Organic Active Ingredients TRIZ Cases

Formula 1 tetrazines cut enzyme inhibition, raise tolerated dose, and simplify synthesis while preserving bioorthogonal ligation.

Complementary sequences fold the poly(A) tail into stem-loop or pseudoknot structures, protecting mRNA and boosting protein expression.

A fixed-dose compound and bile acid combination helps reduce oxidative damage and mitochondrial dysfunction in neuronal cells.

Chemically modified siRNA duplexes silence DGAT2 to curb hepatic triglyceride buildup and liver inflammation in NAFLD and NASH.

Stable salt intermediates 2a and 3 improve finerenone yield and optical purity while avoiding separate desalting and reducing process complexity.

A sugar-sphere modified-release huperzine formulation lowers peak plasma levels, supports higher twice-daily dosing, and reduces adverse events.

Selective fused heterocycles target 5-HT2A over 5-HT2B to treat neurological disorders while lowering valvular toxicity risk.

A quinoline butenamide composition targets rare EGFR mutations such as L861Q, G719X, and S768I to inhibit tumor cell growth.

Reduced pemafibrate dosing for Child-Pugh A or B cirrhosis controls drug exposure while preserving treatment efficacy and safety.

Indented aliphatic polyurethane foam improves fluid distribution and air flow while in-line profiling cuts post-processing time and cost.

A novel benzamide scaffold improves NAMPT inhibition by tuning substituent groups, supporting cancer therapy where existing treatments fall short.

Bifunctional quinazoline compounds recruit E3 ligase to degrade KRAS G12D, addressing targeted pancreatic cancer treatment limits.

Separate phase sterilization and aseptic mixing keep multi-drug ophthalmic drops stable, potent, and microbially safe for extended storage.

Selective MET inhibitor scaffolds tune substituents to target aberrant MET signaling in cancer while limiting off-target toxicity.

Antisense oligonucleotides hybridize with PKK mRNA to lower PKK protein levels and help treat inflammatory and thromboembolic conditions.

Bifunctional compounds recruit α-synuclein to E3 ligases, overcoming weak small-molecule disruption and enabling targeted proteolysis.

Hydrogen-bonded pterostilbene cocrystals raise water solubility and dissolution rate, helping improve bioavailability in medicament and supplement forms.

Small molecules such as concanamycin A block Nef-driven MHC-I loss, helping CTLs detect and clear hidden HIV-infected cells.

By blocking the p53-MDM2 interaction, DRG-MDM2-1 restores p53 function and drives apoptosis and cell cycle arrest in cancer cells.

Modified sugar groups replace complex noviose moieties to preserve Hsp90 binding while improving solubility, stability, and synthesis.

Butaphosphan and trace element complexes keep Vitamin B12 stable in a high-concentration livestock injection while reducing tissue irritation.

Selective p300/CBP bromodomain inhibitors help counter cancer drug resistance and extend anti-tumor efficacy, including in combination therapy.

Combining antibacterial, antifungal, and anti-inflammatory agents in one topical formulation helps treat mixed skin and nail infections while limiting resistance risk.

A freeze-dried polymyxin and zidovudine formulation solves parenteral stability and solubility limits while enabling sterile reconstitution for injection.

Stable heavy isotopes in amide groups slow bond cleavage to improve drug metabolic stability, pharmacokinetics, and tolerability.

Substituted benzoannulene compounds trigger ERα degradation rather than simple blockade, helping address endocrine resistance in ERα-positive breast cancer.

Targeting SARM1 mRNA with antisense oligonucleotides lowers SARM1 levels to prevent or slow axonal degeneration in neurodegenerative disease.

Exosomes from iPSC-derived mesenchymal stem cells target NASH by suppressing lipogenesis, inflammation, and ER stress with improved safety.

Preselected cannabis powder PSD and vortex milling improve cannabinoid extraction yield while preserving free-flowing powder for formulation.

Novel Formula (I) HIV capsid inhibitors balance replication suppression with lower toxicity and a higher barrier to resistance.

