Tigecycline
Tetracyclines · given by intravenous · on the market since 2005
What it's made of
Each functional group on the molecule does a specific, predictable job.
Basic amine
What it does. Neutral enough to slip through membranes, then becomes charged inside the acidic compartments of the cell and gets trapped there. Concentrations inside cells can reach many times the blood level.
What it opens up. Diseases of the cell's internal recycling compartments, and a common reason a drug accumulates in lung, liver, and eye tissue far beyond what the blood level suggests.
Michael acceptor
What it does. Reacts with the sulfur groups on proteins, forming a permanent bond. The cell reads this as a chemical stress signal and switches on its whole antioxidant defence programme.
What it opens up. Any disease driven by oxidative stress or chronic inflammation, because the drug does not treat the disease so much as turn on the body's own repair response.
Phenol
What it does. The liver's favourite attachment point. It tags this group and flushes the molecule out, often within an hour.
What it opens up. Usually shortens the drug's life. Blocking or masking this position is the standard way to make a compound last longer.
Four-ring fused core
What it does. Beyond its known job, this frame binds metal ions inside human enzymes that break down tissue scaffolding — an activity completely separate from its original purpose and active at much lower doses.
What it opens up. Below its usual dose it is not an antibiotic at all but a tissue-protection agent — gum disease, skin inflammation, aneurysm progression.
Where it can get to
Predicted from molecular weight, lipophilicity, polar surface area and hydrogen-bond donor count. A drug can only act where it distributes, so this constrains which conditions are addressable before any biology is considered. derived
What it binds — and whether we can reach it
Binding affinity is only meaningful against the plasma concentration reached at the approved dose. A target requiring higher concentrations cannot be engaged in a patient, whatever the in vitro potency. Most repurposing hypotheses fail at this step, and it is rarely checked before a trial is proposed. measured
No human binding data published for this molecule. Missing data, not an absence of targets.
New uses, and who is already trying them
No human binding data has been published for this molecule, so no conditions can be linked to it yet.
Why nobody will fund it
4 companies make this across 4 approved products. With that many manufacturers the price has fallen to production cost. A company funding a trial could not recover it — competitors could market the same molecule for the new indication immediately, without contributing.
A new route or dosage form qualifies for a 505(b)(2) application, which carries three years of exclusivity for that formulation. It is the only remaining route to exclusivity on a generic molecule.
What it would cost to find out
Derived, not quoted. Events needed is 4(zα+zβ)²/ln(HR)²; enrolment is that divided by the event rate and follow-up. The 1/ln(HR)² term dominates: halving the detectable effect size roughly quadruples enrolment. derived
Cost per person reached is the relevant metric for a non-commercial funder, since there is no revenue to set against the outlay.
Ask for ideas nobody has listed
Reasons from the functional groups and distribution above, excluding conditions already listed. Output is hypotheses for falsification, not findings. Not medical advice.
Who might pay for the trial
Trials of off-patent drugs are rarely funded by venture capital or pharma. They are paid for by government grants and disease foundations. Here is who has funded work on this molecule before, what federal mechanisms are open now, and which foundations fund trials in the disease areas it touches. measured
No federally funded project currently mentions this drug by name. That means work is either funded privately or has not yet been proposed to federal agencies.
Open notices with an explicit mandate to fund work on approved or off-patent molecules.
Grants.gov lists US federal money. Many off-patent drug trials are supported by disease foundations and nonprofits. These are matched to the body systems this drug touches. assumed
Who manufactures it
Companies holding an approved abbreviated application for this molecule in the United States, from the FDA Orange Book. Supply already exists at scale, so a trial would not need a manufacturing programme — but any of these could also be a partner, or an objector.
Nothing on this page is medical advice. Candidate uses are unproven hypotheses derived from public data; established uses are listed for verification only. Figures carry their provenance inline — anything marked assumed or derived is not a measurement.
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