g
s
a
r
e
p
l
a
u
s
i
b
l
e
.
N
o
n
e
o
f
t
h
i
s
i
s
w
e
l
l
c
h
a
r
a
c
t
e
r
i
z
e
d
,
a
n
d
a
n
y
r
e
a
l
-
w
o
r
l
d
c
o
m
b
i
n
a
t
i
o
n
i
s
u
n
s
t
u
d
i
e
d
.

Who should avoid it

Competitive athletes subject to anti-doping testing (banned method; sanction risk)
Anyone with cardiovascular disease, given unknown effects of altering systemic oxygen delivery and observed blood-pressure changes
People with disorders of calcium, phosphate, or bone/mineral metabolism, given the hypercalcemia and electrolyte findings
Pregnant or breastfeeding individuals (no safety data)
Anyone considering injecting unverified gray-market material (sterility and contamination risk)
Anyone seeking a proven performance aid, since human efficacy has never been demonstrated

How it is commonly combined

This site does not provide performance-enhancement stacking guidance, and there is no evidence base for combining ITPP with other agents in humans. In sport, deliberately combining ITPP with EPO, blood transfusion, or other oxygen-transport methods is both an aggravated anti-doping violation and a genuine safety hazard (excessive strain on the oxygen-delivery system). For the health goals people cite (endurance, tissue oxygenation), the evidence-supported and legal options are ordinary aerobic training, adequate iron status, and, where medically indicated, physician-managed care, not investigational hemoglobin modulators.

Legal & regulatory. Not FDA-approved for any indication and not a lawful dietary supplement. ITPP is an investigational compound studied in humans only in one small early-phase oncology trial (as OXY111A); it holds no marketing authorization anywhere. Material sold to consumers online is gray-market, typically labeled "research chemical, not for human consumption," and is not quality-controlled. In sport it is prohibited: the World Anti-Doping Agency treats ITPP as a prohibited hemoglobin/oxygen-transport modulator under Prohibited Methods M1 (manipulation of blood and blood components), banned at all times, and it is also a doping concern in horse racing. It is not a US-scheduled controlled substance, so possessing the bulk chemical is not itself a drug-scheduling offense, but using it as a supplement or drug is unapproved and using it in competition is a doping violation.

Quality & harm reduction

T
h
e
r
e
i
s
n
o
p
h
a
r
m
a
c
e
u
t
i
c
a
l
-
g
r
a
d
e
,
F
D
A
-
a
p
p
r
o
v
e
d
I
T
P
P
p
r
o
d
u
c
t
a
v
a
i
l
a
b
l
e
t
o
c
o
n
s
u
m
e
r
s
.
C
l
i
n
i
c
a
l
-
t
r
i
a
l
m
a
t
e
r
i
a
l
(
O
X
Y
1
1
1
A
)
w
a
s
p
r
o
d
u
c
e
d
t
o
t
r
i
a
l
s
t
a
n
d
a
r
d
s
a
n
d
i
s
n
o
t
w
h
a
t
i
s
s
o
l
d
o
n
l
i
n
e
.
C
o
n
s
u
m
e
r
p
r
o
d
u
c
t
s
m
a
r
k
e
t
e
d
a
s
I
T
P
P
p
o
w
d
e
r
s
o
r
i
n
j
e
c
t
a
b
l
e
s
o
l
u
t
i
o
n
s
a
r
e
u
n
r
e
g
u
l
a
t
e
d
r
e
s
e
a
r
c
h
c
h
e
m
i
c
a
l
s
w
i
t
h
n
o
g
u
a
r
a
n
t
e
e
d
i
d
e
n
t
i
t
y
,
p
u
r
i
t
y
,
s
a
l
t
f
o
r
m
,
e
n
d
o
t
o
x
i
n
c
o
n
t
r
o
l
,
o
r
s
t
e
r
i
l
i
t
y
;
a
v
e
n
d
o
r
c
e
r
t
i
f
i
c
a
t
e
o
f
a
n
a
l
y
s
i
s
i
s
n
o
t
i
n
d
e
p
e
n
d
e
n
t
v
e
r
i
f
i
c
a
t
i
o
n
.
D
i
f
f
e
r
e
n
t
s
a
l
t
f
o
r
m
s
(
e
.
g
.
,
h
e
x
a
s
o
d
i
u
m
,
h
e
x
a
-
t
r
i
e
t
h
y
l
a
m
i
n
e
)
a
p
p
e
a
r
i
n
t
h
e
l
i
t
e
r
a
t
u
r
e
a
n
d
c
a
t
a
l
o
g
s
,
a
d
d
i
n
g
l
a
b
e
l
a
m
b
i
g
u
i
t
y
.
I
n
d
e
p
e
n
d
e
n
t
t
h
i
r
d
-
p
a
r
t
y
t
e
s
t
i
n
g
w
o
u
l
d
b
e
r
e
q
u
i
r
e
d
t
o
k
n
o
w
w
h
a
t
a
n
y
g
i
v
e
n
p
r
o
d
u
c
t
a
c
t
u
a
l
l
y
c
o
n
t
a
i
n
s
,
a
n
d
e
v
e
n
t
h
e
n
i
t
d
o
e
s
n
o
t
m
a
k
e
t
h
e
c
o
m
p
o
u
n
d
a
p
p
r
o
v
e
d
o
r
s
a
f
e
f
o
r
h
u
m
a
n
u
s
e
.