Combining TKIs with anti-EGF immunization blocks EGF/EGFR signaling and helps prevent acquired resistance in NSCLC treatment.

Engineered E. coli and yeast convert anthranilate or indole into tryptamines, replacing slow extraction and costly synthesis.

Substituted bridged morpholine and piperidine compounds modulate monoamine release to treat CNS disorders with fewer side effects.

Targeted ALK2 inhibitor compounds address limited FOP and DIPG therapies by blocking mutant kinase activity and reducing ossification or glioma growth.

A mixed hop and Cynanchum wilfordii extract improves bone formation and blood lipids while avoiding key side effects of estrogen and alendronate.

Enfumafungin-derived triterpenoids inhibit β-D-glucan synthesis to treat Pneumocystis pneumonia with strong lung exposure and better tolerability.

Novel benzamides tune substituent patterns to boost JAK potency and selectivity while reducing side effects and resistance.

Hydroflumethiazide inhibits TNF-α activity to treat rheumatoid arthritis while avoiding costly injections, cold storage, and major adverse effects.

Using Bifidobacterium strains in supplements or medicaments improves insulin sensitivity, glucose tolerance, and inflammation in diabetes.

PFKFB3 inhibition with YC-6 lowers lactate buildup, protects lung epithelial and endothelial cells, and reduces vascular permeability.

LNPs deliver nucleic acids encoding anticancer peptides to tumors, improving local anti-tumor response while limiting severe morbidity.

Condensed mesenchymal cell bodies in a hydrogel enable off-the-shelf, minimally invasive repair of cartilage, tendon, and ligament defects.

A topical DNA-RNA heteroduplex silences androgen receptor mRNA to promote hair growth while avoiding finasteride-like side effects.

Carbohydrate-derived TLR modulators balance Th1/Th2 cytokines to boost clearance while reducing toxicity, tissue injury, and inflammation.

miRNA binding sites in the Poly(A) tail enable tissue-specific mRNA expression, improving stability while reducing off-target effects.

Blocking ATP binding in constitutively active FGFR3 mutants restores bone growth and offers a less painful option for skeletal disorders.

NMN relieves nociceptive pain, allodynia, and hyperalgesia while avoiding the major side effects linked to conventional analgesics.

Monothioglycerol and phosphate buffering help keep hydrocortisone sodium phosphate stable in water while supporting rapid exposure for emergency use.

Fasting-state sepiapterin dosing raises plasma, CSF, and brain exposure by speeding absorption and limiting peripheral conversion to BH4.

Micheliolide boosts muscle fiber, weight, and strength while offering a safer approach for sarcopenia and cachexia treatment.

By recruiting cereblon to ubiquitinate androgen receptors, this PROTAC approach degrades mutated and overexpressed AR linked to therapy resistance.

A pyridopyrazine integrase inhibitor raises the resistance barrier and supports long-acting HIV treatment with fewer painful injections.

Splice-switching ASOs redirect SLAMF6 isoform expression to boost T cell activation and IL-2 secretion while reducing tumor load.

Single-molecule thienopyranone and furanopyranone inhibitors block PI3K, CDK4/6, and BRD4 to reduce resistance, toxicity, and regimen complexity.

Using Hesperaloe-derived saponin extracts in animal feed cuts extract cost while supporting poultry immunity and coccidiosis control.

A stepwise Tezacaftor synthesis with protected intermediates and purification stages improves yield and purity for industrial production.

Specific AhR-binding scaffolds improve selective modulation to reduce inflammation and fibrosis in Crohn's disease and related conditions.

Genotype-guided ARHGEF12 inhibitor dosing targets elevated intraocular pressure and improves glaucoma treatment consistency.

Novel CRM1 inhibitor compounds modulate nuclear transport while reducing toxicity and improving tolerability in cancer, inflammation, and viral disorders.

Topical alpha-adrenergic antagonists reduce pupil diameter and improve visual performance with once-daily dosing and minimal eye redness.

