NOV-002
Also known as: GSSG-Pt complex, NovaBay NOV-002, Novelos NOV-002, Oxidized glutathione-cisplatin
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Summary
NOV-002 is an investigational glutathione disulfide (GSSG) mimetic studied as an adjunct to chemotherapy for solid tumours. Administered by intravenous or subcutaneous injection, it is intended to modulate cellular redox balance, enhance anti‑tumour efficacy and lessen chemotherapy‑induced hematologic toxicity.
Mechanism of Action
NOV-002 is a substrate for glutathione reductase, rapidly converting to reduced glutathione (GSH) and generating a transient oxidative signal in plasma. This promotes protein S‑glutathionylation, especially of actin, and activates redox‑sensitive kinases such as p38, JNK, ERK, AKT, JAK2 and STAT5. The resulting signaling cascade is linked to increased hematopoiesis, immune stimulation and altered tumour cell proliferation, forming the basis of its proposed therapeutic effect.
What the Research Shows
Pre‑clinical work showed that NOV-002 produces dose‑dependent oxidative signals, raises intracellular ROS, and increases S‑glutathionylation, leading to activation of multiple kinase pathways and enhanced proliferation of HL‑60 cells. A mouse pharmacokinetic study reported a short plasma half‑life (~13 min) and conversion to GSH, with a brief decrease in total plasma thiols. Clinically, phase‑II data in advanced non‑small‑cell lung cancer indicated improved survival, tumour response and faster hematologic recovery when combined with standard chemotherapy. A neoadjuvant phase‑II breast‑cancer trial reported a 38 % pathologic complete response rate, higher than historical controls, and suggested mitigation of chemotherapy‑related blood‑count toxicity. Review articles note that NOV-002, along with other redox‑targeting agents, has entered phase‑III evaluation, but detailed outcomes are not provided in the abstracts.
Reported Benefits
Early clinical studies suggest NOV-002 may boost the efficacy of standard chemotherapy, increasing tumour response rates and overall survival in lung cancer, and raising pathologic complete response rates in breast cancer. It also appears to accelerate hematologic recovery and may enhance anti‑tumour immune activity, as reflected by changes in myeloid‑derived suppressor cells. These benefits are supported by pre‑clinical evidence of redox‑mediated activation of growth‑regulating pathways.
Limitations of the Evidence
Evidence is limited to small, early‑phase trials and pre‑clinical models; no large randomized controlled studies have confirmed efficacy or safety. Pharmacokinetic data reveal rapid clearance, raising questions about dosing practicality. The precise contribution of redox modulation to clinical outcomes remains uncertain, and long‑term safety data are lacking. Consequently, regulatory approval for any indication has not been achieved.
Safety Considerations
NOV-002 is not cytotoxic alone and has been reported to cause only transient oxidative stress in plasma. Clinical abstracts note improved hematologic recovery but do not detail specific adverse events. Potential concerns include unintended oxidative damage to normal tissues and interactions with other redox‑active drugs. Careful monitoring in trial settings is advised, and safety in broader patient populations remains to be established.
How It Is Administered
The compound is formulated as disodium glutathione disulfide and administered by intravenous infusion or subcutaneous injection. Dosing schedules in studies have included daily subcutaneous injections concurrent with chemotherapy or single intraperitoneal doses in animal models. Formulation details beyond route and injection frequency are not provided in the abstracts.
Routes of Administration
Goals & Uses
- Hematopoietic protection during chemotherapySupportive CareModerate
- Reduction of chemotherapy-induced myelosuppressionCytoprotectionModerate
- Immune modulation / restoration of immune functionImmunologyLow
- Enhancement of antitumor efficacy of chemotherapyOncology / AdjuvantLow
- Treatment of advanced non-small cell lung cancerOncologyLow
Contraindications
- Severe renal impairmentOrganModerateKidney function concerns
- Known hypersensitivity to glutathione or cisplatin componentsAllergyHigh
Adverse Effects
- Hypersensitivity reactionsImmunologicRare
- Injection site reactionsLocalCommon
- NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
- FatigueGeneralUncommonLow energy or tiredness
Drug Interactions
- CarboplatinLow
- PaclitaxelLow
- CisplatinModerate
Population Constraints
- Pediatric patientsAgeRelative
- Patients with pre-existing renal dysfunctionOrgan ImpairmentRelative
- Pregnant womenReproductiveRelative
Regulatory Status
- European UnionUnapprovedNot approved or filed for approval in the European Union.