Safer, legal alternative we recommend

Liver Let Live. For liver and metabolic support, our Liver Support formula is a legal supplement option covering a similar goal.

See our recommended pick

Find ITPP (myo-inositol trispyrophosphate) →

Know your numbers before you research

Order your own bloodwork online — hormone, metabolic and inflammation panels, no doctor visit needed. Know your baselines before and during any protocol. Independent bloodwork is the cheapest insurance there is.

Get tested with Ulta Lab Tests →

Frequently asked questions

Does ITPP actually improve endurance or athletic performance in humans?

There is no human trial showing it does. The endurance rationale is extrapolated from its mechanism (shifting the oxygen dissociation curve so muscle gets more oxygen) and from animal data. The only human studies are small oncology safety trials, which were not performance studies. Any claim of proven ergogenic benefit in people is unsupported.

Is ITPP the same as inosine triphosphate?

No. That is a common naming error. ITPP here stands for myo-inositol trispyrophosphate, the hemoglobin-affinity modulator (development code OXY111A). Inosine triphosphate is an unrelated nucleotide. Vendor and blog pages sometimes mix these up.

Is ITPP legal to buy or use?

It is not FDA-approved and is not a lawful dietary supplement; it is sold as a research chemical not for human consumption. It is not a US-scheduled controlled substance, but it is a WADA-prohibited method in sport, so any competitive athlete using it faces a doping violation. It also carries a doping ban in horse racing.

What did the human cancer trials actually find?

A Phase Ib dose-escalation study in about 28 patients with liver, pancreatic, biliary, and colorectal-metastatic cancers found it was tolerable up to a maximum tolerated dose, with hypercalcemia and electrolyte shifts as the main related findings and mostly disease stabilization rather than tumor shrinkage. It was a safety study and did not prove clinical efficacy.

How is ITPP different from EPO or blood doping?

EPO and transfusion increase the amount of oxygen the blood can carry by raising red-cell mass. ITPP does not raise red-cell count; it changes how readily existing hemoglobin releases oxygen to tissue. The intended endpoint (more oxygen delivered) overlaps, which is why anti-doping bodies group it with oxygen-transport-enhancing methods.

What can I dose it at?

This site does not provide dosing guidance. The only documented human dosing is hospital-administered intravenous infusion in a supervised oncology trial, which has no relevance to consumer use, and no safe or effective human dose exists for performance or general use. Anyone considering an investigational compound like this should talk to a qualified clinician.

References & further reading

PubMed: myo-inositol trispyrophosphate allosteric effector hemoglobin red blood cell permeation
PubMed: myo-inositol trispyrophosphate ITPP tumour oxygenation irradiation rodent models
PubMed: Phase Ib dose-escalation OXY111A myo-inositol trispyrophosphate hepatopancreatobiliary tumors
PubMed: myo-inositol trispyrophosphate ITPP doping control urine detection mass spectrometry
ClinicalTrials.gov: OXY111A myo-inositol trispyrophosphate hepato-pancreato-biliary neoplasms