Specific L. rhamnosus GM-020 ODN fragments suppress lipid droplet formation and FAS expression, enabling targeted anti-lipogenesis compositions.

A spray-dried polymer dispersion improves TRPC5 inhibitor delivery to curb proteinuria and help preserve kidney function in nephropathies.

Blocking intestinal bile acid reabsorption with ASBT inhibitors lowers serum bile acids and pruritus in cholestatic liver disease.

Topical sulindac reduces inflammation and promotes tissue repair in difficult-to-heal diabetic wounds, helping speed epithelialization.

Substituted monocyclic heteroaryl compounds offer a small-molecule route to target Huntington's disease and address a major treatment gap.

Recombinant TCRs target shared non-mutated tumor epitopes while suppressing endogenous TCR expression to broaden cancer gene therapy use.

pH-responsive ionizable lipids in LNPs protect mRNA from degradation, improve cellular uptake, and enable lower-dose vaccination with fewer adverse reactions.

Galactose-lipid nanoparticles deliver XO-targeting siRNA to the liver while improving stability, specificity, and gout treatment efficacy.

Oral udenafil improves MPI, cardiac output, and exercise capacity in Fontan and single ventricle heart disease patients.

SA-β-gal-cleavable prodrugs release cytotoxic agents in senescent cells, improving selectivity while limiting off-target toxicity and inflammation.

Quaternary amine compounds with isopropylmethylphenol ester moieties target herpes viruses, HPV, bacteria, and Candida resistant to current drugs.

Cysteine-targeting small molecules block gut bacterial BSH, lowering secondary bile acids with selective activity for metabolic and inflammatory disorders.

Esterifying brefeldin A improves water solubility, bioavailability, plasma half-life, and safety while preserving antitumor activity.

Small molecules that activate dynamin help restore podocyte actin structure, reduce proteinuria, and improve kidney function.

Localized TGF-β and CTGF injection promotes collagen repair while reducing swelling and pain in injured tendons, fascia, and joint capsules.

A combined anti-inflammatory and gram-positive-targeting therapy treats atopic dermatitis while limiting resistance and preserving beneficial flora.

A staged sotorasib lead-in before anti-PD-1 or PD-L1 therapy helps limit severe adverse events while sustaining cancer control.

A multi-kinase pyridopyrimidinone targets GCK and ACK1 to overcome compensatory NRAS signaling while limiting cytotoxicity.

Coated pancreatic enzymes target digestive insufficiency to reduce ASD and ADHD symptoms while avoiding sedating side effects.

Sequence-optimized oligonucleotides target lincTreg1 to modulate Treg activity while limiting off-target effects and immunogenicity.

Rose bengal compounds block TDP-43 RNA binding and stabilize SOD1 dimers to inhibit toxic aggregates linked to ALS progression.

Pyrazole-based DDR1 and DDR2 inhibitors improve kinase inhibition and specificity for cancer and fibrotic disease treatment.

A 5-pyridine-1H-indazole scaffold improves CLK2 selectivity, strengthens DYRK1A inhibition, and supports chondroprotection in osteoarthritis.

Dual-acting pyrazole and imidazole compounds target orexin and kappa-opioid receptors to improve efficacy while avoiding multi-drug interactions.

Once-daily fed oral dosing of vepdegestrant balances ER degradation and tumor inhibition with lower adverse event risk.

Phosphatidylglycerol nanovesicles bind tumor-secreted Hsp70 to block M2 macrophage polarization and reduce tumor growth.

SBEβCD inclusion complexing with bicarbonate raises meloxicam solubility and bioavailability for faster oral pain relief.

A sesqui-hydrated Type 4 pritelivir crystal form improves humidity stability and aqueous solubility for more effective HSV treatment.

A self-assembling compound co-assembles with denatured proteins to reduce ER stress, cytotoxicity, and cell death.

Novel crystalline and co-crystal forms replace an unstable amorphous API state to improve dissolution, bioavailability, and storage stability.