- United StatesInvestigationalReceived FDA Fast Track designation for NSCLC; not approved. Development largely discontinued after failed Phase III.
- United KingdomUnapprovedNot approved in the United Kingdom.
NOV-002 was granted Fast Track designation by the FDA for NSCLC. The Phase III GALES trial did not meet its primary endpoint of overall survival improvement, and further development has largely stalled. It is not approved in any jurisdiction.
Evidence & Sources
- Journal ArticleModerateTownsend DM, Findlay VL, Tew KD2005-01-01T00:00:00.000000Z
- Journal ArticleModerateMontero AJ, Jassem J2011-01-01T00:00:00.000000Z
- Journal ArticleLowTownsend DM, Pazoles CJ, Tew KD2008-01-01T00:00:00.000000Z
- Journal ArticleLowUys JD, et al.2010-01-01T00:00:00.000000Z
- Journal ArticleLowTownsend DM, et al.2008-01-01T00:00:00.000000Z
- Journal ArticleModerateMontero AJ, et al.2012-01-01T00:00:00.000000Z
Frequently Asked Questions
What type of cancer has NOV-002 been tested in?
Phase‑II trials have evaluated NOV-002 in advanced non‑small‑cell lung cancer and in HER‑2‑negative stage II‑IIIc breast cancer, both as an addition to standard chemotherapy regimens.
How does NOV-002 differ from regular glutathione supplements?
Unlike dietary glutathione, NOV-002 is a stabilized GSSG mimetic that acts as a substrate for glutathione reductase, creating a brief oxidative signal that modifies protein thiols and activates redox‑sensitive signaling pathways.
Is NOV-002 approved for clinical use?
No. NOV-002 remains investigational; it has been studied in early‑phase clinical trials but has not received regulatory approval for any indication.
What are the main safety concerns with NOV-002?
The main concerns stem from its ability to generate oxidative stress, which could potentially damage normal cells or interact with other redox‑active agents. So far, trials have not reported serious adverse events, but comprehensive safety data are lacking.
Can NOV-002 be used alone to treat cancer?
Pre‑clinical data show NOV-002 is not cytotoxic by itself, and clinical studies have only examined it in combination with chemotherapy. Its proposed benefit is as a chemo‑sensitizer and hematopoietic support, not as a standalone therapy.
What is NOV-002?
NOV-002 is an investigational glutathione disulfide (GSSG) mimetic studied as an adjunct to chemotherapy for solid tumours. Administered by intravenous or subcutaneous injection, it is intended to modulate cellular redox balance, enhance anti‑tumour efficacy and lessen chemotherapy‑induced hematologic toxicity.
What is NOV-002 used for?
NOV-002 is educationally associated with: Hematopoietic protection during chemotherapy, Reduction of chemotherapy-induced myelosuppression, Immune modulation / restoration of immune function, Enhancement of antitumor efficacy of chemotherapy, Treatment of advanced non-small cell lung cancer. Educational only — not medical advice.
How is NOV-002 administered?
Recorded routes of administration: Intravenous, Subcutaneous.
What are the potential side effects of NOV-002?
Reported adverse effects include: Hypersensitivity reactions, Injection site reactions, Nausea, Fatigue. This list is not exhaustive — consult a qualified clinician.
Who should avoid NOV-002?
Recorded contraindications: Severe renal impairment, Known hypersensitivity to glutathione or cisplatin components. Consult a qualified clinician before use.