Modified oil-in-water microemulsions solubilize DHEA and pregnenolone for stable oral absorption with reduced liver stress.

Esterified THCA, CBGA, and CBNA improve resistance to decarboxylation, supporting more stable cannabinoid therapies and combination use.

Engineered T cells with heterologous TCR and CD8 target MAGE-A4 to improve gastroesophageal cancer response with fewer side effects.

Synthetic CBD and omega-3 emulsion enables parenteral delivery with low THC, high bioavailability, low irritation, and year-long stability.

Water-less nanostructures use surfactants and solvents to raise oral active-compound loading while preserving stability and bioavailability.

A stable delgocitinib cream enables topical JAK inhibition for DLE, improving lesion severity and safety versus limited existing treatments.

Apicidin sensitizes cervical cancer cells to bevacizumab, improving apoptosis and tumor growth inhibition in recurrent or resistant disease.

Bacteroides ovatus cell-free metabolites boost IFNγ secretion and CD8+ T cell infiltration to strengthen ICI treatment in NSCLC.

Indazole allosteric modulators potentiate mGluR4 while improving solubility and oral bioavailability for neurological disorders.

ADGRL3 SNP testing adds objective mTBI risk assessment beyond clinical evaluation and supports fasoracetam-based symptom management.

SBEβCD inclusion complexing with bicarbonate raises meloxicam solubility and bioavailability for faster, sustained pain relief.

A topical alpha-adrenergic eyelid composition lifts Müller's muscle to treat ptosis without surgery, improving visual axis and appearance.

Chlorinated tetralin compounds combined with gamma-secretase inhibitors improve anti-tumor activity in Notch-driven cancers and desmoid tumors.

Non-viral lipid vectors and immune cell-specific promoters enable in vivo CAR expression without complex ex vivo cell engineering.

A dual alkylating and HDAC-inhibiting regimen targets relapsed or resistant Hodgkin lymphoma and improves response potential.

Bifunctional compounds recruit TYK2 to cereblon for ubiquitination and degradation, improving selectivity beyond ATP-site JAK inhibition.

Modulating KRAS with structured compound variants helps address hard-to-target mutations and expands treatment options for cancer.

Small heterocyclic compounds block PD-1/PD-L1 binding to counter tumor immune evasion and strengthen immune response against cancer.

Combining a BCL-2 inhibitor with SEL24/MEN1703 blocks resistance pathways in AML and boosts cytotoxicity with lower toxicity.

PolQ-targeting thiadiazolone derivatives block alternative end-joining to help treat HRD cancers resistant to cisplatin and PARP inhibitors.

GalNAc-conjugated antisense oligomers improve hepatocyte uptake and ApoCIII suppression while reducing kidney exposure and tolerability risks.

An enteric coating with a moisture barrier delays pitolisant release to the intestine, reducing nausea and stomach upset while preserving bioequivalence.

A dry powder JAK inhibitor formulation targets COPD inhalation delivery while improving bioavailability consistency and lung function in T2-low patients.

Surfactants and suspending agents keep this hydrophobic ocular drug stable in water, enabling topical pain relief and dry eye treatment.

Combining a piperazine compound with radiotherapy improves anti-tumor consistency and tolerability in solid tumors with variable treatment response.

Electrospun calreticulin polymer matrices promote keratinocyte and fibroblast migration to improve healing of chronic diabetic wounds.

Small-molecule compounds lower mutant huntingtin without invasive delivery, offering a potential disease-modifying option for Huntington's disease.

Covalent compounds bind KRAS G12D in GTP- and GDP-bound states, bypassing tight nucleotide affinity to improve direct RAS inhibition.

A hypromellose-based dispersible dabrafenib mesylate tablet balances rapid reconstitution, bioavailability, and stability for pediatric oral suspension.

Salt co-crystals convert Compound 1 into a shock-safe, more water-soluble solid form for therapeutic use and easier handling.

Phospholipid nano-emulsions keep Vitamin D on the eye longer, improve corneal delivery, and reduce irritation in ocular use.

Substituted macrocyclic orexin-2 agonists improve receptor activity, brain permeability, and safety for narcolepsy treatment.

Dual BTK and JAK3 inhibition with selective 1,3-benzodioxol derivatives helps treat rheumatoid arthritis while minimizing JAK2-linked anemia.

A naloxone-DMF solvate enables seeded or spontaneous crystallization that cuts purification steps, waste, and energy while improving yield and purity.

Selective 1,3,4-oxadiazole HDAC6 inhibitors address class I HDAC side effects while supporting treatment of cancer and other HDAC6-mediated diseases.

A buccal mucoadhesive DMT formulation extends therapeutic blood levels beyond rapid-onset dosing, improving treatment-resistant depression symptoms.

Human serum albumin and soybean oil form elemene nanoparticles that improve solubility while reducing irritation, hemolysis, and side effects.

Hydrogen bonding between polyvinyl alcohol resin and tannic acid builds tablet hardness while sustaining release of water-soluble drugs.

Novel RET-selective compounds target wild type and mutant RET to overcome resistance while limiting off-target kinase toxicity.

Separate granulation and excipient design keep ambrisentan and tadalafil stable together while preserving fast tablet disintegration and dissolution.

SCY-078 maintains and enhances antifungal potency in acidic sites, improving treatment of vaginal and gastrointestinal fungal infections.

An MC1R agonist lowers inflammatory and fibrotic markers to help treat interstitial lung disease and systemic sclerosis symptoms.

Targeted KHK inhibitor compounds curb fructose metabolism while maintaining liver selectivity and metabolic stability for NASH treatment.

Specific HMOs replace inconsistent probiotic and prebiotic approaches by increasing bifidobacteria and supporting infant immune and gut development.

Injected ice slurry destroys subcutaneous fat cells through phase-change cooling, reducing invasiveness and avoiding general anesthesia.

Nitrogen-protected low-dose epinephrine in flexible containers resists oxidation and isomerization for ready-to-inject storage.

Strong and weak anion exchange purification yields a water-soluble β-1,3/1,6-glucan with controlled 1-50 kDa mass, high purity, and stronger antitumor activity.

Selective pyrazolopyrimidine A2a antagonists improve A1 receptor specificity and aqueous solubility, supporting oral treatment use.

Liposome-delivered mitoxantrone combined with capecitabine offers a new option for recurrent or metastatic nasopharyngeal carcinoma after first-line failure.

A nuclease and cleavaging agent target cancer-specific In/Del sequences to kill mutated cells while minimizing damage to normal cells.

Using Polygonum multiflorum extract or THSG, this case addresses sarcopenia by increasing muscle mass, strength, and exercise performance.

A selective 5-heteroaryl-1H-pyrazol-3-amine CHK1 inhibitor uses liposomal sustained release to reduce hepatotoxicity and hemocyte toxicity.

A fixed 2:1 to 4:1 acetaminophen-naproxen oral dosage improves minor pain relief while avoiding opioid-related contraindications.

A TCM and Western drug regimen for ALS slows progression while reducing toxic side effects and supporting muscle strength and recovery.

Targets histone acetylation and glutamine metabolism to treat atopic dermatitis and psoriasis with fewer long-term side effects.

Needle-free epinephrine dry powder uses controlled particle sizing and airflow delivery to improve nasal deposition and absorption for anaphylaxis.

An IV trehalose formulation offers a less invasive way to alleviate mucopolysaccharidosis symptoms while improving distribution to hard-to-reach tissues.

Specific melflufen dosing, often with dexamethasone, targets AL amyloidosis while reducing toxicity and organ damage versus current therapies.

A biphasic drospirenone dosing regimen treats endometriosis pain while inducing amenorrhea and providing contraception without estrogen-related effects.

Compounds that degrade IKZF2 and CK1α address a key AML bottleneck by reducing leukemia cell proliferation and promoting apoptosis.